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1. 发明申请

WO2010042473A1 BIARYL SPIROAMINOOXAZOLINE ANALOGUES AS ALPHA2C ADRENERGIC RECEPTOR MODULATORS 审中-公开
标题翻译：作为ALPHA2C ADRENERGIC受体调节剂的BIARYL SPIROAMINOOXAZOLINE ANALOGUES
公开(公告)号：WO2010042473A1
公开(公告)日：2010-04-15
申请号：PCT/US2009/059636
申请日：2009-10-06
申请人： SCHERING CORPORATION , 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.
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颖的二烯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这类化合物的药物制剂的方法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α2肾上腺素能受体相关的一种或多种病症的方法。

2. 发明申请

WO2010027567A3 TRICYCLIC SPIROCYCLE DERIVATIVES AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：WO2010027567A3
公开(公告)日：2010-03-11
申请号：PCT/US2009/051267
申请日：2009-07-21
申请人： SCHERING CORPORATION , 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.
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 , C07D401/14 , C07D405/14 , C07D417/14 , C07D495/20 , C07D491/107 , A61K31/438 , A61P3/10 , A61P9/00 , A61P25/00 , A61P37/00 , A61P3/00
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.

3. 发明申请

WO2010059611A2 INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE 审中-公开
标题翻译：二乙酰胆碱酯酶抑制剂
公开(公告)号：WO2010059611A2
公开(公告)日：2010-05-27
申请号：PCT/US2009/064762
申请日：2009-11-17
申请人： SCHERING CORPORATION , 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
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基甘油酰基转移酶（“DGAT”）抑制剂的新型杂环化合物，包含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，代谢障碍，肥胖或肥胖相关障碍的用途，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。本发明的示例性化合物如下所示：（我们提请您注意，本发明的说明性化合物不是在该电子版本上提供的，如在本文摘要中提供的）

4. 发明申请

WO2010075069A1 BICYCLIC PYRANONE DERIVATIVES AS NICOTINIC ACID RECEPTOR AGONISTS 审中-公开
标题翻译：作为肌酸受体激动剂的双相吡咯烷酮衍生物
公开(公告)号：WO2010075069A1
公开(公告)日：2010-07-01
申请号：PCT/US2009/068022
申请日：2009-12-15
申请人： SCHERING CORPORATION , XIAO, Dong , PALANI, Anandan , HUANG, Xianhai , ZHU, Xiaohong , ASLANIAN, Robert G.
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.
摘要翻译：本发明涉及双环吡喃酮衍生物，其组合物和用于治疗或预防代谢紊乱，血脂异常，心血管疾病，神经障碍，血液病，癌症，炎症，呼吸系统疾病，胃肠病，糖尿病，糖尿病并发症，肥胖症，肥胖相关障碍或非酒精性脂肪性肝病。（I）。当不存在任选和另外的键时，当存在任选的附加键且Y是-CH-时，Y是-C-; 当Y和Z之间的任选和另外的键不存在时，Z是-O - ， - NH-或-N（烷基），当存在Y和Z之间的任选的和另外的键时，Z是 - R1为H1卤素或-CN; R 2是烷基，链烯基或 - （亚烷基环烷基; t是0或1;当存在Y和R 3之间的任选和另外的键时，R 3是O，并且R 3是烷基卤代烷基-C（O）OR 5 - 亚烷基-O - 烷基或 - 烷基，当Y和R3之间的任选和另外的键不存在时：R 4是H，烷基或芳基，其中芳基可以是未取代的或任选被取代的。

5. 发明申请

WO2009073779A1 GAMMA SECRETASE MODULATORS 审中-公开
标题翻译： GAMMA秘密调节器
公开(公告)号：WO2009073779A1
公开(公告)日：2009-06-11
申请号：PCT/US2008/085520
申请日：2008-12-04
申请人： SCHERING CORPORATION , HUANG, Xianhai , PALANI, Anandan , QIN, Jun , ASLANIAN, Robert G. , ZHU, Zhaoning , GREENLEE, William J.
发明人： HUANG, Xianhai , PALANI, Anandan , QIN, Jun , ASLANIAN, Robert G. , ZHU, Zhaoning , GREENLEE, William J.
IPC分类号： C07D401/10 , C07D403/10 , C07D471/04 , C07D491/04 , C07D498/04 , A61K31/4738 , A61P25/28
CPC分类号： C07D471/04 , C07D401/10 , C07D403/10 , C07D491/04 , C07D498/04
摘要： This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I) wherein R 2 is a fused bicyclic ring of the formula (II). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's disease using the compounds of formula (I).
摘要翻译：本发明提供了作为γ分泌酶调节剂的新型化合物。所述化合物具有式（I），其中R 2是式（II）的稠合双环。还公开了使用式（I）的化合物调节γ-分泌酶活性和治疗阿尔茨海默病的方法的方法。

6. 发明申请

WO2010075068A1 PYRIDOPYRIMIDINE DERIVATIVES AND METHODS OF USE THEREOF 审中-公开
标题翻译：吡咯烷酮衍生物及其使用方法
公开(公告)号：WO2010075068A1
公开(公告)日：2010-07-01
申请号：PCT/US2009/068021
申请日：2009-12-15
申请人： SCHERING CORPORATION , XIAO, Dong , PALANI, Anandan , SOFOLARIDES, Michael J. , ASLANIAN, Robert G.
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.
摘要翻译：本发明涉及式（I）的吡啶并嘧啶衍生物，包含吡啶并嘧啶衍生物的组合物和用于治疗或预防代谢紊乱，血脂异常，心血管疾病，神经障碍，血液病，癌症，炎症的吡啶并嘧啶衍生物的方法呼吸系统疾病，胃肠疾病，糖尿病，糖尿病并发症，肥胖症，肥胖相关障碍或非酒精性脂肪性肝病。

7. 发明公开

EP1966143A2 SUBSTITUTED ANILINE DERIVATIVES USEFUL AS HISTAMINE H3 ANTAGONISTS 审中-公开
标题翻译：取代苯胺衍生物作为组胺H3拮抗剂
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.

8. 发明公开

EP1896453A1 CARBON-LINKED SUBSTITUTED PIPERIDINES AND DERIVATIVES THEREOF USEFUL AS HISTAMINE H3 ANTAGONISTS 有权
标题翻译：连碳取代的哌啶及其衍生物组胺H3拮抗剂
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.

9. 发明公开

EP2318388A2 TRICYCLIC SPIROCYCLE DERIVATIVES AND METHODS OF USE THEREOF 审中-公开
标题翻译：三环类SPIROCYCLE衍生物及其使用方法
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。

10. 发明授权

EP1896453B1 CARBON-LINKED SUBSTITUTED PIPERIDINES AND DERIVATIVES THEREOF USEFUL AS HISTAMINE H3 ANTAGONISTS 有权
标题翻译：连碳取代的哌啶及其衍生物组胺H3拮抗剂
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.

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