A compound is provided which has thyroid-stimulating hormone receptor antagonist activity and is useful for treating thyroid-related diseases. The compound relates to a 3,4-dihydroquinolin-2(1H)-one compound represented by Formula (I) or a pharmacologically acceptable salt thereof. The compound or a pharmacologically acceptable salt thereof have antagonist activity against a thyroid-stimulating hormone receptor and is useful as a therapeutic agent for thyroid-related diseases, for example, hyperthyroidism, Graves' disease, thyroid eye disease and thyroid cancer.
A compound is provided which has thyroid-stimulating hormone receptor antagonist activity and is useful for treating thyroid-related diseases. The compound relates to a 3,4-dihydroquinolin-2(1H)-one compound represented by Formula (I) or a pharmacologically acceptable salt thereof. The compound or a pharmacologically acceptable salt thereof have antagonist activity against a thyroid-stimulating hormone receptor and is useful as a therapeutic agent for thyroid-related diseases, for example, hyperthyroidism, Graves' disease, thyroid eye disease and thyroid cancer.
A61P 5/16 - Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4 for decreasing, blocking or antagonising the activity of the thyroid hormones
The present invention addresses the problem of providing a novel compound that has an OX2R agonist activity. The present invention relates to a substituted sulfonamide compound which is represented by formula (I) or a pharmacologically acceptable salt thereof. A compound according to the present invention, or a pharmacologically acceptable salt thereof, has an agonist activity against OX2R, and is useful as, for example, a therapeutic agent for sleep disorders associated with OX2R (for example, narcolepsy, idiopathic hypersomnia, Kleine-Levin syndrome, hypersomnia associated with a physical disease, hypersomnia associated with a mental disease, hypersomnia associated with a drug or a substance, circadian rhythm sleep-wake disorders, insufficient sleep syndrome, and extended sleep).
C07C 311/07 - Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 239/28 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 401/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 403/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
The present invention addresses the problem of providing a novel compound that has OX2R agonist activity. The present invention relates to a substituted sulfonamide macrocyclic compound represented by formula (I) or a pharmacologically acceptable salt thereof. This compound, or a pharmacologically acceptable salt thereof, has agonist activity against OX2R, and is useful as a treatment agent, etc., for sleep disorders involving OX2R (e.g., narcolepsy, idiopathic hypersomnia, Kleine-Levin syndrome, hypersomnia associated with a physical disease, hypersomnia associated with a mental disease, hypersomnia associated with a drug or a substance, circadian rhythm sleep-wake disorder, insufficient sleep syndrome, and extended sleep).
C07D 225/04 - Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 269/00 - Heterocyclic compounds containing rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms according to more than one of groups
C07D 273/01 - Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups having one nitrogen atom
An object of the present invention is to provide an oral solid preparation having a rapid dissolution property even when the content of Linzagolix or a pharmacologically acceptable salt thereof in the oral solid preparation varies over a wide range.
An object of the present invention is to provide an oral solid preparation having a rapid dissolution property even when the content of Linzagolix or a pharmacologically acceptable salt thereof in the oral solid preparation varies over a wide range.
The present invention relates to an oral solid preparation comprising Linzagolix or a pharmacologically acceptable salt thereof; crystalline cellulose; low-substituted hydroxypropyl cellulose; and one or more disintegrants selected from the group consisting of carmellose sodium, carmellose calcium and croscarmellose sodium, and the like.
The present invention addresses the problem of providing a novel compound that has thyroid-stimulating hormone receptor antagonist activity and is useful for treating thyroid-related diseases. The present invention pertains to a biaryl compound represented by formula (I) or a pharmacologically acceptable salt thereof. The compound according to the present invention or the pharmacologically acceptable salt thereof has antagonist activity with respect to thyroid-stimulating hormone receptors, and is therefor useful as a therapeutic agent and the like for thyroid-related diseases (for example, hyperthyroidism, Graves disease, thyroid-associated ophthalmopathy, and thyroid cancer).
A61K 31/4418 - Non-condensed pyridinesHydrogenated derivatives thereof having a carbocyclic ring directly attached to the heterocyclic ring, e.g. cyproheptadine
A61P 5/14 - Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
A61P 5/16 - Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4 for decreasing, blocking or antagonising the activity of the thyroid hormones
C07D 237/08 - Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
The present invention addresses the problem of providing a novel compound that has a thyroid-stimulating hormone receptor antagonistic activity and is useful for the treatment of thyroid-related diseases. The present invention relates to an N-substituted cyclic amide compound represented by the formula or a pharmacologically acceptable salt thereof. The compound or the pharmacologically acceptable salt thereof according to the present invention has a thyroid-stimulating hormone receptor antagonistic activity and is useful as a therapeutic agent for thyroid-related diseases (e.g., hyperthyroidism, Graves' disease, thyroid eye disease, and thyroid cancer) and others.
C07D 211/76 - Oxygen atoms attached in position 2 or 6
A61K 31/435 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
A61K 31/4365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61K 31/438 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
A61K 31/4412 - Non-condensed pyridinesHydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
A61K 31/45 - Non-condensed piperidines, e.g. piperocaine having oxo groups directly attached to the heterocyclic ring, e.g. cycloheximide
A61K 31/498 - Pyrazines or piperazines ortho- or peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A61K 31/536 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with carbocyclic ring systems
A61P 5/14 - Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
C07D 241/44 - Benzopyrazines with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
C07D 265/36 - 1,4-OxazinesHydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
The present invention addresses the problem of providing a novel compound that has a thyroid-stimulating hormone receptor antagonistic activity and is useful for the treatment of thyroid-related diseases. The present invention relates to a nitrogen-containing condensed ring compound represented by formula (A-I) or a pharmacologically acceptable salt thereof. The present invention relates to a nitrogen-containing condensed ring compound represented by formula (A-I) or a pharmacologically acceptable salt thereof. The compound or the pharmacologically acceptable salt thereof according to the present invention has an antagonistic activity against thyroid-stimulating hormone receptors and is therefore useful as a therapeutic agent for thyroid-related diseases (e.g., hyperthyroidism, Graves' disease, thyroid eye disease, and thyroid cancer) and others.
A61K 31/4365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/473 - QuinolinesIsoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61P 5/16 - Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4 for decreasing, blocking or antagonising the activity of the thyroid hormones
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 455/04 - Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing quinolizine ring systems directly condensed with at least one six-membered carbocyclic ring, e.g. protoberberineAlkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine
The present invention addresses the problem of providing a medicine that, despite of being a non-ergot dopamine agonist (DA), reduces the risk of the drowsiness side effect, and exhibits an excellent therapeutic effect on neurodegenerative disorders such as Parkinson's disease (PD). The present invention relates to a pharmaceutical composition for treating neurodegenerative diseases such as Parkinson's disease, the pharmaceutical composition comprising 1-{[(4aR,6R,8aR)-2-amino-3-cyano-8-methyl-4,4a,5,6,7,8,8a,9-octahydrothieno[3,2-g]quinolin-6-yl]carbonyl}-3-[2-(dimethylamino)ethyl]-1-propylurea or a pharmacologically acceptable salt thereof. The pharmaceutical composition is characterized by being orally administered at a daily dose of 0.25 mg to 2 mg in terms of free form.
A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for diagnostic purposes, treatment and prevention of endometriosis, uterine fibroids and other disorders of the reproductive system, of hormonally dependent conditions, and of inflammatory and immune system disorders
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for diagnostic purposes, treatment and prevention of endometriosis, uterine fibroids and other disorders of the reproductive system, of hormonally dependent conditions, and of inflammatory and immune system disorders
11.
METHOD FOR PRODUCING COMPOUND ENCODED BY OLIGONUCLEOTIDE, AND APPLICATION THEREOF
The purpose of the present invention is to provide a new method for producing a compound encoded by an oligonucleotide. Provided according to the present invention is a method for producing a compound encoded by an oligonucleotide, the method including phosphodiester bonding of oligonucleotide chains to each other by chemical ligation under prescribed conditions.
