Processes and intermediates for preparing benzo-fused azepinone and piperidinone compounds useful in the inhibition of ACE and NEP
    4.
    发明授权
    Processes and intermediates for preparing benzo-fused azepinone and piperidinone compounds useful in the inhibition of ACE and NEP 失效
    制备用于抑制ACE和NEP的苯并稠合氮杂酮和哌啶酮化合物的方法和中间体

    公开(公告)号:US06235922B1

    公开(公告)日:2001-05-22

    申请号:US09205316

    申请日:1998-12-04

    IPC分类号: C07C32734

    摘要: Compounds having the following formula I, and pharmaceutically acceptable salts thereof, including dual inhibitors of ACE and NEP and selective ACE inhibitors: wherein: Y1 and Y2 are each independently hydrogen, alkyl, aryl, halogen, or alkoxy; X is O or S(O)t; A is t is zero, one or two; m and n are independently zero or one; and wherein R, R5, R5a, R5b, R6, R7, R11, q and r are defined herein.

    摘要翻译: 具有下式I的化合物及其药学上可接受的盐,包括ACE和NEP的双重抑制剂和选择性ACE抑制剂:其中:Y1和Y2各自独立地为氢,烷基,芳基,卤素或烷氧基; X为O或S( O)t; A ist为零,一个或两个; m和n独立地为0或1;并且其中R,R 5,R 5a,R 5b,R 6,R 7,R 11,q和r在本文中定义。

    HMG-CoA reductase inhibitors and method
    6.
    发明授权
    HMG-CoA reductase inhibitors and method 有权
    HMG-CoA还原酶抑制剂及方法

    公开(公告)号:US06812345B2

    公开(公告)日:2004-11-02

    申请号:US10602752

    申请日:2003-06-24

    IPC分类号: C07D491044

    摘要: Compounds of the following structure are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids such as lowering LDL cholesterol and/or increasing HDl cholesterol, and treating hyperlipidemia, hypercholesterolemia, hypertriglyceridemia and atherosclerosis and pharmaceutically acceptable salts thereof, wherein X is O, S, SO, SO2 or NR7; Z is n is 0 or 1; R1 and R2 are the same or different and are independently selected from alkyl, arylalkyl, cycloalkyl, alkenyl, cycloalkenyl, aryl, heteroaryl or cycloheteroalkyl; and R3 to R10 are as defined herein.

    摘要翻译: 以下结构的化合物是HMG CoA还原酶抑制剂,因此具有抑制胆固醇生物合成,调节血清脂质如降低LDL胆固醇和/或增加HDL胆固醇和治疗高脂血症,高胆固醇血症,高甘油三酯血症和动脉粥样硬化及其药学上可接受的盐的活性,其中 X是O,S,SO,SO 2或NR 7; Z isn是0或1; R 1和R 2相同或不同,并且独立地选自烷基,芳基烷基,环烷基,烯基,环烯基,芳基,杂芳基或环杂烷基; 和R 3至R 10如本文所定义。