- CDK inhibitor based on organic arsine as well as preparation method and application of CDK inhibitor
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The invention provides a CDK inhibitor based on organic arsine as well as a preparation method and application of the CDK inhibitor. Specifically, the invention providese compounds of Formula I, or stereoisomers or tautomers thereof, or pharmaceutically acceptable salts, hydrates or solvates thereof; and the invention also discloses a preparation method and application thereof. Definitions of allgroups in the formula are shown in the specification.
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- CDK kinase inhibitor as well as preparation method, pharmaceutical composition and application thereof
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The invention provides a CDK kinase inhibitor as well as a preparation method, a pharmaceutical composition and an application thereof. The compound as shown in the formula I, the stereoisomer or thepharmaceutically acceptable salt of the compound have higher bioavailability, longer in-vivo half-life period and better in-vivo efficacy when being used as a CDK kinase inhibitor.
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- PYRAZOLO-TRIAZINE AND/OR PYRAZOLO-PYRIMIDINE DERIVATIVES AS SELECTIVE INHIBITOR OF CYCLIN DEPENDENT KINASE
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The present invention relates to pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[l,5-a]pyrimidine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of cell proliferative diseases, inflammatory diseases, immunological diseases, cardiovascular diseases and infectious diseases. Furthermore, the present invention is directed towards pharmaceutical compositions containing at least one of the pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives and/or pharmaceutically acceptable salts thereof.
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Page/Page column 51-52
(2019/11/04)
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- PHARMACEUTICALLY ACTIVE PYRAZOLO-TRIAZINE AND/OR PYRAZOLO-PYRIMIDINE DERIVATIVES
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The present invention relates to pyrazolo [1,5 -a] [1,3,5 ]triazine and pyrazolo[1,5-a] pyrimidine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of cell proliferative diseases, inflammatory diseases, immunological diseases, cardiovascular diseases and infectious diseases. Furthermore, the present invention is directed towards pharmaceutical compositions containing at least one of the pyrazo lo [1,5-a][1,3,5 ]triazine and pyrazolo [1,5-a]pyrimidine derivatives and/or pharmaceutically acceptable salts thereof.
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Page/Page column 33; 58; 59
(2019/11/04)
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- COMPOUNDS USEFUL FOR INHIBITING CDK7
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The present invention provides novel CDK7 inhibitors and pharmaceutical compositions thereof: or a pharmaceutically acceptable salt thereof.
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- Synthesis method of pyrazolo[1,5-A]pyrimidine heterocyclic compound and derivative
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The invention relates to a pynthesis method of pyrazolo[1,5-A]pyrimidine heterocyclic compounds and derivatives. The synthesis method comprises the following steps: (1) preparing N-boc-1,4-cyclohexanediamine; (2), preparing 2-formyl-3-methyl-butyronitrile; (3), preparing 4-isopropyl-1H-pyrazol-5-amine; (4) preparing 3-isopropylpyrazolo[1,5-a]pyrimidine-5,7-diol; (5), preparing 5,7-dichloro-3-isopropylpyrazolo[1,5-a]pyrimidine; (6) utilizing 5,7-dichloro-3-isopropylpyrazolo[1,5-a]pyridine to prepare 5,7-dibromo-3-isopropylpyrazolo[1,5-a]pyrimidine; (7) preparing 4-(5-bromo-3-isopropylpyrazolo[1,5-a]pyrimidin-7-ylamino)-N,N-dimethylbenzenesulfonamide; and (8) preparing 4-(5-(4-(1,1-dimethylethoxy)carbonyl)-aminocyclohexylamino)-3-isopropylpyrazolo[1,5-a]pyrimidin-7-ylamino)-N,N-dimethylbenzenesulfonamide. According to the method, the reaction process is optimized, the reaction steps are simplified, and the reaction conversion rate and the product yield are improved.
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- INDOLE AHR INHIBITORS AND USES THEREOF
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The present invention provides compounds useful as inhibitors of AHR, compositions thereof, and methods of using the same.