C07H 21/04 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with deoxyribosyl as saccharide radical
C12N 15/11 - DNA or RNA fragmentsModified forms thereof
C40B 30/04 - Methods of screening libraries by measuring the ability to specifically bind a target molecule, e.g. antibody-antigen binding, receptor-ligand binding
C40B 40/06 - Libraries containing nucleotides or polynucleotides, or derivatives thereof
C40B 50/10 - Liquid phase synthesis, i.e. wherein all library building blocks are in liquid phase or in solution during library creationParticular methods of cleavage from the liquid support involving encoding steps
12.
GONADOTROPIN-RELEASING HORMONE ANTAGONIST DOSING REGIMENS FOR THE TREATMENT OF ENDOMETRIOSIS
The invention provides methods of treating endometriosis in a patient by administration of a gonadotropin-releasing hormone (GnRH) antagonist, for instance, according to dosing regimens predicated on the patient's level of anti-Müllerian hormone (AMH) or β17-estradiol (E2).
The present invention addresses the problem of providing a novel compound that has an OX2R agonist activity. The present invention pertains to a cyclopentane compound represented by formula (I) or a pharmacologically acceptable salt thereof. This compound, or a pharmacologically acceptable salt thereof, has an agonist activity against OX2R, and is useful as a treatment agent, etc., for sleep disorders involving OX2R (e.g., narcolepsy, idiopathic hypersomnia, Kleine-Levin syndrome, hypersomnia associated with a physical disease, hypersomnia associated with a mental disease, hypersomnia associated with a drug or a substance, circadian rhythm sleep-wake disorder, insufficient sleep syndrome, and extended sleep).
C07C 311/07 - Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
A61K 31/277 - NitrilesIsonitriles having a ring, e.g. verapamil
A61K 31/341 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
A61P 25/26 - Psychostimulants, e.g. nicotine, cocaine
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 207/06 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
C07D 239/26 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 261/02 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
C07D 263/32 - Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 277/30 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 307/54 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
14.
GONADOTROPIN-RELEASING HORMONE ANTAGONIST DOSING REGIMENS FOR TREATING UTERINE FIBROIDS AND REDUCING MENSTRUAL BLOOD LOSS
The invention provides compositions and methods for reducing the volume of menstrual blood loss in a patient, such as a human patient, for instance, that has uterine fibroids, by administration of a gonadotropin-releasing hormone (GnRH) antagonist. Suitable GnRH antagonists useful in conjunction with the compositions and methods described herein include thieno[3,4d]pyrimidine derivatives, such as 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4d]pyrimidine-5-carboxylic acid and the choline salt thereof.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61P 5/00 - Drugs for disorders of the endocrine system
A61K 31/565 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
A61K 31/57 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
The present invention addresses the problem of providing a novel compound that has a thyroid-stimulating hormone receptor antagonist activity and is useful for the treatment of thyroid-related diseases. The present invention relates to a 3,4-dihydroquinolin-2(1H)-one compound represented by formula (I) or a pharmacologically acceptable salt thereof. The compound according to the present invention or a pharmacologically acceptable salt thereof has an antagonist activity against thyroid-stimulating hormone receptors and is therefore useful as a therapeutic agent for thyroid-related diseases (e.g., hyperthyroidism, Graves' disease, thyroid eye disease and thyroid cancer) and others.
A61P 5/14 - Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
A61P 5/16 - Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4 for decreasing, blocking or antagonising the activity of the thyroid hormones
An object of the present invention is to provide a compound which has high storage stability and is suitable for use as a drug substance. The present invention relates to a succinate salt of 1-{[(4aR,6R,8aR)-2-amino-3-cyano-8-methyl-4,4a,5,6,7,8,8a,9-octahydrothieno[3,2-g]quinolin-6-yl]carbonyl}-3-[2-(dimethylamino)ethyl]-1-propylurea, which is suitable as a drug substance having excellent storage stability and crystallinity and is useful for the treatment or prevention of Parkinson's disease, restless legs syndrome, hyperprolactinemia or the like.
The present invention addresses the problem of providing an oral solid preparation having rapid dissolution even if the content of linzagolix or a pharmacologically acceptable salt thereof in the oral solid preparation differs over a wide range. The present invention relates to an oral solid preparation containing: linzagolix or a pharmacologically acceptable salt thereof; crystalline cellulose; low-substituted hydroxypropyl cellulose; and one or more disintegrating agents selected from the group consisting of carmellose sodium, carmellose calcium, and croscarmellose sodium.
As a drug substance, a crystal having good physical properties is preferable. However, the crystal form that is most excellent as a drug substance may vary with the compound. In general, it is difficult to predict a crystal form of a drug substance having good physical properties, and it is required to variously examine each compound. Therefore, an object of the present invention is to provide a crystal having good physical properties as a drug substance for a novel compound.
As a drug substance, a crystal having good physical properties is preferable. However, the crystal form that is most excellent as a drug substance may vary with the compound. In general, it is difficult to predict a crystal form of a drug substance having good physical properties, and it is required to variously examine each compound. Therefore, an object of the present invention is to provide a crystal having good physical properties as a drug substance for a novel compound.
The present invention relates to a crystal of the compound represented by the following formula (I) useful for the treatment of an inflammatory bowel disease.
As a drug substance, a crystal having good physical properties is preferable. However, the crystal form that is most excellent as a drug substance may vary with the compound. In general, it is difficult to predict a crystal form of a drug substance having good physical properties, and it is required to variously examine each compound. Therefore, an object of the present invention is to provide a crystal having good physical properties as a drug substance for a novel compound.
The present invention relates to a crystal of the compound represented by the following formula (I) useful for the treatment of an inflammatory bowel disease.
C07D 473/18 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
19.
CRYSTAL OF IMIDAZOPYRIDINONE COMPOUND OR SALT THEREOF
As a drug substance, a crystal having good physical properties is preferable. However, the crystal form that is most excellent as a drug substance may vary with the compound. In general, it is difficult to predict a crystal form of a drug substance having good physical properties, and it is required to variously examine each compound. Therefore, an object of the present invention is to provide a crystal having good physical properties as a drug substance for a novel compound or a salt thereof.
As a drug substance, a crystal having good physical properties is preferable. However, the crystal form that is most excellent as a drug substance may vary with the compound. In general, it is difficult to predict a crystal form of a drug substance having good physical properties, and it is required to variously examine each compound. Therefore, an object of the present invention is to provide a crystal having good physical properties as a drug substance for a novel compound or a salt thereof.
The present invention relates to a crystal of the compound represented by the following formula (I) or a salt thereof useful for the treatment of an inflammatory bowel disease.
As a drug substance, a crystal having good physical properties is preferable. However, the crystal form that is most excellent as a drug substance may vary with the compound. In general, it is difficult to predict a crystal form of a drug substance having good physical properties, and it is required to variously examine each compound. Therefore, an object of the present invention is to provide a crystal having good physical properties as a drug substance for a novel compound or a salt thereof.
The present invention relates to a crystal of the compound represented by the following formula (I) or a salt thereof useful for the treatment of an inflammatory bowel disease.
The present disclosure provides compositions and methods for treating estrogen-dependent disorders, such as disorders of the female reproductive system, including uterine fibroids and endometriosis, among others. Compounds described herein that may be used to treat such indications include gonadotropin-releasing hormone (GnRH) antagonists. Suitable GnRH antagonists useful in conjunction with the compositions and methods described herein include thieno[3,4d]pyrimidine derivatives, such as 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno [3,4d]pyrimidine-5-carboxylic acid and the choline salt thereof, among others. Using the compositions and methods described herein, GnRH antagonists may be periodically administered to a patient, such as one or more times per day, week, or month, in combination with periodic add-back therapy, thereby preventing bone mineral density loss that may otherwise accompany estrogen depletion effectuated by GnRH antagonist activity. Advantageously, using the dosing schedules of the present disclosure, the periodic administration the GnRH antagonist and add-back therapy may commence together, such as on the same day.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A61K 31/567 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
A61K 31/57 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
A61K 31/585 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin containing lactone rings, e.g. oxandrolone, bufalin
The present disclosure provides compositions and methods for treating estrogen-dependent disorders, such as disorders of the female reproductive system, including uterine fibroids and endometriosis, among others. Compounds described herein that may be used to treat such indications include gonadotropin-releasing hormone (GnRH) antagonists. Suitable GnRH antagonists useful in conjunction with the compositions and methods described herein include thieno[3,4d]pyrimidine derivatives, such as 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno [3,4d]pyrimidine-5-carboxylic acid and the choline salt thereof, among others. Using the compositions and methods described herein, GnRH antagonists may be periodically administered to a patient, such as one or more times per day, week, or month. Advantageously, using the dosing schedules of the present disclosure, the periodic administration the GnRH antagonist may be temporarily halted, allowing a patient to recover any lost bone mineral density, without an accompanying return in the patient's symptoms.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61P 15/00 - Drugs for genital or sexual disordersContraceptives
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/565 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
A61K 31/567 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
A61K 31/57 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
A61K 31/585 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin containing lactone rings, e.g. oxandrolone, bufalin
22.
