The invention relates to methods of synthesizing 2′-deoxy-2′,2′-difluorotetrahydrouridine with increased purity and uniform particle size distribution. In particular, methods of the invention include crystallization and isolation procedures rendering synthetic reaction intermediates. The invention further includes compositions comprising the final compound in highly pure form, including lower number of impurities and lower levels of individual and total impurities.
The present disclosure relates to novel crystalline forms of sulfonamide compounds, pharmaceutical compositions containing the crystalline form compounds and methods of preparing and using the same.
C07D 271/113 - 1,3,4-OxadiazolesHydrogenated 1,3,4-oxadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
A61K 9/00 - Medicinal preparations characterised by special physical form
3.
PH-DEPENDENT ANTI-SULFATED GLYCOSAMINOGLYCAN ANTIBODY AND ANTIBODY-DRUG CONJUGATE
This invention provides an antibody that binds specifically to sulfated glycosaminoglycan (sGAG) in a pH-dependent manner. The antibody that binds specifically to sulfated glycosaminoglycan is at least one antibody selected from the group consisting of (1) to (3): an antibody comprising a heavy chain that comprises CDR1 consisting of the amino acid sequence represented by SEQ ID NO: 1, CDR2 consisting of the amino acid sequence represented by SEQ ID NO: 2, and CDR3 consisting of the amino acid sequence represented by SEQ ID NO: 3 and a fight chain that comprises CDR1 consisting of the amino acid sequence represented by SEQ ID NO: 4, CDR2 consisting of the amino acid sequence represented by LGS, and CDR3 consisting of the amino acid sequence represented by SEQ ID NO: 6; an antibody comprising a heavy chain that comprises CDR1 consisting of the amino acid sequence represented by SEQ ID NO: 7, CDR2 consisting of the amino acid sequence represented by SEQ ID NO: 8, and CDR3 consisting of the amino acid sequence represented by SEQ ID NO: 9 and a fight chain that comprises CDR1 consisting of the amino acid sequence represented by SEQ ID NO: 10, CDR2 consisting of the amino acid sequence represented by AAS, and CDR3 consisting of the amino acid sequence represented by SEQ ID NO: 12; and an antibody comprising a heavy chain that comprises CDR1 consisting of the amino acid sequence represented by SEQ ID NO: 13, CDR2 consisting of the amino acid sequence represented by SEQ ID NO: 14, and CDR3 consisting of the amino acid sequence represented by SEQ ID NO: 15 and a fight chain that comprises CDR1 consisting of the amino acid sequence represented by SEQ ID NO: 16, CDR2 consisting of the amino acid sequence represented by WAS, and CDR3 consisting of the amino acid sequence represented by SEQ ID NO: 18.
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 47/68 - 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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
In order to provide a novel cancer treatment method using a FTD-TPI combination drug that exhibits markedly excellent anti-tumor effects with fewer side effects, the present invention provides an anti-tumor agent characterized in that the FTD.TPI combination drug and a taxane compound are administered in combination.
A61K 31/7072 - 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 containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
5.
BRAIN-MIGRATING TUMOR TREATMENT AGENT CONTAINING, AS ACTIVE INGREDIENT, N-(4-(4-AMINO-6-ETHYNYL-5-(QUINOLIN-3-YL)-7H-PYRROLO[2,3-D]PYRIMIDIN-7-YL) BICYCLO[2.2.1]HEPTAN-1-YL)-5-METHYLPYRAZINE-2-CARBOXAMIDE OR SALT THEREOF
The present invention provides a brain-migrating anti-tumor agent that exhibits brain migration ability and EGFR inhibitory activity. One embodiment of the present invention provides a brain-migrating anti-tumor agent comprising, as an active ingredient, N-(4-(4-amino-6-ethynyl-5-(quinolin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl) bicyclo[2.2.1]heptan-1-yl)-5-methylpyrazine-2-carboxamide or a salt thereof.
The present invention provides a method for producing a compound represented by formula (I) suitable for mass synthesis as API. Provided according to one aspect of the present invention is a method for producing a compound represented by formula (I) or a salt thereof, the method including deprotecting a protecting group represented by R1 in formula (II) under basic conditions to thereby form a compound represented by formula (I) or a salt thereof.
Embodiments of the present invention provide solid oral dosage forms that upon daily administration to a subject provide plasma levels of decitabine with a 5-day AUC for decitabine that is equivalent to the 5-day AUC for a daily IV dose of decitabine of 20 mg/m2 administered as a one hour (1 h) infusion. Also provided according to embodiments of the present invention are solid oral dosage forms wherein upon daily administration to a subject provides a pharmacodynamic effect that is equivalent to the pharmacodynamic effect for a daily intravenous dose of decitabine of 20 mg/m2 administered as a one hour (1 h) infusion. Also provided are methods of treatment using a solid oral dosage form according to an embodiment of the invention.
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 9/00 - Medicinal preparations characterised by special physical form
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
A61K 31/20 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid
A61K 31/7016 - Disaccharides, e.g. lactose, lactulose
An object of the present disclosure is to provide a crystalline form of 3-(15-methoxypentadecyl)-2, 4, 4-trimethylcyclohex-2-en-1-one, the crystalline form having excellent stability and being preferable in terms of production. The present disclosure provides a crystalline form having characteristic peaks at diffraction angles) (2θ+0.2° of 7.0°, 14.0°, 17.5°, 19.5°, 21.0°, 23.7°, and 24.8° in a powder X-ray diffraction spectrum (CuKα).
