公开(公告)号：EP2413941A1

公开(公告)日：2012-02-08

申请号：EP10759391.5

申请日：2010-04-01

申请人： Merck Sharp & Dohme Corp. ,  Merck Canada Inc.

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： 本发明涉及二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。

公开(公告)号：EP2334666A1

公开(公告)日：2011-06-22

申请号：EP09810959.8

申请日：2009-09-02

申请人： Merck Canada Inc.

发明人： LECLERC, Jean-Philippe ,  LI, Chun, Sing ,  RAMTOHUL, Yeeman, K.

IPC分类号： C07D401/14 ,  A61K31/4192 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/506 ,  A61P3/06 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14

CPC分类号： A61K31/4192 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/506 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14

摘要： Heteroaromatic compounds of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.

公开(公告)号：EP2398796A1

公开(公告)日：2011-12-28

申请号：EP10743371.6

申请日：2010-02-18

申请人： Merck Canada Inc.

发明人： ISABEL, Elise ,  LACHANCE, Nicolas ,  LECLERC, Jean-Philippe ,  LEGER, Serge ,  OBALLA, Renata, M. ,  POWELL, David ,  RAMTOHUL, Yeeman, K. ,  ROY, Patrick ,  TRANMER, Geoffrey, K. ,  ASPIOTIS, Renee ,  LI, Lianhai ,  MARTINS, Evelyn

IPC分类号： C07D417/04 ,  A61K31/454 ,  A61K31/496 ,  A61K31/4995 ,  A61K31/551 ,  C07D403/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D487/08

CPC分类号： C07D413/14 ,  A61K31/454 ,  A61K31/496 ,  A61K31/4995 ,  A61K31/551 ,  C07D403/04 ,  C07D403/14 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14 ,  C07D487/08

摘要： Heterocyclic compounds of structural formula (I), or a pharmaceutically acceptable salt thereof, wherein W is a R
1 -substituted heteroaryl, R
1 is an heteroaryl ring substituted with an ester or carboxylic acid containing radical, X-T is N-CR
5 R
6 , C=CR
5 or CR
13 -CR
5 R
6 , Y is a bond or -C(O)-, a and b represent an integer selected from 1 to 4, and Ar is an optionally substituted phenyl or naphtyl, are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD) The heterocyclic compounds are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, atherosclerosis, obesity, diabetes, neurological disease, Metabolic Syndrome, insulin resistance, cancer, liver steatosis, and non-alcoholic steatohepatitis.