Compositions and methods for the treatment of adenomyosis and rectovaginal endometriosis
The present disclosure provides compositions and methods for treating endometrial growth disorders in a patient, such as a human patient, and particularly pre-menopausal female human patients. Exemplary disorders that may be treated using the compounds and therapeutic regimens described herein include adenomyosis and rectovaginal endometriosis. The compounds described herein that may be used to treat such indications include gonadotropin-releasing hormone (GnRH) antagonists. Suitable GnRH antagonists useful in conjunction with the compositions and methods described herein include thieno[3,4d]pyrimidine derivatives, such as 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4d]pyrimidine-5-carboxylic acid and the choline salt thereof, among others.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61K 31/565 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
A61K 31/567 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
A61K 31/57 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
A61K 31/573 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
A61K 31/585 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin containing lactone rings, e.g. oxandrolone, bufalin
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
A61P 15/00 - Drugs for genital or sexual disordersContraceptives
23.
METHOD FOR PRODUCING OCTAHYDROTHIENOQUINOLINE COMPOUND, AND PRODUCTION INTERMEDIATE OF SAME
11 receptor agonist, or a pharmacologically acceptable salt thereof; and a novel production intermediate. The present invention provides a method for producing a compound (P) or a pharmacologically acceptable salt thereof from 1, 4-cyclohexanedione monoethylene ketal (2) via a compound (AA) or the like, which is a production intermediate. (In the formula, TA represents an optically active tartaric acid derivative, preferably L-tartaric acid.)
[Problem] The present invention addresses the problem of providing a compound that is suitable for use as a pharmaceutical bulk drug and that has high storage stability. [Solution] The present invention relates to a succinate of 1-{[(4aR,6R,8aR)-2-amino-3-cyano-8-methyl-4,4a,5,6,7,8,8a,9-octahydrothieno[3,2-g]quinolin-6-yl]carbonyl}-3-[2-(dimethylamino)ethyl]-1-propylurea, said succinate being suitable as a pharmaceutical bulk drug, having exceptional storage stability and crystallinity, and being useful for the treatment or prevention of Parkinson's disease, restless leg syndrome, or hyperprolactinemia, etc.
A61K 31/4365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
A61P 5/10 - Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH
A61P 25/00 - Drugs for disorders of the nervous system
An object of the present invention is to provide a novel formulation containing sucroferric oxyhydroxide, particularly a novel formulation that can be ingested without being chewed. The present invention relates to a novel formulation discovered based on the finding that a granule containing sucroferric oxyhydroxide that has a specific size and shape and also has specific physicochemical properties can be easily ingested without being chewed, and has formulation properties suitable for industrial manufacturing as a result of intensive studies to provide a novel formulation containing sucroferric oxyhydroxide.
A crystal having excellent physical properties is preferable as an active pharmaceutical ingredient. However, the best crystal form for an active pharmaceutical ingredient differs for each compound. It is generally difficult to predict a crystal form that has excellent physical properties for an active pharmaceutical ingredient, thus various studies are required for each compound. As such, the objective of the present invention is to provide, for a novel compound or a salt thereof, a crystal having excellent physical properties as an active pharmaceutical ingredient. The present invention relates to a crystal of the compound represented by formula (I), or a salt thereof, which is useful in treating an inflammatory bowel disease.
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
Preferred active pharmaceutical ingredients are crystals having satisfactory physical properties. However, what crystal forms of active pharmaceutical ingredients are most superior varies from compound to compound. It is generally difficult to predict a crystal form of an active pharmaceutical ingredient having satisfactory physical properties, and various investigations on each compound are required. The present invention addresses the problem of providing, with respect to a novel compound, a crystal having satisfactory physical properties as an active pharmaceutical ingredient. The present invention relates to a crystal of the compound represented by the formula (I), which is useful for the treatment of inflammatory intestinal diseases.
C07D 473/18 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
The present invention relates to hypoxanthine compound or a pharmaceutically acceptable salt thereof. The compounds of the present invention or pharmaceutically acceptable salts thereof have prolyl hydroxylase inhibitory effect and are useful as agents for the treatment of inflammatory bowel diseases such as ulcerative colitis and the like. In an embodiment, the present invention relates to a method for treating an inflammatory bowel disease, comprising administering a necessary amount of a pharmaceutical composition containing hypoxanthine compound or a pharmaceutically acceptable salt thereof, and pharmaceutical additive to a patient.
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
The present invention aims to provide a novel compound which has prolyl hydroxylase (PHDs) inhibitory effect and which is useful for the treatment of inflammatory bowel diseases such as ulcerative colitis and the like. The present invention relates to a imidazopyridinone compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof. The compounds of the present invention or pharmaceutically acceptable salts thereof which have prolyl hydroxylase inhibitory effect and, are useful as agents for the treatment of inflammatory bowel diseases such as ulcerative colitis and the like. In an embodiment, the present invention relates to a method for treating an inflammatory bowel disease
Disclosed herein are methods, sodium-dependent glucose transporter (SGLT)1 compounds and compositions for the treatment of postprandial hypoglycemia, postprandial hypoglycemia that occurs as a consequence of gastric surgery.
A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
A61P 3/08 - Drugs for disorders of the metabolism for glucose homeostasis
A61K 31/702 - Oligosaccharides, i.e. having three to five saccharide radicals attached to each other by glycosidic linkages
31.
Usage and dosage of therapeutic agents for endometriosis
An object of the present invention is to provide pharmaceutical agents that reduce risk for decrease in bone mineral density due to their effect of reducing estrogen levels and exert excellent therapeutic effects on endometriosis. The present invention relates to pharmaceutical compositions for treating endometriosis comprising 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid or a pharmaceutically acceptable salt thereof, which are administered orally once a day at a daily dose of between 50 mg and 75 mg calculated as a free form.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations; Pharmaceutical preparations for diagnostic purposes, treatment and prevention of conditions in humans; Pharmaceutical preparations for the treatment of endometriosis, uterine fibroids and hormonally dependent conditions.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations, namely, pharmaceutical preparations for diagnostic purposes, treatment and prevention of endometriosis, uterine fibroids, fertility, prostate cancer and hormonally dependent conditions in humans; pharmaceutical preparations for the treatment of endometriosis, uterine fibroids, fertility, prostate cancer and hormonally dependent conditions; pharmaceutical preparations for the treatment of endometriosis, uterine fibroids and hormonally dependent conditions.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for treatment and prevention of endometriosis, uterine fibroids and other disorders of the reproductive system, of hormonally dependent conditions, and of inflammatory and immune system disorders
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for treatment and prevention of endometriosis, uterine fibroids and other disorders of the reproductive system, of hormonally dependent conditions, and of inflammatory and immune system disorders
36.
