Abstract

The present application relates to the technical field of medicines, in particular to fused tricyclic substituted isoxazolidinyl urea derivatives, pharmaceutically acceptable salts and stereoisomers thereof, a pharmaceutical composition thereof and the use of same. The structure of the fused tricyclic substituted isoxazolidinyl urea derivatives is shown as formula (I). The fused tricyclic substituted isoxazolidinyl urea derivatives disclosed in the present application have remarkable TrkA kinase and cell inhibitory activity and selective inhibitory activity.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
• C07D 498/14 - Ortho-condensed systems
• A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems

Goods & Services

Ejiao [donkey-hide gelatin] for Chinese medicinal use; tonics [medicines]; Chinese caterpillar fungus for pharmaceutical use; radioactive medicines; cholesterol reducers; ginseng for medicinal purposes; semen for artificial insemination; medicines for human purposes; adhesive patches for medical purposes; vitamin supplement patches; bouillons for bacteriological cultures for medical purposes or veterinary purposes; disinfectants; chemical conductors for electrocardiograph electrodes; medicinal tea; forest frog oil for pharmaceutical purposes; glossy ganoderma for pharmaceutical purposes; cartilage extract for pharmaceutical purposes; pseudo-ginseng powder for medical purposes; dendrobium stem for pharmaceutical purposes; gastrodia elata for pharmaceutical purposes; collagen for medical purposes; oxygen for medical purposes; greases for medical purposes; solutions for contact lenses; cod liver oil; Chinese patent medicines; ganoderma lucidum spore powder dietary supplements; freeze-dried food adapted for medical purposes; dietetic substances adapted for medical use; food for babies; depuratives; medicines for veterinary purposes; pesticides; disinfectant wipes; medical dressings; drug delivery agents in the form of edible wafers for wrapping powdered pharmaceuticals; preparations to facilitate teething; diapers for pets.

Abstract

Provided is a polymorph and application of a pyrimidine derivative and a pharmaceutically acceptable salt thereof. The polymorph and application of the pyrimidine derivative that is an A2A/A2B dual receptor antagonist having the chemical name 3-(4-amino-5-fluoro-6-(1-((6-(2-hydroxypropan-2-yl)pyridin-2-yl)methyl)-1H-1,2,3-triazol-4-yl)pyrimidine-2-yl)-2-methylbenzonitrile and the pharmaceutically acceptable salt thereof.

IPC Classes  ?

• 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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61P 35/00 - Antineoplastic agents

Abstract

Disclosed are a pharmaceutically acceptable salt of an MOR receptor agonist, and a polymorph thereof and the use thereof. Specifically, disclosed are a pharmaceutically acceptable salt of (4S,6S)-6-isopropyl-N-(2-((R)-9-(pyridin-2yl)-6-oxa spiro[4.5]decyl-9-yl)ethyl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-4-amine, and a polymorph thereof and the use thereof. In addition, further disclosed are a pharmaceutical composition containing the pharmaceutically acceptable salt of the compound or the polymorph thereof, and the use thereof.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• 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
• C07C 55/10 - Succinic acid
• C07C 57/145 - Maleic acid
• C07C 59/255 - Tartaric acid

Abstract

A substituted triazinylmethylcycloalkylcarboxylic acid derivative having a structure as shown in formula (I). In addition, further disclosed are a pharmaceutically acceptable salt, a stereoisomer, a pharmaceutical composition and the use of the derivative. The compound has significant P2X3 inhibitory activity and selectivity, and is high in application value. A substituted triazinylmethylcycloalkylcarboxylic acid derivative having a structure as shown in formula (I). In addition, further disclosed are a pharmaceutically acceptable salt, a stereoisomer, a pharmaceutical composition and the use of the derivative. The compound has significant P2X3 inhibitory activity and selectivity, and is high in application value.

IPC Classes  ?

• 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 31/53 - 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
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

Abstract

Disclosed is a heterocycle-substituted five- and six-membered heteroaryl derivative, the structure of which is shown in formula (I). In addition, also disclosed are a pharmaceutically acceptable salt of the derivative, a stereoisomer thereof, a pharmaceutical composition, and a use thereof. The compound of the present invention has significant selective inhibition on AAK1 kinase activity, a weaker hERG inhibitory effect and better central nervous system penetration, and has great practical value.

IPC Classes  ?

• 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 213/63 - One oxygen atom
• C07D 231/56 - BenzopyrazolesHydrogenated benzopyrazoles
• C07D 239/26 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
• C07D 241/18 - Oxygen or sulfur atoms
• A61K 31/403 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
• A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
• A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
• A61K 31/444 - 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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61P 25/02 - Drugs for disorders of the nervous system for peripheral neuropathies
• A61P 25/04 - Centrally acting analgesics, e.g. opioids

Abstract

Disclosed in the present application is a heterocyclic substituted penta-six-membered heteroaryl derivative, the structure thereof being as represented by formula (I). In addition, the present application further discloses a pharmaceutically acceptable salt of the derivative and a stereoisomer and pharmaceutical composition thereof, as well as a use thereof. The compound of the present application has significant AAK1 selective inhibitory activity, a lower hERG inhibitory effect, more advantageous central nervous system penetration, and has high practical value.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• C07D 487/04 - Ortho-condensed 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
• A61P 25/04 - Centrally acting analgesics, e.g. opioids
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings

Abstract

The present application relates to a solvate solid form of a triazinyl methyl cycloalkyl carboxylic acid derivative as represented by formula (I), a crystal form thereof, a pharmaceutical composition comprising same, a preparation method therefor, and the use of the solvate and polymorph in preventing and/or treating diseases related to P2X3 activity or P2X2/3 activity.

IPC Classes  ?

• 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 251/46 - One nitrogen atom with oxygen or sulfur atoms attached to the two other ring carbon atoms
• 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
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 43/00 - Drugs for specific purposes, not provided for in groups

Abstract

A substituted triazine-2,4-dione derivative intermediate and a preparation method therefor, the intermediate being a compound represented by formula (II), a salt thereof or an isomer thereof. The intermediate and the preparation method therefor can be used to prepare a P2X3 or P2X2/3 inhibitor. The intermediate and the preparation method therefor effectively reduce side reactions, reduce the impurity content in a product, decrease solvent residue in the product, improve quality of the product, and are conducive to subsequent reactions. Moreover, the reaction is simple and easy to perform, and is more suitable for process production.

IPC Classes  ?

• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
• 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
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 43/00 - Drugs for specific purposes, not provided for in groups

Abstract

A substituted pyrazolo[1,5-alpyrimidin-7-amine derivative, the structure of which is represented by formula (1), or pharmaceutically acceptable salts, solvates, stereoisomers, prodrugs, drug compositions thereof. The derivative has significant CDK9-selective inhibitory activity. A substituted pyrazolo[1,5-alpyrimidin-7-amine derivative, the structure of which is represented by formula (1), or pharmaceutically acceptable salts, solvates, stereoisomers, prodrugs, drug compositions thereof. The derivative has significant CDK9-selective inhibitory activity.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• A61P 35/00 - Antineoplastic agents
• A61P 35/02 - Antineoplastic agents specific for leukemia

Abstract

An oxaspiro substituted pyrrolopyrazole derivative, an intermediate thereof, and a preparation method therefor.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems

Abstract

The present invention relates to a heterocyclo-substituted methanone derivative and the use thereof. In particular, the present invention provides a solid form of (S)-(3-amino-5-(1-amino-1,3-dihydrospiro[indene-2,4'-piperidin]-1'-yl)pyrazin-2-yl)(2-amino-7,7-difluoro-6,7-dihydrothiazolo[5,4-c]pyridin-5(4H)-yl)methanone, and the use thereof. In addition, the present invention also discloses a pharmaceutical composition containing the solid form and the use thereof.

IPC Classes  ?

