- 1,5,7-TRISUBSTITUTED ISOQUINOLINE DERIVATIVES, PREPARATION THEREOF, AND USE THEREOF IN MEDICINES
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The present disclosure relates to 1,5,7-trisubstituted isoquinoline derivatives, their preparation and pharmaceutical use. In particular, 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. The definitions of the groups in the formula can be found in the specification and claims.
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Paragraph 0230; 0232; 0234
(2020/08/30)
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- SULFONYL-SUBSTITUTED BENZOHETEROCYCLIC DERIVATIVE, PREPARATION METHOD AND MEDICAL USE THEREOF
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The present invention relates to a sulfonyl-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.
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Paragraph 0162
(2019/10/23)
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- EZH2 INHIBITORS AND USES THEREOF
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The present disclosure provides compounds of any one of Formulae (I) and (II). The compounds described herein are inhibitors of histone methyltransferases (e.g., enhancer of zeste homolog 1 (EZH1) and enhancer of zeste homolog 2 (EZH2)) and are useful in treating and/or preventing a broad range of diseases (e.g., proliferative diseases). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein. Further provided in the present disclosure are methods of identifying EZH1and/or EZH2 inhibitors.
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- PYRIDONAPHTHYRIDINE PI3K/MTOR DUAL INHIBITORS AND PREPARATION AND USE THEREOF
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The present invention relates to a pyridonaphthyridine compound as represented by general formula (I), which has a dual PI3K and mTOR inhibition effect, and its pharmaceutically acceptable salt, stereoisomer and deuteride thereof, wherein R1, R2, R3, R4, R5, R6, R7 and X are as defined in the specification; the present invention also relates to a method for preparing said compound, a pharmaceutical composition and a pharmaceutical formulation containing said compound, and uses of said compound in treating and/or preventing a proliferative disease and in the manufacture of a medicament for treating and/or preventing a proliferative disease.
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- Pyridonaphthyridine PI3K/MTOR Dual Inhibitors and Preparation and Use Thereof
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The present invention relates to a pyridonaphthyridine compound as represented by general formula (I), which has a dual PI3K and mTOR inhibition effect, and its pharmaceutically acceptable salt, stereoisomer and deuteride thereof, wherein R1, R2, R3, R4, R5, R6, R7 and X are as defined in the specification; the present invention also relates to a method for preparing said compound, a pharmaceutical composition and a pharmaceutical formulation containing said compound, and uses of said compound in treating and/or preventing a proliferative disease and in the manufacture of a medicament for treating and/or preventing a proliferative disease.
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- 1,4-BENZODIAZEPINONE COMPOUNDS AND THEIR USE IN TREATING CANCER
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The invention provides a family of 1,4-benzodiazepinone compounds and methods for their use as therapeutic agents in treating cancer. Pharmaceutical compositions and methods of making the 1,4-benzodiazepinone compounds are provided.
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Page/Page column 64
(2010/11/04)
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- BICYCLIC AROMATIC COMPOUNDS USEFUL AS INHIBITORS OF MITOGEN-ACTIVATED PROTEIN KINASE-ACTIVATED PROTEIN KINASE-2
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A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: wherein the groups R1-R6, A and Y are as defined in the specification, as inhibitors of (MK2 or MAPKAP kinase-2).
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Page/Page column 57
(2008/06/13)
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