公开(公告)号：EP2443118A1

公开(公告)日：2012-04-25

申请号：EP10727311.2

申请日：2010-06-15

申请人： Schering Corporation

发明人： HUANG, Xianhai ,  ZHU, Zhaoning ,  GREENLEE, William, J. ,  PALANI, Anandan ,  ASLANIAN, Robert, G.

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P25/28

CPC分类号： C07D471/04

摘要： This invention provides novel compounds that are modulators of gamma secretase. The compounds have the Formula I: Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of Formula I.

公开(公告)号：EP2379565A1

公开(公告)日：2011-10-26

申请号：EP09798990.9

申请日：2009-12-18

申请人： Schering Corporation

发明人： XIAO, Dong ,  PALANI, Anandan ,  ASLANIAN, Robert, G.

IPC分类号： C07D513/04 ,  A61K31/437 ,  A61P3/10

CPC分类号： C07D513/04

摘要： The present invention relates to novel Piperidine and Piperazine Derivatives, pharmaceutical compositions comprising the Piperidine and Piperazine Derivatives and the use of these compounds of formula (I) for treating or preventing treating allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a cognitive disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.

公开(公告)号：EP2367598A2

公开(公告)日：2011-09-28

申请号：EP09752998.6

申请日：2009-11-17

申请人： Schering Corporation

发明人： TING, Pauline, C. ,  ASLANIAN, Robert, G. ,  CAPLEN, Mary Ann ,  CAO, Jianhua ,  CHAN, Tin-Yau ,  KIM, David, Won-Shik ,  KIM, Hyunjin ,  KIM, Jae-Hun ,  KUANG, Rongze ,  LEE, Joe, F. ,  SCHWERDT, John, H. ,  WU, Heping ,  ZORN, Nicolas

IPC分类号： A61P3/00 ,  A61P9/00 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  A61K31/422 ,  A61K31/427

CPC分类号： C07D413/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04

摘要： The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase ("DGAT") inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below: formula (I).

摘要翻译： 本发明涉及作为二酰甘油酰基转移酶（“DGAT”）抑制剂的新型杂环化合物，包含该杂环化合物的药物组合物以及该化合物用于治疗或预防心血管疾病，代谢病症，肥胖症或肥胖相关病症的用途， 糖尿病，血脂异常，糖尿病并发症，葡萄糖耐量降低或空腹血糖受损。 下面显示了本发明的说明性化合物：式（I）。

公开(公告)号：EP2350067A2

公开(公告)日：2011-08-03

申请号：EP09740590.6

申请日：2009-10-14

申请人： Schering Corporation

发明人： PALANI, Anandan ,  BERLIN, Michael, Y. ,  ASLANIAN, Robert, G. ,  VACCARO, Henry, M. ,  CHAN, Tin-Yau ,  XIAO, Dong ,  DEGRADO, Sylvia ,  RAO, Ashwin, U. ,  CHEN, Xiao ,  LEE, Yoon, Joo ,  SOFOLARIDES, Michael, J. ,  SHAO, Ning ,  HUANG, Ying, R. ,  LIU, Zhidan ,  WANG, Li Yuan ,  PU, Haiyan

IPC分类号： C07D417/04 ,  C07D417/14 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D285/135 ,  C07D271/113 ,  C07D491/107 ,  A61K31/4355 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61P3/10

CPC分类号： C07D285/135 ,  C07D271/113 ,  C07D417/04 ,  C07D417/14 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D491/107

摘要： The present invention relates to novel Pyrrolidine, Piperidine and Piperazine Derivatives, pharmaceutical compositions comprising the Pyrrolidine, Piperidine and Piperazine Derivatives and the use of these compounds for treating or preventing treating allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disoder, a metabolic disorder, obesity, an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.

公开(公告)号：EP2350048A2

公开(公告)日：2011-08-03

申请号：EP09744830.2

申请日：2009-10-14

申请人： Schering Corporation

发明人： PALANI, Anandan ,  XIAO, Dong ,  ASLANIAN, Robert, G. ,  BERLIN, Michael, Y. ,  RAO, Ashwin, U. ,  CHEN, Xiao ,  LEE, Yoon, Joo ,  DEGRADO, Sylvia ,  SHAO, Ning ,  HUANG, Ying, R. ,  LIU, Zhidan

IPC分类号： C07D401/12 ,  A61K31/4427 ,  A61P7/12

CPC分类号： C07D401/06 ,  C07D213/643 ,  C07D213/81 ,  C07D401/12 ,  C07D417/04

摘要： The present invention relates to Azine Derivatives, pharmaceutical compositions comprising the Azine Derivatives and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.

公开(公告)号：EP2346853A2

公开(公告)日：2011-07-27

申请号：EP09752999.4

申请日：2009-11-17

申请人： Schering Corporation

发明人： TING, Pauline, C. ,  ASLANIAN, Robert, G. ,  CAPLEN, Mary Ann ,  CAO, Jianhua ,  KIM, David, Won-Shik ,  KIM, Hyunjin ,  KUANG, Rongze ,  LEE, Joe, F. ,  SCHWERDT, John, H. ,  WU, Heping ,  ZHOU, Gang ,  ZORN, Nicolas

IPC分类号： C07D401/12 ,  C07D401/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  A61K31/422 ,  A61K31/427 ,  A61K31/506 ,  A61P3/00 ,  A61P9/00

CPC分类号： C07D413/14 ,  C07D401/12 ,  C07D401/14 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

摘要： The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase ("DGAT") inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below.

