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1. 发明申请

WO2011057382A1 SPIROCYCLIC PIPERIDINE DERIVATIVES USEFUL AS RENIN INHIBITORS 审中-公开
标题翻译：作为RININ抑制剂有用的螺环哌啶衍生物
公开(公告)号：WO2011057382A1
公开(公告)日：2011-05-19
申请号：PCT/CA2010/001632
申请日：2010-10-12
申请人： MERCK FROSST CANADA LTD. , CHEN, Austin , ASPIOTIS, Renee , MCKAY, Daniel , HAN, Yongxin , FOURNIER, Pierre-André
发明人： CHEN, Austin , ASPIOTIS, Renee , MCKAY, Daniel , HAN, Yongxin , FOURNIER, Pierre-André
IPC分类号： C07D491/107 , A61P25/22 , A61P27/02 , A61P5/42 , A61P9/00 , C07D491/20 , A61K31/438 , A61P13/12
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)-, -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 )-.
摘要翻译：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） - 。

2. 发明申请

WO2010114978A1 RENIN INHIBITORS 审中-公开
标题翻译：雷宁抑制剂
公开(公告)号：WO2010114978A1
公开(公告)日：2010-10-07
申请号：PCT/US2010/029588
申请日：2010-04-01
申请人： MERCK SHARP & DOHME CORP. , MERCK FROSST CANADA LTD. , MCKAY, Daniel, J. , ARBOUR, Melissa , ASPIOTIS, Renee , CHEN, Austin , DOLMAN, Sarah Jennifer , FOURNIER, Pierre-Andre , GALLANT, Michel , HAN, Yongxin , HUGHES, Greg , JANEY, Jacob , JUTEAU, Helene , LACOMBE, Patrick , LALIBERTE, Sebastien , LAUZON, Sophie , MACDONALD, Dwight , MACKAY, Bruce , MELLON, Christophe , MOLINARO, Carmela , MORLEY, Krista, L. , O'SHEA, Paul , RAMTOHUL, Yeeman, K. , SIMARD, Daniel , TSUI, Chit
发明人： MCKAY, Daniel, J. , ARBOUR, Melissa , ASPIOTIS, Renee , CHEN, Austin , DOLMAN, Sarah Jennifer , FOURNIER, Pierre-Andre , GALLANT, Michel , HAN, Yongxin , HUGHES, Greg , JANEY, Jacob , JUTEAU, Helene , LACOMBE, Patrick , LALIBERTE, Sebastien , LAUZON, Sophie , MACDONALD, Dwight , MACKAY, Bruce , MELLON, Christophe , MOLINARO, Carmela , MORLEY, Krista, L. , O'SHEA, Paul , RAMTOHUL, Yeeman, K. , SIMARD, Daniel , TSUI, Chit
IPC分类号： A61K31/535
CPC分类号： C07D211/26 , C07D211/22 , C07D211/28 , C07D211/52 , C07D401/04 , C07D401/12 , C07D413/04 , C07D413/14
摘要： The present invention relates to biaryl piperidine-based renin inhibitor compounds, and their use in treating cardiovascular events and renal insufficiency.
摘要翻译：本发明涉及联芳基哌啶基肾素抑制剂化合物及其在治疗心血管事件和肾功能不全中的用途。

3. 发明申请

WO2008141462A9 NOVEL CASE OF RENIN INHIBITORS 审中-公开
公开(公告)号：WO2008141462A9
公开(公告)日：2008-11-27
申请号：PCT/CA2008/001005
申请日：2008-05-23
申请人： MERCK FROSST CANADA LTD. , WU, Tom, Yao-Hsiang , JUTEAU, Helene , GALLANT, Michel , DUBE, Daniel , ROY, Patrick , ASPIOTIS, Renee , GRIMM, Erich, L. , LALIBERTE, Sebastien , CHEN, Austin
发明人： WU, Tom, Yao-Hsiang , JUTEAU, Helene , GALLANT, Michel , DUBE, Daniel , ROY, Patrick , ASPIOTIS, Renee , GRIMM, Erich, L. , LALIBERTE, Sebastien , CHEN, Austin
IPC分类号： C07D211/60 , A61K31/451 , A61K31/4523 , A61K31/5377 , A61P13/10 , A61P9/00 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to piperidine-based renin inhibitor compounds having carboxylate or carboxylic acid terminal groups. The disclosed low molecular weight, orally active renin inhibitors are of non-peptide nature and have long duration of action. The compounds can be used in the treatment of cardiovascular events and renal insufficiency.

