公开(公告)号：EP2318391A1

公开(公告)日：2011-05-11

申请号：EP09790675.4

申请日：2009-07-21

申请人： Schering Corporation

发明人： DE LERA RUIZ, Manuel ,  BERLIN, Michael, Y. ,  ZHENG, Junying ,  ASLANIAN, Robert, G. ,  MCCORMICK, Kevin, D. ,  ZENG, Qingbei

IPC分类号： C07D401/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D495/14 ,  A61P11/02 ,  A61K31/445 ,  A61P37/08

CPC分类号： C07D401/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D495/14

摘要： The present invention relates to novel Tricyclic Heterocylce Derivatives, pharmaceutical compositions comprising the Tricyclic Heterocycle 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. R1 is formula (Ia), (Ib) or (Ic); R
2 is alkvl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl. any of which can be optionally substituted with R
11 ; M
1 is -CH-. -C(halo)- or -N-; Y is -C(O)-, -S-. -S(O)-, -S(O)
2 -, -CH
2 - or -O-, such that Y is not -O- when an adjacent atom is N.

公开(公告)号：EP2318387A1

公开(公告)日：2011-05-11

申请号：EP09790676.2

申请日：2009-07-21

申请人： Schering Corporation

发明人： DE LERA RUIZ, Manuel ,  BERLIN, Michael, Y. ,  ZHENG, Junying ,  ASLANIAN, Robert, G. ,  MCCORMICK, Kevin, D.

IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  A61P11/02 ,  A61P37/08 ,  A61K31/445

CPC分类号： C07D401/14 ,  C07D401/04 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04

摘要： The present invention relates to novel bicyclic heterocycle derivatives, pharmaceutical compositions comprising the bicyclic heterocycle 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. R
1 is: I, Ia, Ib ou Ic. R
2 is alkyl, alkenyl, aryl, cycloalkyl. heterocycloalkyl or heteroaryl, any of which can be optionally substituted with R
3 ; Y is -C(O)-, -S-, -S(O)-, -S(O)
2 -, -CH
2 - or -O-, such that if Y is -O- or -S-, then M is other than N and R
1 is (Ib);

公开(公告)号：EP2125749A2

公开(公告)日：2009-12-02

申请号：EP08714238.6

申请日：2008-02-11

申请人： Schering Corporation ,  Pharmacopeia, LLC

发明人： DE LERA RUIZ, Manuel ,  MCCORMICK, Kevin, D. ,  BOYCE, Christopher, W. ,  ASLANIAN, Robert, G. ,  YU, Younong ,  MANGIARACINA, Pietro ,  ZHENG, Junying ,  BERLIN, Michael, Y. ,  CIESLA, Stephanie, L. ,  HUANG, Chia-yu ,  LIANG, Bo

IPC分类号： C07D233/10 ,  C07D401/14 ,  C07D403/06 ,  C07D403/10 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  A61K31/4035 ,  A61P31/10 ,  A61P29/00 ,  A61P9/00 ,  A61P25/22

CPC分类号： C07D403/14 ,  C07D233/10 ,  C07D401/14 ,  C07D403/06 ,  C07D403/10 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14

摘要： In its many embodiments, the present invention provides a novel class of biaryl compounds as inhibitors of ÿ2C 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 ÿ2C adrenergic receptors using such compounds or pharmaceutical compositions.

公开(公告)号：EP1976848A2

公开(公告)日：2008-10-08

申请号：EP06839411.3

申请日：2006-12-19

申请人： Schering Corporation

发明人： MUTAHI, Mwangi, W. ,  ASLANIAN, Robert, G. ,  BERLIN, Michael, Y. ,  BOYCE, Christopher, W. ,  DE LERA RUIZ, Manuel ,  MCCORMICK, Kevin, D. ,  SOLOMON, Daniel, M. ,  VACCARO, Henry, A. ,  ZHENG, Junying ,  PURAKKATTLE, Biju, J. ,  YU, Younong ,  ZHOU, Wei ,  ZHU, Xiaohong

IPC分类号： C07D401/10 ,  C07D203/12 ,  C07D403/14 ,  C07D471/04 ,  A61K31/4545 ,  A61P11/00

CPC分类号： C07D471/04 ,  C07D213/38 ,  C07D213/73 ,  C07D277/40 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D409/12 ,  C07D417/06 ,  C07D417/14 ,  C07D473/00

摘要： Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: M is CH or N; U and W are each CH, or one of U and W is CH and the other is N; X is a bond, alkylene, -C(O)-, -C(N-OR5)-, -C(N-OR5)-CH(R6)-, -CH(R6)-C(N-OR5)-, -O-, -OCH2-, -CH2O- or -S(O)0-2-; Y is -O-, -(CH2)2-, -C(=O)-, -C(=NOR7)- or -SO0-2-; Z is a bond, optionally substituted alkylene or alkylene interrupted by a heteroatom or heterocyclic group; R1 is optionally substituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heterocycloalkyl, or benzimidazolyl or a derivative thereof; R2 is optionally substituted alkyl, alkenyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; compositions and methods for treating an allergy-induced airway response, congestion, diabetes, obesity, an obesity-related disorder, metabolic syndrome and a cognition deficit disorder using said compounds, alone or in combination with other agents.

公开(公告)号：EP1934203A2

公开(公告)日：2008-06-25

申请号：EP06802156.7

申请日：2006-08-23

申请人： Schering Corporation ,  PHARMACOPEIA, INC.

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：EP2323734A1

公开(公告)日：2011-05-25

申请号：EP09791090.5

申请日：2009-08-03

申请人： Schering Corporation

发明人： YU, Younong ,  DE LERA RUIZ, Manuel ,  BOYCE, Christopher, W. ,  MC CORMICK, Kevin, D.

IPC分类号： A61P25/00 ,  C07D405/08 ,  C07D405/14 ,  C07D413/14 ,  A61K31/353

CPC分类号： C07D405/04 ,  C07D405/14 ,  C07D413/14

摘要： In its many embodiments, the present invention provides a novel class of cyclopropylchromene derivatives as modulators of a2C adrenergic receptor, 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 a2C adrenergic receptors using such compounds or pharmaceutical compositions.

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：EP1931665A1

公开(公告)日：2008-06-18

申请号：EP06803837.1

申请日：2006-09-19

申请人： Schering Corporation

发明人： DE LERA RUIZ, Manuel ,  ASLANIAN, Robert, G. ,  BERLIN, Michael, Y. ,  MCCORMICK, Kevin, D. ,  CELLY, Chander, S.

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P37/08 ,  A61P3/00

CPC分类号： C07D471/04

摘要： The present invention discloses the compound of Formula I and pharmaceutically acceptable salts and solvates thereof. The invention also relates to pharmaceutical compositions comprising the Compound of Formula I and its use in treating obesity, metabolic syndrome, diabetes, hepatic lipidosis or nonalcoholic fatty liver disease. The invention also relates to the use of a combination of the Compound of Formula I with additional therapeutic agents for treating obesity, metabolic syndrome, diabetes, hepatic lipidosis or nonalcoholic 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。

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.