Provided are a quinazoline compound, a composition, and an application thereof, in particular, a compound represented by formula (I), a stereoisomer thereof, a pharmaceutically acceptable salt thereof, a composition thereof, and an application thereof in the preparation for a drug that serves as a tyrosine kinase inhibitor. The compound represented by formula (I) has good inhibitory activity against EGFR and HER2 kinases.
Provided are a quinazoline compound, a composition, and an application thereof, in particular, a compound represented by formula (I), a stereoisomer thereof, a pharmaceutically acceptable salt thereof, a composition thereof, and an application thereof in the preparation for a drug that serves as a tyrosine kinase inhibitor. The compound represented by formula (I) has good inhibitory activity against EGFR and HER2 kinases.
A61K 31/517 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61P 35/04 - Antineoplastic agents specific for metastasis
2.
QUINAZOLINE-BASED COMPOUND, COMPOSITION, AND APPLICATION OF QUINAZOLINE-BASED COMPOUND
Provided are a quinazoline-based compound, a composition, and an application of the quinazoline-based compound, in particular, relating to a compound represented by formula (I), a stereoisomer thereof, a pharmaceutically acceptable salt or deuterated derivative thereof, a composition thereof, and an application thereof in the preparation of a drug that serves as a tyrosine kinase inhibitor. The compound has good inhibitory activity against EGFR, HER2 kinase, and their exon 20 mutations and EGFRviii mutations.
Provided are a quinazoline-based compound, a composition, and an application of the quinazoline-based compound, in particular, relating to a compound represented by formula (I), a stereoisomer thereof, a pharmaceutically acceptable salt or deuterated derivative thereof, a composition thereof, and an application thereof in the preparation of a drug that serves as a tyrosine kinase inhibitor. The compound has good inhibitory activity against EGFR, HER2 kinase, and their exon 20 mutations and EGFRviii mutations.
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 31/517 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
3.
SALT OF DIOXANE QUINOLINE COMPOUND, CRYSTAL FORM THEREOF, PREPARATION METHODS THEREFOR AND USES THEREOF
The present invention provides a salt of a dioxane quinoline compound, a crystal form thereof, preparation methods therefor and uses thereof. Specifically, the present invention relates to N-(3-fluoro-4-((5-(3-morpholinopropoxy) -2,3-dihydro-[1,4] dioxano[2,3-f] quinolin-10-yl) oxy) phenyl)-N-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide, a crystal form thereof and preparation methods therefor, and uses in the preparation of a drug as an inhibitor of tyrosine kinases (e.g. VEGFR -2 and c-MET, etc.). Formula (I).
Provided are a carbonyl bridged heterocyclic compound having a structure represented by formula (I), a stereoisomer or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing these compounds, and an application of these compounds or composition in drug preparation. The compounds, the stereoisomer, the pharmaceutically acceptable salt thereof and the like can be used for treating or preventing autoimmune diseases, tumors and neurodegenerative diseases related to protein 1 kinase (RIPK1).
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 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A cyano-substituted pyridine and cyano-substituted pyrimidine compound and a preparation method therefor and an application thereof, which specifically relate to a compound represented by formula (I) and an isomer, a hydrate, a solvate, a pharmaceutically acceptable salt, and a prodrug thereof, and a preparation method therefor and an application thereof in the preparation of a drug as a kinase inhibitor. The compound has good inhibitory activity against kinases such as FGFR4 and mutant FGFR4V550L.
A cyano-substituted pyridine and cyano-substituted pyrimidine compound and a preparation method therefor and an application thereof, which specifically relate to a compound represented by formula (I) and an isomer, a hydrate, a solvate, a pharmaceutically acceptable salt, and a prodrug thereof, and a preparation method therefor and an application thereof in the preparation of a drug as a kinase inhibitor. The compound has good inhibitory activity against kinases such as FGFR4 and mutant FGFR4V550L.
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 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
6.
