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    • 1. 发明申请
    • SPIROCYCLIC PIPERIDINE DERIVATIVES USEFUL AS RENIN INHIBITORS
    • 作为RININ抑制剂有用的螺环哌啶衍生物
    • WO2011057382A1
    • 2011-05-19
    • PCT/CA2010/001632
    • 2010-10-12
    • MERCK FROSST CANADA LTD.CHEN, AustinASPIOTIS, ReneeMCKAY, DanielHAN, YongxinFOURNIER, Pierre-André
    • CHEN, AustinASPIOTIS, ReneeMCKAY, DanielHAN, YongxinFOURNIER, Pierre-André
    • C07D491/107A61P25/22A61P27/02A61P5/42A61P9/00C07D491/20A61K31/438A61P13/12
    • C07D491/107C07D491/20
    • Renin inhibitors which are spirocyclic piperidine derivatives, of formula (I) and pharmaceutical compositions thereof useful in the treatment of cardiovascular diseases and renal insufficiency. or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt of the stereoisomer thereof, wherein: n, for each instance in which it occurs, is independently 0, 1, or 2; W is a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic monocyclic ring, A is (i) a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic monocyclic ring or (ii) a first five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring which is fused to a second five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring, V is -(C=O)-, -CH 2 - or =CH-; U is a bond or -CH2-, or, when V iS =CH-, U is-CH=; X is =CH-, =CF-, =C(OR 3 )-, or -(C=O)-; and Y is =CH-, =CF-, =N-, or, for the case when X is -(C=O)-, Y is -N(R 3 )-.
    • 作为式(I)的螺环哌啶衍生物的肾素抑制剂及其用于治疗心血管疾病和肾功能不全的药物组合物。 或其立体异构体,或其药学上可接受的盐或其立体异构体的药学上可接受的盐,其中:对于其发生的每一种情况,n独立地为0,1或2; W是五或六元饱和或不饱和的杂环或碳环单环,A是(i)五或六元饱和或不饱和的杂环或碳环单环或(ii)第一个五元或六元 饱和或不饱和的杂环或碳环与第二个五元或六元饱和或不饱和的杂环或碳环稠合,V是 - (C = O) - , - CH 2 - 或= CH-; U是键或-CH 2 - ,或当V iS = CH-时,U是-CH =; X = CH-,= CF-,= C(OR 3) - 或 - (C = O) - ; 并且Y是= CH-,= CF-,= N-,或者对于X是 - (C = O) - 的情况,Y是-N(R 3) - 。