• C07D 513/04 - Ortho-condensed systems
• A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
• A61P 35/00 - Antineoplastic agents
• A61P 35/02 - Antineoplastic agents specific for leukemia

Abstract

The present application relates to a heteroaryl-substituted pyridopyrrolidone derivative, and a pharmaceutical composition and the use thereof. The heteroaryl-substituted pyridopyrrolidone derivative has a structure as shown in formula (I). The compound of the present application has a relatively high selective inhibitory activity on PI3Kγ and an improved in-vivo pharmacokinetic activity, and has practical value.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• C07D 487/04 - Ortho-condensed systems
• A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
• A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
• A61P 3/00 - Drugs for disorders of the metabolism
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 35/00 - Antineoplastic agents

Abstract

Provided is a heterocycle substituted ketone derivative, the structure of which is as shown in formula (I). Further provided are a pharmaceutically acceptable salt of the derivative, a stereoisomer thereof, a pharmaceutical composition and the medicinal use thereof. Provided is a heterocycle substituted ketone derivative, the structure of which is as shown in formula (I). Further provided are a pharmaceutically acceptable salt of the derivative, a stereoisomer thereof, a pharmaceutical composition and the medicinal use thereof.

IPC Classes  ?

• 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
• C07D 487/14 - Ortho-condensed systems
• C07D 513/04 - Ortho-condensed systems
• C07D 498/04 - Ortho-condensed systems
• C07D 471/04 - Ortho-condensed 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
• A61P 35/00 - Antineoplastic agents

Abstract

The present application relates to a pharmaceutically acceptable salt and polymorph of a substituted pyrazolo[1,5-a]pyrimidin-7-amine derivative as represented by formula (I), a pharmaceutical composition comprising same, a preparation method therefor, and a use of the pharmaceutically acceptable salt and polymorph in the treatment or prevention of CDK9 activity-related diseases or CDK9 activity-mediated diseases.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 35/00 - Antineoplastic agents

Abstract

The present application relates to a six-membered aromatic ring-pyrrolidone derivative, and a pharmaceutical composition thereof and the use thereof. The six-membered aromatic ring-pyrrolidone derivative has the structure as shown in formula (I).

IPC Classes  ?

• 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 487/04 - Ortho-condensed systems
• A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
• A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
• A61P 3/00 - Drugs for disorders of the metabolism
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 35/00 - Antineoplastic agents

Goods & Services

Chinese traditional medicinal herbs; Confectionery for medicinal purposes; Dietary and nutritional supplements; Dietary fiber for use as an ingredient in the manufacture of dietary supplements; Dietary supplements; Dietary supplements for human beings; Dietary supplements for human consumption; Dietetic foods adapted for medical use; Medicinal herbs; Vitamins and vitamin preparations

Goods & Services

Chinese traditional medicinal herbs; Confectionery for medicinal purposes; Dietary and nutritional supplements; Dietary fiber for use as an ingredient in the manufacture of dietary supplements; Dietary supplements; Dietary supplements for human beings; Dietary supplements for human consumption; Dietetic foods adapted for medical use; Medicinal herbs; Vitamins and vitamin preparations

Abstract

The present disclosure relates to the field of drugs. Specifically, the present disclosure relates to a compound as represented by formula (I), or a stereoisomer, tautomer, metabolite, pharmaceutically acceptable salt or prodrug of the compound as represented by formula (I).

IPC Classes  ?

• 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 249/08 - 1,2,4-TriazolesHydrogenated 1,2,4-triazoles
• 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 31/4196 - 1,2,4-Triazoles
• A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
• A61P 35/00 - Antineoplastic agents
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

Abstract

The present application relates to a substituted pyrimidone derivative, and a pharmaceutically acceptable salt, stereoisomer, pharmaceutical composition and medical use thereof. The substituted pyrimidone derivative is a compound having a structure represented by formula (I), and the compound has significant CSF-1R selective inhibitory activity, and is very practical.

IPC Classes  ?

• 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 471/04 - Ortho-condensed systems
• C07D 487/04 - Ortho-condensed systems
• A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 35/00 - Antineoplastic agents

Abstract

Disclosed is a substituted naphthyridinone derivative, which has a structure as shown in formula (I). Further provided are a pharmaceutically acceptable salt, stereoisomer and pharmaceutical composition of the derivative and the medicinal use thereof.

IPC Classes  ?

• C07D 221/02 - Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups condensed with carbocyclic rings or 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 471/04 - Ortho-condensed 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
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention relates to a solid pharmaceutical preparation and a preparation method therefor. Specifically, disclosed are a solid pharmaceutical preparation that comprises an orexin receptor antagonist compound and a preparation method therefor, the solid pharmaceutical preparation comprising an active ingredient of a compound represented by formula I, a filler, a binder, a disintegrant, and a lubricant. The solid pharmaceutical preparation has good dissolution, stability and in vivo bioavailability. The present invention relates to a solid pharmaceutical preparation and a preparation method therefor. Specifically, disclosed are a solid pharmaceutical preparation that comprises an orexin receptor antagonist compound and a preparation method therefor, the solid pharmaceutical preparation comprising an active ingredient of a compound represented by formula I, a filler, a binder, a disintegrant, and a lubricant. The solid pharmaceutical preparation has good dissolution, stability and in vivo bioavailability.

IPC Classes  ?

• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/00 - Medicinal preparations characterised by special physical form

Abstract

Disclosed are an optically pure oxaspiro-substituted pyrrolopyrazole derivative, a preparation method therefor and the pharmaceutical use thereof. The compounds are compounds as shown in formula (I) and formula (II) or a pharmaceutically acceptable salt thereof, or a solvate thereof, or a prodrug thereof. Also disclosed are a preparation method therefor and the use thereof Disclosed are an optically pure oxaspiro-substituted pyrrolopyrazole derivative, a preparation method therefor and the pharmaceutical use thereof. The compounds are compounds as shown in formula (I) and formula (II) or a pharmaceutically acceptable salt thereof, or a solvate thereof, or a prodrug thereof. Also disclosed are a preparation method therefor and the use thereof

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems

Abstract

Provided is a substituted pyrimidine or pyridine amine derivative represented by formula (I), and a pharmaceutically acceptable salt, solvate, stereoisomer, prodrug, and pharmaceutical composition thereof, as well as medical application thereof. The derivative has significant adenosine A2A receptor and/or adenosine A2B receptor antagonistic activities.

IPC Classes  ?

• 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 498/04 - Ortho-condensed systems
• 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 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
• C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
• 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

Abstract

Provided are an azabicyclic substituted oxaspiro derivative, a preparation method therefor and a medical use thereof. Specifically, provided are compounds represented by formula (I) and formula (II) or pharmaceutically acceptable salts, stereoisomers or solvates thereof, and a preparation method therefor and an application thereof. Provided are an azabicyclic substituted oxaspiro derivative, a preparation method therefor and a medical use thereof. Specifically, provided are compounds represented by formula (I) and formula (II) or pharmaceutically acceptable salts, stereoisomers or solvates thereof, and a preparation method therefor and an application thereof.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• C07D 491/20 - Spiro-condensed systems

Abstract

Provided is a polymorph and application of a pyrimidine derivative and a pharmaceutically acceptable salt thereof. The polymorph and application of the pyrimidine derivative that is an A2A/A2B dual receptor antagonist having the chemical name 3-(4-amino-5-fluoro-6-(1-((6-(2-hydroxypropan-2-yl)pyridin-2-yl)methyl)-1H-1,2,3-triazol-4-yl)pyrimidine-2-yl)-2-methylbenzonitrile and the pharmaceutically acceptable salt thereof.

IPC Classes  ?

• 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
• 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

Abstract

2A2B2B dual receptor antagonist having the chemical name 3-(4-amino-5-fluoro-6-(1-((6-(2-hydroxypropan-2-yl)pyridin-2-yl)methyl)-1H-1,2,3-triazol-4-yl)pyrimidine-2-yl)-2-methylbenzonitrile and the pharmaceutically acceptable salt thereof.

IPC Classes  ?

• 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
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
• A61P 35/00 - Antineoplastic agents
• A61P 37/00 - Drugs for immunological or allergic disorders

Abstract

2A2B2B receptor.

IPC Classes  ?

• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61P 35/00 - Antineoplastic agents
• A61P 37/00 - Drugs for immunological or allergic disorders

Abstract

A traditional Chinese medicine composition for treating EGFR-TKIs related skin rash and a use thereof, characterized by comprising a therapeutically effective amount of the following components: honeysuckle, dandelion, radix sophorae flavescentis, Kochia scoparia, Dictamnus dasycarpus, tree peony root barks, Cortex Phellodendri, and peppermint. The traditional Chinese medicine composition for treating EGFR-TKIs related skin rash has a certain effect for the treatments of EGFR-TKIs related skin rash and paronychia. The raw materials coordinate with each other, thus can play medicinal effects to a maximum extent, thus significantly improving life quality of patients and prolonging survival period of patients. In addition, the traditional Chinese medicine composition also has advantages of non-toxic side effects and lower treatment cost.

