The present invention relates to multiple crystalline forms of a pharmaceutically acceptable salt of a compound N-cyclopropyl-5-(4-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl)picolinamide, a preparation method therefor, and a use thereof in medicine.
The present invention relates to a crystal form of a compound N-cyclopropyl-5-(4-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl)pyridine carboxamide and a preparation method therefor, and the use thereof in the preparation of a related drug.
The present invention relates to a compound represented by general formula (I) or a stereoisomer, a deuterated product, a solvate, a prodrug, a metabolite, a pharmaceutically acceptable salt, or a co-crystal thereof, an intermediate thereof, and use thereof in AR-related diseases such as cancer. B-L-K (I)
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
The present invention relates to a compound as represented by general formula (A) or a stereoisomer, a deuterated substance, a solvate, a prodrug, a metabolite, a pharmaceutically acceptable salt or a cocrystal thereof, an intermediate thereof, a preparation method therefor, and the use thereof in the preparation of a drug for treating diseases related to PARP7 activity or expression quantity.
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
5.
SUSTAINED-RELEASE PHARMACEUTICAL FORMULATION OF FUSED TRICYCLIC ?-AMINO ACID DERIVATIVE AND PREPARATION METHOD THEREFOR
Disclosed are a sustained-release pharmaceutical formulation of a fused tricyclic γ-amino acid derivative and a preparation method therefor. The fused tricyclic γ-amino acid derivative is a compound represented by formula (I) or a stereoisomer, a solvate, a prodrug, a metabolite, a pharmaceutically acceptable salt or a eutectic crystal thereof.
Disclosed are a sustained-release pharmaceutical formulation of a fused tricyclic γ-amino acid derivative and a preparation method therefor. The fused tricyclic γ-amino acid derivative is a compound represented by formula (I) or a stereoisomer, a solvate, a prodrug, a metabolite, a pharmaceutically acceptable salt or a eutectic crystal thereof.
A preparation method for a 2-aminopyridine derivative and an intermediate thereof, i.e., a preparation method for a compound shown in formula (VII) and an intermediate thereof. The method is mild in reaction conditions, simple to operate, high in reaction yield, high in product purity, convenient to post-treat, and suitable for industrial production.
C07F 7/10 - Compounds having one or more C—Si linkages containing nitrogen
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
7.
PHARMACEUTICAL COMPOSITION FOR INJECTION COMPRISING CYCLIC LACTAM COMPOUND AND METHOD FOR PREPARING SAME
Disclosed are a pharmaceutical composition for injection comprising a cyclic lactam compound (I), a method for preparing the pharmaceutical composition for injection, and use of the pharmaceutical composition in preparing a medicament for treating a disease or condition related to factor XIa.
A61K 31/122 - Ketones having the oxygen atom directly attached to a ring, e.g. quinones, vitamin K1, anthralin
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
A nitrogen-containing heterocyclic compound represented by formula (I-c), or a stereoisomer, a deuterated compound or a pharmaceutically acceptable salt, and a pharmaceutical composition thereof. Also provided is a use of the compound in the preparation of a drug for treating a DNA polymerase θ-mediated disease. Each group in formula (I-c) is as defined in the description.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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
Disclosed is a preparation method of a nitrogen-containing heterocyclic compound represented by formula (I). The method comprises: carrying out a coupling reaction on a compound 1A and a compound 2a, and sequentially carrying out deprotection, amidation and deprotection reactions, which are four steps in total, to obtain a target compound. The method is short in reaction route, mild in condition, simple to operate, convenient in post-treatment, high in yield and high in purity, and is suitable for industrial amplification production.
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 267/10 - Seven-membered rings having the hetero atoms in positions 1 and 4 not condensed with other rings
10.
DIPEPTIDYL PEPTIDASE 1 INHIBITOR POLYMORPH, PREPARATION METHOD AND USE THEREFOR
Disclosed in the present invention are a polymorph of a compound as shown in formula I, and a preparation method and use therefor. The polymorph of the present invention comprises a crystal form B, a crystal form C, and a crystal form D. The polymorph has excellent characteristics of high purity, good solubility, stable physical and chemical properties, high temperature resistance, high humidity, strong illumination, low hygroscopicity, etc.
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 267/10 - Seven-membered rings having the hetero atoms in positions 1 and 4 not condensed with other rings
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
A61P 11/00 - Drugs for disorders of the respiratory system
11.
SALT AND CRYSTAL FORM OF DIPEPTIDYL PEPTIDASE INHIBITOR COMPOUND
Disclosed are a crystal of the compound (S)-N-((S)-1-cyano-2-(2-fluoro-4-(3-methyl-2-oxo-2,3-dihydrobenzo[d]oxazole-5-yl)phenyl)ethyl)-1,4-oxazacycloheptane-2-carboxamide salt or a salt thereof, a preparation method therefor, and the uses thereof in pharmaceutical compositions and in medicine.
C07D 267/10 - Seven-membered rings having the hetero atoms in positions 1 and 4 not condensed with other rings
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
A61P 11/00 - Drugs for disorders of the respiratory system
12.
PYRAZOLOPYRIDINE DERIVATIVE AND APPLICATION THEREOF IN MEDICINE
The present invention relates to the compound shown in general formula (I) or to a stereoisomer, tautomer, deuterated substance, solvate, prodrug, metabolite, pharmaceutically-acceptable salt or eutectic crystal thereof, and to an intermediate and a preparation method thereof, and also to an application thereof in the preparation of a medicine for treating diseases related to USP1 activity or expression.