COMPOSITIONS AND METHODS FOR TREATING METABOLIC DISEASE
The invention described herein relates to oral dosage form therapies for treating metabolic disorders using combinations of inhibitors of SGLT1 and SGLT2. In such dosage forms, SGLT1 is effective in the intestinal lumen, and is either not absorbed, or poorly absorbed, while the SGLT2 inhibitor inhibits sugar reabsorption in the kidney by inhibiting SGLT2 activity. Metabolic disorders treated by combined SGLT1 and SGLT2 oral dosage forms include disorders associated with abnormal accumulation of liver lipids, which may also be copresent with hyperglycemia. Combinations of SGLT1 and SGLT2 inhibitors are contemplated herein, particularly combinations
A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
KYOTO PREFECTURAL PUBLIC UNIVERSITY CORPORATION (Japan)
Inventor
Nakazawa Yozo
Saito Shoji
Yagyu Shigeki
Nakano Shigeru
Momose Takaki
Hitomi Kenta
Abstract
A problem addressed by the present invention is to develop a chimeric antigen receptor (CAR) effective against solid tumors that express anaplastic lymphoma kinase (ALK). The present invention provides a polynucleotide encoding a CAR protein having a target-binding domain that binds to an extracellular ligand binding region of ALK, a transmembrane domain, and an intracellular signal transduction domain, wherein the target-binding domain is selected from FAM150A, FAM150B, and fragments thereof that bind to the extracellular ligand binding region of ALK, and a genetically modified cell into which the polynucleotide has been introduced.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations; pharmaceutical preparations for
diagnostic purposes, treatment and prevention of conditions
in humans; pharmaceutical preparations for the treatment of
endometriosis, uterine fibroids and hormonally dependent
conditions.
7 is alkyl or the like. The compounds of the present invention or a pharmaceutically acceptable salt thereof have an excellent CGRP receptor antagonist activity, and thus are useful as agents for the treatment of various diseases mediated by CGRP receptors.
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations, namely, pharmaceutical preparations for diagnostic purposes, treatment and prevention of endometriosis, uterine fibroids, fertility, prostate cancer and hormonally dependent conditions in humans; pharmaceutical preparations for the treatment of endometriosis, uterine fibroids, fertility, prostate cancer and hormonally dependent conditions; pharmaceutical preparations for the treatment of endometriosis, uterine fibroids and hormonally dependent conditions.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for diagnostic purposes, treatment and prevention of endometriosis, uterine fibroids and other disorders of the reproductive system, of hormonally dependent conditions, and of inflammatory and immune system disorders
42.
Gonadotropin-releasing hormone antagonist dosing regimens for treating uterine fibroids and reducing menstrual blood loss
The invention provides compositions and methods for reducing the volume of menstrual blood loss in a patient, such as a human patient, for instance, that has uterine fibroids, by administration of a gonadotropin-releasing hormone (GnRH) antagonist. Suitable GnRH antagonists useful in conjunction with the compositions and methods described herein include thieno[3,4d]pyrimidine derivatives, such as 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxypheny I]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4d]pyrimidine-5-carboxylic acid and the choline salt thereof.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/565 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
A61P 5/00 - Drugs for disorders of the endocrine system
A61K 31/57 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
43.
Gonadotropin-releasing hormone antagonist dosing regimens for the treatment of endometriosis
The invention provides methods of treating endometriosis in a patient by administration of a gonadotropin-releasing hormone (GnRH) antagonist, for instance, according to dosing regimens predicated on the patient's level of anti-Müllerian hormone (AMH) or β17-estradiol (E2).
The purpose of the present invention is to improve efficiency in a method for producing chimeric antigen receptor (CAR)-expressing cells. Provided is a method for producing genetically modified mammalian cells, the method comprising: a) a step of introducing, by a transposon method, a polynucleotide coding for a chimeric antigen receptor (CAR) protein into a cell population that contains T-cells derived from a mammal to obtain a genetically modified cell population; b) a step of preparing an endogenous cell population derived from the mammal that expresses a protein that binds to the CAR; and c) a step of coculturing the genetically modified cell population of step a) and the endogenous cell population of step b).
The present invention addresses the problem of providing a novel compound which has an inhibitory effect on prolyl hydroxylases (PHDs), and which is useful as a therapeutic agent for inflammatory bowel diseases such as ulcerative colitis. The present invention relates to an imidazopyridinone compound represented by formula (I) or a pharmacologically acceptable salt thereof. A compound of the present invention or a pharmacologically acceptable salt thereof has an inhibitory effect on prolyl hydroxylases, and is thus useful as a therapeutic agent for inflammatory bowel diseases such as ulcerative colitis. One embodiment of the present invention relates to a method of therapy for inflammatory bowel diseases.
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
The present invention addresses the problem of providing a novel compound that has an inhibitory effect on prolyl hydroxylases (PHDs), and that is useful as a therapeutic agent for inflammatory intestinal diseases, such as ulcerative colitis. The present invention pertains to a hypoxanthine compound or a pharmaceutically acceptable salt thereof. This compound or a pharmaceutically acceptable salt thereof has an inhibitory effect on prolyl hydroxylases, and is useful as, for example, a therapeutic agent for inflammatory intestinal diseases, such as ulcerative colitis. In one embodiment, the present invention pertains to a therapeutic method that is for inflammatory intestinal diseases and that comprises administering, to a patient, a required amount of a pharmaceutical composition containing a medicinal additive and a hypoxanthine compound or a pharmaceutically acceptable salt thereof.
C07D 473/18 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 43/00 - Drugs for specific purposes, not provided for in groups
47.
SUCROFERRIC OXYHYDROXIDE-CONTAINING GRANULES AND PHARMACEUTICAL COMPOSITION
[Problem] The present invention addresses the problem of providing a novel preparation containing sucroferric oxyhydroxide, particularly a novel preparation that can be ingested without being chewed. [Solution] The present invention relates to a novel preparation which, as a result of in-depth investigations intended to provide a novel preparation containing sucroferric oxyhydroxide, was discovered on the basis of the finding that granules which contain sucroferric oxyhydroxide, and which have a specific size and shape and specific physicochemical properties can be easily ingested without being chewed, and possess preparation properties that are suitable for industrial production.
Provided is a production of a cell expressing a variant chimeric antigen receptor (CAR) having excellent target cytotoxicity. Provided is a genetically modified cell into which a polynucleotide is introduced, the polynucleotide encoding a chimeric antigen receptor (CAR) protein having: a target binding domain which specifically binds to a human granulocyte-macrophage colony-stimulating factor (GM-CSF) receptor; a transmembrane domain; and an intracellular signaling domain, wherein the target binding domain is a variant in which a glutamic acid of the 21st in the amino acid sequence represented by SEQ ID NO: 1 is substituted with another amino acid.
[Problem] To provide a novel therapeutic agent for nocturnal pollakiuria. [Solution] A therapeutic agent for nocturnal pollakiuria which contains, as an active ingredient, (6S)-N-[4-({(2S,5R)-5-[(R)-hydroxy(phenyl)methyl]pyrrolidin-2-yl}methyl)phenyl]-4-oxo-4,6,7,8-tetrahydropyrrolo[1,2-a]pyrimidine-6-carboxamide.
An object of the present invention is to provide pharmaceutical agents that reduce risk for decrease in bone mineral density due to their effect of reducing estrogen levels and exert excellent therapeutic effects on endometriosis. The present invention relates to pharmaceutical compositions for treating endometriosis comprising 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid or a pharmaceutically acceptable salt thereof, which are administered orally once a day at a daily dose of between 50 mg and 75 mg calculated as a free form.
The present invention addresses the problem of providing a novel compound which has CGRP receptor antagonistic action and is useful for treatment of various diseases mediated by CGRP receptors. The present invention pertains to a pyrrolidine compound represented by formula (I) or a pharmaceutically acceptable salt thereof [in the formula, R1or the like represents -OH, -OZ122, -NHZ2, -NZ2Z3, or the like]. The compound according to the present invention or a pharmaceutically acceptable salt thereof has excellent CGRP receptor antagonistic action and is useful as a therapeutic drug for various diseases mediated by CGRP receptors.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
The present invention addresses the problem of providing a novel compound that exhibits CGRP-receptor antagonism and is useful for treatment of a variety of diseases involving CGRP receptors. The present invention pertains to a condensed heterocyclic compound represented by formula (I) or a pharmacologically acceptable salt thereof. [In formula (I), the ring W, or the like represents a phenyl group or the like that may have an arbitrary group.] The compound according to the present invention or the pharmacologically acceptable salt thereof exhibits excellent CGRP-receptor antagonism and is useful as a therapeutic medicine for a variety of diseases involving CGRP receptors.
A61K 31/438 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
53.