4. 发明申请

WO2009018662A9 RENIN INHIBITORS 审中-公开
公开(公告)号：WO2009018662A9
公开(公告)日：2009-02-12
申请号：PCT/CA2008/001429
申请日：2008-08-04
申请人： MERCK FROSST CANADA LTD. , DUBE, Daniel , CHEN, Austin , MCKAY, Daniel J.
发明人： DUBE, Daniel , CHEN, Austin , MCKAY, Daniel J.
IPC分类号： C07D213/75 , A61K31/165 , A61K31/4045 , A61K31/44 , A61K31/4406 , A61P9/00 , C07C237/08 , C07D209/08 , C07D213/56
摘要： The present invention relates to acyclic amino amides of formula (I). These compounds are renin inhibitors of a non-peptidic nature and of low molecular weight. The invention further relates to processes for the preparation of these compounds, pharmaceutical compositions containing them, as well as their use and method of treatment of cardiovascular events and renal insufficiency.

5. 发明申请

WO2009018662A1 RENIN INHIBITORS 审中-公开
标题翻译：雷宁抑制剂
公开(公告)号：WO2009018662A1
公开(公告)日：2009-02-12
申请号：PCT/CA2008/001429
申请日：2008-08-04
申请人： MERCK FROSST CANADA LTD. , DUBE, Daniel , CHEN, Austin , MCKAY, Daniel J.
发明人： DUBE, Daniel , CHEN, Austin , MCKAY, Daniel J.
IPC分类号： C07D213/75 , A61K31/165 , A61K31/4045 , A61K31/44 , A61K31/4406 , A61P9/00 , C07C237/08 , C07D209/08 , C07D213/56
CPC分类号： C07D209/08 , C07C237/20 , C07C2601/02 , C07D213/56 , C07D213/73
摘要： The present invention relates to acyclic amino amides of formula (I). These compounds are renin inhibitors of a non-peptidic nature and of low molecular weight. The invention further relates to processes for the preparation of these compounds, pharmaceutical compositions containing them, as well as their use and method of treatment of cardiovascular events and renal insufficiency.
摘要翻译：本发明涉及式（I）的无环氨基酰胺。这些化合物是非肽性质和低分子量的肾素抑制剂。本发明还涉及制备这些化合物的方法，含有它们的药物组合物，以及它们在治疗心血管事件和肾功能不全方面的用途和方法。

6. 发明申请

WO2014025736A1 HCV NS3 PROTEASE INHIBITORS 审中-公开
标题翻译： HCV NS3蛋白酶抑制剂
公开(公告)号：WO2014025736A1
公开(公告)日：2014-02-13
申请号：PCT/US2013/053725
申请日：2013-08-06
申请人： MERCK SHARP & DOHME CORP. , MERCK CANADA INC. , BARA, Thomas , BHAT, Sathesh , BISWAS, Dipshika , BROCKUNIER, Linda , BURNETTE, Duane , CHACKALAMANNIL, Samuel , CHELIAH, Mariappan, V. , CHEN, Austin , CLASBY, Martin , COLANDREA, Vince, J. , GUO, Zhuyan , HAN, Yongxin , JAYNE, Charles , JOSIEN, Hubert , MARCANTONIO, Karen , MIAO, Shouwu , NEELAMKAVIL, Santhosh , PINTO, Patrick , RAJAGOPALAN, Murali , SHAH, Unmesh , VELAZQUEZ, Francisco , VENKATRAMAN, Srikanth , XIA, Yan
发明人： BARA, Thomas , BHAT, Sathesh , BISWAS, Dipshika , BROCKUNIER, Linda , BURNETTE, Duane , CHACKALAMANNIL, Samuel , CHELIAH, Mariappan, V. , CHEN, Austin , CLASBY, Martin , COLANDREA, Vince, J. , GUO, Zhuyan , HAN, Yongxin , JAYNE, Charles , JOSIEN, Hubert , MARCANTONIO, Karen , MIAO, Shouwu , NEELAMKAVIL, Santhosh , PINTO, Patrick , RAJAGOPALAN, Murali , SHAH, Unmesh , VELAZQUEZ, Francisco , VENKATRAMAN, Srikanth , XIA, Yan
IPC分类号： C07D491/107 , A61K31/343 , A61K31/407 , A61P1/16 , A61P31/14
CPC分类号： C07K5/08 , A61K38/06 , A61K45/06 , C07D419/00 , C07D491/22
摘要： The present invention relates to hepatitis C virus (HCV) NS3 protease inhibitors containing a spirocyclic moeity, uses of such compounds, and synthesis of such compounds.
摘要翻译：本发明涉及含有螺环状的丙型肝炎病毒（HCV）NS3蛋白酶抑制剂，这些化合物的用途，以及这些化合物的合成。

7. 发明公开

EP2162436A1 NOVEL CASE OF RENIN INHIBITORS 审中-公开
标题翻译：肾素抑制剂新案例
公开(公告)号：EP2162436A1
公开(公告)日：2010-03-17
申请号：EP08757142.8
申请日：2008-05-23
申请人： Merck Frosst Canada Ltd.
发明人： WU, Tom, Yao-Hsiang , JUTEAU, Helene , GALLANT, Michel , DUBE, Daniel , ROY, Patrick , ASPIOTIS, Renee , GRIMM, Erich, L. , LALIBERTE, Sebastien , CHEN, Austin
IPC分类号： C07D211/60 , A61K31/451 , A61K31/4523 , A61K31/5377 , A61P13/10 , A61P9/00 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12
CPC分类号： C07D211/60 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D417/12
摘要： The present invention relates to piperidine-based renin inhibitor compounds having carboxylate or carboxylic acid terminal groups. The disclosed low molecular weight, orally active renin inhibitors are of non-peptide nature and have long duration of action. The compounds can be used in the treatment of cardiovascular events and renal insufficiency.

