公开(公告)号：EP2318388A2

公开(公告)日：2011-05-11

申请号：EP09775391.7

申请日：2009-07-21

申请人： Schering Corporation

发明人： MCCORMICK, Kevin D. ,  ASLANIAN, Robert G. ,  MANGIARACINA, Pietro ,  BERLIN, Michael Y. ,  DE LERA RUIZ, Manuel ,  BOYCE, Christopher W ,  CHAO, Jianhua ,  TING, Pauline C. ,  ZHENG, Junying ,  ROSENBLUM, Stuart B.

IPC分类号： C07D401/06

CPC分类号： C07D471/10 ,  C07D401/06 ,  C07D401/14 ,  C07D405/14 ,  C07D417/14 ,  C07D491/107 ,  C07D491/20 ,  C07D495/20 ,  C07D498/10

摘要： The present invention relates to novel Tricyclic Spirocycle Derivatives, pharmaceutical compositions comprising the Tricyclic Spirocycle 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 disoder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.

摘要翻译： 本发明涉及新的三环螺环衍生物，包含三环螺环衍生物的药物组合物以及这些化合物用于治疗或预防过敏症，过敏引起的气道反应，充血，心血管疾病，炎性疾病，胃肠道病症， 神经系统疾病，代谢疾病，肥胖或肥胖相关疾病，糖尿病，糖尿病并发症，葡萄糖耐量降低或空腹血糖受损。

公开(公告)号：EP1896453B1

公开(公告)日：2009-12-02

申请号：EP06785168.3

申请日：2006-06-19

申请人： Schering Corporation

发明人： ASLANIAN, Robert G. ,  BERLIN, Michael Y. ,  HUANG, Ying ,  MCCORMICK, Kevin D. ,  MUTAHI, Mwangi W. ,  SHIH, Neng-Yang ,  TING, Pauline, C. ,  TOM, Wing, C. ,  ZHENG, Junying

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

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14

摘要： Disclosed are 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, alkyl, alkenyl, or optionally substituted cycloalkyl, aryl, heteroaryl, heterocycloalkyl or a group of the formula (II); where ring A is a monoheteroaryl ring; R2 is optionally substituted alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; compositions and methods of treating allergy-induced airway responses, congestion, obesity, metabolic syndrome nonalcoholic fatty liver disease, hepatic steatosis, nonalcoholic steatohepatitis, cirrhosis, hepatacellular carcinoma or cognition deficit disorders using said compounds, alone or in combination with other agents.

公开(公告)号：EP1966143A2

公开(公告)日：2008-09-10

申请号：EP06845817.3

申请日：2006-12-19

申请人： Schering Corporation

发明人： SOLOMON, Daniel M. ,  ASLANIAN, Robert G. ,  BERLIN, Michael Y. ,  DE LERA RUIZ, Manuel ,  MCCORMICK, Kevin D. ,  MUTAHI, Mwangi W. ,  TOM, Wing C.

IPC分类号： C07D213/74 ,  C07D401/12 ,  C07D401/14 ,  A61K31/44 ,  A61P29/00

CPC分类号： C07D401/12 ,  C07D213/73 ,  C07D213/74 ,  C07D401/14 ,  C07D471/04

摘要： Disclosed are compounds of the formula Chemical formula (I) or a pharmaceutically acceptable salt thereof, wherein M2 is N; X is a bond, optionally substituted alkylene, alkenylene, -O-, -CH2N(R12)-, -N(R12)CH2-, -N(R12)-, -NHC(O)-, -OCH2-, -CH2O-, or -S(O)0-2-; and Y is -(CH2)1-2-, -C(=O)-, -C(=NOR13)- or -SO0-2-; or M1 is N; M2 is N or CH; X is a bond, alkylene, alkenylene, -C(O)-, -NHC(O)-, -OC(O)- or -S(O)1-2-; Y is -(CH2)1-2-, -C(=O)- or -SO0-2-; and when M2 is CH, Y is also Y is -O- or -C(=NOR13)-; Z is a bond or optionally substituted alkylene or alkenylene; U and W are CH, or one is CH and one is N; R1 is optionally substituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heterocycloalkyl; R2 is optionally substituted alkyl, alkenyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; and compositions and methods of treating obesity, metabolic syndrome and a cognition deficit disorder, alone or in combination with other agents.