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 31/4353 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
A61K 31/435 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
A61K 31/438 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 487/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups in which the condensed system contains four or more hetero rings
C07D 487/12 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups in which the condensed system contains three hetero rings
C07D 471/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups in which the condensed systems contains four or more hetero rings
C07D 471/02 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups in which the condensed system contains two hetero rings
C07D 471/12 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups in which the condensed system contains three hetero rings
C07D 401/02 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
The present invention relates to a compound represented by general formula (I) or a stereoisomer, a tautomer, a deuterated substance, a solvate, a prodrug, a metabolite and a pharmaceutically acceptable salt or eutectic crystal thereof, an intermediate thereof, and a use of the compound in METTL3-related diseases such as cancer.
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61P 35/02 - Antineoplastic agents specific for leukemia
Provided are a preparation method of a pyridazinone derivative, an intermediate thereof, and a preparation method of the intermediate. The method has the advantages of easily available raw materials, simple steps, low costs, good intermediate stability, high purity and high yield, and is suitable for large-scale industrial production.
Disclosed in the present invention are a polymoroh of a compound of formula I (R)-2-(3,5-dichloro-4-((7-(methyl-d3)-1-oxo-2,5,6,7-tetrahydro-1H-cyclopenta[d] pyridazin-4-yl)oxy)phenyl)-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile, a preparation method, pharmaceutical composition, and pharmaceutical use therefor.
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
The present invention relates to a compound as represented by general formula (I) or a stereoisomer, a tautomer, a deuterated substance, a solvate, a prodrug, a metabolite, a pharmaceutically acceptable salt, or an eutectic thereof, an intermediate thereof, a preparation method therefor, and an application in the preparation of a pharmaceutical for treating a disease related to USP1 activity or expression.
The present invention relates to a compound represented by general formula (I), or stereoisomers, deuterated substances, solvates, prodrugs, metabolites, pharmaceutically acceptable salts or eutectic crystals thereof, an intermediate thereof, and the use thereof in BRD9-related diseases such as cancer. B-L-K (I)
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
The present invention relates to a compound represented by general formula (I) or a stereoisomer, a tautomer, a deuterated substance, a solvate, a prodrug, a metabolite, a pharmaceutically acceptable salt, or a eutectic thereof, an intermediate thereof, and a use thereof for a HPK1 kinase-related disease such as a cancer. B-L-K (I)
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
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
A61K 31/407 - 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 31/4353 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
A61K 31/4436 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
Disclosed in the present invention are a tricyclic fused heterocyclic compound having PDE3/4 dual inhibitory effect as represented by formula (I), and a stereoisomer, a solvate, or a pharmaceutically acceptable salt thereof, and the use thereof in the preparation of a drug for treating/preventing PDE3/4-mediated diseases, wherein each group in formula (I) is as defined in the description.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A compound of general formula (I) or a stereoisomer, a deuterated compound, a solvate, a prodrug, a metabolite, a pharmaceutically acceptable salt, or a co-crystal thereof, an intermediate thereof, and a use thereof in Bcl-2 family proteins-related diseases such as cancer. B-L-K (I)
Disclosed are a nitrogen-containing heterocyclic compound as shown in formula (I), or a stereoisomer, a solvate, a deuterated form, a pharmaceutically acceptable salt, or a cocrystal thereof or a pharmaceutical composition containing same, and the use thereof in the preparation of a drug for treating/preventing diseases mediated by autotaxin. Each group in formula (I) is as defined in the description.
Disclosed are a nitrogen-containing heterocyclic compound as shown in formula (I), or a stereoisomer, a solvate, a deuterated form, a pharmaceutically acceptable salt, or a cocrystal thereof or a pharmaceutical composition containing same, and the use thereof in the preparation of a drug for treating/preventing diseases mediated by autotaxin. Each group in formula (I) is as defined in the description.
C07D 491/147 - Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 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
22.
BENZO NITROGEN-CONTAINING HETEROAROMATIC RING DERIVATIVE AND USE THEREOF IN MEDICINE
Provided are a compound as shown in general formula (I), or a stereoisomer, deuterate, solvate, prodrug, metabolite, pharmaceutically acceptable salt or co-crystal thereof, an intermediate thereof, a preparation method therefor, and the use thereof in the preparation of a drug for treating a disease associated with the activity or expression quantity of complement factor B.
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 401/02 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 403/02 - 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
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
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
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
23.
HETEROCYCLIC DERIVATIVE, AND COMPOSITION AND PHARMACEUTICAL USE THEREOF
Disclosed are a compound as represented by general formula (I) or a stereoisomer, deuterated compound, solvate, prodrug, metabolite, pharmaceutically acceptable salt or co-crystal thereof and an intermediate thereof; and the use thereof in AR-related diseases such as cancer. B-L-K (I)
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
The present invention relates to a compound as represented by formula (I) and a stereoisomer, solvate, deuterated compound or pharmaceutically acceptable salt or pharmaceutical composition thereof, and the use thereof in the preparation of a drug for treating/preventing ER-mediated diseases, wherein each group in formula (I) is as defined in the description.
C07D 217/14 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 31/435 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
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 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A compound of formula (I) and a stereoisomer, deuterated compound, solvate, prodrug, metabolite, pharmaceutically acceptable salt or co-crystal thereof, or a pharmaceutical composition containing same, and the use thereof as an AAK1 inhibitor in the preparation of a drug for treating related diseases.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61P 25/00 - Drugs for disorders of the nervous system
Disclosed is a compound of formula (I), and a stereoisomer, a pharmaceutically acceptable salt, a solvate, a co-crystal or a deuterated product thereof, or a pharmaceutical composition containing same, and the use thereof as a CD73 antagonist in the preparation of a drug for treating related diseases, wherein the definition of each group in formula (I) is consistent with the definition in the description.