QUINAZOLINE COMPOUND, COMPOSITION, AND APPLICATION THEREOF
Provided are a quinazoline compound, a composition, and an application thereof, in particular, a compound represented by formula (I), a stereoisomer thereof, a pharmaceutically acceptable salt thereof, a composition thereof, and an application thereof in the preparation for a drug that serves as a tyrosine kinase inhibitor. The compound represented by formula (I) has good inhibitory activity against EGFR and HER2 kinases.
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 31/498 - Pyrazines or piperazines ortho- or peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
Provided are an acylamino bridged heterocyclic compound of formula (I) or a pharmaceutically acceptable salt, an isomer, a solvate, a crystal, or a prodrug thereof, and a pharmaceutical composition comprising the compound, and an application of the compound or composition in drug preparation. The compound and the pharmaceutically acceptable salt, the isomer, the solvate, the crystal, or the prodrug thereof and the like can be used for treatment or prevention of autoimmune diseases, tumors, and neurodegenerative diseases related to receptor-interacting protein kinase-1 (RIPK1).
Provided are an acylamino bridged heterocyclic compound of formula (I) or a pharmaceutically acceptable salt, an isomer, a solvate, a crystal, or a prodrug thereof, and a pharmaceutical composition comprising the compound, and an application of the compound or composition in drug preparation. The compound and the pharmaceutically acceptable salt, the isomer, the solvate, the crystal, or the prodrug thereof and the like can be used for treatment or prevention of autoimmune diseases, tumors, and neurodegenerative diseases related to receptor-interacting protein kinase-1 (RIPK1).
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 413/12 - 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
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
8.
QUINAZOLINE-BASED COMPOUND, COMPOSITION, AND APPLICATION OF QUINAZOLINE-BASED COMPOUND
Provided are a quinazoline-based compound, a composition, and an application of the quinazoline-based compound, in particular, relating to a compound represented by formula (I), a stereoisomer thereof, a pharmaceutically acceptable salt or deuterated derivative thereof, a composition thereof, and an application thereof in the preparation of a drug that serves as a tyrosine kinase inhibitor. The compound has good inhibitory activity against EGFR, HER2 kinase, and their exon 20 mutations and EGFRviii mutations.
A61P 1/06 - Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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
9.
QUINAZOLINE-BASED COMPOUND, COMPOSITION, AND APPLICATION OF QUINAZOLINE-BASED COMPOUND
Provided are a quinazoline-based compound, a composition, and an application of the quinazoline-based compound, in particular, relating to a compound represented by formula (I), a stereoisomer thereof, a pharmaceutically acceptable salt or deuterated derivative thereof, a composition thereof, and an application thereof in the preparation of a drug that serves as a tyrosine kinase inhibitor. The compound has good inhibitory activity against EGFR, HER2 kinase, and their exon 20 mutations and EGFRviii mutations.
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 31/517 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61P 17/14 - Drugs for dermatological disorders for baldness or alopecia
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
A61P 1/06 - Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Disclosed are a class of compounds as inhibitors of kinases such as TRK, c-MET, AXL, MER and/or VEGFR2, compositions and use thereof. In particular, disclosed are a class of compounds (as shown in formula (1)) or isomers, solvates, hydrates, pharmaceutically acceptable salts, and prodrugs thereof having strong inhibition activities for kinases such as TRK, c-MET, AXL, MER and/or VEGFR2, and pharmaceutical compositions comprising said compounds. Also disclosed is use of the compounds or pharmaceutical compositions in the preparation of a medicament for treating autoimmune diseases or cancers.
Disclosed are a class of compounds as inhibitors of kinases such as TRK, c-MET, AXL, MER and/or VEGFR2, compositions and use thereof. In particular, disclosed are a class of compounds (as shown in formula (1)) or isomers, solvates, hydrates, pharmaceutically acceptable salts, and prodrugs thereof having strong inhibition activities for kinases such as TRK, c-MET, AXL, MER and/or VEGFR2, and pharmaceutical compositions comprising said compounds. Also disclosed is use of the compounds or pharmaceutical compositions in the preparation of a medicament for treating autoimmune diseases or cancers.
