公开(公告)号：EP1945626B1

公开(公告)日：2011-07-27

申请号：EP06789950.0

申请日：2006-08-23

申请人： Schering Corporation ,  Pharmacopeia, LLC

发明人： MCCORMICK, Kevin, D. ,  BOYCE, Christopher, W. ,  ASLANIAN, Robert, G. ,  SHIH, Neng-Yang ,  FEVRIER, Salem ,  MANGIARCINA, Pietro ,  HUANG, Chia-Yu ,  LIANG, Bo ,  LIU, Rong-Qiang ,  LU, Huagang

IPC分类号： C07D401/06 ,  C07D403/06 ,  A61K31/435 ,  A61K31/41 ,  A61P29/00

CPC分类号： C07D403/02 ,  C07D401/06 ,  C07D403/06

摘要： In its many embodiments, the present invention provides imidazole derivatives which are inhibitors of alPha2C 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 alpha2C adrenergic receptors using such compounds or pharmaceutical compositions. Formula (I).

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：EP2257546A2

公开(公告)日：2010-12-08

申请号：EP09713459.7

申请日：2009-02-19

申请人： Schering Corporation

发明人： ZHENG, Junying ,  CHAO, Jianhua ,  MCCORMICK, Kevin, D. ,  ASLANIAN, Robert, G. ,  MUTAHI, Mwangi, W. ,  BOYCE, Christopher, W. ,  WON, Walter, S.

IPC分类号： C07D403/06 ,  C07D403/08 ,  A61K31/47 ,  A61K31/403 ,  A61P29/00 ,  A61P25/00 ,  A61P3/10 ,  A61P9/00

CPC分类号： C07D403/06 ,  C07D403/08

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

公开(公告)号：EP2235035A2

公开(公告)日：2010-10-06

申请号：EP08866275.4

申请日：2008-12-18

申请人： Schering Corporation ,  Wang, Hongwu ,  Lim, Yeon-Hee ,  Lee, Yoon Jon ,  Bitar, Rema Danielle

发明人： ANTHES, John, C. ,  MCCORMICK, Kevin, D. ,  HEY, John, A. ,  ASLANIAN, Robert, G. ,  BIJU, Purakkattle, J. ,  BERLIN, Michael, Y. ,  SOLOMON, Daniel, M.

IPC分类号： C07J43/00 ,  C07J31/00 ,  C07J71/00 ,  A61P5/44 ,  A61K31/573 ,  A61K31/58

CPC分类号： C07J43/003 ,  C07J31/006 ,  C07J71/0031

摘要： The present invention provides compounds of Formula (VII) and 11-keto analogs thereof, and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, and isomers of said compounds and said 11-keto analogs, having the general structure formula (VII): wherein L, R
1 , R
2 , R
3 , R
4 , and R
5 are selected independently of each other and as defined herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions. The novel compounds of the present invention possess useful pharmacological activity while having unexpectedly low systemic activiy. Thus, the compounds of the invention represent a safer alternative to those known glucocorticoids which have poor side-effect profiles.

公开(公告)号：EP0823906A1

公开(公告)日：1998-02-18

申请号：EP96915342.0

申请日：1996-05-01

申请人： SCHERING CORPORATION

发明人： SHUE, Ho-Jane ,  SHIH, Neng-Yang ,  BLYTHIN, David, J. ,  CHEN, Xiao ,  TOM, Wing, C. ,  PIWINSKI, John, J. ,  MCCORMICK, Kevin, D.

IPC分类号： C07D487 ,  A61K31 ,  A61P1 ,  A61P9 ,  A61P11 ,  A61P13 ,  A61P15 ,  A61P25 ,  A61P27 ,  A61P29 ,  A61P37 ,  A61P43 ,  C07D401 ,  C07D403 ,  C07D405 ,  C07D409 ,  C07D453

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D453/02 ,  C07D487/04 ,  C07D487/10

摘要： The invention relates to compounds of formula (I). These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.

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：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：EP0823896B1

公开(公告)日：2001-07-11

申请号：EP96915341.0

申请日：1996-05-01

申请人： SCHERING CORPORATION

发明人： REICHARD, Gregory, A. ,  ASLANIAN, Robert, G. ,  ALAIMO, Cheryl, L. ,  KIRKUP, Michael, P. ,  LUPO, Andrew ,  MANGIARACINA, Pietro ,  MCCORMICK, Kevin, D. ,  PIWINSKI, John, J. ,  SHANKAR, Bandarpalle ,  SHIH, Neng-Yang ,  SPITLER, James, M. ,  TING, Pauline, C. ,  GANGULY, Ashit ,  CARRUTHERS, Nicholas, I.

IPC分类号： C07D211/52 ,  C07D211/58 ,  C07D211/76 ,  C07D295/12 ,  C07D295/18 ,  C07D401/04 ,  C07D417/12 ,  C07D413/14 ,  C07D413/12 ,  A61K31/445

CPC分类号： C07D295/185 ,  C07D211/52 ,  C07D211/58 ,  C07D211/76 ,  C07D295/13 ,  C07D333/22 ,  C07D401/04 ,  C07D401/06 ,  C07D409/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

公开(公告)号：EP0850236A1

公开(公告)日：1998-07-01

申请号：EP96931188.0

申请日：1996-08-29

申请人： SCHERING CORPORATION

发明人： SHUE, Ho-Jane ,  SHIH, Neng-Yang ,  BLYTHIN, David, J. ,  CHEN, Xiao ,  PIWINSKI, John, J. ,  MCCORMICK, Kevin, D.

IPC分类号： C07D487 ,  A61K31 ,  A61P1 ,  A61P9 ,  A61P11 ,  A61P13 ,  A61P15 ,  A61P25 ,  A61P27 ,  A61P29 ,  A61P37 ,  A61P43 ,  C07D241 ,  C07D401 ,  C07D403 ,  C07D405 ,  C07D409 ,  C07D413 ,  C07D417 ,  C07D453 ,  C07D471

CPC分类号： C07D241/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D453/02 ,  C07D487/04

摘要： The invention relates to compounds of formula (I) wherein Z, Rc, y, m, u, Ar2, n, X, Rc',(I) and Ar2 are as described herein. These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.