IPC Classes  ?

• A61K 36/185 - Magnoliopsida (dicotyledons)
• A61K 36/288 - Taraxacum (dandelion)
• A61K 36/355 - Lonicera (honeysuckle)
• A61K 36/489 - Sophora, e.g. necklacepod or mamani
• A61K 36/534 - Mentha (mint)
• A61K 36/65 - Paeoniaceae (Peony family), e.g. Chinese peony
• A61K 36/71 - Ranunculaceae (Buttercup family), e.g. larkspur, hepatica, hydrastis, columbine or goldenseal
• A61K 36/756 - Phellodendron, e.g. corktree

Abstract

Provided are a pyrazole derivative, and an intermediate thereof and a preparation method therefor. The method has the characteristics of a simple operation, high selectivity, low cost, environmental friendliness, etc., and is suitable for industrial production.

IPC Classes  ?

• C07D 231/06 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
• C07D 487/04 - Ortho-condensed systems
• C07D 311/96 - Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings spiro-condensed with carbocyclic rings or ring systems
• A61K 31/4152 - 1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
• A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
• A61K 31/4433 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
• A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• A61P 25/04 - Centrally acting analgesics, e.g. opioids

Abstract

Disclosed are a pharmaceutically acceptable salt of an MOR receptor agonist, and a polymorph thereof and the use thereof. Specifically, disclosed are a pharmaceutically acceptable salt of (4S,6S)-6-isopropyl-N-(2-((R)-9-(pyridin-2yl)-6-oxa spiro[4.5]decyl-9-yl)ethyl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-4-amine, and a polymorph thereof and the use thereof. In addition, further disclosed are a pharmaceutical composition containing the pharmaceutically acceptable salt of the compound or the polymorph thereof, and the use thereof.

IPC Classes  ?

• A61K 31/4436 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
• C07D 487/04 - Ortho-condensed systems

Abstract

Disclosed are a pharmaceutically acceptable salt of an MOR receptor agonist, and a polymorph thereof and the use thereof. Specifically, disclosed are a pharmaceutically acceptable salt of (4S,6S)-6-isopropyl-N-(2-((R)-9-(pyridin-2-yl)-6-oxaspiro[4.5]decan-9-yl)ethyl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-4-amine, and a polymorph thereof and the use thereof. In addition, further disclosed are a pharmaceutical composition containing the pharmaceutically acceptable salt of the compound or the polymorph thereof, and the use thereof.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed 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
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

Abstract

The present application relates to an intermediate of a phenylpropyl pyridine derivative and a preparation method for the intermediate. The intermediate is a compound as represented by formula (I) or a pharmaceutically acceptable salt thereof.

IPC Classes  ?

• C07D 263/57 - Aryl or substituted aryl radicals

Abstract

A substituted triazinylmethylcycloalkylcarboxylic acid derivative having a structure as shown in formula (I). In addition, further disclosed are a pharmaceutically acceptable salt, a stereoisomer, a pharmaceutical composition and the use of the derivative. The compound has significant P2X3 inhibitory activity and selectivity, and is high in application value.

IPC Classes  ?

• C07D 251/46 - One nitrogen atom with oxygen or sulfur atoms attached to the two other ring carbon atoms
• 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
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 43/00 - Drugs for specific purposes, not provided for in groups

Abstract

Provided is a heterocycle substituted ketone derivative, the structure of which is as shown in formula (I). Further provided are a pharmaceutically acceptable salt of the derivative, a stereoisomer thereof, a pharmaceutical composition and the medicinal use thereof.

IPC Classes  ?

• A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
• A61P 35/00 - Antineoplastic agents
• A61P 35/02 - Antineoplastic agents specific for leukemia
• C07D 221/20 - Spiro-condensed ring systems
• C07D 241/20 - Nitrogen atoms
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 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 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
• C07D 471/10 - Spiro-condensed systems
• C07D 487/04 - Ortho-condensed systems
• C07D 495/04 - Ortho-condensed systems
• C07D 498/04 - Ortho-condensed systems

Abstract

Provided is a heterocycle substituted ketone derivative, the structure of which is as shown in formula (I). Further provided are a pharmaceutically acceptable salt of the derivative, a stereoisomer thereof, a pharmaceutical composition and the medicinal use thereof.

IPC Classes  ?

• 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 403/14 - 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 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 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 241/20 - Nitrogen atoms
• C07D 221/20 - Spiro-condensed ring systems
• C07D 487/04 - Ortho-condensed systems
• C07D 495/04 - Ortho-condensed systems
• C07D 498/04 - Ortho-condensed systems
• C07D 471/10 - Spiro-condensed systems
• A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
• A61P 35/00 - Antineoplastic agents
• A61P 35/02 - Antineoplastic agents specific for leukemia

Abstract

The use of a traditional Chinese medicine composition in the preparation of a drug for preventing or treating a chronic skin ulcer, wherein the traditional Chinese medicine composition comprises the following raw materials in parts by weight: 8-30 parts of Coptidis rhizoma, 6-25 parts of Sanguisorbae radix, 20-50 parts of a fatty acid obtained by means of refining mature larvae of Musca domestica Viciua, 4-18 parts of Angelicae sinensis radix, 5-20 parts of Cera flava and 1-5 parts of Borneolum syntheticum. The chronic skin ulcer comprises a diabetic skin ulcer, a pressure ulcer, a venous ulcer and a blood insufficiency ulcer.

IPC Classes  ?

• A61K 36/739 - Sanguisorba (burnet)
• A61K 36/718 - Coptis (goldthread)
• A61K 36/232 - Angelica
• A61K 35/644 - BeeswaxPropolisRoyal jellyHoney
• A61K 35/64 - Insects, e.g. bees, wasps or fleas
• A61K 31/045 - Hydroxy compounds, e.g. alcoholsSalts thereof, e.g. alcoholates
• A61P 17/02 - Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like

Abstract

Provided are compounds represented by formula (I), formula (II), formula (III) and formula (IV) as influenza virus replication inhibitors and the use thereof in the preparation of a medicament for preventing or treating influenza.

IPC Classes  ?

• C07D 471/14 - Ortho-condensed systems
• C07D 498/14 - Ortho-condensed systems
• C07D 471/04 - Ortho-condensed systems
• C07D 495/04 - Ortho-condensed systems
• C07D 495/00 - Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
• A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses
• 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
• A61K 31/5025 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
• A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems

Abstract

A fudosteine solution preparation for inhalation, a preparation method therefor and the use thereof, which belong to the field of pharmaceutical preparations. The concentration of fudosteine in the solution preparation for inhalation is 25-300 mg/mL. The fudosteine solution preparation for inhalation is an aerosol inhalation solution, which contains fudosteine with a specific concentration. The preparation has a good aerosol forming property, and can be effectively deposited at the drug effect site of the respiratory tract, so as to achieve the optimal drug concentration, and overcome the problem of the aerosol of the fudosteine aerosol inhalation preparation in the prior art not being able to achieve the optimal inhalation treatment effect, such that the drug efficacy of the preparation is better. In addition, compared with oral administration, the preparation has a higher drug distribution in the respiratory system at the same dose, a better phlegm-removing effect, and a low system exposure and better safety. The fudosteine solution preparation for inhalation has a better application prospect.

IPC Classes  ?

• A61K 9/72 - Medicinal preparations characterised by special physical form for smoking or inhaling
• A61K 9/08 - Solutions
• A61K 31/198 - Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
• A61P 11/00 - Drugs for disorders of the respiratory system

Abstract

A substituted morpholine derivative with a structure as shown in a formula (I). In addition, further disclosed are a pharmaceutically acceptable salt, a stereoisomer, a pharmaceutical composition and the use of the derivative.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 487/04 - Ortho-condensed systems
• C07D 265/30 - 1,4-OxazinesHydrogenated 1,4-oxazines not condensed with other rings
• A61K 31/5375 - 1,4-Oxazines, e.g. morpholine
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61P 13/00 - Drugs for disorders of the urinary system
• A61P 25/04 - Centrally acting analgesics, e.g. opioids
• A61P 11/06 - Antiasthmatics

Abstract

A substituted pyrazolo[1,5-alpyrimidin-7-amine derivative, the structure of which is represented by formula (l), or pharmaceutically acceptable salts, solvates, stereoisomers, prodrugs, drug compositions thereof. The derivative has significant CDK9-selective inhibitory activity.