The present invention provides a quinazoline compound, a preparation method therefor and an application thereof, and specifically relates to a compound represented by formula (I), an isomer, a hydrate, a solvate, a pharmaceutically acceptable salt thereof, and a prodrug thereof, a preparation method therefor and an application thereof in the preparation of a drug that acts as a tyrosine kinase inhibitor. The compound in the present invention has good inhibitory activity on EGFR and HER2 kinase, and exhibits excellent performance of passing through the blood-brain barrier at the same time.
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
A61K 31/517 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61P 17/14 - Drugs for dermatological disorders for baldness or alopecia
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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 35/02 - Antineoplastic agents specific for leukemia
A61P 35/04 - Antineoplastic agents specific for metastasis
12.
CYANO-SUBSTITUTED PYRIDINE AND CYANO-SUBSTITUTED PYRIMIDINE COMPOUND AND PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
A cyano-substituted pyridine and cyano-substituted pyrimidine compound and a preparation method therefor and an application thereof, which specifically relate to a compound represented by formula (I) and an isomer, a hydrate, a solvate, a pharmaceutically acceptable salt, and a prodrug thereof, and a preparation method therefor and an application thereof in the preparation of a drug as a kinase inhibitor. The compound has good inhibitory activity against kinases such as FGFR4 and mutant FGFR4V550L.
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
13.
CYANO-SUBSTITUTED PYRIDINE AND CYANO-SUBSTITUTED PYRIMIDINE COMPOUND AND PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
A cyano-substituted pyridine and cyano-substituted pyrimidine compound and a preparation method therefor and an application thereof, which specifically relate to a compound represented by formula (I) and an isomer, a hydrate, a solvate, a pharmaceutically acceptable salt, and a prodrug thereof, and a preparation method therefor and an application thereof in the preparation of a drug as a kinase inhibitor. The compound has good inhibitory activity against kinases such as FGFR4 and mutant FGFR4V550L.
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
The present disclosure relates to a novel compound as a JAK inhibitor, a composition, and an application thereof. Specifically, the present disclosure provides a compound having high JAK inhibitory activity (as represented by formula (I)) or its isomer, solvate, hydrate, pharmaceutically-acceptable salt, and prodrug, and a pharmaceutical composition containing the compound. Also disclosed is a use of the present compound or pharmaceutical composition in preparation of a medicament for treating autoimmune diseases or cancers.
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 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61P 35/02 - Antineoplastic agents specific for leukemia
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 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
15.
Oxazino-quinazoline and oxazino-quinoline type compound, preparation method and uses thereof
Provided are an oxazino-quinazoline and oxazino-quinoline type compound, a preparation method, and uses thereof. More particularly provided is a compound shown in formula (I), an isomer, a hydrate, a solvate, a pharmaceutically acceptable salt, a prodrug thereof, a preparation method, and uses thereof in preparing a drug acting as a kinase inhibitor.
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 11/00 - Drugs for disorders of the respiratory system
The present invention relates to an urea-substituted aromatic ring-linked dioxinoquinoline compound of formula (I), or a pharmaceutically acceptable salt or a hydrate thereof. The invention also provides a preparation method of the compound of formula (I) and a pharmaceutically acceptable salt thereof, as well as uses thereof as a drug, wherein the drug acting as a tyrosine kinase (i.e. VEGFR-2, C-RAF, B-RAF, and RET) inhibitor is used for treating disorders related to tyrosine kinase.
C07D 491/056 - Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
A61K 31/4741 - Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having oxygen as a ring hetero atom, e.g. tubocuraran derivatives, noscapine, bicuculline
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/54 - 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 sulfur as the ring hetero atoms, e.g. sulthiame
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
17.
Dioxinoquinoline compounds, preparation method and uses thereof
The present invention relates to a dioxinoquinoline compound of formula (I) or a pharmaceutically acceptable salt thereof. The invention also provides a preparation method of the compound of formula (I) and a pharmaceutically acceptable salt thereof, as well as uses thereof as a drug, wherein the drug acting as a tyrosine kinase (i.e. VEGFR-2 and c-MET) inhibitor is used for treating disorders related to tyrosine kinase.