Provided are a novel cancer treatment method and immunostimulant which exhibit a remarkably excellent antitumor effect with little side effects. An antitumor agent and an immunostimulant include an azabicyclo compound and an immune checkpoint molecule regulator which are administered in combination.
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 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
Provided is a method of treating malignant tumor by an azabicyclic compound, particularly, with eye disorder reduced. The present invention provides a method for treating malignant tumor, comprising administering an effective amount of 3-ethyl-4-[3-(1-methylethyl)-4-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-1H-pyrazolo[3,4-b]pyridin-1-yl]benzamide (compound 1) or a salt thereof to a patient in need thereof according to a dosing regimen, wherein the dosing regimen comprises administering the compound 1 or the salt thereof at a dose from 40 mg/body/day to 240 mg/body/day in terms of the amount of the compound 1 for consecutive days, and then providing a withdrawal period of at least 2 days.
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 9/00 - Medicinal preparations characterised by special physical form
This invention provides an antibody that binds specifically to sulfated glycosaminoglycan (sGAG) in a pH-dependent manner. The antibody that binds specifically to sulfated glycosaminoglycan is at least one antibody selected from the group consisting of (1) to (3): (1) an antibody comprising a heavy chain that comprises CDR1 consisting of the amino acid sequence represented by SEQ ID NO: 1, CDR2 consisting of the amino acid sequence represented by SEQ ID NO: 2, and CDR3 consisting of the amino acid sequence represented by SEQ ID NO: 3 and a light chain that comprises CDR1 consisting of the amino acid sequence represented by SEQ ID NO: 4, CDR2 consisting of the amino acid sequence represented by LGS, and CDR3 consisting of the amino acid sequence represented by SEQ ID NO: 6; (2) an antibody comprising a heavy chain that comprises CDR1 consisting of the amino acid sequence represented by SEQ ID NO: 7, CDR2 consisting of the amino acid sequence represented by SEQ ID NO: 8, and CDR3 consisting of the amino acid sequence represented by SEQ ID NO: 9 and a light chain that comprises CDR1 consisting of the amino acid sequence represented by SEQ ID NO: 10, CDR2 consisting of the amino acid sequence represented by AAS, and CDR3 consisting of the amino acid sequence represented by SEQ ID NO: 12; and (3) an antibody comprising a heavy chain that comprises CDR1 consisting of the amino acid sequence represented by SEQ ID NO: 13, CDR2 consisting of the amino acid sequence represented by SEQ ID NO: 14, and CDR3 consisting of the amino acid sequence represented by SEQ ID NO: 15 and a light chain that comprises CDR1 consisting of the amino acid sequence represented by SEQ ID NO: 16, CDR2 consisting of the amino acid sequence represented by WAS, and CDR3 consisting of the amino acid sequence represented by SEQ ID NO: 18.
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 47/68 - 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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
Provided is a novel method for treating cancer using an HSP90 inhibitor which exhibits a markedly superior antitumor effect and has a reduced side effect.
Provided is a novel method for treating cancer using an HSP90 inhibitor which exhibits a markedly superior antitumor effect and has a reduced side effect.
An antitumor agent is characterized in that an azabicyclo compound of the following Formula (1) or a salt thereof is administered in combination with other antitumor agent (s).
Provided is a novel method for treating cancer using an HSP90 inhibitor which exhibits a markedly superior antitumor effect and has a reduced side effect.
An antitumor agent is characterized in that an azabicyclo compound of the following Formula (1) or a salt thereof is administered in combination with other antitumor agent (s).
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 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/555 - Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 31/7068 - 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 containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
The present invention provides an antitumor agent for treating a malignant tumor patient expressing EGFR having at least one mutation selected from the group consisting of L718X mutation in exon 18 and L792X mutation in exon 20, wherein X represents an arbitrary amino-acid residue, the antitumor agent comprising (S)-N-(4-amino-6-methyl-5-(quinolin-3-yl)-8,9-dihydropy-rimido[5,4-b]indolizin-8-yl)acrylamide (Compound (A)) or a salt thereof.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; immunomodulators; immunosuppressive agents; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; immunomodulators; immunosuppressive agents; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders, pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood, pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders, pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood, pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders, pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood, pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders, pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood, pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders, pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood, pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders, pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood, pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; chemical reagents for medical purposes in the field of oncology
Provided is a pharmaceutical composition containing compound 1, the pharmaceutical composition having excellent disintegratability and bioavailability. The pharmaceutical composition comprises: a granulated product containing 3-ethyl-4-{4-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl}benzamide or a pharmaceutically acceptable salt thereof; and crystalline cellulose, and has a disintegration time of within 360 seconds in a coated tablet form.
A61K 9/36 - Organic coatings containing carbohydrates or derivatives thereof
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
Crystalline forms of N-(4-(4-amino-6-ethynyl-5-(quinolin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-7- yl)bicyclo[2.2.1]heptan-1-yl)-5-methylpyrazine-2-carboxamide (TAS3351), a compound having an inhibitory effect against EGFR and an acid. The crystalline forms have advantageous physical properties including stability, hygroscopicity, and oral absorption. The crystalline forms have peaks in a powder X-ray diffraction spectrum at specific diffraction angles (2θ ± 0.2°).
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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
The present disclosure relates to methods of treating a cancer in a subject in need thereof, comprising administering to the subject futibatinib or a pharmaceutically acceptable salt thereof, pembrolizumab or a pharmaceutically acceptable salt thereof, and at least one additional anti-cancer therapy agent or a pharmaceutically acceptable salt thereof. In some embodiments, the at least one additional anti-cancer therapy agent is a chemotherapeutic agent.