IPC Classes  ?

• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 35/00 - Antineoplastic agents
• C07D 487/04 - Ortho-condensed systems

Abstract

A substituted pyrazolo[1,5-a]pyrimidin-7-amine derivative, the structure of which is represented by formula (I), or pharmaceutically acceptable salts, solvates, stereoisomers, prodrugs, drug compositions thereof. The derivative has significant CDK9-selective inhibitory activity.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 35/00 - Antineoplastic agents

Abstract

An oxaspiro substituted pyrrolopyrazole derivative, an intermediate thereof, and a preparation method therefor.

IPC Classes  ?

• C07D 311/96 - Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings spiro-condensed with carbocyclic rings or ring systems
• C07D 487/04 - Ortho-condensed systems

Abstract

The present invention relates to an intermediate of a substituted azabicyclo[3.2.1]octane compound, and a preparation method therefor. Specifically, disclosed in the present invention are an intermediate (the compound of formula (I)), a preparation method therefor, and a method for preparing an azabicyclo[3.2.1]octane compound by means of the intermediate. The definitions of groups in the formula are detailed in the description and the claims.

IPC Classes  ?

• C07D 451/06 - Oxygen atoms
• C07D 451/02 - 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 containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropaneCyclic acetals thereof

Abstract

The present invention relates to a pharmaceutical composition containing N-(2-(4-(dimethylamino)piperidin-1-yl)-5-(5-fluoro-4-(1-methyl-1H-pyrazol-4-yl)pyrimidin-2-ylamino)-4-methoxyphenyl)acrylamide maleate, and a preparation method therefor and a use thereof. According to the pharmaceutical composition, sticking in a preparation process is avoided, and the stability of the pharmaceutical composition is improved.

IPC Classes  ?

• A61K 9/20 - Pills, lozenges or tablets
• 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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/4468 - Non-condensed piperidines, e.g. piperocaine having a nitrogen atom directly attached in position 4, e.g. clebopride, fentanyl
• A61P 35/00 - Antineoplastic agents
• A61P 37/00 - Drugs for immunological or allergic disorders

Abstract

Provided are a substituted bis(pyridin-2-yl)amine derivative represented by formula (I), a pharmaceutically acceptable salt, solvate, stereoisomer, prodrug and pharmaceutical composition thereof, and a medical application thereof. The derivative has significant CDK9 selective inhibitory activity and is of great practical value.

IPC Classes  ?

• 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 471/04 - Ortho-condensed 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 498/04 - Ortho-condensed systems
• 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 401/12 - 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 487/04 - Ortho-condensed 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 31/538 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
• A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
• A61K 31/554 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
• A61K 31/537 - 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 spiro-condensed or forming part of bridged ring systems
• A61P 35/00 - Antineoplastic agents

Abstract

Provided are a polymorph of a Bruton's tyrosine kinase inhibitor, and a preparation method therefor and the use thereof, and specifically provided are two crystal forms of (R)-6-((1-acryloylpiperidin-3-yl)amino)-7-fluoro-4-((2-fluoro-4-morpholinophenyl)amino)-1,2-dihydro-3H-pyrrolo[3,4-c]pyridin-3-one, and a preparation method therefor and the use thereof. The two crystal forms have better stability, are less hygroscopic, have improved solubility and pharmacokinetic characteristics, and a stable preparation method, so that same can be mass-produced.

IPC Classes  ?

• C07D 471/00 - 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
• 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 35/00 - Antineoplastic agents

Abstract

Provided is a dezocine derivative crystal form A. The X-ray powder diffraction spectrum of the crystal form A, expressed by a diffraction angle of 2θ±0.2°, shows characteristic peaks at 8.894, 9.496, 10.974, 13.334, 15.338, 15.942, 17.707 and 24.178. The crystal form A of the dezocine derivative has a good stability and solubility, does not generate crystal transformation during a grinding process, and can be used as an opioid receptor modulator, and has an analgesic effect and broad application prospects.

IPC Classes  ?

• C07C 215/64 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with rings other than six-membered aromatic rings being part of the carbon skeleton
• A61K 31/135 - Amines, e.g. amantadine having aromatic rings, e.g. methadone
• A61P 25/04 - Centrally acting analgesics, e.g. opioids

Abstract

The present invention provides a BTK inhibitor, a pharmaceutically acceptable salt, a polymorph and an application thereof. Specifically, the present invention provides (R)-6-((1-acryloylpiperidin-3-yl)amino)-7-fluoro-4-((2-fluoro-4-morpholinophenyl)amino)-1,2-dihydro-3H-pyrrolo[3,4-c]pyridin-3-one, or the polymorph of a pharmaceutically acceptable salt thereof, and an application thereof. In addition, the present invention further discloses a pharmaceutical composition comprising the inhibitor and an application thereof.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems

Abstract

The present invention relates to a solid pharmaceutical preparation and a preparation method therefor. Specifically, disclosed are a solid pharmaceutical preparation that comprises an orexin receptor antagonist compound and a preparation method therefor, the solid pharmaceutical preparation comprising an active ingredient of a compound represented by formula I, a filler, a binder, a disintegrant, and a lubricant. The solid pharmaceutical preparation has good dissolution, stability and in vivo bioavailability.

IPC Classes  ?

• A61K 9/14 - Particulate form, e.g. powders
• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 31/46 - 8-Azabicyclo [3.2.1] octaneDerivatives thereof, e.g. atropine, cocaine
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 25/20 - HypnoticsSedatives
• A61P 25/22 - Anxiolytics
• A61P 25/30 - Drugs for disorders of the nervous system for treating abuse or dependence

Abstract

The present invention relates to a solid pharmaceutical preparation and a preparation method therefor. Specifically, disclosed are a solid pharmaceutical preparation that comprises an orexin receptor antagonist compound and a preparation method therefor, the solid pharmaceutical preparation comprising an active ingredient of a compound represented by formula I, a filler, a binder, a disintegrant, and a lubricant. The solid pharmaceutical preparation has good dissolution, stability and in vivo bioavailability.

IPC Classes  ?

• A61K 9/14 - Particulate form, e.g. powders
• A61K 9/20 - Pills, lozenges or tablets
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 31/46 - 8-Azabicyclo [3.2.1] octaneDerivatives thereof, e.g. atropine, cocaine
• A61P 25/30 - Drugs for disorders of the nervous system for treating abuse or dependence
• A61P 25/20 - HypnoticsSedatives
• A61P 25/22 - Anxiolytics
• A61P 11/00 - Drugs for disorders of the respiratory system

Abstract

The present disclosure relates to the technical field of medicines. Provided is a substituted pyrimidine or pyridine amine derivative represented by formula (I), and a pharmaceutically acceptable salt, solvate, stereoisomer, prodrug, and pharmaceutical composition thereof, as well as medical application thereof. The present disclosure provides a substituted pyrimidine or pyridine amine derivative with higher activity, higher selectivity, better pharmacokinetic parameters and higher tumor-inhibitory efficacy. The derivative has significant adenosine A2a receptor and/or adenosine A2b receptor antagonistic activities, which can be used to prevent and/or treat a disease mediated by an adenosine A2a receptor and/or an adenosine A2b receptor.

IPC Classes  ?

• 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
• 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 403/04 - 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 403/14 - 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

Abstract

2A 2B 2B receptor antagonistic activities.

IPC Classes  ?