C07H 19/20 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
C07H 19/207 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids the phosphoric or polyphosphoric acids being esterified by a further hydroxylic compound, e.g. flavine-adenine dinucleotide or nicotinamide-adenine dinucleotide
A61K 31/7052 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
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
Provided are the compound shown in general formula (I) or a stereoisomer, a deuterated compound, a solvate, a prodrug, a metabolite, a pharmaceutically acceptable salt, or co-crystal thereof, an intermediate thereof, and a use thereof in EGFR-related diseases such as cancer. B-L-K (I)
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
Provided are a compound represented by general formula (I), or a stereoisomer, deuterated product, solvate, prodrug, metabolite, pharmaceutically acceptable salt, or co-crystal thereof, an intermediate thereof, and a preparation method therefor, as well as an application in the preparation of a drug for treating diseases related to PAR P7 activity or expression level.
C07D 471/12 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups in which the condensed system contains three hetero rings
C07D 498/12 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
Use of a compound represented by formula (I) or a stereoisomer, hydrate, metabolite, solvate, pharmaceutically acceptable salt, eutectic, or a composition thereof in preparation of a drug for treating pruritus. Also provided is a method for treating pruritus, the method comprising administering an effective dose of the compound represented by formula (I) or the stereoisomer, hydrate, metabolite, solvate, pharmaceutically acceptable salt, eutectic, or a composition thereof.
Disclosed are a pharmaceutically acceptable salt of an HA inhibitor (1S, 2S)-2-fluoro-N-(2-(2-(4-((R)-(5-methyl-2H-tetrazol-2-yl) (phenyl) methyl) piperidine-1-formyl) pyridine-4-yl) benzo[d]oxazol-5-yl) cyclopropyl-1-carboxamide, or a hydrate or solvate of a salt thereof, a preparation method therefor, and a use thereof.
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
A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses
31.
CRYSTAL FORM OF ANTI-INFLUENZA VIRUS COMPOUND, PREPARATION METHOD FOR CRYSTAL FORM, AND USE OF CRYSTAL FORM
Disclosed are a crystal form of a compound (1S, 2S)-2-fluoro-N-(2-(2-(4-((R)-(5-methyl-2H-tetrazol-2-yl) (phenyl) methyl) piperidine-1-formyl) pyridin-4-yl) benzo [d] oxazol-5-yl) cyclopropyl-1-carboxamide having a structure of formula (A), a preparation method for the crystal form, and a use of the crystal form in the preparation of a drug for treating/preventing influenza.
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
A61K 31/4995 - Pyrazines or piperazines forming part of bridged ring systems
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
A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses
32.
FIVE-MEMBERED RING DERIVATIVE AND MEDICAL USE THEREOF
A compound represented by general formula (I) or a stereoisomer, tautomer, deuterated substance, solvate, prodrug, metabolite, pharmaceutically acceptable salt or co-crystal thereof, an intermediate thereof, and a preparation method therefor, as well as an application in preparation of a drug for treating diabetes.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
Provided are a compound of formula (I), a stereoisomer, a deuterated compound, a solvate, a prodrug, a metabolite, a pharmaceutically acceptable salt or a eutectic thereof, or a pharmaceutical composition comprising same, and use thereof as a ketohexokinase inhibitor in the preparation of drugs for treating related diseases. Each group in formula (I) is as defined in the description.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 403/04 - 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 directly linked by a ring-member-to-ring- member bond
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
The present invention relates to a method for preparing a compound as represented by formula (I) and an intermediate thereof. The method has mild reaction conditions, does not involve a high-temperature and high-pressure reaction, has low-toxicity or non-toxicity raw materials, a simple operation, a high reaction yield, a high product purity, a convenient post-treatment, and a good reproducibility, and is suitable for industrial production.
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A BTK Inhibitor compound and a preparation method for an intermediate thereof. In the method, reaction conditions are mild, no high temperature and high pressure reaction is involved, raw materials are low-toxic or non-toxic, the operation is simple, reaction yield and product purity are high, post-treatment is convenient, and reproducibility is good; and the method is suitable for industrial production.
C07D 403/02 - 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
C07D 403/00 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group
A method for preparing a compound as represented by formula (I) and an intermediate thereof. The method has mild reaction conditions, does not involve a high-temperature and high-pressure reaction, has low-toxicity or non-toxicity raw materials, simple operation, a high reaction yield, a high product purity, convenient post-treatment, and good reproducibility, and is suitable for industrial production.
C07D 403/00 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group
37.
BENZENE RING DERIVATIVE, AND COMPOSITION AND PHARMACEUTICAL USE THEREOF
Disclosed are a compound as represented by general formula (I) or a stereoisomer, deuterated compound, solvate, prodrug, metabolite, pharmaceutically acceptable salt or co-crystal thereof, and an intermediate thereof, and the use thereof in AR or AR splicing mutant-related diseases such as cancer.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/4439 - 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
Disclosed are a compound of formula (I), a stereoisomer, solvate, prodrug, metabolite, pharmaceutically acceptable salt, or eutectic thereof, or a pharmaceutical composition comprising same, and an application thereof as an ATX inhibitor in preparation of a drug for treating a related disease. Groups in formula (I) are as defined in the description.
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61P 37/00 - Drugs for immunological or allergic disorders
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
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
A61P 11/00 - Drugs for disorders of the respiratory system
A61P 9/00 - Drugs for disorders of the cardiovascular system
39.
