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Mineralocorticoid receptor antagonists
专利权人:
MERCK SHARP & DOHME CORP.
发明人:
CRESPO, Alejandro,LAN, Ping,MAL, Rudrajit,OGAWA, Anthony,SHEN, Hong,SINCLAIR, Peter J.,SUN, Zhongxiang,BUNTE, Ellen K. Vande,WU, Zhicai,LIU, Kun,DEVITA, Robert J.,SHEN, Dong-Ming,SHU, Min,TAN, John Qi
申请号:
ES12736795
公开号:
ES2618812T3
申请日:
2012.01.19
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
The compound of Formula IV: ** Formula ** or a pharmaceutically acceptable salt thereof, in which: Y is N or CRY; each RY is independently H or C1-C6 alkyl, said alkyl is optionally substituted with halo or OH; each Rx is independently H, halo, OR, or C1-C6 alkyl, said alkyl is optionally substituted with 1 to 3 substituents selected from halo, OR and C1-C6 alkyl; each R is independently H, CF3, C1-C6 alkyl or aryl, said alkyl and aryl are optionally substituted with 1 to 3 substituents selected from halo, aryl and C1-C6 alkyl; R1 is: 1) 5-membered heteroaryl or heterocyclyl, said heteroaryl or heterocyclyl are optionally substituted with one to three R5, 2) C1-C6 alkyl, said alkyl is optionally substituted with one to three substituents C1-C6 alkyl, OR, NR2 , CF3, SR, OS (O) 2R8, CN or halo, 3) - (CRa 2) nC (O) OR11, 4) (CRa 2) 0-4C (O) Rc, 5) C3-C10-R5 cycloalkyl , or 6) - (CRa 2) nOC (O) Rc; R2 is 1) C1-C6 alkyl, 2) - (CRb 2) m-C3-C6 cycloalkyl, 3) - (CRa 2) mC (O) OR11, 4) - (CRb 2) m-C2-C6 alkenyl, or 5) - (CRb 2) m-C2-C6 alkynyl, wherein said alkyl, cycloalkyl, alkenyl and alkynyl are optionally substituted with one to three groups selected from R12; R3 is phenyl, wherein said phenyl is optionally substituted with one to three R9; R4 is 1) -NR6S (O) 2R8, 2) C1-C6 alkyl, 3) halo, 4) -C (O) OR11, 5) -NH2, 6) -OR, or 7) - (CRa 2) t -SO2R10, wherein said alkyl may be optionally substituted with one to three halo, OR or C1-C6 alkyl substituents; Each R5 is independently H, OR, CN, C (O) OR11, C (O) NRR7, C1-C6 alkyl, CF3 or C3-C10 cycloalkyl, wherein said alkyl, cycloalkyl, aryl and heteroaryl may be optionally substituted with each other. three halo, OR or CF3; Each R6 is independently H, C1-C6 alkyl, C (O) OR11 or S (O) 2R8; Each R7 is independently 1) H, 2) C1-C6 alkyl, optionally substituted with 1 to 3 substituents selected from halo, OR, CN, CF3, aryl and C3-C10 cycloalkyl, wherein said aryl and cycloalkyl are optionally substituted with aryl, 3) C3-C10 cyclo
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