• 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 403/14 - 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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
• A61P 35/00 - Antineoplastic agents
• A61P 37/00 - Drugs for immunological or allergic disorders

Goods & Services

(1) Dietary supplements for general health and well-being; analgesics; anti-infectives; anti-inflammatories; botanicals for the treatment of colds and flu; electrolytes; herbal supplements for general health and well being; medical imaging contrast media; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for the treatment of cancer; pharmaceutical preparations for the treatment of cardiovascular diseases; pharmaceutical preparations for the treatment of diabetes; pharmaceutical preparations for the treatment of genitourinary and pelvic diseases, disorders and infections, namely infertility, sexually transmitted diseases, incontinence and sexual dysfunction; pharmaceutical preparations for the treatment of the central nervous system, namely, encephalitis, epilepsy, Alzheimer's, cerebral palsy, Parkinson's disease; pharmaceutical preparations for the treatment of the respiratory system; pharmaceutical preparations for use in gastroenterology; pharmaceutical preparations for use in oncology; pharmaceutical preparations for use in ophthalmology; radiopharmaceuticals; chemical conductors for electrocardiograph electrodes; herbal supplements for general health and well-being; herbal supplements for the treatment of cancer; nutritional supplements for general health and well-being; food for babies; vitamin preparations; botanical supplements for general health and well-being; throat lozenges.

Abstract

Disclosed are an optically pure oxaspiro-substituted pyrrolopyrazole derivative, a preparation method therefor and the pharmaceutical use thereof as therapeutic agents, particularly as MOR receptor agonists, and use thereof in the preparation of drugs for treating pain and pain-associated diseases. The compounds are compounds as shown in formula (I) and formula (II) or a pharmaceutically acceptable salt thereof, or a solvate thereof, or a prodrug thereof. The compounds can treat MOR receptor agonist-mediated disease. Also disclosed are a preparation method therefor and the use thereof.

IPC Classes  ?

• A61K 31/4436 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
• A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• C07D 487/04 - Ortho-condensed systems

Abstract

Provided are an azabicyclic substituted oxaspiro derivative, a preparation method therefor and a medical use thereof. Specifically, provided are compounds represented by formula (I) and formula (II) or pharmaceutically acceptable salts, stereoisomers or solvates thereof, and a preparation method therefor and an application thereof.

IPC Classes  ?

• A61K 31/4188 - 1,3-Diazoles condensed with heterocyclic ring systems, e.g. biotin, sorbinil
• 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 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 25/04 - Centrally acting analgesics, e.g. opioids
• C07D 471/04 - Ortho-condensed systems
• C07D 487/04 - Ortho-condensed systems

Abstract

Provided are an azabicyclic substituted oxaspiro derivative, a preparation method therefor and a medical use thereof. Specifically, provided are compounds represented by formula (I) and formula (II) or pharmaceutically acceptable salts, stereoisomers or solvates thereof, and a preparation method therefor and an application thereof.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• C07D 471/04 - Ortho-condensed systems
• 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 31/444 - 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 25/04 - Centrally acting analgesics, e.g. opioids
• 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

Abstract

Disclosed are an optically pure oxaspiro-substituted pyrrolopyrazole derivative, a preparation method therefor and the pharmaceutical use thereof. The compounds are compounds as shown in formula (I) and formula (II) or a pharmaceutically acceptable salt thereof, or a solvate thereof, or a prodrug thereof, Also disclosed are a preparation method therefor and the use thereof.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• 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 31/4436 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

Abstract

The present invention relates to a bi-heterocyclic methylethylamine substituted oxaspiro derivative, a preparation method therefor, and a pharmaceutical use thereof. In particular, disclosed are a compound of formula (I) or a pharmaceutically acceptable salt, a stereoisomer or a solvate thereof, a preparation method therefor and the use thereof. The definition of each group in the formula is detailed in the description and claims.

IPC Classes  ?

• 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 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• A61K 31/4436 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

Goods & Services

Medicines for veterinary purposes; pesticides; disinfectant wipes; first aid bags containing Chinese medicines; preparations to facilitate teething; diapers for pets; tonics [medicines]; medicines for human purposes; radiopharmaceutical; oxygen for medical purposes; chemical conductors for electrocardiograph electrodes; semen for artificial insemination; disinfectants; solutions for contact lenses; bacteriological culture mediums; dietetic substances adapted for medical use; food for babies; depuratives.

Abstract

Disclosed are a substituted phenylpropenylpyridine derivative, a preparation method therefor and the use thereof as a PD-1/PD-L1 inhibitor. In particular, disclosed are a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof, a preparation method therefor and the use thereof. The definition of each group in the formula is detailed in the description and claims.

IPC Classes  ?

• 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 401/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
• C07D 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 31/4418 - Non-condensed pyridinesHydrogenated derivatives thereof having a carbocyclic ring directly attached to the heterocyclic ring, e.g. cyproheptadine
• A61P 35/00 - Antineoplastic agents

Abstract

A nitrogen heterocycle substituted sulfonylbenzamide derivative, a preparation method therefor and use thereof in medicine are involved. Specifically, a compound of formula (I) or a pharmaceutically acceptable salt, a stereoisomer, a solvent compound or a prodrug thereof, and a preparation method therefor and use thereof are disclosed.

IPC Classes  ?

• C07D 207/08 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
• 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 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

Abstract

The present invention relates to a sulfonylbenzamide derivative, a preparation method therefor, and a medical use thereof. Specifically, disclosed are a compound of formula (II) or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof, a preparation method therefor, and an application thereof.

IPC Classes  ?

• C07C 311/31 - Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atoms of the sulfonamide groups bound to acyclic carbon atoms
• C07C 233/44 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to a carbon atom of an unsaturated carbon skeleton
• A61K 31/166 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon atom of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
• A61K 31/18 - Sulfonamides
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 25/24 - Antidepressants
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 25/00 - Drugs for disorders of the nervous system

Abstract

Disclosed are a tetrahydroisoquinoline sulfonylamide derivative, a preparation method therefor and the medical use thereof. In particular, disclosed are compounds of formula (III) and formula (IV) or a pharmaceutically acceptable salt, a stereoisomer, a solvate or a prodrug thereof, and a preparation method therefor and the use thereof, wherein the definition of each group in the formulae is detailed in the description.

IPC Classes  ?

• C07D 209/46 - Iso-indolesHydrogenated iso-indoles with an oxygen atom in position 1
• C07D 217/08 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ringAlkylene-bis-isoquinolines with a hetero atom directly attached to the ring nitrogen atom
• C07D 217/24 - Oxygen atoms
• 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
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61K 31/4035 - Isoindoles, e.g. phthalimide
• A61K 31/4015 - 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 having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
• 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

Abstract

The present invention relates to an alkylsulfamoyl indazole carboxamide derivative, a preparation method therefor, and a pharmaceutical use thereof. In particular, disclosed are a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof, a preparation method therefor, and an application thereof. The definition of each group in the formula is detailed in the description.

IPC Classes  ?

• 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 231/56 - BenzopyrazolesHydrogenated benzopyrazoles
• A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
• A61K 31/4412 - Non-condensed pyridinesHydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
• A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 9/00 - Drugs for disorders of the cardiovascular system

Abstract

The present invention relates to a sulfonyl-substituted benzoheterocyclic formamide derivative, and a preparation method therefor and a medical use thereof. Specifically, a compound of formula (I) or a pharmaceutically acceptable salt, a stereoisomer, a solvate compound or a prodrug thereof, a preparation method therefor, and a use thereof are disclosed in the present invention, and the definition of each group in the formula is detailed in the description. (I)

IPC Classes  ?

• 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 231/56 - BenzopyrazolesHydrogenated benzopyrazoles
• A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
• A61K 31/4412 - Non-condensed pyridinesHydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
• A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 9/00 - Drugs for disorders of the cardiovascular system

Abstract

The present invention provides a BTK inhibitor, a pharmaceutically acceptable salt, a polymorph and an application thereof. Specifically, the present invention provides (R)-6-((1-Acryloylpiperidin-3-yl)amino)-7-fluoro-4-((2-fluoro-4-morpholinophenyl)amino)-1,2-dihydro-3H-pyrrolo[3,4-c]pyridin-3-one, or the polymorph of a pharmaceutically acceptable salt thereof, and an application thereof. In addition, the present invention further discloses a pharmaceutical composition comprising the inhibitor and an application thereof.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• 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 35/00 - Antineoplastic agents

Abstract

Disclosed is a preparation method of an orexin receptor antagonist compound 5-3. Crystalline forms I-IV of an orexin receptor antagonist compound 5-3 are provided. Also provided are processes of preparing crystalline forms of the orexin receptor antagonist compound 5-3, as well as methods of using the crystalline forms I-IV for treating an orexin-related disease.

