Cholesteryl ester transfer protein inhibitors
    71.
    发明授权
    Cholesteryl ester transfer protein inhibitors 有权
    胆固醇酯转移蛋白抑制剂

    公开(公告)号:US08865707B2

    公开(公告)日:2014-10-21

    申请号:US12087189

    申请日:2006-12-29

    CPC分类号: C07D265/10 C07D413/06

    摘要: Compounds of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), A1 is a cyclic group, and B is a cyclic group which is attached to the heterocyclic ring directly or through a methylene group.

    摘要翻译: 包括化合物的药学上可接受的盐的式(I)化合物是CETP抑制剂,可用于升高HDL-胆固醇,降低LDL-胆固醇,以及用于治疗或预防动脉粥样硬化。 在式(I)的化合物中,A1是环状基团,B是直接或通过亚甲基与杂环连接的环状基团。

    Diazeniumdiolate cyclohexyl derivatives
    73.
    发明授权
    Diazeniumdiolate cyclohexyl derivatives 有权
    二氮烯二硫代环己基衍生物

    公开(公告)号:US08623846B2

    公开(公告)日:2014-01-07

    申请号:US13698444

    申请日:2011-05-16

    摘要: A compound having the structure (I) or a pharmaceutically acceptable salt thereof, wherein R3 is hydrogen, deuterium, —OH, —OC1-6alkyl, or halogen; R8 is hydrogen, deuterium, or C1-6alkyl; R11 and R12 are independently hydrogen, —C1-6alkyl, —OH, —OC1-6alkyl, or halogen; R13 and R14 are independently —C1-6alkyl, —(CH2)1-2OH, or —OC1-6alkyl, or, together with the nitrogen atom to which they are attached, form a 4- to 7-membered heterocyclic ring containing one nitrogen atom and 0 or 1 oxygen atoms, wherein said ring is unsubstituted or mono-, di- or tri-substituted with halogen or —C1-6alkyl; R15 is —C(O)OH, —C(O)OCH2CH2N+CH3)3 wherein n is 0, 1 or 2, —C(O)NHCH(R17)OR16, or —C(O)NHCH(R17)C(O)NHCH(R18)C(O)OR16; R16 is hydrogen, C1-6alkyl, or (CH2)1-2N+R19R20R21; R1, R2, R4, R5, R6, R7, R9, R10, R17, R18, R19, R20, and R21 are independently hydrogen or —C1-6alkyl; and stereoisomers thereof, and pharmaceutically acceptable salts thereof, and pharmaceutically acceptable salts of stereoisomers thereof.

    摘要翻译: 具有结构(I)的化合物或其药学上可接受的盐,其中R 3是氢,氘,-OH,-OC 1-6烷基或卤素; R8是氢,氘或C1-6烷基; R 11和R 12独立地是氢,-C 1-6烷基,-OH,-OC 1-6烷基或卤素; R 13和R 14独立地为C 1-6烷基, - (CH 2)1-2 OH或-OC 1-6烷基,或者与它们所连接的氮原子一起形成含有一个氮的4-至7-元杂环 原子和0或1个氧原子,其中所述环是未取代的或被卤素或-C 1-6烷基单取代,二取代或三取代; R 15是-C(O)OH,-C(O)OCH 2 CH 2 N + CH 3)3,其中n是0,1或2,-C(O)NHCH(R 17)OR 16或-C(O)NHCH(R 17)C (O)NHCH(R 18)C(O)OR 16; R16是氢,C1-6烷基或(CH2)1-2N + R19R20R21; R 1,R 2,R 4,R 5,R 6,R 7,R 9,R 10,R 17,R 18,R 19,R 20和R 21独立地为氢或-C 1-6烷基; 其立体异构体及其药学上可接受的盐及其立体异构体的药学上可接受的盐。