Salt of fused heterocyclic derivative and crystal thereof
The present invention provides 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyl-oxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid choline salt having excellent solubility and storage stability.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61P 5/04 - Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin for decreasing, blocking or antagonising the activity of the hypothalamic hormones
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations; pharmaceutical preparations for
diagnostic purposes, treatment and prevention of conditions
in humans (term considered too vague by the International
Bureau - rule 13 (2) (b) of the Common Regulations);
pharmaceutical preparations for the treatment of
endometriosis, uterine fibroids and hormonally dependent
conditions.
55.
THIAZOLE DERIVATIVE OR PHARMACOLOGICALLY ACCEPTABLE SALT OF SAME
The present invention addresses the problem of providing: a novel thiazole derivative or a pharmacologically acceptable salt thereof; a pharmaceutical composition which contains the thiazole derivative or a pharmacologically acceptable salt thereof; and a pharmaceutical use of the pharmaceutical composition. The present invention provides a compound represented by formula (I), which has TRPM 8 inhibitory activity, or a pharmacologically acceptable salt of the compound. (In the formula, ring A represents thiazole or the like; ring B represents a C6-10 aryl or the like; each of R2a and R2b independently represents a hydrogen atom or the like; R3 represents a hydrogen atom or the like; R4a represents a hydrogen atom or the like; R4b represents a hydrogen atom or the like; R5 represents a hydrogen atom or the like; R6 represents a hydrogen atom or the like; R7a represents a hydrogen atom or the like; R7b represents a hydrogen atom or the like; and n represents 0 or 1.) In addition, a compound represented by formula (I) or a pharmacologically acceptable salt of the compound is able to be used as a therapeutic or prophylactic agent for diseases or conditions associated with hyperexcitement or disorder of afferent nerves.
C07D 277/30 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61P 13/10 - Drugs for disorders of the urinary system of the bladder
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
56.
Pyrazole derivative or pharmaceutically acceptable salt thereof
The present invention is to provide a novel pyrazole derivative, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and a pharmaceutical use thereof.
The present invention provides a compound represented by the formula (I) or a pharmaceutically acceptable salt thereof, which has TRPM8 inhibitory effects:
8 is a hydrogen atom or the like; n is 0, 1 or 2. Therefore, the compound represented by the formula (I) of the present invention or a pharmaceutically acceptable salt thereof is useful as an agent for treating or preventing diseases or symptoms caused by hyperexcitability or disorder of afferent neurons.
C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 491/052 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
A61K 31/436 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
The purpose of the present invention is to produce chimeric antigen receptor (CAR)-expressing cells having superior target cell cytotoxicity. Provided are genetically-modified cells obtained by introducing polynucleotides that encode chimeric antigen receptor (CAR) proteins comprising a target binding domain that specifically binds to human granulocyte-macrophage colony-stimulating factor (GM-CSF), a transmembrane domain, and an intercellular signaling domain.
The present invention addresses the problem of providing a drug that reduces the risk of a reduction in bone mineral content associated with the hypoestrogenic effect, and that exhibits an excellent therapeutic effect with respect to endometriosis. The present invention pertains to a therapeutic pharmaceutical composition for endometriosis, the composition containing 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid or a pharmacologically acceptable salt thereof, wherein the pharmaceutical composition is characterized in that 50 mg to 75 mg of a compound in terms of free form is orally administered once per day as the daily dose.
The present invention addresses the problem of providing a novel compound which has an antagonistic activity against CGRP receptors and is useful for the treatment of various diseases associated with CGRP receptors. That is, the present invention relates to a pyrrolidine derivative represented by formula (I) or a pharmacologically acceptable salt thereof. In the formula, W represents a ring, X represents a carbon atom or the like, Y1 to Y4 independently represent a carbon atom or the like, and R1 to R7 independently represent an alkyl group or the like. The compound or a pharmacologically acceptable salt thereof according to the present invention has an excellent antagonistic activity against CGRP receptors and is useful as a therapeutic agent for various diseases associated with CGRP receptors.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
60.
Salt of fused heterocyclic derivative and crystal thereof
The present invention provides 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyl-oxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid choline salt having excellent solubility and storage stability.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61P 15/00 - Drugs for genital or sexual disordersContraceptives
A61P 15/08 - Drugs for genital or sexual disordersContraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
A61P 5/06 - Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
A61P 5/08 - Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH for decreasing, blocking or antagonising the activity of the anterior pituitary hormones
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations; pharmaceutical preparations for
diagnostic purposes, treatment and prevention of conditions
in humans; pharmaceutical preparations for the treatment of
endometriosis, uterine fibroids and hormonally dependent
conditions.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations; pharmaceutical preparations for
diagnostic purposes, treatment and prevention of conditions
in humans; pharmaceutical preparations for the treatment of
endometriosis, uterine fibroids and hormonally dependent
conditions.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations; pharmaceutical preparations for
diagnostic purposes, treatment and prevention of conditions
in humans; pharmaceutical preparations for the treatment of
endometriosis, uterine fibroids and hormonally dependent
conditions.
Disclosed is a method for producing mutant human erythropoietin with high purity and high yield. The method is a method for producing mutant human erythropoietin, comprising causing the mutant human erythropoietin to be produced by a transgenic mammalian animal cell and then subjecting a culture supernatant to hydrophobic column chromatography, multimodal anion-exchange column chromatography, anion-exchange column chromatography, phosphate-affinity column chromatography and gel filtration column chromatography sequentially in this order.
The present invention addresses the problem of providing a novel compound which has NK1 receptor antagonistic activity and which is useful in the prevention and treatment of nausea and vomiting accompanying the administration of antineoplastic agents. The present invention pertains to a compound represented by formula (I) (in the formula, W represents a fluorine atom or the like, ring A represents a cycloalkyl or the like, X1 represents CH or N, R represents a methyl group or the like, Y represents a number from 0 to 2, and U1, U2, and U3 each independently represent a single bond or the like), or a pharmacologically acceptable salt thereof. This compound or pharmacologically acceptable salt thereof has excellent NK1 receptor antagonistic activity and is useful as a prophylactic or therapeutic agent for nausea and vomiting accompanying the administration of antineoplastic agents.
C07D 241/04 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
A61P 1/08 - Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigoAntiemetics
C07D 211/62 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
A61K 31/4418 - Non-condensed pyridinesHydrogenated derivatives thereof having a carbocyclic ring directly attached to the heterocyclic ring, e.g. cyproheptadine
C07D 213/76 - Nitrogen atoms to which a second hetero atom is attached
68.
DOSING REGIMEN OF THERAPEUTIC AGENT FOR ATAXIA ASSOCIATED WITH SPINOCEREBELLAR DEGENERATION
The present invention addresses the problem of providing a medicinal composition for treating ataxia associated with spinocerebellar degeneration, said medicinal composition reducing a risk of side effects caused by an increase in parathyroid hormone level and being excellent. Provided is a medicinal composition for treating ataxia associated with spinocerebellar degeneration, said medicinal composition being characterized by being to be dosed once a day and containing, as an active ingredient, rovatirelin in a daily dose of 1.6-3.2 mg or a pharmacologically acceptable salt of rovatirelin in a daily dose of 1.6-3.2 mg in terms of a free salt. The medicinal composition according to the present invention is highly useful as a therapeutic agent for ataxia associated with spinocerebellar degeneration.
[Problem] The purpose of the present invention is to provide a novel pyrazole derivative, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing same and a pharmaceutical use thereof. [Solution] The present invention provides a composition having a TRPM8 inhibitory activity and represented by formula (I) (in the formula, ring A is C6-10 aryl or the like, X is CR4a or the like, R1 and R2 are a hydrogen atom or the like, R3 is a hydrogen atom or the like, R4 is a hydrogen atom or the like, ring B is C6-10 aryl or the like, R5 is a hydrogen atom or the like, R6a is a hydrogen atom or the like, R7a is a hydrogen atom or the like, R7b is a hydrogen atom or the like, R6b is a hydrogen atom or the like, R8 is a hydrogen atom or the like, and n is 0, 1, or 2), or a pharmaceutically acceptable salt thereof. Furthermore, the composition of the present invention represented by formula (I) or the pharmaceutically acceptable salt thereof can be used as a therapeutic agent or prophylactic agent for diseases or conditions caused by hyperexcitability or disorders of afferent nerves.