IPC Classes  ?

• C07D 451/02 - 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 containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropaneCyclic acetals thereof
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/46 - 8-Azabicyclo [3.2.1] octaneDerivatives thereof, e.g. atropine, cocaine
• A61P 25/34 - Tobacco-abuse
• A61P 25/20 - HypnoticsSedatives
• A61P 25/22 - Anxiolytics
• A61P 11/08 - Bronchodilators

Abstract

Provided are 4,5,6-tri-substituted indazoles derivatives, a preparation method therefor, and a use thereof in medicines. Specifically, provided are compounds of formula (I) or pharmaceutically acceptable salts, stereoisomers, solvates, or prodrugs thereof, a preparation method therefor, and a use thereof.

IPC Classes  ?

• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Abstract

Disclosed are a preparation method of an orexin receptor antagonist compound 5-3. Crystalline forms I-IV of an orexin receptor antagonist compound 5-3 are provided. Also provided are processes of preparing crystalline forms of the orexin receptor antagonist compound 5-3, as well as methods of using the crystalline forms I-IV for treating an orexin-related disease.

IPC Classes  ?

• C07D 451/02 - 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 containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropaneCyclic acetals thereof
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/46 - 8-Azabicyclo [3.2.1] octaneDerivatives thereof, e.g. atropine, cocaine
• A61P 25/34 - Tobacco-abuse
• A61P 25/20 - HypnoticsSedatives
• A61P 25/22 - Anxiolytics
• A61P 11/08 - Bronchodilators

Abstract

Disclosed is a preparation method of an orexin receptor antagonist compound 5-3. Crystalline forms I-IV of an orexin receptor antagonist compound 5-3 are provided. Also provided are processes of preparing crystalline forms of the orexin receptor antagonist compound 5-3, as well as methods of using the crystalline forms I-IV for treating an orexin-related disease.

IPC Classes  ?

• C07D 451/02 - 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 containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropaneCyclic acetals thereof
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/46 - 8-Azabicyclo [3.2.1] octaneDerivatives thereof, e.g. atropine, cocaine
• A61P 25/34 - Tobacco-abuse
• A61P 25/20 - HypnoticsSedatives
• A61P 25/22 - Anxiolytics
• A61P 11/08 - Bronchodilators

Abstract

Provided are a tricyclic substituted oxaspiro derivative, a preparation method therefor, and a pharmaceutical use thereof. In particular, compounds of formula (I) and formula (II) or pharmaceutically acceptable salts, stereoisomers, or solvates thereof, preparation methods therefor, and uses thereof are disclosed.

IPC Classes  ?

• C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 409/14 - 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
• A61K 31/4427 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems
• A61K 31/4433 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
• 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 31/45 - Non-condensed piperidines, e.g. piperocaine having oxo groups directly attached to the heterocyclic ring, e.g. cycloheximide
• 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]

Abstract

Provided are an amide derivative substituted by cycloalkyl, a preparation method for the amide derivative, and a use in medicine. Specifically, provided are a compound of formula (I), or a pharmaceutically acceptable salt or stereisomer of the compound, and a preparation method and application of the compound, and the definitions of the groups in the formula are stated in detail in the description.

IPC Classes  ?

• C07D 215/18 - Halogen atoms or nitro 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
• C07C 233/64 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
• A61K 31/47 - QuinolinesIsoquinolines
• A61P 35/00 - Antineoplastic agents

Abstract

The present disclosure relates to 4,6,7-trisubstituted 1,2-dihydropyrrolo[3,4-c]pyridin/pyrimidin-3-one derivatives, and their preparations and medicinal use. Specifically, the present disclosure discloses a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof, and a preparation method and use thereof, wherein the definition of each group is as described in the specification and claims.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• 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 35/04 - Antineoplastic agents specific for metastasis
• A61P 35/00 - Antineoplastic agents
• C07D 487/04 - Ortho-condensed systems

Abstract

The present invention relates to an amino-substituted pyridone derivative, a preparation method therefor, and a pharmaceutical use thereof. Specifically, disclosed are a compound of formula (I), or a pharmaceutically acceptable salt, a stereoisomer or a solvent compound thereof, and a preparation method therefor and a use thereof. Each group in the formula is defined in the description.

IPC Classes  ?

• 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 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
• C07D 213/74 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
• C07D 213/16 - Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom containing only hydrogen and carbon atoms in addition to the ring nitrogen atom containing only one pyridine ring
• C07D 213/63 - One oxygen atom
• C07D 471/04 - Ortho-condensed systems
• C07D 493/04 - Ortho-condensed systems
• C07D 513/04 - Ortho-condensed systems
• A61K 31/4427 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems
• A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
• A61K 31/4704 - 2-Quinolinones, e.g. carbostyril
• A61P 35/00 - Antineoplastic agents

Abstract

Provided is a diheterocycle-substituted pyridine-2(1H)-ketone derivative, a preparation method therefore and a pharmaceutical use thereof. Specifically, provided are a compound of formula (I) or pharmaceutically acceptable salts thereof, a stereoisomer or a solvate, a preparation method therefor and an application thereof. (I)

IPC Classes  ?

• 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 487/04 - Ortho-condensed systems
• A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
• A61P 9/00 - Drugs for disorders of the cardiovascular system

Abstract

Disclosed is a crystal form of dezocine. The X-ray powder diffraction (XRD) pattern thereof is determined using Cu/K-α1 and has diffraction peaks at the 2θ value of 9.1±0.2 and 12.2±0.2, with the height % of these diffraction peaks greater than 20. Also disclosed are a preparation method for the crystal form, a pharmaceutical composition and use thereof. The crystal form of dezocine has good solubility, the preparation method has simple operations, good reproducibility, suitability for industrial production and the like.

IPC Classes  ?

• C07C 215/64 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with rings other than six-membered aromatic rings being part of the carbon skeleton
• C07C 213/10 - SeparationPurificationStabilisationUse of additives

Abstract

The present disclosure discloses sodium ion channel inhibitors, pharmaceutically acceptable salts and polymorphs thereof, and uses thereof. Specifically, the present disclosure discloses a polymorph of a compound of formula (X) and a preparation method thereof. The preparation method of the present disclosure is simple in operation and suitable for industrialization. The polymorph prepared by the preparation method has advantages of good stability, low hygroscopicity and high water solubility.

IPC Classes  ?

• C07D 241/04 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members

Abstract

The present invention relates to a 1,2-dihydropyrrol[3,4-c]pyridin/pyrimidin-3-one derivative substituted by N-(3-aminophenyl)acrylamide and a preparation method and pharmaceutical use thereof. In particular, the present invention relates to a compound of formula (II) or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof and a preparation method and application of the same. The definition of each substituent in the formula is described in detail in the specification and claims.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• A61P 35/00 - Antineoplastic agents
• C07D 487/04 - Ortho-condensed systems
• A61P 35/04 - Antineoplastic agents specific for metastasis
• 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

Abstract

The present disclosure relates to pyridinamine-substituted heterotricyclo compounds, a preparation method thereof, and a use thereof in medicines. Specifically, a compound of formula (I), or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof, a preparation method and a use thereof are disclosed, wherein the groups in the formula (I) are as defined in the Description and claims.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• C07D 487/10 - Spiro-condensed systems
• 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 495/14 - Ortho-condensed systems
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 35/00 - Antineoplastic agents

Abstract

Provided are a CDK4/6 inhibitor and a pharmaceutically acceptable salt and a polymorph thereof, and the use thereof. In particular, provided are a polymorph of 2-cyclopropyl-N-(5-((4-ethylpiperazin-1-yl)methyl)pyridin-2-yl)-3-isopropyl-3,8-dihydroimidazo[4',5',4,5]cyclopentadieno[1,2-d]pyrimidin-5-amine and a pharmaceutically acceptable salt thereof, and the use thereof. In addition, also disclosed are a pharmaceutical composition of the compound and the use thereof.

IPC Classes  ?

