- CDK KINASE INHIBITOR, PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION, AND APPLICATION
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Disclosed in the present invention are a CDK kinase inhibitor, a preparation method therefor, a pharmaceutical composition, and an application. The present invention provides a compound as represented by formula I-a, a cis-trans isomer thereof, a pharmaceutically acceptable salt thereof, a solvate of the pharmaceutically acceptable salt thereof, a tautomer thereof, or a polymorph thereof. The compound of the present invention has good CDK7 inhibitory activity, cell activity, and tumor growth inhibitory activity.
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- 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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- SUBSTITUTED PYRAZOLE COMPOUNDS AS TOLL RECEPTOR INHIBITORS
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Disclosed are compounds of Formula (I) N-oxides, or salts thereof, wherein G, A, R1, and R5 are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
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- Heterocyclic compound as well as pharmaceutical composition, preparation method, intermediate and application thereof
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The invention discloses a heterocyclic compound as well as a pharmaceutical composition, a preparation method, an intermediate and application thereof. The structure of the heterocyclic compound is shown as a formula I, and the heterocyclic compound has CDK7 inhibitory activity and can be used for treating diseases such as tumors.
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- 2-pyridine substituted urea structural small molecule compounds as well as synthesis and application thereof
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The invention relates to 2-pyridine substituted urea structural small molecule compounds as well as synthesis and application thereof. Specifically, the invention discloses the compounds represented by a formula (I) shown in the specification, enantiomers, diastereomers, racemates or a mixture of the compounds, or a pharmaceutically acceptable salt, hydrate and solvate of the compounds, a preparation method of the above materials, and applications of the above materials in preparation of an ASK1 small molecule inhibitor, or medicines for preventing and/or treating diseases related to ASK1, especially liver diseases, lung diseases, cardiovascular diseases, kidney diseases and metabolic diseases.
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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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- 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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- 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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- 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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- 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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- 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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- 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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- INHIBITORS OF CYCLIN-DEPENDENT KINASE 7 (CDK7)
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The present invention provides novel compounds described herein, such as of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, 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 cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.
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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
(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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- PYRAZOLOPYRIMIDINES AS CYCLIN DEPENDENT KINASE INHIBITORS
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In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
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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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- Studies on nonpeptide angiotensin II receptor antagonists. I. Synthesis and biological evaluation of pyrazolo [1,5-b][1,2,4]triazole derivatives with alkyl substituents
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Alkyl-substituted pyrazolo[1,5-b][1,2,4]triazole derivatives were synthesized and evaluated for activity as angiotensin II receptor antagonists. Molecules with the (methylbiphenylyl)tetrazole moiety at N-5 were the preferred compounds. Ethyl substitutions
- Okazaki, Toshio,Suga, Akira,Watanabe, Toshihiro,Kikuchi, Kazumi,Kurihara, Hiroyuki,Shibasaki, Masayuki,Fujimori, Akira,Inagaki, Osamu,Yanagisawa, Isao
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- Pyrazolotriazole derivatives
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This invention relates to a pyrazolotriazole derivative represented by the general formula: STR1 wherein each symbol means as follows; R1, R3 and R4 : one of them represents hydrogen, tetrazolylated biphenylmethyl or lower
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