C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
A61K 31/436 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 491/052 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
Provided is an Fc-fused high affinity IgE receptor α-chain having excellent stability at low pH. An Fc fusion protein characterized by comprising (i) a high affinity IgE receptor α-chain and (ii) a Fc region of IgG1, wherein the linker fragment region between (i) and (ii) has the amino acid sequence of SEQ ID NO. 2.
The present invention provides pyrazole derivatives, uses thereof for medical purposes and so on. More particularly, the present invention relates to pharmaceuticals useful for the prevention or treatment of constipation, which comprise as an active ingredient 3-(3-{4-[3-(β-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2-dimethylpropionamide, or a pharmaceutically acceptable salt thereof. The pharmaceuticals of the present invention exert an effect of increasing the frequency of bowel movement or the like, and are useful for the prevention or treatment of constipation.
A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
C07H 17/02 - Heterocyclic radicals containing only nitrogen as ring hetero atoms
The present invention is to provide a novel α-substituted glycinamide derivative, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and a pharmaceutical use thereof.
The present invention provides a compound represented by the general formula (I), which has TRPM8 inhibitory effects:
4 independently represent a halogen atom and the like, n is 1 or 2], or a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing diseases or symptoms caused by hyperexcitability or disorder of afferent neurons.
A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
C07C 233/81 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
C07C 255/60 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton at least one of the singly-bound nitrogen atoms being acylated
C07C 271/22 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
C07D 215/54 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
C07D 217/26 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
C07D 221/04 - Ortho- or peri-condensed ring systems
C07D 317/62 - Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to atoms of the carbocyclic ring
C07D 231/14 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
C07D 333/38 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 333/70 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
C07D 233/90 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 237/08 - Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 237/24 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
C07D 239/26 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 239/28 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 241/12 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 241/24 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 263/34 - Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
C07C 237/22 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
C07C 237/36 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
C07D 275/02 - Heterocyclic compounds containing 1, 2-thiazole or hydrogenated 1,2-thiazole rings not condensed with other rings
C07D 277/20 - Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
C07D 277/30 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 277/56 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
C07D 307/82 - Benzo [b] furansHydrogenated benzo [b] furans with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
73.
ORAL PREPARATION IN WHICH BITTER TASTE OF BITTER-TASTING DRUG IS MASKED
Provided is a novel oral preparation (specifically, an intraoral quickly-disintegrating preparation) that allows a bitter-tasting drug such as silodosin, which has a very strong bitter taste, to be taken without an uncomfortable feeling and even without water, and that has solubility sufficient for reproducing a blood concentration effective for treating dysuria accompanying benign prostatic hyperplasia. The present invention pertains to masking particles and a novel oral preparation containing said masking particles. The masking particles are obtained by granulating or coating drug particles containing a bitter-tasting drug (e.g. silodosin) with a coating agent containing a methyl methacrylate-diethylaminoethyl methacrylate copolymer, wherein the content of said copolymer is 80-400 parts by mass relative to 100 parts by mass of the bitter-tasting drug (e.g. silodosin).
A61K 31/403 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
The present invention provides 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid choline salt having excellent solubility and storage stability.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61P 35/04 - Antineoplastic agents specific for metastasis
A61P 15/10 - Drugs for genital or sexual disordersContraceptives for impotence
A61P 15/02 - Drugs for genital or sexual disordersContraceptives for disorders of the vagina
A61P 13/08 - Drugs for disorders of the urinary system of the prostate
A61P 15/08 - Drugs for genital or sexual disordersContraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
The present invention pertains to: a cyanothiophene derivative represented by formula (I), exhibiting NK1 receptor antagonist activity, and useful in the prevention or treatment of the nausea and vomiting which accompanies the administration of antineoplastic agents; or a pharmaceutically acceptable salt thereof. In the formula, R1a represents an alkyl or the like, R1b represents a halogen atom or the like, R2 represents an alkyl or the like, R3a and R3b represent an alkyl or the like, R4a, R4b and R4c represent a hydrogen atom or a haloalkyl or the like, ring A represents a heterocycloalkyl or the like, U1 and U2 represent a single bond or an alkylene or the like, V represents a single bond or an alkylene or the like, and R5 represents a carboxy or an acyl or the like.
C07D 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
A61K 31/4025 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
A61P 1/08 - Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigoAntiemetics
C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
Provided is a novel compound which has an NK1 receptor antagonistic action and which is useful in the prevention and treatment of nausea and vomiting accompanying the administration of antineoplastic drugs, which have a diminished CYP3A4 inhibitory action compared to aprepitant. That is to say, the present invention pertains to a cyclohexyl-pyridine derivative represented by formula (I), or a pharmacologically acceptable salt thereof. In the formula, ring A is 4-fluoro-2-methyl phenyl or the like, X is a hydrogen atom or the like, R1 is a carboxymethyl or the like, R2 is an alkyl or the like, Y is from 0-2 or the like, U is -N(CH3)COC(CH3)2-3,5-bis(trifluoromethyl)phenyl or the like.
C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
A61K 31/4418 - Non-condensed pyridinesHydrogenated derivatives thereof having a carbocyclic ring directly attached to the heterocyclic ring, e.g. cyproheptadine
A61P 1/08 - Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigoAntiemetics
C07D 213/76 - Nitrogen atoms to which a second hetero atom is attached
2 receptors.
[Solution] The present invention provides a compound represented by the general formula (I):
2 receptor simulating activities and thus are useful as a treating or preventing agent for Parkinson's disease and the like.
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
[Problem] To provide a novel compound having an S1P1 receptor-antagonizing effect. [Solution] Provided are a compound represented by general formula (I): (in the formula, R1, R2, and R3 are each a hydrogen atom, halogen atom, C1-6 alkyl group, halo C1-6 alkyl group, or the like; R4 is a C1-6 alkyl group or the like; R5 is a C1-6 alkyl group or the like; R6 is a C1-6 alkyl group or the like; R7 is a hydrogen atom, halogen atom, C1-6 alkyl group, or the like; R8 is a halogen atom, C1-6 alkyl group, halo C1-6 alkyl group, C1-6 alkoxy group, or the like; and R9 is a hydrogen atom or C1-6alkyl group.) or a pharmacologically acceptable salt thereof, a pharmaceutical composition containing same, and the use thereof. This compound has an exceptional antagonistic effect on S1P1 receptors, and is therefore useful as an agent for the treatment or prevention of autoimmune diseases and the like.
C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
The present invention provides: a novel α-substituted glycinamide derivative or a pharmacologically acceptable salt thereof; a pharmaceutical composition containing the compound or the pharmacologically acceptable salt; and a use of the compound or the pharmacologically acceptable salt for medical purposes. The present invention provides: a compound which has a TRPM8-inhibiting activity and is represented by general formula (I) [wherein A1 represents a C6-10 aryl group or the like; A2 represents a C6-10 aryl group or the like; A3 represents a C6-10 aryl group or the like; L1 represents a single bond or the like; R1 represents a C1-6 alkyl group or the like; R2 represents a hydrogen atom or the like; and L2 represents a single bond or the like] or a pharmacologically acceptable salt thereof. The compound (I) according to the present invention can be used in a pharmaceutical composition for treating or preventing diseases or conditions associated with excessive excitation or damage of an afferent nerve.
C07C 237/22 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
A61K 31/166 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon atom of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
A61K 31/215 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
A61K 31/216 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
A61K 31/277 - NitrilesIsonitriles having a ring, e.g. verapamil
A61K 31/341 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
A61K 31/351 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
A61K 31/401 - ProlineDerivatives thereof, e.g. captopril
A61K 31/4353 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
A61K 31/4402 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
A61K 31/4406 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 3, e.g. zimeldine
A61K 31/4409 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
C07C 255/60 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton at least one of the singly-bound nitrogen atoms being acylated
C07C 311/08 - Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
C07D 207/34 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
C07D 209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 215/48 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
C07D 231/14 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
C07D 233/64 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
C07D 233/90 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 241/24 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 241/26 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
C07D 263/32 - Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 277/20 - Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
C07D 277/30 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 277/56 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
C07D 307/54 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 309/08 - Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
C07D 333/38 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
80.