Provided are a class of new compounds which act as a JAK kinase inhibitor, a composition and use thereof. In particular, provided are a class of compounds having a strong JAK kinase inhibitory activity (as represented in formula (1)), or a stereoisomer, a geometric isomer, a tautomer, a pharmaceutically acceptable salt, a prodrug, a metabolic product, an isotope derivative and a solvate thereof, and a pharmaceutical composition containing the compound. Also disclosed is the use of the compound or the pharmaceutical composition of the present invention in the preparation of pharmaceuticals used for treating autoimmune diseases or cancers.
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
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61P 17/14 - Drugs for dermatological disorders for baldness or alopecia
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
A61P 37/00 - Drugs for immunological or allergic disorders
19.
ALKYNYLPYRIMIDINE OR ALKYNYLPYRIDINE COMPOUND, AND COMPOSITION AND APPLICATION THEREOF
An alkynylpyrimidine or alkynylpyridine compound represented by formula (I), or a pharmaceutically acceptable salt, isomer, solvate, crystal or prodrug thereof, as well as pharmaceutical compositions containing such compounds and an application of such compounds or compositions in the preparation of a drug, wherein the drug may be used as an inhibitor for kinases such as ABL, ABL-T315I, KIT, VEGFR-2, and so on for the treatment of related diseases.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 11/00 - Drugs for disorders of the respiratory system
Provided are an acylamino bridged heterocyclic compound of formula (I) or a pharmaceutically acceptable salt, an isomer, a solvate, a crystal, or a prodrug thereof, and a pharmaceutical composition comprising the compound, and an application of the compound or composition in drug preparation. The compound and the pharmaceutically acceptable salt, the isomer, the solvate, the crystal, or the prodrug thereof and the like can be used for treatment or prevention of autoimmune diseases, tumors, and neurodegenerative diseases related to receptor-interacting protein kinase-1 (RIPK1).
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
Provided are an acylamino bridged heterocyclic compound of formula (I) or a pharmaceutically acceptable salt, an isomer, a solvate, a crystal, or a prodrug thereof, and a pharmaceutical composition comprising the compound, and an application of the compound or composition in drug preparation. The compound and the pharmaceutically acceptable salt, the isomer, the solvate, the crystal, or the prodrug thereof and the like can be used for treatment or prevention of autoimmune diseases, tumors, and neurodegenerative diseases related to receptor-interacting protein kinase-1 (RIPK1).
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
A61P 37/00 - Drugs for immunological or allergic disorders
Disclosed are a class of compounds as inhibitors of kinases such as TRK, c-MET, AXL, MER and/or VEGFR2, compositions and use thereof In particular, disclosed are a class of compounds (as shown in formula (1)) or isomers, solvates, hydrates, pharmaceutically acceptable salts, and prodrugs thereof having strong inhibition activities for kinases such as TRK, c-MET, AXL, MER and/or VEGFR2, and pharmaceutical compositions comprising said compounds. Also disclosed is use of the compounds or pharmaceutical compositions in the preparation of a medicament for treating autoimmune diseases or cancers.
The present invention relates to a novel compound serving as VEGFR-2 and CSF1R, a composition and an application thereof. Specifically, the present invention provides a compound (as represented by formula (I)) capable of strongly inhibiting VEGFR-2 and CSF1R activities, or isomers, solvates, hydrates, pharmaceutically acceptable salts, and prodrugs thereof, as well as a pharmaceutical composition comprising said compound. Also disclosed is an application of the compound or the pharmaceutical composition of the present invention in the preparation of drugs, wherein the drug are used for treating diseases such as autoimmune diseases, tumors, and Alzheimer's disease. (I)
C07D 491/056 - Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
A61K 31/4741 - Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having oxygen as a ring hetero atom, e.g. tubocuraran derivatives, noscapine, bicuculline
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
24.