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 31/407 - 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 31/7115 - Nucleic acids or oligonucleotides having modified bases, i.e. other than adenine, guanine, cytosine, uracil or thymine
The present disclosure relates to methods of treating a cancer in a subject in need thereof, comprising administering to the subject futibatinib or a pharmaceutically acceptable salt thereof, pembrolizumab or a pharmaceutically acceptable salt thereof, and at least one additional anti-cancer therapy agent or a pharmaceutically acceptable salt thereof. In some embodiments, the at least one additional anti-cancer therapy agent is a chemotherapeutic agent.
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 31/407 - 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 31/7115 - Nucleic acids or oligonucleotides having modified bases, i.e. other than adenine, guanine, cytosine, uracil or thymine
The present disclosure relates to a juniper pollen protein selected from (a)-(c) below. (a) A protein comprising an amino acid sequence represented by SEQ ID NO: 2. (b) A protein comprising an amino acid sequence represented by SEQ ID NO: 2 with one or several amino acids substituted, deleted, or added, and having a juniper pollen allergen activity. (c) A protein having at least 90% amino acid identity with the amino acid sequence represented by SEQ ID NO: 2, and having a juniper pollen allergen activity.
The problem to be solved by the present invention is to provide a novel combination therapy exhibiting an excellent antitumor effect. The present invention provides an antitumor agent (that does not contain pemblolizumab as an active ingredient) that contains, as an active ingredient, futibatinib or a salt thereof that is administered to a cancer patient in combination with an immune checkpoint inhibitor (excluding CD155/TIGIT pathway antagonist) and at least one or more other antitumor agents.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
A61K 31/357 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
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 31/475 - QuinolinesIsoquinolines having an indole ring, e.g. yohimbine, reserpine, strychnine, vinblastine
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 31/7068 - 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 containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
A61K 31/7072 - 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 containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
A61K 31/7076 - 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 containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
The present invention addresses the problem of providing a novel combination therapy having an excellent antitumor effect. The present invention provides an antitumor agent that is administered to a cancer patient in combination with an immune checkpoint inhibitor (other than CD155/TIGIT pathway antagonist) and at least one other antitumor agent and that contains futibatinib or a salt thereof as an active ingredient (but does not contain pembrolizumab as an active ingredient).
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
A61K 31/357 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
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 31/475 - QuinolinesIsoquinolines having an indole ring, e.g. yohimbine, reserpine, strychnine, vinblastine
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 31/7068 - 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 containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
A61K 31/7072 - 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 containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
A61K 31/7076 - 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 containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
The present invention attempts to solve the problem of providing a novel combination therapy that exhibits an excellent antitumor effect. The present invention provides an antitumor agent (the antitumor agent does not contain pembrolizumab as an active ingredient) containing, as an active ingredient, futibatinib or a salt thereof that is administered to a cancer patient in combination with an immune checkpoint inhibitor (excluding CD155/TIGIT pathway antagonists) and at least one other antitumor agent.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
A61K 31/357 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
A61K 31/475 - QuinolinesIsoquinolines having an indole ring, e.g. yohimbine, reserpine, strychnine, vinblastine
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
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 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 31/7068 - 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 containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
A61K 31/7072 - 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 containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
A61K 31/7076 - 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 containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
An object of the present disclosure is to provide a crystalline form of 3-(15-methoxypentadecyl)-2,4,4- trimethylcyclohex-2-en-1-one, the crystalline form having excellent stability and being preferable in terms of production. The present disclosure provides a crystalline form having characteristic peaks at diffraction angles (20+0.2°) of 7.0°, 14.0°, 17.5°, 19.5°, 21.0°, 23.7°, and 24.8° in a powder X-ray diffraction spectrum (CuKa).
Provided is a novel method for treating castration resistant prostate cancer (CRPC), particularly CRPC that has acquired resistance to antiandrogen agents. This antitumor agent is characterized by the co-administration of an antiandrogen agent and 3-ethyl-4-{4-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl}benzamide or a salt thereof.
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 31/568 - 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 positions 10 and 13 by a chain having at least one carbon atom, e.g. androstane, testosterone
A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
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 45/00 - Medicinal preparations containing active ingredients not provided for in groups
05 - Pharmaceutical, veterinary and sanitary products
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Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; immunomodulators; immunosuppressive agents; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology
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Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; immunomodulators; immunosuppressive agents; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology
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Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; immunomodulators; immunosuppressive agents; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology
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Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; immunomodulators; immunosuppressive agents; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology
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Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; immunomodulators; immunosuppressive agents; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology.
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Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; immunomodulators; immunosuppressive agents; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology
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Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; immunomodulators; immunosuppressive agents; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology
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Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; immunomodulators; immunosuppressive agents; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology.
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Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology
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Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology.
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Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; anti-cancer preparations; tumor suppressing agents; pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of immune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for treating hematological disorders; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations; chemical reagents for medical purposes in the field of oncology.
45.