Pyrazole derivative and use thereof for medical purposes
The present invention provides pyrazole derivatives, uses thereof for medical purposes and so on. More particularly, the present invention relates to pharmaceuticals useful for the prevention or treatment of constipation, which comprise as an active ingredient 3-(3-{4-[3-(β-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2-dimethylpropionamide, or a pharmaceutically acceptable salt thereof. The pharmaceuticals of the present invention exert an effect of increasing the frequency of bowel movement or the like, and are useful for the prevention or treatment of constipation.
A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
C07H 17/02 - Heterocyclic radicals containing only nitrogen as ring hetero atoms
The present invention provides a novel compound useful in the prevention or treatment of nausea and vomiting associated with the administration of antineoplastics, the compound having an NK1 receptor-antagonizing effect, and an inhibitory effect on CYP3A4 that is attenuated to a greater extent than in aprepitant. Specifically, the present invention relates to a carboxymethyl piperidine derivative represented by formula (I) or a pharmacologically acceptable salt thereof. In the formula, ring A is a benzene ring or the like, ring B is a pyridine ring or the like, R1 is a C1-6 alkyl or C1-6 alkoxy, R2 and R3 are hydrogen atoms or methyl, and n represents an integer of from 0 to 5.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61P 1/08 - Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigoAntiemetics
The present invention addresses the problem of providing a different mode of a 4-(3-cyanoindol-1-yl)-2-hydroxybenzoic acid which has xanthine oxidase inhibitory activity and is useful as a preventive and therapeutic agent for diseases caused by abnormalities in the serum uric acid level. The present invention provides: a 4-(3-cyanoindol-1-yl)-2-hydroxybenzoic acid sodium salt which has excellent solubility and other physical properties, is useful as a drug substance, and is suitable for industrial production of a medicine; and a method for producing the same.
The present invention provides: a novel α-substituted glycineamide derivative or a pharmacologically acceptable salt thereof; a pharmaceutical composition containing the α-substituted glycineamide derivative or a pharmacologically acceptable salt thereof; and a use of the α-substituted glycineamide derivative or a pharmacologically acceptable salt thereof for medical purposes. The present invention provides a compound which has an inhibitory activity on TRPM8 and is represented by general formula (I) [wherein A1 represents a C6-10 aryl group or the like; A2 represents a C6-10 aryl group or the like; X represents CH or the like; Y represents -CR1R2- or the like; R1 and R2 independently represent a hydrogen atom or the like; R3 and R4 independently represent a halogen atom or the like; and n represents 1 or 2] or a pharmacologically acceptable salt thereof. The compound (I) according to the present invention can be used as a therapeutic or prophylactic agent for diseases or conditions associated with afferent nerve hyperexcitability or injury.
C07C 237/22 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
A61K 31/166 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon atom of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
A61K 31/36 - Compounds containing methylenedioxyphenyl groups, e.g. sesamin
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
A61K 31/435 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/4402 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
A61K 31/4406 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 3, e.g. zimeldine
A61K 31/4409 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
A61K 31/443 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
A61K 31/4436 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/455 - Nicotinic acid, i.e. niacinDerivatives thereof, e.g. esters, amides
C07C 237/36 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
C07D 215/54 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
C07D 217/26 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
C07D 221/04 - Ortho- or peri-condensed ring systems
C07D 231/14 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
C07D 233/90 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 237/08 - Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 237/24 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
C07D 239/26 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 239/28 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
C07D 241/12 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 241/24 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 261/18 - Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen
C07D 263/34 - Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
C07D 275/02 - Heterocyclic compounds containing 1, 2-thiazole or hydrogenated 1,2-thiazole rings not condensed with other rings
C07D 277/20 - Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
C07D 277/30 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 277/56 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
C07D 307/82 - Benzo [b] furansHydrogenated benzo [b] furans with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
C07D 317/62 - Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to atoms of the carbocyclic ring
C07D 333/38 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 333/70 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
Provided is a novel oral administration preparation that allows a subject to easily take, even without water, silodosin that is a highly bitter drug without getting a feeling of strangeness and has such dissolution properties as to re-achieve a blood silodosin concentration effective for treating dysuria, etc. caused by prostatic hypertrophy. The present invention relates to masking grains, said masking grains being prepared by granulating drug grains that contain micropowdery silodosin using a coating agent that contains a non-enteric polymer or coating the drug grains with the coating agent, wherein the content of the non-enteric polymer is 80-400 parts by mass per 100 parts by mass of silodosin, a novel oral administration preparation comprising the masking grains, etc.
A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharidesDerivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
A61K 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61K 47/36 - PolysaccharidesDerivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
To provide: an industrially useful method for producing a nitrogen-containing heterocyclic derivative which has xanthine oxidase inhibitory activity and is useful as a prophylactic or therapeutic agent for diseases caused by an abnormal serum uric acid level; and a production intermediate for the nitrogen-containing heterocyclic derivative. By using a compound represented by formula (1), a compound represented by formula (2) or a salt thereof can be produced with high yield and high purity. (In formula (1), R1 represents a hydrogen atom or the like; R2 represents a hydroxy group or the like; Y represents a CX4 group or the like; X5 represents a chlorine atom or the like; and each of X1, X2, X3 and X4 independently represents a halogen atom or the like.) (In formula (2), X1-X4, R2 and Y are as defined above.)
C07D 209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07C 253/30 - Preparation of carboxylic acid nitriles by reactions not involving the formation of cyano groups
C07C 255/42 - Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being further bound to other hetero atoms
C07C 255/43 - Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being further bound to other hetero atoms the carbon skeleton being further substituted by singly-bound oxygen atoms
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61P 13/02 - Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
86.
Octahydrothienoquinoline derivative, pharmaceutical composition comprising derivative, and use of these
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 31/4365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
87.
NOVEL OCTAHYDROQUINOLINE DERIVATIVE, PHARMACEUTICAL COMPOSITION CONTAINING SAME, AND USE THEREOF
[Problem] To provide novel compounds having agonist activity on dopamine D2 receptors. [Solution] Provided are compounds represented by general formula (I) (in the formula, R1 is a C1-6 alkyl or the like; R2 is a C1-6 alkyl, aralkyl, heteroaryl C1-6 alkyl, C1-6 alkoxy C1-6 alkyl, R10R11NC1-6 alkyl, or the like; R3 and R4 are each hydrogen, a C1-6 alkyl, aralkyl, heteroaryl C1-6 alkyl, R12R13NC1-6 alkyl, or the like; and ring A is a heteroaryl ring, however, the heteroaryl ring is not thiophene), pharmaceutically acceptable salts thereof, pharmaceutical compositions containing the same, and the use thereof. These compounds have an excellent dopamine D2 receptor-stimulating effect and are therefore useful as agents for the treatment or prevention of Parkinson's disease and the like.
A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
C07D 209/30 - IndolesHydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
C07D 209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
89.
NOVEL OCTAHYDROPYRIDOQUINAZOLINE DERIVATIVE, PHARMACEUTICAL COMPOSITION CONTAINING SAME, AND USES FOR SAID DERIVATIVE AND COMPOSITION
[Problem] To provide a novel compound that exhibits an agonistic effect on dopamine D2 receptors. [Solution] A compound that can be represented by general formula (I) (in which R1 represents a C1-6 alkyl or the like; R2 represents hydrogen or the like; R3 and R4 each represent either hydrogen, a C1-6 alkyl, a R10R11N-C1-6 alkyl, an aralkyl, or the like; R5 and R6 each represent hydrogen or the like; and R7 represents hydrogen or the like) or a pharmacologically permitted salt thereof is provided, as are a pharmaceutical composition containing same and uses for said compound/salt and composition. This compound exhibits a superb stimulatory effect on dopamine D2 receptors and thus is useful as a therapeutic or prophylactic agent for Parkinson's disease and the like.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61P 5/06 - Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
Provided are an industrially useful method for producing a fused-heterocyclic derivative or salt thereof which is useful as a preventive agent, therapeutic agent, reproductive adjustment agent, contraceptive, ovulation-inducing agent, or sex-hormone-dependent-cancer-post-operation-recurrence preventive agent which target sex-hormone-dependent diseases and the like such as prostate enlargement, uterine myoma, endometriosis, uterine fibroma, precocious puberty, amenorrhea, premenstrual syndrome, dysmenorrhea, polycystic ovary syndrome, lupus erythematosus, hypertrichosis, dwarfism, sleep disorders, acne, baldness, Alzheimer's disease, infertility, irritable bowel syndrome, prostate cancer, uterine cancer, ovarian cancer, breast cancer, and pituitary tumors; and a production intermediate thereof. The present invention makes it possible to produce a compound or salt thereof represented by general formula (A) in high yield and purity by using a compound represented by general formula (D) (R1 and R2 represent identical or different C1-6 alkyl groups, and R3 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group, or a nitro group).