Urea-substituted aromatic ring-linked dioxane-quinazoline and -linked dioxane-quinoline compounds, preparation method therefor and use thereof
The present invention relates to a urea-substituted aromatic ring-linked dioxinoquinazoline and a urea-substituted aromatic ring-linked dioxinoquinoline of Formula (I), or a pharmaceutically acceptable salt thereof or a hydrate thereof. Also provided are the preparation of the compound as shown in Formula (I) and the pharmaceutically acceptable salt thereof and the use thereof as a drug. The drug is used as an inhibitor of tyrosine kinases (e.g., VEGFR-2, C-RAF, B-RAF) for treating tyrosine kinase-related diseases.
A61K 31/517 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/4741 - Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having oxygen as a ring hetero atom, e.g. tubocuraran derivatives, noscapine, bicuculline
C07D 491/056 - Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
25.
CYANO-SUBSTITUTED PYRIDINE AND CYANO-SUBSTITUTED PYRIMIDINE COMPOUND, AND PREPARATION METHOD AND APPLICATION THEREOF
Provided is a compound as shown in formula (I), an isomer thereof, hydrate thereof, solvate thereof, pharmaceutically acceptable salt thereof, and prodrug thereof, and a preparation method and use of same in the preparation of a drug as a kinase inhibitor. The compound has good inhibitory activity against FGFR4, mutant FGFR4 V550L, and other kinases.
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
Provided in the present invention are a pyrrolopyrimidine compound containing an arylamine substitution, a preparation method and an application thereof, which specifically relate to a compound represented by the formula (I), an isomer thereof, a hydrate, a solvate, a pharmaceutically acceptable salt thereof, and a prodrug thereof, a preparation method therefor, and the application thereof in the preparation of a drug that acts as a kinase inhibitor.
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
Provided are an oxazino-quinazoline and oxazino-quinoline type compound, a preparation method, and uses thereof. More particularly provided is a compound shown in formula (I), an isomer, a hydrate, a solvate, a pharmaceutically acceptable salt, a prodrug thereof, a preparation method, and uses thereof in preparing a drug acting as a kinase inhibitor. (see formula I)
Provided are an oxazino-quinazoline and oxazino-quinazoline type compound, a preparation method therefor, and uses thereof. More particularly provided is a compound shown in formula (I), an isomer, a hydrate, a solvate, a pharmaceutically acceptable salt, a prodrug thereof, a preparation method therefor, and uses thereof in preparing a drug acting as a kinase inhibitor.
Provided are an acyl-substituted oxazino-quinazoline compound, a preparation method therefor, and uses thereof. More particularly provided is a compound shown in formula (I), an isomer, a hydrate, a solvate, a pharmaceutically acceptable salt, a prodrug thereof, a preparation method therefor, and uses thereof in preparing a drug acting as a kinase inhibitor. Said compound has a good inhibitory activity on mutant EGFR kinases and a moderate inhibitory activity on wild-type EGFR kinases. (I)
The present invention relates to an urea-substituted aromatic ring-linked dioxinoquinoline compound of formula (I), or a pharmaceutically acceptable salt or a hydrate thereof. The invention also provides a preparation method of the compound of formula (I) and a pharmaceutically acceptable salt thereof, as well as uses thereof as a drug, wherein the drug acting as a tyrosine kinase (i.e. VEGFR-2, C-RAF, B-RAF, and RET) inhibitor is used for treating disorders related to tyrosine kinase. (see formula I)
The present invention relates to a dioxazoline compound of formula (I) or a pharmaceutically acceptable salt thereof. The invention also provides a preparation method of the compound of formula (I) and a pharmaceutically acceptable salt thereof, as well as uses thereof as a drug, wherein the drug acting as a tyrosine kinase (i.e. VEGFR-2, and c-MET) inhibitor is used for treating disorders related to tyrosine kinase.
The present invention relates to a dioxazoline compound of formula (I) or a pharmaceutically acceptable salt thereof. The invention also provides a preparation method of the compound of formula (I) and a pharmaceutically acceptable salt thereof, as well as uses thereof as a drug, wherein the drug acting as a tyrosine kinase (i.e. VEGFR-2, and c-MET) inhibitor is used for treating disorders related to tyrosine kinase.