PROCESS FOR PREPARING A BENZOATE SALT OF A 1-(3-AMINOPYRROLIDINE-1-CARBONYL)-3,4-DIPHENYLBENZENE COMPOUND
A process for preparation of benzoate salt of 4-[5-[(3S)-3-aminopyrrolidine-1-carbonyl]-2-[2-fluoro-4-(2-hydroxy-2-methyl-propyl)phenyl]phenyl]-2-fluoro-benzonitrile, designated herein as Compound (A), and methods of using Compound (A) are provided. (I)
A process for preparation of benzoate salt of 4-[5-[(3S)-3-aminopyrrolidine-1-carbonyl]-2-[2-fluoro-4-(2-hydroxy-2-methyl-propyl)phenyl]phenyl]-2-fluoro-benzonitrile, designated herein as Compound (A), and methods of using Compound (A) are provided. (I)
C07C 67/48 - SeparationPurificationStabilisationUse of additives
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 31/4025 - 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
C07C 67/52 - SeparationPurificationStabilisationUse of additives by change in the physical state, e.g. crystallisation
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Anti-cancer preparations; pharmaceutical preparations for the treatment of tumor; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of immune disorders; pharmaceutical preparations for the treatment of hematological disorders.
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Anti-cancer preparations; pharmaceutical preparations for the treatment of tumor; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of immune disorders; pharmaceutical preparations for the treatment of hematological disorders
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Anti-cancer preparations; pharmaceutical preparations for the treatment of tumor; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of immune disorders; pharmaceutical preparations for the treatment of hematological disorders.
51.
TREATMENT METHODS FOR SUBJECTS WITH NON-SMALL CELL LUNG CANCER HAVING AN ABERRATION IN EGFR
A method of treating a subject with a cancer having at least one aberration in EGFR, whereby the subject is administered (S)-N-(4-amino-6-methyl-5-(quinolin-3-yl)-8,9-dihydropyrimido[5,4-b]indolizin-8-yl)acrylamide (also known as zipalertinib and as TAS6417) or a pharmaceutically acceptable salt thereof, to a subject who has previously been treated with a molecularly targeted therapeutic. The molecularly targeted therapeutic may be an EGFR-targeting therapeutic other than Compound (1) or a non-EGFR-targeting therapeutic. The method may optionally involve administering to the subject an additional therapeutic agent.
A method of treating a subject with cancer having a dysregulated MAPK and/or PI3K pathway, whereby the subject is administered an effective amount of 4-(4-(3-((2-(tert-butylamino)ethyl)amino)-6-(5-(trifluoromethyl)-1,3,4-oxadiazol-2-yl)pyridin-2-yl)piperidin-1-yl)-5,5-dimethyl-5H-pyrolo[2,3-d]pyrimidin-6(7H)-one or a pharmaceutically acceptable salt thereof.
The present invention addresses the problem of providing a crystal of a compound having EGFR inhibition ability or a salt thereof, said crystal being excellent in the characteristic of stability (heat, purity) and/or low hygroscopicity. One aspect of the present invention provides a crystal form of (S)-N-(4-amino-6-methyl-5-(quinolin-3-yl)-8,9-dihydropyrimido[5,4-b]indolizin-8-yl)acrylamide that has a peak at a prescribed angle as the diffraction angle (2θ±0.2°) in a powder X-ray diffraction spectrum.
In one embodiment, the present invention provides an antibody specifically binding to human GH or an antigen-binding fragment thereof. In one embodiment, the present invention relates to an antibody specifically binding to human GH or an antigen-binding fragment thereof, comprising a heavy chain variable region (VH) and a light chain variable region (VL), wherein the VH comprises an amino acid sequence set forth in SEQ ID NO: 5 as a VH complementarity-determining region (CDR) 1 (VHCDR1), an amino acid sequence set forth in SEQ ID NO: 6 as a VHCDR2, and an amino acid sequence set forth in SEQ ID NO: 7 as a VHCDR3, and the VL comprises an amino acid sequence set forth in SEQ ID NO: 8 as a VL complementarity-determining region (CDR) 1 (VLCDR1), an amino acid sequence set forth in SEQ ID NO: 9 as a VLCDR2, and an amino acid sequence set forth in SEQ ID NO: 10 as a VLCDR3.
The purpose of the present invention is to provide a pharmaceutical composition containing naproxen or a salt thereof and acetaminophen or a salt thereof and having excellent storage stability. For this purpose, provided is a composition in which at least one selected from the group consisting of a specific basic compound and glycine or a salt thereof is used.
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
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Pharmaceutical preparations for use in dermatology, wounds, treating diabetes, analgesics, eye-wash, febrifuges, hemorrhoid preparations, plasters for medical purposes, skincare, digestives, ointment, cold symptoms, athlete's foot; medicinal drinks; tonics in the nature of medicines for the improvement of poor appetite, gastroenteric weakness, poor blood circulation, chills, fatigue, weak constitution and weakness following disease; vitamin preparations; nutritional preparations for medical use in the nature of nutritional supplements; nutritional additives for medical purposes; nutritional food supplements for medical purposes in the nature of natural food extracts derived from fish, meat and vegetables; food supplements for medical purposes for humans; dental materials in the nature of medicated toothpastes; bracelets for medical purposes; oiled paper for medical purposes; sanitary masks; pharmaceutical wafer in the nature of drug delivery agents in the form of edible wafers for wrapping powdered pharmaceuticals; gauze for dressings; capsules sold empty for pharmaceutical purposes; capsules for medicines for the treatment of cardiovascular disorders; eye patches for medical purposes; ear bandages; incontinence diapers; semen for artificial insemination; menstruation bandages; menstruation tampons; sanitary napkins; menstruation pads; sanitary pads; sanitary panties; sanitary knickers; menstruation knickers; absorbent cotton for medical purposes; absorbent wadding for medical purposes; lacteal flour for babies; milk sugar for medical purposes being lactose; fly catching paper; adhesive plaster for medical purposes; court plaster; sticking plasters for medical use; bandages for dressings; collodion for pharmaceutical purposes; mothproofing paper; breast-nursing pads; dietetic foods adapted for medical purposes; dietetic beverages adapted for medical purposes
58.