C07D 333/38 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 5/10 - Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH
A61P 5/24 - Drugs for disorders of the endocrine system of the sex hormones
A61P 13/08 - Drugs for disorders of the urinary system of the prostate
A61P 15/00 - Drugs for genital or sexual disordersContraceptives
A61P 15/08 - Drugs for genital or sexual disordersContraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
[Problem] To provide a novel compound having EP1 receptor antagonist activity. [Solution] A pyrazolopyridine derivative indicated by general formula (I) or a pharmacologically acceptable salt thereof was found to have powerful EP1 receptor antagonist activity. The compound (I) or a pharmacologically acceptable salt thereof is effective as a therapeutic medication or preventative medication for lower urinary tract symptoms (LUTS), for example, and for overactive bladder syndromes (OABs), etc., in particular. In addition, same are highly useful in the treatment, prevention, or suppression of a variety of conditions involving EP1 receptors, in addition to lower urinary tract symptoms (LUTS), (e.g., inflammatory conditions, painful conditions, osteoporosis, cancer, etc.).
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61P 13/02 - Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
A61P 19/10 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
[Problem] To provide a novel compound having EP1 receptor antagonist activity, or a pharmacologically acceptable salt thereof. [Solution] A benzene ring-fused, nitrogen-containing 5-membered heterocyclic compound indicated by general formula (I) or a pharmacologically acceptable salt thereof was found to have powerful EP1 receptor antagonist activity. The compound (I) or a pharmacologically acceptable salt thereof is effective as a therapeutic medication or preventative medication for lower urinary tract symptoms (LUTS), for example, and overactive bladder syndrome (OABs), etc., in particular. In addition, the compound (I) or a pharmacologically acceptable salt thereof is highly useful in the treatment, prevention, or suppression of a variety of conditions involving EP1 receptors, in addition to lower urinary tract symptoms (LUTS) (e.g., inflammatory conditions, painful conditions, osteoporosis, cancer, etc.).
C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
A61K 31/423 - Oxazoles condensed with carbocyclic rings
A61K 31/428 - Thiazoles condensed with carbocyclic rings
A61K 31/4355 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having oxygen as a ring hetero atom
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61P 13/02 - Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
A61P 13/10 - Drugs for disorders of the urinary system of the bladder
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 491/113 - Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
The present invention provides a compound represented by general formula (I), which has an EP1 receptor antagonist activity, or a pharmacologically acceptable salt thereof. The compound (I) of the present invention can be used as a therapeutic agent or prophylactic agent for LUTS, especially for various symptoms of OABs. (In the formula, A represents a pyridine ring or the like; Y1 represents a C1-6 alkylene group or the like; Y2 represents a single bond or the like; R1 represents a hydrogen atom or the like; R2 represents a C1-6 alkyl group; R3 represents a hydrogen atom or the like; R4 represents a hydrogen atom or the like; R5 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group or the like; R6 represents a C1-6 alkyl group, a C3-6 cycloalkyl group or the like; R7 represents a hydrogen atom or the like; X represents a methylene group; and Q represents a single bond or the like.)
C07D 209/18 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
A61K 31/4045 - Indole-alkylaminesAmides thereof, e.g. serotonin, melatonin
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61P 13/02 - Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
C07D 491/056 - Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
The present invention provides: a pyrazole derivative; a use of the pyrazole derivative for medical purposes; and others. More specifically, the present invention relates to a medicinal agent useful for the prevention or treatment of constipation, which comprises 3-(3-{4-[3-(β-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2-dimethylpropionamide or a pharmacologically acceptable salt thereof as an active ingredient. The medicinal agent according to the present invention has an activity of increasing stool frequency and the like and is therefore effective for the prevention or treatment of constipation.
A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
C07D 209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 209/30 - IndolesHydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 491/056 - Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
C07D 405/10 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
96.
Salt of fused heterocyclic derivative and crystal thereof
An objective of the present invention is to improve the solubility of 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid.
The present invention provides 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyl-oxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid choline salt has excellent solubility and storage stability.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61P 15/08 - Drugs for genital or sexual disordersContraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
Provided is a compound that is useful as a prophylactic or therapeutic agent for diseases or the like caused by an abnormal serum uric acid level. The present invention relates to a fused heterocyclic derivative represented by formula (I), a prodrug thereof or a salt thereof, said fused heterocyclic derivative exhibiting xanthine oxidase inhibitory activity and useful as a prophylactic or therapeutic agent for diseases caused by an abnormal serum uric acid level. In formula (I), ring U represents a C6-10 aryl group or the like; each R1 independently represents a hydrogen atom, a hydroxyl group, a C1-6 alkyl group or the like; m represents an integer of 1-2; ring Q represents a five-membered heteroaryl group; n represents an integer of 1-3; and each R2 independently represents a hydrogen atom, a halogen atom, a C1-6 alkyl group or the like.
C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents
A61P 43/00 - Drugs for specific purposes, not provided for in groups
Underactive bladder is such a clinical condition that urination disorder is developed as the result of the reduction in contraction of a detrusor muscle (a detrusor muscle of the bladder) during urination, is characterized by the feeling of having to urinate immediately, and is different from overactive bladder. The present invention provides a pharmaceutical composition useful for the prevention or treatment of underactive bladder. The present invention relates to a pharmaceutical composition for preventing or treating underactive bladder, which contains silodosin or a pharmacologically acceptable salt thereof as an active ingredient. This pharmaceutical composition has an effect of improving the urinary flow rate, an effect of improving the overdistension of the bladder (an effect of reducing a bladder capacity) and an effect of improving residual urine, and is therefore useful for the prevention or treatment of underactive bladder.
The present invention addresses the problem of providing a compound having human SGLT2 inhibitory activity, a prodrug of the compound, a pharmacologically acceptable salt of the compound, and a pharmaceutical use of the compound. The present invention provides a compound which is represented by general formula (1) (wherein RA represents a hydrogen atom, a C1-6 alkyl group or the like; RB represents a C1-6 alkoxy group or the like; each of RC and RD independently represents a hydrogen atom, a halogen atom or the like; and n represents a number of 1-3) and has human SGLT2 inhibitory activity, a prodrug of the compound, or a pharmacologically acceptable salt of the compound. In addition, the compound of the present invention can be utilized as a therapeutic or prophylactic agent for diseases associated with high blood sugar.
A61K 31/64 - Sulfonylureas, e.g. glibenclamide, tolbutamide, chlorpropamide
A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 43/00 - Drugs for specific purposes, not provided for in groups
100.
METHOD FOR PRODUCING BENZYLPYRAZOLE DERIVATIVE AND PRODUCTION INTERMEDIATE THEREOF
A production intermediate of a glucopyranosyloxypyrazole derivative which is represented by general formula (E) (wherein R3 and R4 are as defined below) and is useful as a therapeutic agent for diabetes or the like, and a method for producing a benzylpyrazole derivative, said method being indistrially more advantageous than conventional methods for producing a benzylpyrazole derivative, can be provided by causing a reaction of a compound represented by general formula (D) (wherein each of R1 and R2 represents a C1-6 alkyl group or the like; R3 represents a halogen atom, a C1-6 alkoxy group or the like; and R4 represents a hydrogen atom, a halogen atom, a C1-6 alkoxy group or the like).
C07D 317/30 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 231/20 - One oxygen atom attached in position 3 or 5
