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HYDROXIMETHYL PIRROLIDINS AS AGENISTS OF THE BETA 3 ADRENERGIC RECEIVER.
专利权人:
MERCK SHARP & DOHME CORP.
发明人:
BERGER, RICHARD,CHANG, LEHUA,EDMONDSON, SCOTT,GOBLE, STEPHEN,HA, SOOKHEE,KAR, NAM,KOPKA, IHOR,LI, BING,MORRIELLO, GREGORI,MOYES, CHRIS,SHEN, DONG-MING,WANG, LIPING,ZHU, CHENG
申请号:
ES09726601
公开号:
ES2376278T3
申请日:
2009.04.02
申请国别(地区):
ES
年份:
2012
代理人:
摘要:
A compound of Formula I, or a pharmaceutically acceptable salt thereof, or a stereoisomer thereof, or a pharmaceutically acceptable salt of the stereoisomer thereof: wherein the burn is 0, 1, 2, 3 or 4; n is 0, 1, 2, 3, 4 or 5, p is 0, 1 or 2; q is 0, 1, 2, 3 or 4; t is 0, 1, 2, 3, 4 or 5; X is -CO- or -SO2 -; And is selected from the group consisting of: (1) C1-C5 alkanediyl, C2-C5 alkenodiyl, and C2-C5 alkynediyl, wherein each of alkanediyl, alkenodiyl and alkynediyl is optionally substituted with one to three groups that are independently selected from halogen, -ORa15, -S (O) p-C1-C3 alkyl; (2) - (CRaRa) jQ- (CRaRa) k, in which jyk are integers that are independently selected from 0, 1 and 2, (3) a bond, and (4) phenylene optionally substituted with one to three groups which are independently selected from R120; Z is selected from the group consisting of: (1) phenyl, (2) a 5- or 6-membered heterocyclic ring, with 1 to 4 heteroatoms that are selected from oxygen, sulfur and nitrogen, (3) a benzene ring condensed with a C5-C10 carbocyclic ring, (4) a 5- or 6-membered heterocyclic ring, with 1 to 4 heteroatoms selected from oxygen, sulfur and nitrogen fused to a 5-heterocyclic ring or 6 members, with 1 to 4 heteroatoms that are selected from oxygen, sulfur and nitrogen, and (5) a 5 or 6 member heterocyclic ring, with 1 to 4 heteroatoms that are selected from oxygen, sulfur and nitrogen condensed with a C5-C10 carbocyclic ring; R1 is selected from the group consisting of: (1) alkyl C1-C5 optionally substituted with 1 to 5 halogen atoms, (2) C3-C6 cycloalkyl, (3) halogen, (4) nitro, (5) cyano, (6) -C (O) Ra, (7) -C (O) 2Ra, (8) -C (O) NRaRb, and (9) -QRb40; R2 is selected from the group consisting of halogen and C1-C5 alkyl; R3 is selected from the group consisting of: (1) C1-C6 alkyl optionally substituted with 1 to 5 groups which are independently selected from halogen, -ORa, -CO2Ra, and -CONRaRb, (2) - (CH2) t-phenyl or - (CH2) tO-phenyl , and wherein said phenyl i
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