HETEROCYCLIC DERIVATIVE AND MEDICAL APPLICATION THEREOF
A compound represented by general formula (I) or a stereoisomer, tautomer, deuterated substance, solvate, prodrug, metabolite, pharmaceutically acceptable salt or co-crystal thereof, an intermediate thereof, and a preparation method therefor, as well as an application in the preparation of a drug for treating diseases related to JAK kinase activity or expression.
C07D 247/02 - Heterocyclic compounds containing rings having two nitrogen atoms as the only ring hetero atoms, according to more than one of groups having the nitrogen atoms in positions 1 and 3
C07D 249/00 - Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
Provided are a compound of general formula (I) or a stereoisomer, deuterium, solvate, prodrug, metabolite, and pharmaceutically acceptable salt or co-crystal thereof, an intermediate thereof, and a preparation method therefor, and an application in the preparation of drugs for treating diseases related to JAK3 kinase activity or expression.
A61K 31/4188 - 1,3-Diazoles condensed with heterocyclic ring systems, e.g. biotin, sorbinil
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 37/00 - Drugs for immunological or allergic disorders
41.
NITRILE DERIVATIVE THAT ACTS AS INHIBITOR OF DIPEPTIDYL PEPTIDASE 1 AND USE THEREOF
Provided is a nitrile derivative compound represented by formula (I), a stereoisomer, a deuterated product, a co-crystal, a solvate or a pharmaceutically acceptable salt thereof, wherein each group is as defined in the description. The compound has dipeptidyl peptidase 1 inhibitory activity and can be used to prepare a drug for treating obstructive airway diseases, bronchiectasis, cystic fibrosis, asthma, emphysema, chronic obstructive pulmonary diseases and other diseases.
C07D 267/10 - Seven-membered rings having the hetero atoms in positions 1 and 4 not condensed with other rings
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
A61P 11/00 - Drugs for disorders of the respiratory system
42.
METHOD AND SYSTEM FOR DETERMINING POPULATION PHARMACOKINETIC MODEL OF PROPOFOL AND DERIVATIVE THEREOF
G16B 5/00 - ICT specially adapted for modelling or simulations in systems biology, e.g. gene-regulatory networks, protein interaction networks or metabolic networks
A61B 5/00 - Measuring for diagnostic purposes Identification of persons
Disclosed are a sustained-release pharmaceutical formulation of a fused tricyclic γ-amino acid derivative and a preparation method therefor. The fused tricyclic γ-amino acid derivative is a compound represented by formula (I) or a stereoisomer, a solvate, a prodrug, a metabolite, a pharmaceutically acceptable salt or a eutectic crystal thereof.
C07C 229/28 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and containing rings
A61K 31/195 - Carboxylic acids, e.g. valproic acid having an amino group
A61P 25/04 - Centrally acting analgesics, e.g. opioids
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
44.
COMPOUND HAVING BTK KINASE DEGRADING ACTIVITY, AND PREPARATION METHOD AND PHARMACEUTICAL USE THEREFOR
A compound as shown in general formula (I) or stereoisomers, deuterated compounds, solvates, prodrugs, metabolites, pharmaceutically acceptable salts or co-crystals thereof, and intermediates thereof, a preparation method therefor, and a use thereof for treating BTK-related diseases, such as cancer or autoimmune diseases. B-L-K (I)
C07D 403/00 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
A compound as shown in general formula B-L-K (I) or stereoisomers, deuterated compounds, solvates, prodrugs, metabolites, pharmaceutically acceptable salts or co-crystals thereof, and intermediates thereof and uses thereof for AR-related diseases such as prostate cancer.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
The present invention relates to a compound as represented by general formula (I) or a stereoisomer, a deuterated compound, a solvate, a prodrug, a metabolite, a pharmaceutically acceptable salt or a co-crystal thereof, an intermediate thereof, a preparation method therefor, and the use thereof in the preparation of a drug for treating diseases related to the activity or expression level of JAK kinases.
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 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
A61K 31/4353 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
48.
PHARMACEUTICAL PREPARATION AND PREPARATION METHOD THEREFOR
AAA receptor reinforcing agent is as represented by formula (I) or a stereoisomer, a pharmaceutically acceptable salt or a prodrug thereof, wherein R1, R2 and n are defined in the description.
An oral pharmaceutical composition of a peptide amide compound (compound A). The present invention further relates to a method for preparing an oral pharmaceutical composition, and the use of the oral pharmaceutical composition in preparing a drug for treating diseases or conditions related to the κ-opioid receptor.
Disclosed are a compound as shown in general formula (I) or stereoisomers, deuterated compounds, solvates, prodrugs, metabolites, pharmaceutically acceptable salts or co-crystals thereof, intermediates thereof, a preparation method therefor, and the use thereof in the preparation of a drug for treating JAK-mediated diseases.
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61P 11/00 - Drugs for disorders of the respiratory system
Disclosed are a compound of formula (I), a stereoisomer, a pharmaceutically acceptable salt, a solvate, and an eutectic or deuterated compound thereof, or a pharmaceutical composition comprising same, and a use thereof as an EZH2 inhibitor in the preparation of a medication for treating related diseases. The definition of each group in formula (I) is consistent with that in the description.
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
Disclosed is a pharmaceutical composition of an aerosol inhalant and a preparation method thereof. The pharmaceutical composition comprises indacaterol or a salt thereof, magnesium stearate, and a propellant. The pharmaceutical composition is prepared by means of uniformly mixing the aforementioned components and filling the same into an aluminum can. The aerosol inhalant avoids the complexity and poor controllability of the conventional process of preparing an aerosol inhalant of indacaterol suspension into engineered particles with auxiliary materials. The aerosol inhalant is more suitable for clinical demands.