SMALL MOLECULE INHIBITORS OF KRAS MUTATED PROTEINS
Compounds of Formula (I) or their pharmaceutically acceptable salts can inhibit the G12C, G12D and/or G12V mutants of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
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
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 31/554 - 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 sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
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
59.
PROPHYLACTIC DRUG/THERAPEUTIC DRUG FOR PROGRESSIVE SUPRANUCLEAR PALSY
Provided is a novel prophylactic drug and/or a novel therapeutic drug useful for progressive supranuclear palsy (PSP), the prophylactic drug and/or the therapeutic drug containing, as an active ingredient, a growth arrest and DNA damage-inducible protein 34 (GADD34) inhibitor including guanabenz that is a compound represented by formula [I-1].
A61K 31/4706 - 4-Aminoquinolines8-Aminoquinolines, e.g. chloroquine, primaquine
A61P 25/00 - Drugs for disorders of the nervous system
A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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
Provided is an antibody-drug conjugate (ADC) that specifically binds to CD138 and exhibits an excellent antitumor effect. In the ADC, monomethyl auristatin E is bound via a linker to an anti-CD138 antibody having a specific amino acid sequence.
A61K 47/68 - 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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
Provided are: an anti-tumor agent having a high anti-tumor effect and fewer side effects; and others. The present invention relates to: a combination preparation containing trifluridine and tipiracil hydrochloride at a molar ratio of 1:0.5; an anti-tumor agent containing a PD-1 pathway antagonist, which is used in such a manner that the anti-tumor agent is administered in combination with a VEGF pathway antagonist; and others.
A61K 31/7072 - 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 containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
A61P 43/00 - Drugs for specific purposes, not provided for in groups
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
C07H 19/073 - Pyrimidine radicals with 2-deoxyribosyl as the saccharide radical
05 - Pharmaceutical, veterinary and sanitary products
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Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
63.
TREATMENT METHODS FOR SUBJECTS WITH CANCER HAVING AN ABERRATION IN EGFR AND/OR HER2
A method of treating a subject with cancer having an aberration in EGFR and/or HER2, whereby the subject is administered 7-((3R,5S)-1-acryloyl-5-methylpyrrolidin-3-yl)-4-amino-6-(cyclopropylethynyl)-N—((R)-1-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carboxamide or a pharmaceutically acceptable salt thereof.
Forms of 4-[5-[(3S)-3-aminopyrrolidine-1-carbonyl]-2-[2-fluoro-4-(2-hydroxy-2-methyl-propyl)phenyl]phenyl]-2-fluoro-benzonitrile, designated herein as Compound I, were prepared and characterized in the solid state. Also provided are processes of manufacture and methods of using the forms of Compound I.
C07D 207/14 - Nitrogen atoms not forming part of a nitro radical
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
The present invention provides I form crystals of 4-piperidinyl 2,2-diphenyl-2-(propoxy-1,1,2,2,3,3,3-d7)acetate hydrochloride having at least one diffraction angle (2θ±0.2°) selected from group (a) below and at least one diffraction angle (2θ±0.2°) selected from group (b) below in a powder x-ray diffraction spectrum (CuKα). (a) 11.3°, 11.4°, and 17.2° (b) 12.7°, 15.9°, 16.1°, 20.5°, 20.7°, 23.1°, 23.2°, 25.9°, and 28.4°
The present invention provides a substituted polypeptide having the effect of inhibiting MMP2 and represented by formula [I′], or a pharmaceutically acceptable salt thereof.
The present invention provides a substituted polypeptide having the effect of inhibiting MMP2 and represented by formula [I′], or a pharmaceutically acceptable salt thereof.
A method of treating a subject with cholangiocarcinoma having a co-occurring genetic alteration in FGFR2 and a cancer driver gene selected from TP53, BAP1, ARID1A, MLL2, PIK3C2B, IKBKE, MCL1, MDM4, and MYC, whereby the subject is administered (S)-1-[(3)-[4-amino-3-[(3,5-dimethoxyphenyl)ethynyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-pyrrolidinyl]-2-propen-1-one or a pharmaceutically acceptable salt thereof.
C12Q 1/6886 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
68.
COMBINATION THERAPY USING AZABICYCLO COMPOUND FOR CANCER
Provided is a novel method for treating cancer using an HSP90 inhibitor which exhibits a markedly superior antitumor effect and has a reduced side effect.
Provided is a novel method for treating cancer using an HSP90 inhibitor which exhibits a markedly superior antitumor effect and has a reduced side effect.
An antitumor agent is characterized in that an azabicyclo compound of the following Formula (1) or a salt thereof is administered in combination with other antitumor agent(s).
Provided is a novel method for treating cancer using an HSP90 inhibitor which exhibits a markedly superior antitumor effect and has a reduced side effect.
An antitumor agent is characterized in that an azabicyclo compound of the following Formula (1) or a salt thereof is administered in combination with other antitumor agent(s).
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 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/555 - Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 31/7068 - 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 containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
A method for treating cancer in patients with creatinine clearance of 15 mL/min or more and less than 30 mL/min, including dividing a combination drug containing α,α,α-trifluorothymidine (FTD) and 5-chloro-6-[(2-iminopyrrolidine-1-yl)methyl]pyrimidine-2,4(1H,3H)-dione hydrochloride in a molar ratio of 1:0.5, in a dose of 30 to 40 mg/m2/day as FTD-equivalent, into two to four times a day, and orally administering it to the patient.