8. 发明公开

EP2188256A1 RENIN INHIBITORS 审中-公开
标题翻译：肾素抑制剂
公开(公告)号：EP2188256A1
公开(公告)日：2010-05-26
申请号：EP08783340.6
申请日：2008-08-04
申请人： Merck Frosst Canada Ltd.
发明人： DUBE, Daniel , CHEN, Austin , MCKAY, Daniel J.
IPC分类号： C07D213/75 , A61K31/165 , A61K31/4045 , A61K31/44 , A61K31/4406 , A61P9/00 , C07C237/08 , C07D209/08 , C07D213/56
CPC分类号： C07D209/08 , C07C237/20 , C07C2601/02 , C07D213/56 , C07D213/73
摘要： The present invention relates to acyclic amino amides of formula (I). These compounds are renin inhibitors of a non-peptidic nature and of low molecular weight. The invention further relates to processes for the preparation of these compounds, pharmaceutical compositions containing them, as well as their use and method of treatment of cardiovascular events and renal insufficiency.
摘要翻译：式（I）的无环氨基酰胺本发明涉及式（I）的无环氨基酰胺。这些化合物是非肽类性质和低分子量的肾素抑制剂。本发明进一步涉及制备这些化合物的方法，含有它们的药物组合物，以及它们的用途和治疗心血管事件和肾功能不全的方法。

9. 发明申请

WO2017049069A1 HETEROARYL COMPOUNDS AS IRAK INHIBITORS AND USES THEREOF 审中-公开
标题翻译：异丙酚化合物作为IRAK抑制剂及其用途
公开(公告)号：WO2017049069A1
公开(公告)日：2017-03-23
申请号：PCT/US2016/052107
申请日：2016-09-16
申请人： MERCK PATENT GMBH , JORAND-LEBRUN, Catherine , LAN, Ruoxi , CHEN, Austin , CLARK, Ryan C.
发明人： JORAND-LEBRUN, Catherine , LAN, Ruoxi , CHEN, Austin , CLARK, Ryan C.
IPC分类号： C07D233/88 , C07D401/04 , C07D403/04 , C07D405/04 , C07D413/04 , C07D471/08 , A61K31/4184 , A61K31/454 , A61P1/00 , A61P3/00 , A61P17/00 , A61P19/00 , A61P25/00 , A61P35/00
CPC分类号： C07D401/04 , A61K31/4184 , A61K31/4439 , A61K31/506 , C07D235/30 , C07D403/04 , C07D405/04 , C07D413/04 , C07D451/02 , C07D471/08
摘要： The present invention relates to compounds of Formula (I) and pharmaceutically acceptable compositions thereof, useful as IRAK inhibitors.
摘要翻译：本发明涉及可用作IRAK抑制剂的式（I）化合物及其药学上可接受的组合物。

10. 发明申请

WO2017049068A1 HETEROARYL COMPOUNDS AS IRAK INHIBITORS AND USES THEREOF 审中-公开
标题翻译：杂芳基化合物作为IRAK抑制剂及其用途
公开(公告)号：WO2017049068A1
公开(公告)日：2017-03-23
申请号：PCT/US2016/052104
申请日：2016-09-16
申请人： MERCK PATENT GMBH , JORAND-LEBRUN, Catherine , LAN, Ruoxi , CHEN, Austin , CLARK, Ryan C.
发明人： JORAND-LEBRUN, Catherine , LAN, Ruoxi , CHEN, Austin , CLARK, Ryan C.
IPC分类号： C07D413/14 , C07D491/08 , C07D403/04 , C07D413/04 , C07D417/04 , C07D487/08 , A61K31/4184 , A61P35/00 , A61P29/00
CPC分类号： C07D413/14 , A61K31/4184 , C07D401/04 , C07D403/04 , C07D413/04 , C07D417/04 , C07D471/08 , C07D487/08 , C07D491/08 , C07D498/08
摘要： The present invention relates to compounds of Formula (I) and pharmaceutically acceptable compositions thereof, useful as IRAK inhibitors.
摘要翻译：本发明涉及用作IRAK抑制剂的式（I）化合物及其药学上可接受的组合物。

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