Provided are a compound of formula (I), a stereoisomer, a pharmaceutically acceptable salt, a solvate and a eutectic crystal thereof, or a pharmaceutical composition containing same, and the use thereof as an EZH2 inhibitor in the preparation of a drug for treating related diseases. Each group in formula (I) is as defined in the description.
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 471/02 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups in which the condensed system contains two hetero rings
C07D 487/02 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups in which the condensed system contains two hetero rings
A61K 31/435 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
54.
Composition of fused tricyclic gamma-amino acid derivatives and the preparation thereof
The present disclosure provides a pharmaceutical composition of fused tricyclic gamma-amino acid derivatives and the use thereof. The pharmaceutical composition includes: (i) a compound having a structure represented by formula (I) or a pharmaceutically acceptable salt thereof, as an active material, in an amount of 1% to 45% by weight; (ii) optionally one or more fillers in an amount of 50% to 95% by weight; (iii) optionally one or more lubricating agents in an amount of 0.1% to 5.5% by weight; and the sum of weight percentages of the all components is 100%, wherein the pharmaceutically acceptable salt of the compound of formula (I) has a structure as follows:
Disclosed are a nitrogen-containing heterocyclic compound as shown in formula (I), or a stereoisomer, a solvate, a deuterated compound, a pharmaceutically acceptable salt, or a eutectic thereof or a pharmaceutical composition containing same, and the use thereof in the preparation of a drug for treating/preventing diseases mediated by autotaxin. Each group in formula (I) is as defined in the description.
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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61P 39/00 - General protective or antinoxious agents
56.
PYRIMIDO DERIVATIVE AND APPLICATION THEREOF IN MEDICINE
A compound represented by general formula (I), or a stereoisomer, deuterated product, solvate, prodrug, metabolite, co-crystal or pharmaceutically acceptable salt thereof, an intermediate of the compound, and a preparation method for the compound, as well as an application in the preparation of a drug for preventing or treating diseases related to KRAS G12C activity or amount of expression.
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/527 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim spiro-condensed
An inhalation solution pharmaceutical composition and a preparation method therefor. The composition comprises indacaterol or salts thereof, a pH regulator, and water, and an optional osmotic pressure regulator and a buffer ion pair, and is prepared by dissolving ingredients into water. The pharmaceutical composition is suitable for forming a mist from an active substance with the aid of a nebulizer for administration to patients in asthma and COPD symptoms by means of inhalation.
A method for preparing a peptide amide compound represented by formula (N) and an intermediate thereof; the method has mild reaction conditions, simple operations, high reaction yield, high product purity and convenient post-treatment, and is suitable for industrial production.
Disclosed is a hexahydrobenzopyrazole compound shown in formula (I), and a stereoisomer, a pharmaceutically acceptable salt, a solvate, a hydrate, an N-oxide, a prodrug, and a pharmaceutical composition thereof, a preparation method therefor, and the use thereof in the prevention and treatment of diseases mediated by the cannabinoid CB2 receptor.
C07D 403/02 - 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
C07D 403/04 - 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 directly linked by a ring-member-to-ring- member bond
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 451/00 - Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamineCyclic acetals thereof
A61K 31/352 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. cannabinols, methantheline
Disclosed is a tricyclic pyrazole compound shown in formula (I), and a stereoisomer, a pharmaceutically acceptable salt, a solvate, a hydrate, an N-oxide, a prodrug, and a pharmaceutical composition thereof, a preparation method therefor, and the use in the prevention and treatment of diseases mediated by the cannabinoid CB2 receptor.
C07D 231/54 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
61.
IMPURITY DETECTION METHOD FOR 2-((1S,2S,3R,6S,8S)-2-(AMINOMETHYL)TRICYCLO[4.2.1.0 3,8]NONANE-2-YL)ACETATE BENZENESULFONATE OR COMPOSITION THEREOF
Provided is a content, related substance and chiral isomer detection method for 2-((1S,2S,3R,6S,8S)-2-(aminomethyl)tricyclo[4.2.1.03,8]nonane-2-yl)acetate benzenesulfonate or a composition thereof. The content and related substance I are detected using a HPLC-CAD method, and related substance II and chiral isomers are detected using LC-MS. The present method can implement effective separation and quantitative detection of related substances I and II and chiral isomers from 2-((1S,2S,3R,6S,8S)-2-(aminomethyl)tricyclo[4.2.1.03,8]nonane-2-yl)acetate benzenesulfonate or a composition thereof, the degree of separation being greater than 1.5; specificity, repeatability, and stability are good, ensuring medicine quality and patient medication safety; and detection costs are greatly reduced, facilitating industrial production.
C07C 229/28 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and containing rings
62.
PEPTIDE AMIDE COMPOSITION AND PREPARATION METHOD THEREFOR
Disclosed are a peptide amide compound composition, a preparation method therefor and medical use thereof. Specifically, the composition contains a compound of formula (I) and pH regulators, and the pH of the solution thereof is 3-5.5. The composition is stable and requires few excipients, and is stable in clinical use.
Provided are a compound of formula (I-a), an isomer thereof or a pharmaceutically acceptable salt thereof as a Hemagglutinin inhibitor, and a preparation method thereof. The compound is useful for preparing a medicament for treating a disease related to Hemagglutinin.
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
A61K 31/4995 - Pyrazines or piperazines forming part of bridged ring systems
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
A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses
64.
PEPTIDE AMIDE SALT, PREPARATION METHOD THEREFOR AND USE THEREOF IN MEDICINE
A compound represented by general formula (I) or stereoisomers thereof, a preparation method therefor, and use thereof in medicine, general formula (I) being shown below, and the definition of each substituent being consistent with that in the description.