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/7072 - 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 containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
An antitumor agent comprising a compound selected from the group consisting of Compounds A to D described in the specification, or a salt thereof, for treating a malignant tumor patient expressing EGFR having exon 20 insertion mutation.
A method of treating a subject with a cancerous tumor exhibiting an inactivating mutation in the PTEN gene including administering to the subject trans-3-amino-1-methyl-3-(4-(3-phenyl-5H-imidazo[1,2-c]pyrido[3,4-e][1,3]oxazin-2-yl)phenylcyclobutanol or a pharmaceutically acceptable salt thereof.
A61K 31/5365 - 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 heterocyclic ring systems
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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 31/7072 - 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 containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
05 - Pharmaceutical, veterinary and sanitary products
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Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Pharmaceutical, veterinary and sanitary products
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Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Pharmaceutical, veterinary and sanitary products
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Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Pharmaceutical, veterinary and sanitary products
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Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Pharmaceutical, veterinary and sanitary products
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Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Pharmaceutical, veterinary and sanitary products
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Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Pharmaceutical, veterinary and sanitary products
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Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
05 - Pharmaceutical, veterinary and sanitary products
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Pharmaceutical preparations for the treatment of tumor; pharmaceutical preparations for the treatment of cancer; chemical reagents for medical purposes in the field of oncology; pharmaceutical preparations for the treatment of cardiovascular diseases and disorders; pharmaceutical preparations for the treatment of respiratory diseases and disorders; pharmaceutical preparations for the treatment of dermatological diseases and disorders; pharmaceutical preparations for the treatment of muscular diseases and disorders; pharmaceutical preparations for the treatment of urological diseases and disorders; pharmaceutical preparations for the treatment of digestive diseases and disorders; pharmaceutical preparations for the treatment of gastroesophageal reflux diseases and disorders; pharmaceutical preparations for the treatment of hepatic diseases and disorders; pharmaceutical preparations for the treatment of renal diseases and disorders; pharmaceutical preparations for the treatment of autoimmune diseases and disorders; pharmaceutical preparations for the treatment of diseases of the central and peripheral nervous system; pharmaceutical preparations for the treatment of rheumatoid arthritis; pharmaceutical preparations for the treatment of diseases of the blood; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for use in chemotherapy; anti-emetic medicines; pharmaceutical preparations for the treatment of pain; analgesic preparations; antiphlogistic preparations
81.
BRAIN-MIGRATING TUMOR THERAPEUTIC AGENT CONTAINING FUSED PYRIMIDINE COMPOUND AS ACTIVE INGREDIENT
An object to be solved of the present invention is to provide a brain-penetrable antitumor agent showing an excellent brain penetration property and RET inhibitory activity.
An object to be solved of the present invention is to provide a brain-penetrable antitumor agent showing an excellent brain penetration property and RET inhibitory activity.
The present invention provides brain-penetrable antitumor agent including a compound represented by Formula (I) below or a salt thereof as an active ingredient:
An object to be solved of the present invention is to provide a brain-penetrable antitumor agent showing an excellent brain penetration property and RET inhibitory activity.
The present invention provides brain-penetrable antitumor agent including a compound represented by Formula (I) below or a salt thereof as an active ingredient:
An object to be solved of the present invention is to provide a brain-penetrable antitumor agent showing an excellent brain penetration property and RET inhibitory activity.
The present invention provides brain-penetrable antitumor agent including a compound represented by Formula (I) below or a salt thereof as an active ingredient:
wherein R1, R2, and R3 are as described in Specification.
Crystalline Forms of 4-amino-N-[4-(methoxymethyl)phenyl]-7-(1-methylcyclopropyl)-6-(3-morpholinoprop-1-yn-1-yl)-7H-pyrrolo[2,3-d]pyrimidine-5-carboxamide
Provided herein are various crystalline forms of 4-amino-N-[4-(methoxymethyl)phenyl]-7-(1-methylcyclopropyl)-6-(3-morpholinoprop-1-yn-1-yl)-7H-pyrrolo[2,3-d]pyrimidine-5-carboxamide, methods of producing same, and methods of using same to for RET inhibition.
Provided is a type-I crystal of a free form of 4-(4-(3-((2-(tert-butylamino)ethyl)amino)-6-(5-(trifluoromethyl)-1,3,4-oxadiazol-2-yl)piperidin-2-yl)piperidin-1-yl)-5,5-dimethyl-5H-pyrrolo[2,3-d]pyrimidin-6(7H)-one that has, in a powder X-ray diffraction spectrum (CuKα), peaks at at least two diffraction angles (2θ±0.2°) selected from the following (a) and at least two diffraction angles (2θ±0.2°) selected from the following (b). (a) 6.2°, 9.3°, 9.7°, 11.1°, 15.4°, and 25.1° (b) 6.7°, 8.3°, 8.7°, 13.0°, 13.7°, 16.3°, 16.9°, 17.7°, 18.7°, 19.4°, 20.3°, 25.9°, and 26.5°
Methods of Using 4-Amino-N-[4-(Methoxymethyl)Phenyl]-7-(1-Methylcyclopropyl)-6-(3-Morpholinoprop-1-YN-1-YL)-7H-Pyrrolo[2,3-D]Pyrimidine-5-Carboxamide for the Treatment of Tumors
The present invention relates to compositions and methods for treating patients with cancer having a RET gene abnormality comprising administering HM06/TAS0953, for example patients with non-small cell lung cancer (NSCLC), and that may also have brain and/or leptomeningeal metastases, or another solid tumor; where the patient is administered an effective amount of HM06/TAS0953, where the HM06/TAS0953 can be formulated in a composition and administered orally in a single or multiple doses; and where the patients may have previously received and/or have developed resistance to another RET-selective or multi-kinase inhibitor.
