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US 10,519,148 B2Granted
Acrylic acid derivative, preparation method and use in medicine thereof
AssigneeZhejiang Hisun Pharmaceutical Co., Ltd.
InventorsDongliang Guan, Shouyi Sheng, Hua Bai
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Abstract
The present invention relates to an acrylic acid derivative as shown in general formula (I), a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, the preparation method thereof, a pharmaceutical composition containing same, and the use thereof as therapeutic agents, in particular as selective estrogen receptor degraders (SERD), wherein the substituents of general formula (I) are the same as those defined in the description.
Claims29
A compound represented by general formula (I), or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof:
- wherein:
- R1 and R2 are each independently selected from halogen;
- R3 is selected from the following groups:
- cycloalkyl, heterocyclyl, aryl or heteroaryl, wherein said cycloalkyl, heterocyclyl, aryl or heteroaryl is optionally further substituted by one or more groups selected from hydroxy, halogen, haloalkyl, nitro, cyano, alkyl, alkoxy, cycloalkyl, heterocyclyl, aryl, heteroaryl, —NR5R6, —C(O)NR5R6, —C(O)R7, —SO2R7, —C(O)OR7 or —NR5C(O)R6;
- R4 is each independently selected from a hydrogen atom, halogen, alkyl, alkoxy, trifluoromethyl, or cyano, wherein said alkyl or alkoxy is optionally further substituted by one or more groups selected from halogen;
- R5 is selected from a hydrogen atom or alkyl;
- R6 is selected from a hydrogen atom, alkyl, cycloalkyl, aryl or heteroaryl, wherein said alkyl, cycloalkyl, aryl or heteroaryl is optionally further substituted by one or more groups selected from hydroxy, halogen, haloalkyl, nitro, cyano, alkyl, alkoxy, cycloalkyl, heterocyclyl, aryl, heteroaryl, —NR8R9, —C(O)NR8R9, —C(O)R10, —SO2R10, —C(O)OR10 or —NR8C(O)R9;
- or, R5 and R6 together with the atoms attached to R5 and R6 form a 4- to 8-membered heterocyclyl, wherein said heterocyclyl is optionally further substituted by one or more groups selected from alkyl, halogen, hydroxy, cyano, nitro, cycloalkyl, heterocyclyl, aryl, heteroaryl, —NR8R9, —C(O)NR8R9, —C(O)R10, —SO2R10, —C(O)OR10 or —NR8C(O)R9;
- R7 is selected from a hydrogen atom, alkyl, cycloalkyl, heterocyclyl, aryl or heteroaryl, wherein said alkyl, cycloalkyl, heterocyclyl, aryl or heteroaryl is optionally further substituted by one or more groups selected from hydroxy, halogen, haloalkyl, nitro, cyano, alkyl, alkoxy, cycloalkyl, heterocyclyl, aryl, heteroaryl, —NR8R9, —C(O)NR8R9, —C(O)R10, —SO2R10, —C(O)OR10 or —NR8C(O)R9;
- R8, R9 and R10 are each independently selected from a hydrogen atom, alkyl, cycloalkyl, heterocyclyl, aryl or heteroaryl, wherein said alkyl, cycloalkyl, heterocyclyl, aryl or heteroaryl is optionally further substituted by one or more groups selected from hydroxy, halogen, haloalkyl, nitro, cyano, alkyl, alkoxy, cycloalkyl, heterocyclyl, aryl, heteroaryl, carboxy or carboxylate group;
- and
- n is 0, 1, 2, 3 or 4.
9 more elements
Dependencies are inferred from the claim text.