• 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 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• 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 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• A61P 35/00 - Antineoplastic agents
• A61P 37/00 - Drugs for immunological or allergic disorders
• A61P 43/00 - Drugs for specific purposes, not provided for in groups

Abstract

The present invention provides an EZH2 inhibitor and pharmaceutically acceptable salts and polymorphic substances thereof, and application of the EZH2 inhibitor. Specifically, the present invention provides N-((4,6-dimethyl-2-oxo-1,2-dihydropyridine-3-yl)methyl)-5-ethyl-4-(ethyl((1S,4S)-4-(3-methyl azacyclobutanazine-1-yl)cyclohexyl)amino)-1-methyl-1H-indazol-6-formamide or polymorphic substances of pharmaceutically acceptable salts thereof, and application of N-((4,6-dimethyl-2-oxo-1,2-dihydropyridine-3-yl)methyl)-5-ethyl-4-(ethyl((1S,4S)-4-(3-methyl azacyclobutanazine-1-yl)cyclohexyl)amino)-1-methyl-1H-indazol-6-formamide. In addition, also disclosed are a pharmaceutical composition containing the inhibitor and application thereof.

IPC Classes  ?

• C07D 231/56 - BenzopyrazolesHydrogenated benzopyrazoles
• 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 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
• A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
• 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
• A61P 35/00 - Antineoplastic agents
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 19/08 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
• A61P 31/12 - Antivirals

Abstract

The present invention provides pharmaceutically acceptable salts of a benzodicycloalkane derivative, a polymorphic substance thereof, and an application thereof. Specifically, the present invention provides a benzodicycloalkane derivative or pharmaceutically acceptable salts thereof and an application thereof. In addition, also disclosed are a pharmaceutical composition of the compound and an application thereof.

IPC Classes  ?

• C07D 305/08 - 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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring atoms
• A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
• A61P 25/04 - Centrally acting analgesics, e.g. opioids

Abstract

The present invention relates to a sulfuryl-substituted benzoheterocyclic derivative, a preparation method and medical use thereof. Particularly, disclosed is a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof, and a preparation method and application thereof. The definition of each group in the formula can be found in the specification and the claims.

IPC Classes  ?

• 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 209/04 - IndolesHydrogenated indoles
• C07D 209/56 - Ring systems containing three or more rings
• C07D 247/00 - Heterocyclic compounds containing rings having two nitrogen atoms as the only ring hetero atoms, according to more than one of groups
• 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 401/12 - 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 487/00 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups
• A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
• A61P 35/00 - Antineoplastic agents
• A61K 31/4045 - Indole-alkylaminesAmides thereof, e.g. serotonin, melatonin
• A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
• A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof

Goods & Services

Chemico-pharmaceutical preparations, namely, anti-infectives, pain relief medication, cardiovascular pharmaceuticals, digestives for pharmaceutical purposes, Chinese traditional medicinal herbs, tumor suppressing agents, X-ray contrast agents, pharmaceutical preparations acting on the central nervous system; collyrium; analgesics; medicines for human purposes, namely, anti-infectives, pain relief medication, cardiovascular pharmaceuticals, digestives for pharmaceutical purposes, Chinese traditional medicinal herbs, tumor suppressing agents, X-ray contrast agents, pharmaceutical preparations acting on the central nervous system; medicinal drinks; ointment for pharmaceutical use, namely, medicated ointments for treating dermatological conditions; Chinese medicine nostrum namely, medicinal herbs; adhesive patches for medical use, namely medical plasters; biochemical pharmaceutical preparations, namely, anti-infectives, pain relief medication, cardiovascular pharmaceuticals, digestives for pharmaceutical purposes, Chinese traditional medicinal herbs, tumor suppressing agents, X-ray contrast agents, pharmaceutical preparations acting on the central nervous system; blood for medical use; blood plasma; blood substitutes for human, veterinary use; medicines in form of glue balls, namely anti-infectives, pain relief medication, cardiovascular pharmaceuticals, digestives for pharmaceutical purposes, Chinese traditional medicinal herbs, tumor suppressing agents, X-ray contrast agents, pharmaceutical preparations acting on the central nervous system; medical drinks in the nature of flavored tonic liquors; dietetic foods adapted for medical purposes; depuratives for the body; animal feed additives for medical purpose for use as nutritional supplements; parasiticides; wadding for medical purposes; pharmaceutical preparations to facilitate teething

Goods & Services

Medical preparations, namely, foot, hand and skin creams for diabetics; Medical preparation, namely, anti-cancer preparations; chemico-pharmaceutical preparations, namely, anti-infectives, pain relief medication, Chinese traditional medicinal herbs; radiological contrast substances for medical purposes; analgesics; drug delivery agents in the form of capsules that provide controlled release of the active ingredients for a wide variety of pharmaceuticals; medicines for human purposes, namely, anti-infectives, pain relief medication, cardiovascular pharmaceuticals, digestives for pharmaceutical purposes, Chinese traditional medicinal herbs, tumor suppressing agents, X-ray contrast agents, pharmaceutical preparations acting on the central nervous system; medicinal drinks; injectable pharmaceuticals for treatment of anaphylactic reactions; medicinal ointments for treating dermatological conditions; Chinese medicine nostrum namely, medicinal herbs; pills for pharmaceutical purposes namely anti-infectives, pain relief medication, cardiovascular pharmaceuticals, digestives for pharmaceutical purposes, Chinese traditional medicinal herbs, tumor suppressing agents, X-ray contrast agents, pharmaceutical preparations acting on the central nervous system; sticking plasters for medical purposes; biochemicial drug in the nature of biological preparations for the treatment of cancer; blood for medical purposes; gelatin capsules sold empty for pharmaceuticals; alcohol for medicinal purposes; medicated eye-wash; dietetic foods adapted for medical purposes; depuratives for the body; non medicated additives for animal feed for use as nutritional supplement; vermin destroying preparations; wadding for medical purposes; preparations to facilitate teething, namely, teething gels

Goods & Services

Medical preparation; chemico-pharmaceutical preparations; radiological contrast substances for medical purposes; analgesics; drug capsule; medicines for human purposes; medicinal drinks; injectable pharmaceuticals; medicinal ointments; Chinese medicine nostrum; pills for pharmaceutical purposes; sticking plasters for medical purposes; biochemicial drug; blood for medical purposes; gelatin capsules for pharmaceuticals; alcohol for medicinal purposes; eye-wash; dietetic foods adapted for medical purposes; depuratives; feed additives for medical purpose; vermin destroying preparations; wadding for medical purposes; preparations to facilitate teething. Medical apparatus and instruments; dental apparatus and instruments; electric acupuncture instruments; soporific pillows for insomnia; sterile sheets, surgical; babies' bottles; condoms; artificial limbs; orthopaedic articles; suture materials. Tea; tea-based beverages; pollen paste for use as a seasoning; pear paste for use as a seasoning; longan paste for use as a seasoning; litchi paste for use as a seasoning; loquat leaf extract for use as a seasoning; cereal preparations; soya flour; gluten prepared as foodstuff.

Abstract

The present invention relates to an immunomodulator, a preparation method thereof, and an application of the same as a PD-1/PD-L1 inhibitor. In particular, disclosed are a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof and a preparation method and application thereof. The definition of each substituent in the formula is described in detail in the specification and claims.

IPC Classes  ?

• C07D 213/38 - Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
• 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 401/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
• C07D 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 31/4418 - Non-condensed pyridinesHydrogenated derivatives thereof having a carbocyclic ring directly attached to the heterocyclic ring, e.g. cyproheptadine
• A61P 35/00 - Antineoplastic agents

Abstract

The present application relates to an N-(2-cyclohexylethyl)formamide derivative, a preparation method therefor, and pharmaceutical use thereof. Specifically, a compound of formula (I) or a pharmaceutically acceptable salt, a stereoisomer or a solvate compound thereof, a preparation method therefor and use thereof are disclosed.

IPC Classes  ?