Provided are novel compounds which are analogues to be removed from APIs and formulations. Also provided are standard products of analogues to be used in controlling the qualities of medicines. Analogue 1: 3-ethyl-4-\{4-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-3,3'-di(propan-2-yl)-1'H-[1,4'-bipyrazolo[3,4-b]pyridin]-1'-yl\}benzamide. Analogue 2: 3-ethyl-4-fuluorobenzamide. Analogue 3: N-[1-(4-carbamoyl-2-ethylphenyl)-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-4-yl]-3-ethyl-4-\{4-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl\}benzamide. Analogue 4: 3-ethyl-4-\{14-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-13,23,33-tri(propan-2-yl)-31H-[11,24:21, 34-terpyrazolo[3,4-b]pyridin]-31-yl\}benzamide. Analogue 5: 4,4'-(1H,1'H-[4,4'-biimidazol]-1,1'-diylbis\{[3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-4,1-diyl]\})bis(3-ethylbenzamide). Analogue 6: 4-\{4,6-bis[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin]-1-yl\}-3-ethylbenzonitrile. Analogue 7: 4-\{4,6-bis[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl\}-3-ethylbenzamide. Analogue 8: 4-[4-ethoxy-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl]-3-ethylbenzamide. Analogue 9: 3-ethyl-4-[4-methoxy-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl]benzamide.
C07C 233/65 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
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 31/437 - 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
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
Provided is a pharmaceutical composition containing compound 1 and having excellent disintegrability and bioavailability. This pharmaceutical composition contains crystalline cellulose and a granulated substance containing 3-ethyl-4-{4-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-3-(propan-2-yl)-1H-pyrazolo[3,4-b]pyridine-1-yl}benzamide or a pharmaceutically acceptable salt thereof, and has a disintegration time of 360 seconds or less in a coated tablet state.
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 9/36 - Organic coatings containing carbohydrates or derivatives thereof
The present invention provides a pharmaceutical composition for preventing and/or treating an RNR-related disease in a patient in need thereof, wherein the pharmaceutical composition comprises 5-chloro-2-(N-((1S,2R)-2-(6-fluoro-2,3-dimetylphenyl)-1-(5-oxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)propyl)sulfamoyl)benzamide or a salt thereof, and is administered to the patient on an intermittent administration schedule for two weeks comprising dosing 1 to 5 days per week. The present invention also provides a method of treating an RNR-related diseases in a patient in need thereof, the method comprising administering an effective amount of 5-chloro-2-(N-((1S,2R)-2-(6-fluoro-2,3-dimetylphenyl)-1-(5-oxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)propyl)sulfamoyl)benzamide or a salt thereof to the patient on an intermittent administration schedule for two weeks comprising dosing 1 to 5 days per week.
The present invention relates to a compound having inhibitory activity against KRAS G12D mutation or a salt thereof, and relates to a pharmaceutical composition comprising the compound as an active ingredient.
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
The present invention provides a pharmaceutical composition for preventing and/or treating an RNR-related disease in a patient in need thereof, wherein the pharmaceutical composition comprises 5-chloro-2-(N-((1S,2R)-2-(6-fluoro-2,3-dimetylphenyl)-1-(5-oxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)propyl)sulfamoyl)benzamide or a salt thereof, and is administered to the patient on an administration schedule comprising continuous, daily dosing for one week, followed by a resting period of one week. The present invention also provides a method of treating an RNR-related diseases in a patient in need thereof, the method comprising administering an effective amount of 5-chloro-2-(N-((1S,2R)-2-(6-fluoro-2,3-dimetylphenyl)-1-(5-oxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)pr opyl)sulfamoyl)benzamide or a salt thereof to the patient on an administration schedule comprising daily dosing for one week, followed by a resting period of one week.
Provided is a novel therapeutic agent useful for the prevention or treatment of lung inflammation and fibrosis, the agent containing, as an active ingredient, a compound which has an MMP2 inhibitory activity and is represented by formula [IX], or a pharmaceutically acceptable salt thereof.
Provided is a crystal of a compound having EGFR inhibition ability or a salt thereof, said crystal being excellent in one or more characteristics of stability, hygroscopicity and oral absorbability. One aspect of the present invention provides a crystal form of N-(4-(4-amino-6-ethynyl-5-(quinolin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)bicyclo[2.2.1]heptan-1-yl)-5-methylpyrazine-2-carboxamide the diffraction angle (2θ±0.2°) of which has a peak at a preset angle in the X-ray powder diffraction spectrum.
A crystal of 7-((3R,5S)-1-acryloyl-5-methylpyrrolidin-3-yl)-4-amino-6-(cyclopropylethynyl)-N-((R)-1-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carboxamide (compound (I)), and a crystal thereof with an acid (salt crystal or co-crystal) are provided.
A crystal of 7-((3R,5S)-1-acryloyl-5-methylpyrrolidin-3-yl)-4-amino-6-(cyclopropylethynyl)-N-((R)-1-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carboxamide (compound (I)), and a crystal thereof with an acid (salt crystal or co-crystal) are provided.