A compound as represented by general formula (I) or a stereoisomer, a hydrate, a metabolite, a solvate, a pharmaceutically acceptable salt, or a co-crystal thereof, a composition thereof, a preparation method therefor, and an application thereof in medicine. The general formula (I) is as shown below, and the definitions of the substituents are the same as those in the description.
A BTK inhibitor ring derivative, a preparation method therefor and a pharmaceutical application thereof. The BTK inhibitor ring derivative is a compound represented by a general formula (I) or a stereoisomer, a solvate, a prodrug, a metabolite, a pharmaceutically acceptable salt or co-crystal thereof, and the BTK inhibitor ring derivative is used to treat BTK-related diseases such as tumors or autoimmune system diseases.
C07D 403/00 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group
Described herein are methods and compositions for the treatment of conditions, diseases, or disorders associated with autotaxin activity. The methods and compositions disclosed herein include the use of at least one autotaxin inhibitor compound.
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
A61K 9/00 - Medicinal preparations characterised by special physical form
A61P 11/00 - Drugs for disorders of the respiratory system
Described herein are ASK1 inhibitors and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of blood disease, autoimmune disorders, pulmonary disorders, hypertension, inflammatory diseases, fibrotic diseases, diabetes, diabetic nephropathy, renal diseases, respiratory diseases, cardiovascular diseases, acute lung injuries, acute or chronic liver diseases, and neurodegenerative diseases.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 9/00 - Medicinal preparations characterised by special physical form
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
69.
PREPARATION METHOD FOR FUSED TRICYCLIC DERIVATIVE AND INTERMEDIATE
The present invention provides a preparation method for a fused tricyclic derivative and an intermediate. The fused tricyclic derivative has a structure represented by formula (I). In the preparation method, raw materials are easy to obtain, simple steps are comprised, and the preparation method is suitable for large-scale industrial production.
C07C 229/28 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and containing rings
70.
FUSED TRICYCLIC DEUTERATED DERIVATIVE, COMPOSITION AND USE THEREOF
Provided are a fused tricyclic deuterated derivative, a composition and the use thereof. Particularly, provided are a fused tricyclic deuterated derivative as shown in general formula (I) or a stereoisomer, solvate, metabolite, pharmaceutically acceptable salt, eutectic crystal or prodrug thereof, and a pharmaceutical composition containing the derivative or the stereoisomer, solvate, metabolite, pharmaceutically acceptable salt, eutectic crystal or prodrug thereof, and the use of same as a medicament for treating and/or preventing pain.
C07C 229/28 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and containing rings
A61K 31/195 - Carboxylic acids, e.g. valproic acid having an amino group
A61P 25/04 - Centrally acting analgesics, e.g. opioids
A preparation method for a fused tricyclic γ-amino acid derivative and an intermediate thereof, and a method for preparing an intermediate of the fused tricyclic γ-amino acid derivative. The fused tricyclic γ-amino acid derivative has a structure as represented by formula (I). The preparation method uses readily available raw materials and comprises simple steps; the entire synthesis process uses crystallization purification, while silica gel column chromatography or other preparatory chromatography methods are not used, being suitable for large-scale industrial production.
C07C 229/28 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and containing rings
C07C 227/12 - Formation of amino and carboxyl groups
C07C 227/32 - Preparation of optical isomers by stereospecific synthesis
C07C 53/136 - Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen containing rings containing condensed ring systems
C07C 61/125 - Saturated polycyclic compounds having a carboxyl group bound to a condensed ring system
C07C 211/19 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of a saturated carbon skeleton containing rings other than six-membered aromatic rings containing condensed ring systems
C07C 211/38 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of a saturated carbon skeleton containing condensed ring systems
C07C 205/00 - Compounds containing nitro groups bound to a carbon skeleton
72.
AEROSOL PHARMACEUTICAL COMPOSITION CONTAINING GLYCOPYRROLATE SALT AND INDACATEROL SALT, PREPARATION METHOD THEREFOR, AND USES THEREOF
Provided is a propellant-free aerosol pharmaceutical composition comprising a pharmaceutical glycopyrrolate salt, an indacaterol pharmaceutical salt and water, wherein each 100ml of the pharmaceutical composition contains from 0.045 +/- 0.001g to 0.090 +/-0.001g of the glycopyrrolate, and 0.099 +/-0.001g to 0.198 +/-0.001g of the indacaterol. The pharmaceutical composition is particularly suitable for converting an active substance into an aerosol by means of atomization so as to ensure inhalation administration of a surfactant for treating asthma and COPD symptoms.
A61K 9/72 - Medicinal preparations characterised by special physical form for smoking or inhaling
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
Provided is a propellant-free aerosol pharmaceutical composition comprising a pharmaceutical glycopyrrolate salt and water, wherein each 100 ml of the pharmaceutical composition contains from 0.045 +/- 0.001g to 0.090 +/-0.001g of the glycopyrrolate. The pharmaceutical composition is particularly suitable for converting an active substance into an aerosol by means of atomization so as to ensure inhalation administration of a surfactant for treating asthma and COPD symptoms.
A61K 9/72 - Medicinal preparations characterised by special physical form for smoking or inhaling
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
A61P 11/00 - Drugs for disorders of the respiratory system
74.