• C07D 215/18 - Halogen atoms or nitro radicals
• C07D 215/16 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
• C07D 215/02 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 413/12 - 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 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 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• A61K 31/47 - QuinolinesIsoquinolines
• A61P 35/00 - Antineoplastic agents

Goods & Services

Tonics [medicines]; preparations to facilitate teething; radioactivity drug; medicinal ointments; gelatin capsules for pharmaceuticals; air deodorising preparations; pharmaceutical preparations in the form of troche; semen for artificial insemination; medicines for human purposes; pesticides; biochemicial drug; medicines for veterinary purposes; pharmaceutical preparations in the form of aqua; disinfectants; impregnated antiseptic wipes; chemical conductors for electrocardiograph electrodes; medicinal drinks; cultures of microorganisms for medical and veterinary use; oxygen for medical purposes; drugs for medical purposes; dietetic substances adapted for medical use; contact lens cleaning preparations; raw material drug; injectable pharmaceuticals; Chinese medicine nostrum; Chinese medicine bag; pharmaceutical preparations in the form of tincture. Medical apparatus and instruments; radiological apparatus for medical purposes; surgical implants comprised of artificial materials; dental apparatus, electric; contraceptives, non-chemical; orthopaedic articles; surgical apparatus and instruments; furniture especially made for medical purposes; babies' bottles; suture materials. Tea; loquat leaf syrup; gluten prepared as foodstuff; honey; royal jelly; tortoise herb jelly; rock candy bird's nest being confectionery; extract of local chicken being seasonings; yeast; ice cream.

Abstract

The present invention relates to a PI3K inhibitor, and a pharmaceutically acceptable salt, polycrystalline form, and application thereof. The invention specifically provides a polycrystalline form of 4-chloro-5-(6-(1-(methylsulfonyl)cyclopropyl)-2-morpholinopyrimidin-4-yl)pyridin-2-amine, a pharmaceutically acceptable salt thereof, or a polycrystalline form of the salt. The invention further discloses a pharmaceutical composition comprising the inhibitor and an application of the pharmaceutical composition.

IPC Classes  ?

• 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 401/04 - 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
• A61P 35/02 - Antineoplastic agents specific for leukemia
• A61P 35/00 - Antineoplastic agents
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol

Abstract

Disclosed is a method for preparing a propofol medium/long chain fat emulsion injection, the preparation method comprising: under the protection of nitrogen, dissolving glycerin and sodium hydroxide in water for injection, and controlling the aqueous phase temperature at 50ºC-80ºC; and under the protection of nitrogen, dissolving propofol, oleic acid and egg yolk lecithin in an soybean oil and a medium chain triglyceride, heating the oil phase to 50ºC-80ºC, shearing and stirring, and mixing the aqueous phase and the oil phase, shearing same to prepare a primary emulsion, and homogenizing the primary emulsion to obtain a final emulsion. A propofol medium/long chain fat emulsion injection prepared by the method is also disclosed.

IPC Classes  ?

• A61K 9/107 - Emulsions
• A61K 31/05 - Phenols
• A61P 23/00 - Anaesthetics

Abstract

The present invention relates to a 1,2-dihydropyrrol[3,4-c]pyridin/pyrimidin-3-one derivative substituted by N-(3-aminophenyl)acrylamide and a preparation method and pharmaceutical use thereof. In particular, the present invention relates to a compound of formula (II) or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof and a preparation method and application of the same. The definition of each substituent in the formula is described in detail in the specification and claims.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• C07D 487/04 - Ortho-condensed systems
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 35/00 - Antineoplastic agents
• A61P 37/00 - Drugs for immunological or allergic disorders

Abstract

Provided are a 4,6,7-trisubstituted 1,2-dihydropyrrol[3,4-c]pyridin/pyrimidin-3-one derivative and a preparation method and pharmaceutical use thereof. In particular, the present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof and a preparation method and application of the same. The definition of each substituent in the formula is described in detail in the specification and claims.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• C07D 487/04 - Ortho-condensed systems
• 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 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 35/00 - Antineoplastic agents

Abstract

Disclosed are a sodium ion channel inhibitor and a pharmaceutically acceptable salt and a polymorph thereof. The sodium ion channel inhibitor is a compound having the structure as shown in formula (X). Disclosed are a method for preparing the sodium ion channel inhibitor, a polymorph thereof and a preparation method therefor, and a pharmaceutical composition thereof. The compound and the pharmaceutical composition are used for treating pain, depression, cardiovascular diseases, respiratory disease or psychotic disorder.

IPC Classes  ?

• C07D 295/00 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
• C07B 61/00 - Other general methods
• A61K 31/4965 - Non-condensed pyrazines
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 25/24 - Antidepressants
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

Abstract

The present invention discloses an N-sulfonyl benzamide derivative with a heterocyclic substituent, and a preparation method therefor and a pharmaceutical application thereof. More specifically, the invention discloses a compound represented by formula (II) or a pharmaceutically acceptable salt, stereoisomer, solvent compound, or prodrug thereof, and a preparation method therefor and an application thereof. Refer to the specification for definitions of each group in the formula.

IPC Classes  ?

• A61K 31/166 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon atom of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
• C07C 233/64 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
• C07D 207/09 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
• 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 211/46 - Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
• C07D 295/155 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
• A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• A61K 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
• C07D 213/74 - Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• C07D 207/08 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
• 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
• C07D 213/80 - AcidsEsters in position 3
• C07D 241/04 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members

Goods & Services

Tonics, namely, medicines for the treatment of gastrointestinal diseases; preparations to facilitate teething, namely, teething gels; radioactivity drug in the nature of radioactive substances for medical purposes; medicinal ointments, namely, mentholated ointment for medical use; gelatin capsules sold empty for pharmaceuticals; air deodorising preparations; pharmaceutical preparations in the form of troche being medicated lozenges; semen for artificial insemination; antiallergic medicines for human purposes; pesticides; biochemicial drug preparations for medical purposes for the treatment of headaches; medicines being enzymes for veterinary purposes; pharmaceutical preparations in the form of aqua, namely, medicated water for the treatment of gastrointestinal diseases; disinfectants; impregnated antiseptic wipes; chemical conductors for electrocardiograph electrodes; medicinal drinks; cultures of microorganisms for medical and veterinary use; oxygen for medical purposes; drugs for medical purposes, namely, antibiotic preparations; dietetic substances in the nature of beverages and foods adapted for medical use; contact lens cleaning preparations; raw material drug in the nature of medicinal roots; injectable pharmaceuticals in the nature of injectable dermal fillers; Chinese medicine nostrum, namely, medicinal herbs; pharmaceutical preparations in the form of herbal tincture for medical purposes

Abstract

Disclosed is a crystal form of dezocine. The X-ray powder diffraction (XRD) pattern thereof is determined using Cu/K-α1, and has a diffraction peak at the 2θ value of 9.1±0.2 and 12.2±0.2, and the height% of these diffraction peaks are both greater than 20. Also disclosed are a preparation method for the crystal form, a pharmaceutical composition and the use thereof. The crystal form of dezocine has a good solubility, the operations of the preparation method are simple, and the method has good reproducibility, and is suitable for industrial production.

IPC Classes  ?

• C07C 213/10 - SeparationPurificationStabilisationUse of additives
• C07C 215/64 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with rings other than six-membered aromatic rings being part of the carbon skeleton

Abstract

Disclosed are a preparation method of an orexin receptor antagonist compound 5-3, Crystalline forms I-IV of an orexin receptor antagonist compound 5-3 are provided. Also provided are processes of the preparing the orexin receptor antagonist compound 5-3 and its crystalline forms, as well as methods of using the crystalline forms I-IV for treating an orexin-related disease.

IPC Classes  ?

• C07D 451/02 - 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 containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropaneCyclic acetals thereof
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/46 - 8-Azabicyclo [3.2.1] octaneDerivatives thereof, e.g. atropine, cocaine
• A61P 25/34 - Tobacco-abuse
• A61P 25/20 - HypnoticsSedatives
• A61P 25/22 - Anxiolytics
• A61P 11/08 - Bronchodilators

Abstract

Provided are a benzodicycloalkane derivative, and a preparation method and use thereof. In particular, provided is a compound of formula (I), or a pharmaceutically acceptable salt, stereoisomer or solvate thereof, a preparation method therefor and a use thereof in the preparation of drugs for treating pain.

IPC Classes  ?

• C07C 215/64 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with rings other than six-membered aromatic rings being part of the carbon skeleton
• C07C 217/94 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings being part of condensed ring systems and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
• C07C 271/58 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring
• A61K 31/135 - Amines, e.g. amantadine having aromatic rings, e.g. methadone
• A61P 25/04 - Centrally acting analgesics, e.g. opioids