发明公开
EP1610779A1 3-OXO-1,3-DIHYDRO-INDAZOLE-2-CARBOXYLIC ACID AMIDE DERIVATIVES AS PHOSPHOLIPASE INHIBITORS
有权
3-氧代-1,3-二氢 - 吲唑-2-羧酰胺衍生物作为抑制剂磷脂酶
- 专利标题: 3-OXO-1,3-DIHYDRO-INDAZOLE-2-CARBOXYLIC ACID AMIDE DERIVATIVES AS PHOSPHOLIPASE INHIBITORS
- 专利标题(中): 3-氧代-1,3-二氢 - 吲唑-2-羧酰胺衍生物作为抑制剂磷脂酶
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申请号: EP04723448.9申请日: 2004-03-25
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公开(公告)号: EP1610779A1公开(公告)日: 2006-01-04
- 发明人: EACHO, Patrick, Irving , FOXWORTHY-MASON, Patricia, Sue , LIN, Ho-Shen , LOPEZ, Jose, Eduardo , MOSIOR, Marian, Kazimierz , RICHETT, Michael, Enrico
- 申请人: ELI LILLY AND COMPANY
- 申请人地址: Lilly Corporate Center Indianapolis, Indiana 46285 US
- 专利权人: ELI LILLY AND COMPANY
- 当前专利权人: ELI LILLY AND COMPANY
- 当前专利权人地址: Lilly Corporate Center Indianapolis, Indiana 46285 US
- 代理机构: Kingsbury, Oliver William
- 优先权: US459362P 20030331
- 国际公布: WO2004093872 20041104
- 主分类号: A61K31/416
- IPC分类号: A61K31/416 ; C07D231/56 ; C07C275/26 ; A61P3/06
摘要:
The present invention provides a compound of formula I (1) wherein; R, is selected from the group consisting of C5-C13alky1;:C,-C,2haloalkyl, C4C,2alkenyl, C4-C12alkynyl, or C,- C5alkylcycloalkyl, C3-C8cycloalkyl, C, C5alkylheterocyclic, and aryl, wherein the, cycloalkyl, cycloalkenyl, heterocyclic and aryl substituents are optionally substituted with onf to three substituents independently selected from C,-C8a)kyl, C,-C8haloalkyl,`C2-CBalkenyl, C2-C8a)kynyl, phenyl, benzyl, hydroxy, C,-C5 alkoxy, (C}12)m000C,-Csalkyl, (CH2)mNRaRb, and C,C4alkylcycloalkyl; wherein Wand Rb are independently selected from hydrogen, C,CBalkyl, C2-CBalkenyl, C2-CBalkynyl, and C,- C5alkylcycloalkyl; R2 is hydrogen; R3, R4, R5, and R6, are independently selected from hydrogen, C,-C12alkyl, C2C,2haloalkyl, C2-C,2 alkenyl, C2-C12alkynyl, C,-Ct2alkylaryl, C,-C12alkylcyclohexyl, C, C12alkylcyclopentyl, C,-C1zalkylheterocyclic, (CH2)m000H, (CH2)mC0(C,-C,o)alkyl, (CH2)m COO(C,-C,o)alkyl, (CH2)mCOO(C,-C,o)alkylaryl, C,-C,oalkylamino, halo, (CH2)mCONH2, (CH2)rCONRaRb, phenyl, or aryl wherein each of the phenyl or aryl groups is optionally substituted with one to three groups independently selected from CBalkyl, C,-CBhaloalkyl, C2-CBalkenyl, CZ CBalkynyl, phenyl, benzyl, hydroxy, C,-C5 alkoxy, (CH2)m000C,-Csalkyl, and C,-C4alkylcycloalkyl; and wherein m is 0, 1, 2, or 3; R7 is selected from the group consisting of hydrogen, C,-Cloalkyl, C,C,ohaloalkyl, C2-C,oalkenyl, C2-C,oalkynyl, C,-C6alkylaryl, C,-C6alkylcyclohexyl, C - C6aikylcyclopentyl, C,-C6alkylheterocyclic, or aryl; or a pharmaceutically acceptable sal lvate thereofi together with the use of such compounds for inhibiting hepatic lipase and/or endothelial lipase activity for treatment, amelioration or prevention of hepatic lipase and/or endothelial lipase-mediated diseases.
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