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Paragraph 001063; 001065
(2018/11/22)
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- INHIBITORS OF CYCLIN-DEPENDENT KINASES
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The present invention provides novel compounds of Formula (I), (II), or (III), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing proliferative diseases (e.g., cancers (e.g., leukemia, acute lymphoblastic leukemia, lymphoma, Burkitt's lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, ovarian cancer, neuroblastoma, lung cancer, colorectal cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g., CDK7, CDK12, or CDK13), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.
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Paragraph 00366
(2017/05/28)
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- CARM1 INHIBITORS AND USES THEREOF
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Provided herein are compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X, R1, R2a, R2b, R2c, R2d, are as defined herein, and Ring HET is an optionally substituted 6,5-bicyclic heteroaryl ring system comprising 2 to 5 nitrogen atoms, inclusive, wherein the point of attachment is provided on the 6-membered ring of the 6,5-bicyclic heteroaryl ring system, and wherein the 6-membered ring is further substituted with a group of formula -L1-R3, wherein L1 and R3 are as defined herein. Compounds of the present invention are useful for inhibiting CARM1 activity. Methods of using the compounds for treating CARM1-mediated disorders are also described.
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- 1 -PHENOXY-3-(ALKYLAMINO)-PROPAN-2-OL DERIVATIVES AS CARM1 INHIBITORS AND USES THEREOF
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Provided herein are compounds of Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X, R1, R2a, R2b, R2c, R2d, are as defined herein, and Ring HET is an optionally substituted 6,5-bicyclic heteroaryl ring system comprising 2 to 5 nitrogen atoms, inclusive, wherein the point of attachment is provided on the 6-membered ring of the 6,5-bicyclic heteroaryl ring system, and wherein the 6-membered ring is further substituted with a group of formula -L1 -R3, wherein L1 and R3 are as defined herein. Compounds of the present invention are useful for inhibiting CARM1 activity. Methods of using the compounds for treating CARM1-mediated disorders are also described.
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- Process for Preparing 5,7 Diaminopyrazolo [1,5-a] Pyrimidine Compounds
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Processes for the preparation of certain 5,7-diaminopyrazolo[1,5-α]pyrimidine compounds comprising the reaction of a primary or secondary amine and a protected 5-halo-7-aminopyrazolo[1,5-α]pyrimidine compound in solvent system comprising water and one or more organic solvents, optionally in the presence of an exogenous base.
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- PROCESSES FOR PREPARING 5,7 DIAMINOPYRAZOLO[1,5-α] PYRIMIDINE COMPOUNDS
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Processes for the preparation of certain 5,7-diaminopyrazolo[1,5-α]pyrimidine compounds comprising the reaction of a primary or secondary amine and a protected 5-halo-7-aminopyrazolo[1,5-α]pyrimidine compound in solvent system comprising water and one or more organic solvents, optionally in the presence of an exogenous base.
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Page/Page column 54-55
(2010/07/02)
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- SELECTIVE INHIBITORS FOR CYCLIN-DEPENDENT KINASES
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This invention provides a class of compounds which are useful for specifically inhibiting cyclin-dependent kinases. This class of compounds finds use in treating diseases resulting from inappropriate activity of cyclin-dependent kinases, including cancer, viral infections (e.g., HIV) neurodegenerative disorders (e.g. Alzheimer's disease), and cardiovascular disorders (e.g. atherosclerosis). Moreover, certain members of this class are particularly useful for inhibiting cyclin-dependent kinase 7 and are especially useful for the treatment of breast cancer.
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- PYRAZOLOPYRIMIDINE COMPOUNDS AND THEIR USE IN MEDICINE
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Compounds of formula (I) or salts, N-oxides, hydrates or solvates thereof are inhibitors of kinase activity, and useful for the treatment of, for example, cancer, psoriasis or restenosis: wherein ring A is an optionally substituted carbocyclic or heterocy
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