09-06-2022 дата публикации
Номер: US20220177450A1
The present invention relates to a piperazine amide derivative as represented by formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition thereof, and use of same as a therapeutic agent, especially as a selective Rearranged During Transfection (RET) kinase inhibitor. Ring a, ring e, X, X, X, X, R, R, R, R, R, R, R, R, R, R, R, R, m and n have the same definitions as those in the specification. 3. The compound claim 1 , or a stereoisomer or tautomer thereof claim 1 , or a pharmaceutically acceptable salt thereof according to claim 1 , wherein Ris selected from hydrogen claim 1 , cyano claim 1 , C-Calkyl claim 1 , —CHOH claim 1 , —C(CH)OH claim 1 , C-Calkoxy claim 1 , C-Ccycloalkyl claim 1 , and —RCOR claim 1 , wherein the C-Calkyl is optionally further substituted with one or more halogen atoms; alternatively claim 1 , R claim 1 , Rand the two carbon atoms attached thereto together form an aryl group claim 1 , which is optionally further substituted with one or more halogen atoms or C-Calkyl;{'sup': '9', 'sub': 1', '4, 'Ris selected from a chemical bond and C-Calkylene group;'}{'sup': '10', 'sub': 1', '6, 'Ris selected from hydrogen and C-Calkyl.'}4. The compound claim 3 , or a stereoisomer or tautomer thereof claim 3 , or a pharmaceutically acceptable salt thereof according to claim 3 , wherein Ris selected from hydrogen claim 3 , methyl claim 3 , trifluoromethyl claim 3 , —CHOH claim 3 , —C(CH)OH claim 3 , —COOH and —COOMe; alternatively claim 3 , R claim 3 , Rand the two carbon atoms attached thereto together form a benzene ring.5. The compound claim 1 , or a stereoisomer or tautomer thereof claim 1 , or a pharmaceutically acceptable salt thereof according to claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and R are each independently selected from hydrogen claim 1 , methyl claim 1 , —CHOH and —CHCHOH; alternatively claim 1 , Rand R claim 1 , Rand R claim 1 , Rand R claim 1 , ...
Подробнее