公开(公告)号：EP1896453A1

公开(公告)日：2008-03-12

申请号：EP06785168.3

申请日：2006-06-19

申请人： Schering Corporation

发明人： ASLANIAN, Robert G. ,  BERLIN, Michael Y. ,  HUANG, Ying ,  MCCORMICK, Kevin D. ,  MUTAHI, Mwangi W. ,  SHIH, Neng-Yang ,  TING, Pauline, C. ,  TOM, Wing, C. ,  ZHENG, Junying

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

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14

摘要： Disclosed are 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, alkyl, alkenyl, or optionally substituted cycloalkyl, aryl, heteroaryl, heterocycloalkyl or a group of the formula (II); where ring A is a monoheteroaryl ring; R2 is optionally substituted alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; compositions and methods of treating allergy-induced airway responses, congestion, obesity, metabolic syndrome nonalcoholic fatty liver disease, hepatic steatosis, nonalcoholic steatohepatitis, cirrhosis, hepatacellular carcinoma or cognition deficit disorders using said compounds, alone or in combination with other agents.

公开(公告)号：EP2376454A2

公开(公告)日：2011-10-19

申请号：EP09753000.0

申请日：2009-11-17

申请人： Schering Corporation

发明人： TING, Pauline C. ,  ASLANIAN, Robert G. ,  CAO, Jianhua ,  CAPLEN, Mary Ann ,  CHAN, Tin-Yau ,  KIM, Hyunjin ,  KIM, Jae-Hun ,  KUANG, Rongze ,  LEE, Joe F. ,  WU, Heping

IPC分类号： C07D213/74 ,  C07D401/04 ,  C07D403/14 ,  C07D407/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/08 ,  C07D493/10 ,  A61K31/422 ,  A61K31/427

CPC分类号： C07D413/12 ,  A61K31/422 ,  A61K31/427 ,  C07D213/74 ,  C07D401/04 ,  C07D403/14 ,  C07D407/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/08 ,  C07D493/10

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: (We bring to your attention that the illustrative compound of the invention is not provided on this electronic version as it is provided in the abstract of the paper copy)

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。 下面示出了本发明的示例性化合物:(我们引起您的注意，在该电子版本中没有提供本发明的说明性化合物，因为它在纸质副本的摘要中提供）

公开(公告)号：EP2091534A1

公开(公告)日：2009-08-26

申请号：EP07838186.0

申请日：2007-09-13

申请人： Schering Corporation

发明人： ASLANIAN, Robert G. ,  CHAN, Tin-Yau ,  HARRIS, Joel M. ,  MCKITTRICK, Brian A. ,  NEUSTADT, Bernard R. ,  PALANI, Anandan ,  PRIESTLEY, Tony ,  SMITH, Elizabeth M. ,  STAMFORD, Andrew W. ,  VACCARO, Henry M. ,  XIAO, Dong

IPC分类号： A61K31/4427 ,  A61P3/06 ,  A61P3/10 ,  A61P9/10 ,  A61P25/28 ,  C07D401/04

CPC分类号： A61K31/4427 ,  C07D471/10 ,  C07D519/00

摘要： The present invention relates to methods for treating or preventing a disorder of lipid metabolism, pain, diabetes, a vascular condition, demyelination or nonalcoholic fatty liver disease, comprising administering a compound having the formula (I) or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof, wherein: R1 and R2 are defined in Tables 1-6 herein, and R3 is -phenyl, -4-chlorophenyl, -2-pyridyl, or -3-pyridyl.

公开(公告)号：EP2059519A2

公开(公告)日：2009-05-20

申请号：EP07861898.0

申请日：2007-11-09

申请人： Schering Corporation

发明人： PALANI, Anandan ,  SU, Jing ,  XIAO, Dong ,  HUANG, Xianhai ,  RAO, Ashwin U. ,  CHEN, Xiao ,  TANG, Haiqun ,  QIN, Jun ,  HUANG, Ying R. ,  ASLANIAN, Robert G. ,  MCKITTRICK, Brian A. ,  DEGRADO, Sylvia J.