COMPOSITION OF FUSED TRICYCLIC γ-AMINO ACID DERIVATIVE AND PREPARATION THEREFOR
Disclosed are a pharmaceutical composition of a fused tricyclic γ-amino acid derivative and the use thereof. The pharmaceutical composition comprises: (i) the structure as shown in formula (I) or a pharmaceutically acceptable salt thereof, as an active substance, wherein the weight percentage is 1%-45%; (ii) optionally one or more fillers, wherein the weight percentage is 50%-95%; and (iii) optionally one or more lubricants, wherein the weight percentage is 0.1%-5.5%. The sum of the weight percentages of all components is 100%. The structure of the pharmaceutically acceptable salt of the structure as shown in formula (I) is as shown in formula (I-A).
C07C 229/28 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and containing rings
A61K 31/195 - Carboxylic acids, e.g. valproic acid having an amino group
A61P 25/04 - Centrally acting analgesics, e.g. opioids
Provided are a crystal form of a salt of a fused tricyclic γ-amino acid derivative and the preparation and use thereof. As shown in formula (I), Y is selected from maleic acid, fumaric acid, haloid acid (preferably hydrobromic acid and hydrochloric acid), sulfuric acid, phosphoric acid, L-tartaric acid, citric acid, L-malic acid, hippuric acid, D-glucuronic acid, glycollic acid, mucic acid, succinic acid, lactic acid, orotic acid, pamoic acid, malonic acid, gentisic acid, oxalic acid, glutaric acid or saccharin.
C07C 229/28 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and containing rings
A61K 31/195 - Carboxylic acids, e.g. valproic acid having an amino group
Described herein are methods and compositions for the treatment of conditions, diseases, or disorders associated with autotaxin activity. The methods and compositions disclosed herein include the use of at least one autotaxin inhibitor compound.
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
A61P 11/00 - Drugs for disorders of the respiratory system
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 47/20 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
Described herein are compounds, including pharmaceutically acceptable salts thereof, methods of making such compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat, prevent or diagnose blood-based diseases, disorders or conditions.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 403/04 - 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 directly linked by a ring-member-to-ring- member bond
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/198 - Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
The present invention relates to a composition of a compound of general formula (A), a pharmaceutically acceptable salt or a prodrug, and a preparation method therefor. (A)
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 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
A61K 31/4188 - 1,3-Diazoles condensed with heterocyclic ring systems, e.g. biotin, sorbinil
A61K 31/438 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
A61K 31/538 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
The present invention relates to a pharmaceutical composition comprising a compound of formula (II) or a stereoisomer, hydrate, metabolite, solvate, pharmaceutically acceptable salt, cocrystal, or prodrug thereof and a method for treating an obstructive airway disease. (II)
The present invention relates to the salt of an azacyclic amide derivative, a crystal form thereof and a preparation method therefor and the medical use thereof. In particular, the salt of the azacyclic amide derivative is the compound as shown in formula (I).
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A peptide amide compound shown in general formula (I) and a preparation method and medical use thereof. The compound is used to treat or prevent a disease or condition related to κ-opioid receptor in mammals. (I)
The present invention relates to a crystal form of a substituted aminopyran compound, and a pharmaceutical composition, a preparation method and a use thereof in the preparation of a drug for treating type II diabetes. In particular, the present invention relates to a crystal form IV of a compound as shown by formula (I) and a pharmaceutical composition, a preparation method and a use thereof in the preparation of a drug for treating type II diabetes.
The present invention relates to a diazaspiro[5.5]undecane derivative and a use thereof. The derivative is a compound represented by general formula (I) or a stereoisomer, hydrate, metabolite, solvate, pharmaceutically acceptable salt, eutectic crystal, or prodrug thereof. The present invention also relates to a preparation method of the derivative and an application of the same in preparing a drug for treating an obstructive airway disease. The definition of each substituent is consistent with the definition in the specification.
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
A61K 31/535 - 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
85.
FUSED TRICYCLIC Γ-AMINO ACID DERIVATIVE, PREPARATION METHOD THEREFOR, AND MEDICAL USE THEREOF
Disclosed are a fused tricyclic γ-amino acid derivative and a medical use thereof, in particular, the present invention relates to a fused cyclic γ-amino acid derivative as shown in general formula (I), or a stereoisomer, solvate, metabolite, prodrug, pharmaceutically acceptable salt or eutectic thereof, a pharmaceutical composition containing same, and the use of a compound or the composition in the field of analgesia, wherein the definitions of each substituent in general formula (I) are the same as the definitions in the description.
C07C 229/28 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and containing rings
A61K 31/195 - Carboxylic acids, e.g. valproic acid having an amino group
A61P 25/04 - Centrally acting analgesics, e.g. opioids
The present invention relates to a phenol-containing derivative, an etomidate pharmaceutical composition, a preparation method thereof, and application of same in the field of central nervous system treatment. A phenol derivative is a compound represented by formula (I) or a stereoisomer, pharmaceutically acceptable salt, or prodrug thereof.
The present invention relates to a benzene derivative, and a manufacturing method and pharmaceutical application thereof. The invention specifically relates to a benzene derivative as represented by formula (A), or a stereoisomer, solvate, metabolite, prodrug, pharmaceutically acceptable salt, or cocrystal thereof, a manufacturing method of the derivative, a pharmaceutical composition comprising the derivative, and an application of a compound or the composition in the field of central nervous system. Definitions for each substituent in the formula (A) are identical to the definitions provided in the specification.
C07C 39/17 - Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a six-membered aromatic ring polycyclic with no unsaturation outside the aromatic rings containing other rings in addition to the six-membered aromatic rings
C07F 9/12 - Esters of phosphoric acids with hydroxyaryl compounds
Provided is a method for preparing a trifluoromethyl-substituted pyran derivative, that is, a method for preparing the compound shown in formula (I) and an intermediate thereof. The method has the advantages of having mild reaction conditions, simple operations, high reaction yield, high product purity and convenient post-treatment, rendering the method suitable for industrial production.
