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US 10,214,515 B2Granted
Substituted pyrazoles as inhibitors of fibroblast growth factor receptor
AssigneeZhejiang Hisun Pharmaceutical Co., Ltd.
InventorsLei Chen, Dongliang Guan, Hua Bai, Xing Yan, Shuai Miao, Songsong Zhu
Life of this patent
Estimating the term…
Abstract
An indole derivative as expressed by Formula (I), a preparation method thereof, a pharmaceutical salt, and use thereof as a therapeutic agent, especially as a FGFR inhibitor. Each substituent in Formula (I) has identical definition as specified in the specification.
Claims28
A compound represented by formula (I):
- or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof,
- wherein:
- D is selected from N or CR3;
- each R1 is independently selected from the group consisting of hydrogen, alkyl, alkoxy, hydroxy, halogen, nitro, cyano, cycloalkyl, heterocyclyl, aryl, heteroaryl, —NR4R5, —C(O)NR4R5, —C(O)R6, —OC(O)R6, —C(O)OR6 and —NR4C(O)R5, wherein the alkyl, alkoxy, cycloalkyl, heterocyclyl, aryl or heteroaryl is optionally further substituted by one or more substituents selected from the group consisting of halogen, hydroxy, cyano, nitro, alkyl, alkoxy, cycloalkyl, heterocyclyl, aryl, heteroaryl, —NR4R5, —C(O)NR4R5, —C(O)R6, —OC(O)R6, —C(O)OR6 and —NR4C(O)R5;
- each R2 is independently selected from the group consisting of hydrogen, alkyl, alkoxy, hydroxy, halogen, nitro, cyano, cycloalkyl, heterocyclyl, —NR4R5, —C(O)NR4R5, —C(O)R6, —OC(O)R6, —C(O)OR6 and —NR4C(O)R5, wherein the alkyl, alkoxy, cycloalkyl or heterocyclyl is optionally further substituted by one or more substituents selected from the group consisting of alkyl, halogen, hydroxy, cyano, nitro, cycloalkyl, heterocyclyl, aryl, heteroaryl, —NR4R5, —C(O)NR4R5, —C(O)R6, —OC(O)R6, —C(O)OR6 and —NR4C(O)R5;
- R3 is selected from the group consisting of cycloalkyl, cyano, —NR4R5, —C(O)OR6, —OC(O)R6, —NR4C(O)R5 and —C(O)NR4R5, wherein the cycloalkyl is optionally further substituted with one or more halogens;
- R4, R5 and R6 are each independently selected from the group consisting of hydrogen, alkyl, cycloalkyl, heterocyclyl, sodium, aryl and heteroaryl, wherein the alkyl, cycloalkyl, heterocyclyl, aryl or heteroaryl is optionally further substituted by one or more substituents selected from the group consisting of hydroxy, halogen, nitro, cyano, alkyl, alkoxy, cycloalkyl, heterocyclyl, aryl, heteroaryl, —NR7R8, —C(O)NR7R8, —C(O)R9, —C(O)OR9 and —NR7C(O)R8;
- or
- R4 and R5, together with the attached nitrogen atom, form a 4- to 8-membered heterocyclyl, wherein the 4- to 8-membered heterocyclyl contains one or more atoms selected from the group consisting of N, O and S(O)p, and the 4- to 8-membered heterocyclyl is further substituted by one or more substituents selected from the group consisting of hydroxy, halogen, nitro, cyano, alkyl, alkoxy, cycloalkyl, heterocyclyl, aryl, heteroaryl, oxo, —NR7R8, —C(O)NR7R8, —C(O)R9, —C(O)OR9 and —NR7C(O)R8;
- R7, R8 and R9 are each independently selected from the group consisting of hydrogen, alkyl, cycloalkyl, heterocyclyl, aryl and heteroaryl, wherein the alkyl, cycloalkyl, heterocyclyl, aryl or heteroaryl is optionally substituted by one or more substituents selected from the group consisting of hydroxy, halogen, nitro, cyano, alkyl, alkoxy, cycloalkyl, heterocyclyl, aryl, heteroaryl, carboxy and carboxylate;
- m is 0, 1, 2, 3 or 4;
- n is 0, 1, 2 or 3;
- and
- p is 0, 1 or 2.
11 more elements
Dependencies are inferred from the claim text.