The present invention relates to an urea-substituted aromatic ring-linked dioxazoline compound of formula (I), a pharmaceutically acceptable salt or hydrate thereof. The invention also provides a preparation method of the compound of formula (I) and a pharmaceutically acceptable salt thereof, as well as uses thereof as a drug, wherein the drug acting as a tyrosine kinase (i.e. VEGFR -2, C-RAF, B-RAF, and RET) inhibitor is used for treating disorders related to tyrosine kinase.
The present disclosure relates to a novel compound as a JAK inhibitor, a composition, and an application thereof. Specifically, the present disclosure provides a compound having high JAK inhibitory activity (as represented by formula (I)) or its isomer, solvate, hydrate, pharmaceutically-acceptable salt, and prodrug, and a pharmaceutical composition containing the compound. Also disclosed is a use of the present compound or pharmaceutical composition in preparation of a medicament for treating autoimmune diseases or cancers. (see formula I)
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 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
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
35.
2-SUBSTITUTED PYRAZOLE AMINO-4-SUBSTITUTED AMINO-5-PYRIMIDINE FORMAMIDE COMPOUND, COMPOSITION, AND APPLICATION THEREOF
The present invention relates to a novel compound as a JAK inhibitor, a composition, and an application thereof. Specifically, the present invention provides a compound having high AK inhibitory activity (as represented by formula (I)) or its isomer, solvate, hydrate, pharmaceutically-acceptable salt, and prodrug, and a pharmaceutical composition containing the compound. Also disclosed is an application of the present compound or pharmaceutical composition in preparation of a drug, and the drug is used for treating autoimmune diseases or cancers.
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 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 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
The present invention relates to a urea-substituted aromatic ring-linked dioxane-quinazoline compound of formula (1) and a urea-substituted aromatic ring-linked dioxane-quinoline, or a pharmaceutically acceptable salt thereof or a hydrate thereof. Also provided are the preparation of the compound as shown in formula (1) and the pharmaceutically acceptable salt thereof and the use thereof as a drug. The drug is used as an inhibitor of tyrosine kinases (e.g., VEGFR-2, C-RAF, B-RAF) for treating tyrosine kinase-related diseases.
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
A61P 11/00 - Drugs for disorders of the respiratory system
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
The present invention relates to dioxanoquinazoline of formula (I) and a dioxanoquinazoline-type compound or a pharmaceutically acceptable salt thereof. The present invention further provides a preparation method of the compound of formula (I) and a pharmaceutically acceptable salt thereof and use of same as a medicament. The medicament is used for treating tyrosine kinase-related diseases as a tyrosine kinase (such as VEGFR-2 and c-Met) inhibitor.
The present invention relates to an N-substituted-phenyl-5-substituted-alkoxy-2,3-dihydro-[1,4]dioxane[2,3-f]quinazolin-10-amine (I) or 4-substituted-arylamino-6-substituted-alkyl-6H-[1,4]oxazino[3,2-g]quinazoline-7(8H)-one (II) type compounds, a preparation method thereof and an application thereof as an inhibitor for epidermal growth factor receptor (EGFR) (comprising some mutant forms of EGFR) to treat cancer. These compounds and salts thereof can be used to treat or prevent various cancer diseases.
A61K 31/357 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
A61K 31/517 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
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
A61P 35/02 - Antineoplastic agents specific for leukemia
39.
QUINAZOLINE HETEROCYCLIC COMPOUND AS EGFR KINASE INHIBITOR, AND PREPARATION AND APPLICATION THEREOF
The present invention relates to an N-substituted-phenyl-5-substituted-alkoxy-2,3-dihydro-[1,4]dioxane[2,3-f] quinazoline-10-amine(I) or 4-substituted-arylamino-6-substituted-alkyl-6H-[1,4]oxazino[3,2-g] quinazoline-7(8H)-one (II) type compound, a preparation method thereof and an application thereof as an inhibitor for epidermal growth factor receptor (EGFR) (comprising some mutant forms of EGFR) to treat cancer. These compounds and salts thereof can be used to treat or prevent various cancer diseases.
patents