IPC分类号： C07D471/04 ,  C07D491/04 ,  A61K31/519 ,  A61P3/00 ,  A61P9/00

CPC分类号： C07D491/04 ,  C07D471/04

摘要： The present invention provides compounds of Formula (I) and pharmaceutically acceptable salts, solvates, esters, and tautomers thereof, wherein: Q is selected from the group consisting of: (a), (b), (c), (d) and (e); and L is selected from the group consisting of: (f), (g), (h), and (i); pharmaceutically compositions comprising one or more compounds of formula (I), and methods of using the compounds of formula (I).

公开(公告)号：EP2379562A1

公开(公告)日：2011-10-26

申请号：EP09775054.1

申请日：2009-12-15

申请人： Schering Corporation

发明人： XIAO, Dong ,  PALANI, Anandan ,  HUANG, Xianhai ,  ZHU, Xiaohong ,  ASLANIAN, Robert G.

IPC分类号： C07D491/052 ,  A61K31/4162 ,  A61P9/00 ,  A61P29/00 ,  A61P7/00 ,  A61P11/00 ,  A61P25/00 ,  A61P1/00 ,  A61P35/00 ,  A61P3/00

CPC分类号： C07D491/052

摘要： The present invention relates to Bicyclic Pyranone Derivatives, their compositions and uses 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.Formula (I). Y is -C- when an optional and additional bond is present and Y is -CH- when an optional and additional bond is not present; Z is -O-, -NH- or -N(alkyl)- when the optional and additional bond between Y and Z Is absent, and Z Is -N- when the optional and additional bond between Y and Z is present; R
1 is H1 halo or -CN; R
2 is alkyl, alkenyl or -(alkyleneVcydoalkyl; t is 0 or 1; R
3 is O when the optional and additional bond between Y and R
3 is present, and R
3 is alkyl. haloalkyl. -C(O)OR
5 . -alkylene-O-alkyt or -O-alkyl when the optional and additional bond between Y and R
3 is absent: R
4 is H, alkyl or aryl, wherein an aryl group can be unsubstituted or optionally substituted.

公开(公告)号：EP2379547A1

公开(公告)日：2011-10-26

申请号：EP09793410.3

申请日：2009-12-15

申请人： Schering Corporation

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

IPC分类号： C07D471/04

CPC分类号： C07D471/04

摘要： The present invention relates to Pyridopyrimidine Derivatives of formula (I), compositions comprising a Pyridopyrimidine Derivative and methods for using the Pyridopyrimidine 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 complication, obesity, an obesity-related disorder or non-alcoholic fatty liver disease.

公开(公告)号：EP2356106A1

公开(公告)日：2011-08-17

申请号：EP09793312.1

申请日：2009-10-06

申请人： Schering Corporation

发明人： MCCORMICK, Kevin D. ,  DONG, Li ,  BOYCE, Christopher W ,  DE LERA RUIZ, Manuel ,  FEVRIER, Salem ,  WU, Jie ,  ZHENG, Junying ,  YU, Younong ,  CHAO, Jianhua ,  WON, Walter S. ,  RAO, Ashwin U. ,  KUANG, Rongze ,  TING, Pauline C. ,  HUANG, Xianhai ,  SHAO, Ning ,  PALANI, Anandan ,  BERLIN, Michael Y. ,  ASLANIAN, Robert G.

IPC分类号： C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D409/10 ,  C07D413/10 ,  C07D417/10 ,  C07D235/02 ,  C07D263/52 ,  C07D498/10 ,  C07D519/00 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/424 ,  A61P11/02

CPC分类号： A61K31/5377 ,  A61K31/437 ,  A61K31/501 ,  A61K31/506 ,  A61K31/537 ,  C07D235/02 ,  C07D263/52 ,  C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D409/10 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D471/04 ,  C07D498/10 ,  C07D519/00

摘要： In its many embodiments, the present invention provides a novel class of biaryi spiroaminooxazoline analogues as modulators of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions.

摘要翻译： 在其许多实施方案中，本发明提供了一类新的二氨基螺氨基恶唑啉类似物作为α2C肾上腺素能受体激动剂的调节剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备包含一种或多种此类化合物 以及使用这些化合物或药物组合物治疗，预防，抑制或改善与α2C肾上腺素能受体相关的一种或多种病症的方法。