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1. 发明申请

WO2004093872A1 3-OXO-1, 3-DIHYDRO-INDAZOLE-2-CARBOXYLIC ACID AMIDE DERIVATIVES AS PHOSPHOLIPASE INHIBITORS 审中-公开
标题翻译： 3-氧代-1,3-二氢吲哚-2-羧酸酰胺衍生物作为磷脂酶抑制剂
公开(公告)号：WO2004093872A1
公开(公告)日：2004-11-04
申请号：PCT/US2004/006092
申请日：2004-03-25
申请人： ELI LILLY AND COMPANY , EACHO, Patrick, Irving , FOXWORTHY-MASON, Patricia, Sue , LIN, Ho-Shen , LOPEZ, Jose, Eduardo , MOSIOR, Marian, Kazimierz , RICHETT, Michael, Enrico
发明人： EACHO, Patrick, Irving , FOXWORTHY-MASON, Patricia, Sue , LIN, Ho-Shen , LOPEZ, Jose, Eduardo , MOSIOR, Marian, Kazimierz , RICHETT, Michael, Enrico
IPC分类号： A61K31/416
CPC分类号： C07D231/56 , C07D405/12 , C07D409/12
摘要： The present invention provides a compound of formula I (1) wherein; R, is selected from the group consisting of C 5 -C 13 alky1;:C,-C, 2 haloalkyl, C 4 C,2alkenyl, C 4 -C 12 alkynyl, or C,- C5alkylcycloalkyl, C3-C8cycloalkyl, C, C 5 alkylheterocyclic, and aryl, wherein the, cycloalkyl, cycloalkenyl, heterocyclic and aryl substituents are optionally substituted with onf to three substituents independently selected from C,-C 8 a)kyl, C,-C 8 haloalkyl,`C 2 -C B alkenyl, C2-C 8 a)kynyl, phenyl, benzyl, hydroxy, C,-C5 alkoxy, (C}12) m 000C,-Csalkyl, (CH2) m NR a R b , and C,C 4 alkylcycloalkyl; wherein Wand R b are independently selected from hydrogen, C,C B alkyl, C 2 -C B alkenyl, C 2 -C B alkynyl, and C,- C5alkylcycloalkyl; R 2 is hydrogen; R3, R4 , R5, and R6, are independently selected from hydrogen, C,-C 12 alkyl, C 2 C,2haloalkyl, C2-C,2 alkenyl, C 2 -C 12 alkynyl, C,-C t2 alkylaryl, C,-C 12 alkylcyclohexyl, C, C 12 alkylcyclopentyl, C,-C 1z alkylheterocyclic, (CH2) m 000H, (CH2) m C0(C,-C,o)alkyl, (CH 2 ) m COO(C,-C, o )alkyl, (CH2) m COO(C,-C, o )alkylaryl, C,-C, o alkylamino, halo, (CH 2 ) m CONH 2 , (CH 2 ) r CONRaR b , phenyl, or aryl wherein each of the phenyl or aryl groups is optionally substituted with one to three groups independently selected from C B alkyl, C,-C B haloalkyl, C 2 -C B alkenyl, C Z C B alkynyl, phenyl, benzyl, hydroxy, C,-C5 alkoxy, (CH2) m 000C,-Csalkyl, and C,-C4alkylcycloalkyl; and wherein m is 0, 1, 2, or 3; R7 is selected from the group consisting of hydrogen, C,-C lo alkyl, C,C, o haloalkyl, C 2 -C, o alkenyl, C 2 -C, o alkynyl, C,-C 6 alkylaryl, C,-C 6 alkylcyclohexyl, C - C 6 aikylcyclopentyl, C,-C 6 alkylheterocyclic, 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.
摘要翻译：本发明提供式I（1）的化合物，其中： R 5选自C 5 -C 13烷基; C 1 -C 2卤代烷基，C 4 -C 2烯基，C 4 -C 12炔基或C 1 -C 5烷基环烷基，C 3 -C 8环烷基，C 5 C 5烷基杂环和芳基，其中环烷基，环烯基，杂环和芳基取代基任选被至少三个独立地选自C 1 -C 8烷基，C 1 -C 8卤代烷基，C 2 -C 12链烯基，C 2 -C 8α-炔基，苯基，苄基，羟基，C - C5烷氧基，（C）12）m000C，-Cs烷基，（CH2）mNRaRb和C，C4烷基环烷基; 其中W 1和R 2独立地选自氢，C 1 -C 8烷基，C 2 -C 12链烯基，C 2 -C 12炔基和C 1 -C 5烷基环烷基; R2是氢; R 3，R 4，R 5和R 6独立地选自氢，C 1 -C 12烷基，C 2 C 2卤代烷基，C 2 -C 2烯基，C 2 -C 12炔基，C 1 -C 12烷基芳基，C 1 -C 12烷基环己基，C 12 C 12烷基环戊基，C ，（CH 2）m COO（C 1 -C 6）烷基，（CH 2）m COO（C 1 -C 10）烷基，（CH 2）m COO（C 1 -C 6）烷基芳基，C 1 -C 8烷基氨基，卤素，（CH 2）m CONH 2，（CH 2）r CONR a R b，苯基或芳基，其中每个苯基或芳基任选地被一至三个独立地选自C烷基，C C 1 -C 6烷基，C 1 -C 4烷基，C 1 -C 4烷基，C 1 -C 4烷基，C 1 -C 4烷基，并且其中m为0,1,2或3; R 7选自氢，C 1 -C 4烷基，C，C，卤代烷基，C 2 -C，链烯基，C 2 -C 6炔基，C 1 -C 6烷基芳基，C 1 -C 6烷基环己基，C 1 -C 6烷基环戊基，C 1 -C 6烷基环戊基， C6烷基杂环或芳基; 或其药学上可接受的盐酸盐以及用于抑制肝脂肪酶和/或内皮脂肪酶活性用于治疗，改善或预防肝脂肪酶和/或内皮脂肪酶介导的疾病的用途。

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