摘要翻译： 本发明涉及作为二酰甘油酰基转移酶（“DGAT”）抑制剂的新型杂环化合物，包含该杂环化合物的药物组合物以及该化合物用于治疗或预防心血管疾病，代谢病症，肥胖症或肥胖相关病症的用途， 糖尿病，血脂异常，糖尿病并发症，葡萄糖耐量降低或空腹血糖受损。 下面显示了本发明的说明性化合物。

公开(公告)号：EP1934203B1

公开(公告)日：2010-08-18

申请号：EP06802156.7

申请日：2006-08-23

申请人： Schering Corporation ,  Pharmacopeia, LLC

发明人： MCCORMICK, Kevin, D. ,  BOYCE, Christopher, W. ,  SHIH, Neng-Yang ,  ASLANIAN, Robert, G. ,  MANGIARACINA, Pietro ,  DE LERA RUIZ, Manuel ,  YU, Younong ,  BIJU, Purakkattle, J. ,  HUANG, Chia-Yu ,  LIANG, Bo ,  LIU, Ruiyan ,  LIU, Rong-Qiang ,  GUISE-ZAWACKI, Lisa

IPC分类号： C07D403/06 ,  C07D413/06 ,  C07D417/06 ,  A61K31/435 ,  A61K31/41 ,  A61P29/00

CPC分类号： C07D413/06 ,  C07D403/06 ,  C07D413/04 ,  C07D413/14 ,  C07D417/06 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

摘要： In its many embodiments, the present invention relates to a novel class of phenylmorpholine and phenylthiomorpholine compounds useful as a2C adrenergic receptor agonists, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the a2C adrenergic receptor agonists using such compounds or pharmaceutical compositions.

公开(公告)号：EP2158203A2

公开(公告)日：2010-03-03

申请号：EP08742664.9

申请日：2008-04-09

申请人： Schering Corporation

发明人： HUANG, Xianhai ,  PALANI, Anandan ,  ASLANIAN, Robert, G.

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61K31/522 ,  A61P1/00 ,  A61P3/00 ,  A61P9/00

CPC分类号： C07D487/04

摘要： The present invention relates to Pyrimidinedione Derivatives, compositions comprising a Pyrimidinedione Derivative and methods for using the Pyrimidinedione Derivatives for treating or preventing a metabolic disorder, dyslipidemia, a cardiovascular disease, a neurological disorder, a hematological disease, cancer, inflammation, a respiratory disease, a gastroenterological disease, diabetes, a diabetic complicaton, obesity, an obesity-related disorder or non-alcoholic fatty liver disease.

摘要翻译： 本发明涉及嘧啶二酮衍生物，包含嘧啶二酮衍生物的组合物以及使用嘧啶二酮衍生物用于治疗或预防代谢疾病，血脂异常，心血管疾病，神经疾病，血液疾病，癌症，炎症，呼吸系统疾病， 胃肠疾病，糖尿病，糖尿病综合征，肥胖症，肥胖相关病症或非酒精性脂肪肝病。

公开(公告)号：EP1902046B1

公开(公告)日：2009-12-02

申请号：EP06773528.2

申请日：2006-06-19

申请人： Schering Corporation

发明人： ASLANIAN, Robert, G. ,  BERLIN, Michael, Y. ,  BOYCE, Christopher, W. ,  CHAO, Jianhua ,  DE LERA RUIZ, Manuel ,  MANGIARACINA, Pietro ,  MCCORMICK, Kevin, D. ,  MUTAHI, Mwangi, W. ,  ROSENBLUM, Stuart, B. ,  SHIH, Neng-Yang ,  SOLOMON, Daniel, M. ,  TOM, Wing, C. ,  VACCARO, Henry, A. ,  ZHENG, Junying ,  ZHU, Xiaohong

IPC分类号： C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  A61P3/04 ,  A61P29/00 ,  A61P37/00 ,  C07D409/14 ,  C07D471/04

CPC分类号： C07D295/185 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  Y02P20/582

摘要： Disclosed are novel compounds of the formula (I) or a pharmaceutically acceptable salt thereof, wherein: M1 and M3 are CH or N; M2 is CH, CF or N; Y is -C(=O)-, -C(=S)-, -(CH2)q-, -C(=NOR7)- or -SO1-2-; Z is a bond or optionally substituted alkylene or alkenylene; R1 is H, or alkyl, cycloalkyl, aryl, heteroaryl, heterocycloalkyl, all optionally substituted, or a group of the formula (II) where ring A is a heteroaryl ring; R2 is optionally substituted alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl; R3 is H, -C(O)NH2, or alkyl, aryl, cycloalkyl, heterocycloalkyl or heteroaryl, all optionally substituted; and the remaining variables are as defined in the specification; compositions and methods of treating allergy-induced airway responses, congestion, obesity, metabolic syndrome, alcoholic fatty liver disease, hepatic steatosis, nonalcoholic steatohepatitis, cirrhosis, hepatacellular carcinoma and cognition deficit disorders using said compounds, alone or in combination with other agents.

公开(公告)号：EP1318993B1

公开(公告)日：2008-08-20

申请号：EP01971115.9

申请日：2001-09-18

申请人： Schering Corporation

发明人： SHIH, Neng-Yang ,  ASLANIAN, Robert, G. ,  PIWINSKI, John, J. ,  LUPO, Andrew, T., Jr. ,  AFONSO, Adriano

IPC分类号： C07D401/12

CPC分类号： C07D401/12 ,  C07D401/14

摘要： The present invention discloses novel substituted imidazole compounds which have H3 receptor antagonist activity or dual histamine-H1 and H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy, congestion, inflammatory and CNS-related diseases and others.