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    SPIROCYCLIC PIPERIDINE DERIVATIVES USEFUL AS RENIN INHIBITORS
    1.
    发明申请
    SPIROCYCLIC PIPERIDINE DERIVATIVES USEFUL AS RENIN INHIBITORS 审中-公开
    作为瑞宁抑制剂有用的螺环哌啶衍生物

    公开(公告)号：US20120202837A1

    公开(公告)日：2012-08-09

    申请号：US13501401

    申请日：2010-10-12

    申请人： Austin Chen ,  Reneé Aspiotis ,  Daniel McKay ,  Yongxin Han ,  Pierre-André Fournier

    发明人： Austin Chen ,  Reneé Aspiotis ,  Daniel McKay ,  Yongxin Han ,  Pierre-André Fournier

    IPC分类号： A61K31/438 ,  C07D491/20 ,  A61P9/12 ,  A61P9/00 ,  A61P27/02 ,  A61P27/06 ,  A61P25/22 ,  C07D491/107 ,  A61P9/04

    CPC分类号： C07D491/107 ,  C07D491/20

    摘要： 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)—, —CH2— or ═CH—; U is a bond or —CH2-, or, when V iS ═CH—, U is —CH═; X is ═CH—, ═CF—, ═C(OR3)—, or —(C═O)—; and Y is ═CH—, ═CF—, ═N—, or, for the case when X is —(C═O)—, Y is —N(R3)—.

    摘要翻译： 作为式（I）的螺环哌啶衍生物，可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的肾素抑制剂， 其中：对于其发生的每个实例，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，其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是≡CH-，≡CF-，≡C（OR3） - 或 - （C = O） - ; 并且Y为≡CH-，≡CF-，≡N-，或者对于X为 - （C = O） - 的情况，Y为-N（R 3） - 。

    Adaptive control of a cam phase adjustment mechanism
    5.
    发明申请
    Adaptive control of a cam phase adjustment mechanism 审中-公开
    凸轮相位调整机构的自适应控制

    公开(公告)号：US20070185640A1

    公开(公告)日：2007-08-09

    申请号：US10668384

    申请日：2003-09-23

    申请人： Jeffrey Pfeiffer ,  Amanpal Grewal ,  Daniel McKay

    发明人： Jeffrey Pfeiffer ,  Amanpal Grewal ,  Daniel McKay

    IPC分类号： G06G7/70

    CPC分类号： F01L1/344 ,  F01L2201/00 ,  F01L2800/00 ,  F02D35/0007 ,  F02D2041/001 ,  F02D2041/1409 ,  F02D2041/1422

    摘要： A closed-loop control for a cam phase adjustment mechanism includes gain terms that are adaptively adjusted to optimize the rate of response of the control to changes in the desired cam phase. The rate of response of the cam phase adjustment mechanism is sampled under specified operating conditions or during certain repeated engine events that involve a change in the desired cam phase, and the deviation of the measured rate of response from the nominal rate of response is determined and used to adjust the closed-loop control gains for restoring the nominal response.

    摘要翻译： 用于凸轮相位调节机构的闭环控制包括被自适应地调整以使控制对所需凸轮相位变化的响应速率最优化的增益项。 凸轮相位调整机构的响应速率在规定的运行条件下或在涉及所需凸轮相位变化的某些重复发动机事件期间进行采样，并且确定测量的响应速率与标称响应速率的偏差， 用于调整闭环控制增益以恢复标称响应。

    RENIN INHIBITORS
    8.
    发明申请
    RENIN INHIBITORS 审中-公开
    雷宁抑制剂

    公开(公告)号：US20120190701A1

    公开(公告)日：2012-07-26

    申请号：US13390465

    申请日：2010-08-17

    申请人： Austin Chih-Yu Chen ,  Sebastien Laliberte ,  Guillaume Larouche ,  Yongxin Han ,  Daniel McKay

    发明人： Austin Chih-Yu Chen ,  Sebastien Laliberte ,  Guillaume Larouche ,  Yongxin Han ,  Daniel McKay

    IPC分类号： A61K31/438 ,  C07D491/20 ,  A61K31/4709 ,  A61K31/4725 ,  A61P9/12 ,  A61P25/22 ,  A61P9/00 ,  A61P9/10 ,  A61P13/12 ,  A61P25/00 ,  A61P27/02 ,  A61P27/06 ,  C07D491/107 ,  A61P9/04

    CPC分类号： A61K31/438 ,  C07D491/107 ,  C07D519/00

    摘要： Renin inhibitors, which are spirocyclic piperidine amides, of structural formula (I) and pharmaceutical compositions thereof useful in the treatment of cardiovascular diseases and renal insufficiency. wherein n, for each instance in which it occurs, is independently 0, 1, or 2; R1 is hydrogen, C1-6-alkyl or C3-6-cycloalkyl, wherein said C1-6-alkyl or C3-6-cycloalkyl group can be independently substituted with 1-3 halogens; A is (i) a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic monocyclic ring or (ii) a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring which is fused to another five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring, V is a bond or —(C═O)—, —CH(OH)—, —CH2—or ═CH—; U is a bond or —CH2-, or for the case when V is ═CH—, U is —CH═; X is ═CH—, ═CF—, ═C(OR3)—, or —C═O—; and Y is ═CH—, ═CF—, ═N—, or for the case when X is —C═O—, Y is —N(R3)—.

    摘要翻译： 作为结构式（I）的螺环哌啶酰胺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。 其中对于其发生的每个实例，n独立地为0,1或2; R 1是氢，C 1-6 - 烷基或C 3-6 - 环烷基，其中所述C 1-6 - 烷基或C 3-6 - 环烷基可以独立地被1-3个卤素取代; A是（i）五或六元饱和或不饱和杂环或碳环单环或（ii）五元或六元饱和或不饱和的杂环或碳环，其与另一个五元或六元饱和 或不饱和杂环或碳环，V是一个键或 - （C = O） - ， - CH（OH） - ， - CH 2 - 或= CH-; U是键或-CH 2 - ，或者当V是= CH-的情况下，U是-CH =; X是≡CH-，≡CF-，≡C（OR3） - 或-C = O-; 并且Y为≡CH-，≡CF-，═N-，或者对于X为-C≡O-的情况，Y为-N（R 3） - 。