There are provided: a type II crystal of compound (I) with fumaric acid, having characteristic peaks at three or more diffraction angles (2θ ± 0.2 °) selected from 5.5°, 6.8°, 9.3°, 13.4°, 15.3°, 16.3°, 18.5°, 19.8°, 22.0°, and 24.5° in a powder X-ray diffraction spectrum;
a (free-form) type II crystal of compound (I) having characteristic peaks at three or more diffraction angles selected from 8.3°, 14.8°, 17.3°, 18.0°, 19.1°, 20.3°, 21.0°, 22.5°, 23.0°, and 26.2° in a powder X-ray diffraction spectrum;
a (free-form) type I crystal of compound (I) having characteristic peaks at three or more diffraction angles selected from 9.9°, 11.7°, 13.2°, 17.7°, 18.1°, 18.8°, and 20.8° in a powder X-ray diffraction spectrum;
a type V crystal of compound (I) with fumaric acid, having characteristic peaks at four or more diffraction angles selected from 6.9°, 9.4°, 10.2°, 13.7°, 21.1°, 23.6°, and 26.5° in a powder X-ray diffraction spectrum; and
a type I crystal of compound (I) with fumaric acid, having characteristic peaks at four or more diffraction angles selected from 6.4°, 10.3°, 12.8°, 15.0°, 20.7°, 23.4°, and 26.6° in a powder X-ray diffraction spectrum.
Provided is an antibody that exhibits pH dependence and specifically binds to a sulfated glycosaminoglycan (sGAG). An antibody specifically binding to a sulfated glycosaminoglycan that is at least one selected from the group consisting of the following (1) to (3): (1) an antibody that contains a heavy chain having CDR1 comprising an amino acid sequence represented by SEQ ID NO: 1, CDR2 comprising an amino acid sequence represented by SEQ ID NO: 2 and CDR3 comprising an amino acid sequence represented by SEQ ID NO: 3, and a light chain having CDR1 comprising an amino acid sequence represented by SEQ ID NO: 4, CDR2 comprising an amino acid sequence represented by LGS and CDR3 comprising an amino acid sequence represented by SEQ ID NO: 6; (2) an antibody that contains a heavy chain having CDR1 comprising an amino acid sequence represented by SEQ ID NO: 7, CDR2 comprising an amino acid sequence represented by SEQ ID NO: 8 and CDR3 comprising an amino acid sequence represented by SEQ ID NO: 9, and a light chain having CDR1 comprising an amino acid sequence represented by SEQ ID NO: 10, CDR2 comprising an amino acid sequence represented by AAS and CDR3 comprising an amino acid sequence represented by SEQ ID NO: 12; and (3) an antibody that contains a heavy chain having CDR1 comprising an amino acid sequence represented by SEQ ID NO: 13, CDR2 comprising an amino acid sequence represented by SEQ ID NO: 14 and CDR3 comprising an amino acid sequence represented by SEQ ID NO: 15, and a light chain having CDR1 comprising an amino acid sequence represented by SEQ ID NO: 16, CDR2 comprising an amino acid sequence represented by WAS and CDR3 comprising an amino acid sequence represented by SEQ ID NO: 18.
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 47/68 - 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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
The invention relates to methods of synthesizing 2′-deoxy-2′,2′-difluorotetrahydrouridine with increased purity and uniform particle size distribution. In particular, methods of the invention include crystallization and isolation procedures rendering synthetic reaction intermediates. The invention further includes compositions comprising the final compound in highly pure form, including lower number of impurities and lower levels of individual and total impurities.
The present invention addresses the problem of providing: an injectable formulation that contains fosnetupitant or a pharmaceutically acceptable salt in a stable form as a medicinal product; and a method for producing the same. The present invention provides an injectable formulation containing a) fosnetupitant or a pharmaceutically acceptable salt thereof, b) trehalose, and c) a nonionic surfactant.
Provided are a compound represented by formula (I) or a salt thereof, a nerve growth promoter containing the compound or a salt thereof as an active ingredient, a pharmaceutical composition containing the compound or a salt thereof, a therapeutic agent for neurodegenerative diseases containing the compound or a salt thereof as an active ingredient, a therapeutic agent for amyotrophic lateral sclerosis containing the compound or a salt thereof as an active ingredient, a therapeutic agent for pain containing the compound or a salt thereof as an active ingredient, and a therapeutic agent for lower urinary tract dysfunction containing the compound or a salt thereof as an active ingredient.
Provided is a therapeutic agent for a disease associated with EGFR, the agent comprising a compound that has EGFR inhibitory activity and has brain penetration properties as an active ingredient. The present invention provides a compound represented by the formula (I) wherein R1, R2, R3, R4 and R5 are as defined in the present specification, or a salt thereof, and a therapeutic agent for a disease associated with EGFR, the agent comprising a compound represented by the following formula (I), or a salt thereof as an active ingredient.
Provided is a therapeutic agent for a disease associated with EGFR, the agent comprising a compound that has EGFR inhibitory activity and has brain penetration properties as an active ingredient. The present invention provides a compound represented by the formula (I) wherein R1, R2, R3, R4 and R5 are as defined in the present specification, or a salt thereof, and a therapeutic agent for a disease associated with EGFR, the agent comprising a compound represented by the following formula (I), or a salt thereof as an active ingredient.
2 administered as a one hour (1 h) infusion. Also provided are methods of treatment using a solid oral dosage form according to an embodiment of the invention.
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 9/00 - Medicinal preparations characterised by special physical form
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
A61K 31/20 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid
A61K 31/7016 - Disaccharides, e.g. lactose, lactulose