Provided are a preparation method for a trifluoromethyl-substituted pyran derivative and an intermediate thereof, namely, a preparation method for a compound as shown in formula (I) and an intermediate thereof. The method is characterized by mild reaction conditions, simple operations, high reaction yield, high product purity and convenient post-treatment, rendering the method suitable for industrial production.
C07D 309/14 - Nitrogen atoms not forming part of a nitro radical
A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
A61K 31/351 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 25/00 - Drugs for disorders of the nervous system
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
The present invention relates to a benzyl bisphenol derivative, and a preparation method and pharmaceutical application thereof. The benzyl bisphenol derivative provided by the invention can promote a sedative-hypnotic effect, offer brain protection, and treat and/or prevent a central nervous system disease.
C07C 39/17 - Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a six-membered aromatic ring polycyclic with no unsaturation outside the aromatic rings containing other rings in addition to the six-membered aromatic rings
C07C 50/08 - Quinones with polycyclic non-condensed quinoid structure
Disclosed are a phosphamide derivative, a method for manufacturing the same, and uses thereof Particularly disclosed are a compound shown by general formula (I) as well as a pharmaceutically acceptable salt or stereisomer (I) thereof, wherein, G, L, Q and s are as defined in the description.
C07C 229/02 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
Provided in the present invention are an alkylalkoxy ester prodrug of a nucleoside analogue as shown in formula IV and a preparation method thereof, and the use thereof in preparing drugs for preventing and/or treating viral infections, in particular, the hepatitis B virus (HBV) and/or the human immunodeficiency virus (HIV) infection.
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
Provided are a compound represented by formula (I) or a stereoisomer, hydrate, metabolite, solvate, pharmaceutically acceptable salt, eutectic mixture, or prodrug thereof, and a preparation method thereof, and an application for preparing a pharmaceutical product for treating a disease related to obstructed airways, wherein each substituent in the compound represented by formula (I) is as described in the specification.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61P 11/00 - Drugs for disorders of the respiratory system
Provided in the present invention are a phosphate prodrug of a nucleoside analogue as shown in formula IV and a preparation method thereof, and the use thereof in preparing drugs for preventing and/or treating viral infections, in particular, the hepatitis B virus (HBV) and/or the human immunodeficiency virus (HIV) infection.
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
95.
BENZYL HETEROCYCLIC COMPOUND DERIVATIVE AND PHARMACEUTICAL APPLICATION THEREOF
The present invention provides a compound represented by formula (I) or a stereoisomer, hydrate, metabolite, or solvate thereof, or a pharmaceutically acceptable salt, eutectic, or prodrug of the compound. The invention also provides a manufacturing method of the compound and an application in preparing a pharmaceutical drug for treating an airway obstruction disease. Each substituent in the compound represented by formula (I) is as described in the specification.
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/538 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
The present invention relates to a fused tricyclic γ-amino acid derivative and a pharmaceutical application thereof. Specifically, the present invention relates to a fused tricyclic γ-amino acid derivative depicted by general formula (I) or a stereoisomer, solvate, metabolite, prodrug, pharmaceutically acceptable salt or eutectic thereof, a pharmaceutical composition comprising same, and a use of the compound or composition of the present invention in the field of analgesia, wherein the substituents in the general formula (I) are as defined in the description.
C07C 229/28 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and containing rings
C07C 229/32 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing rings other than six-membered aromatic rings
A61K 31/195 - Carboxylic acids, e.g. valproic acid having an amino group
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 25/04 - Centrally acting analgesics, e.g. opioids
The present invention relates to a crystal form of a substituted aminopyran compound, and a pharmaceutical composition, a preparation method and a use thereof in the preparation of a drug for treating type II diabetes. In particular, the present invention relates to a crystal form IV of a compound as shown by formula (I) and a pharmaceutical composition, a preparation method and a use thereof in the preparation of a drug for treating type II diabetes.
Disclosed is a compound as shown by general formula (I) or a stereoisomer, a hydrate, a metabolite, a solvate, a pharmaceutically acceptable salt, a cocrystal or a prodrug thereof, and a preparation method and a use in the preparation of a drug for treating obstructive airway diseases, wherein the compound of general formula (I) is as follows: the definitions of the substituents are consistent with those in the description.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61P 11/00 - Drugs for disorders of the respiratory system
The present invention relates to a condensed ring γ-amino acid derivative and a medical use thereof, and in particular relates to the condensed ring γ-amino acid derivative as shown in formula (I), or a stereisomer, a solvate, a metabolite, a prodrug, a pharmaceutically acceptable salt or a cocrystal thereof, a pharmacuetical composition comprising same and a use of the compound or composition of the present invention in the field of analgesia, wherein the definitions of various substituent groups in formula (I) are the same as those in the description.
C07C 229/32 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing rings other than six-membered aromatic rings
C07C 227/18 - Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof by reactions involving amino or carboxyl groups, e.g. hydrolysis of esters or amides, by formation of halides, salts or esters
C07D 305/06 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring atoms
A61K 31/195 - Carboxylic acids, e.g. valproic acid having an amino group
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 25/04 - Centrally acting analgesics, e.g. opioids
The present disclosure relates to an amino pyran ring derivative and a composition and use thereof, and in particular, to an amino pyran ring derivative represented by general formula (I) or a stereoisomer, a pharmaceutically acceptable salt or a prodrug thereof, a pharmaceutical composition comprising the derivative, and their medical use in the manufacture of a di-peptidyl peptidase IV (DPP-IV) inhibitor,
in formula (I) the substituents are defined the same as those in the specification.
patents
