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：EP2268636A1

公开(公告)日：2011-01-05

申请号：EP08858841.3

申请日：2008-12-09

申请人： Schering Corporation

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

IPC分类号： C07D455/02 ,  A61K31/4375 ,  A61P25/00 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

CPC分类号： C07D455/02

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).

摘要翻译： 本发明提供了γ分泌酶调节剂的新化合物。 该化合物具有式（I）。 还公开了使用式（I）化合物调节γ分泌酶活性的方法和治疗阿尔茨海默病的方法。

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：EP2257542A1

公开(公告)日：2010-12-08

申请号：EP09715421.5

申请日：2009-02-26

申请人： Schering Corporation

发明人： HUANG, Xianhai ,  PALANI, Anandan ,  ASLANIAN, Robert, G. ,  ZHU, Zhaoning ,  PISSARNITSKI, Dmitri, A. ,  LI, Hongmei ,  GREENLEE, William, J. ,  ZHAO, Zhiqiang ,  MAZZOLA, JR., Robert, D. ,  QIN, Jun ,  DHONDI, Pawan

IPC分类号： C07D401/12 ,  C07D498/20 ,  A61K31/445 ,  A61P25/28

CPC分类号： C07D401/12 ,  C07D498/20

摘要： This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula: 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：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：EP2136805A2

公开(公告)日：2009-12-30

申请号：EP08714243.6

申请日：2008-02-27

申请人： Schering Corporation

发明人： ASLANIAN, Robert, G. ,  LACHOWICZ, Jean, E. ,  BERLIN, Michael, Y. ,  HWA, Joyce, J.

IPC分类号： A61K31/4545 ,  A61P3/10 ,  A61P3/00 ,  A61P3/08 ,  A61P25/04 ,  A61P25/06 ,  A61P29/00 ,  A61P29/02

CPC分类号： A61K31/4545 ,  A61K45/06 ,  A61K2300/00

摘要： The present invention relates to Compounds of Formula (I), compositions comprising the compounds, and methods of using the compounds to treat or prevent pain, diabetes, a diabetic complication, impaired glucose tolerance (IGT) or impaired fasting glucose (IFG) in a patient.

公开(公告)号：EP1326858B1

公开(公告)日：2005-12-14

申请号：EP01983968.7

申请日：2001-10-15

申请人： SCHERING CORPORATION

发明人： ASLANIAN, Robert, G. ,  SHIH, Neng-Yang ,  TING, Pauline, C. ,  BERLIN, Michael, Y. ,  ROSENBLUM, Stuart, B. ,  MC CORMICK, Kevin, D. ,  TOM, Wing, C. ,  BOYCE, Christopher, W. ,  MANGIARACINA, Pietro ,  MUTAHI, Mwangi, Wa ,  PIWINSKI, John, J.

IPC分类号： C07D401/14 ,  C07D413/14 ,  C07D401/12 ,  C07D409/14 ,  C07D498/04 ,  C07D417/14

CPC分类号： C07D213/73 ,  A61K31/435 ,  A61K31/445 ,  A61K31/495 ,  C07D401/12 ,  C07D401/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D498/04

公开(公告)号：EP1539742A1

公开(公告)日：2005-06-15

申请号：EP03761216.5

申请日：2003-06-20

申请人： SCHERING CORPORATION

发明人： ASLANIAN, Robert, G. ,  BERLIN, Michael, Y. ,  MANGIARACINA, Pietro ,  MC CORMICK, Kevin, D. ,  MUTAHI, Mwangi, W. ,  ROSENBLUM, Stuart, B.

IPC分类号： C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04 ,  A61K31/445 ,  A61P25/06 ,  A61P25/18 ,  A61P25/28 ,  A61P25/20 ,  A61P27/14

CPC分类号： C07D405/14 ,  C07D401/14 ,  C07D409/14 ,  C07D471/04

摘要： Disclosed are novel compounds of the formula I wherein M1 is CH or N and M2 is C(R3) or N; R1 is optionally substituted indolyl or an aza derivative thereof; R2 is optionally substituted aryl or heteroaryl; and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of formula I in combination with a H1 receptor antagonist.

公开(公告)号：EP1499316A1

公开(公告)日：2005-01-26

申请号：EP03719766.2

申请日：2003-04-16

申请人： SCHERING CORPORATION

发明人： ZENG, Qingbei ,  ASLANIAN, Robert, G. ,  BERLIN, Michael, Y. ,  BOYCE, Christopher, W. ,  CAO, Jianhua ,  KOZLOWSKI, Joseph, A. ,  MANGIARACINA, Pietro ,  MC CORMICK, Kevin, D. ,  MUTAHI, Mwangi, W. ,  ROSENBLUM, Stuart, B. ,  SHIH, Neng-Yang ,  SOLOMON, Daniel, M. ,  TOM, Wing, C.

IPC分类号： A61K31/4545 ,  C07D471/04 ,  C07D401/14 ,  A61K31/4184 ,  A61P37/08

CPC分类号： C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

摘要： Disclosed are histamine H3 antagonists of the formula (I) wherein R1 is optionally substituted benzimidazolyl or a derivative thereof; R2 is optionally substitutd aryl or heteroaryl; M1 and M2 are C(R3) or N; Q is -N(R8)-, -S- or -O-; and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating various diseases or conditions, such as allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of formula I. Also disclosed are methods of treating said diseases or conditions using the compounds of formula I in combination with an H1 receptor antagonist.

公开(公告)号：EP1373251A2

公开(公告)日：2004-01-02

申请号：EP02709808.6

申请日：2002-03-11

申请人： Schering Corporation ,  PHARMACOPEIA, INC.

发明人： ROSENBLUM, Stuart, B. ,  ZENG, Qingbei ,  MUTAHI, Mwangi, Wa ,  ASLANIAN, Robert, G. ,  TING, Pauline, C. ,  SHIH, Neng-Yang ,  SOLOMON, Daniel, M. ,  CAO, Jianhua ,  VACCARO, Henry, A. ,  MC CORMICK, Kevin, D. ,  BALDWIN, John, J. ,  LI, Ge

IPC分类号： C07D401/14

CPC分类号： C07D401/14 ,  C07D211/26 ,  C07D211/38 ,  C07D211/62 ,  C07D211/96 ,  C07D243/08 ,  C07D401/06 ,  C07D407/12 ,  C07D407/14 ,  C07D409/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14 ,  C07D451/02 ,  C07D487/06

摘要： Disclosed are novel compounds of the formula (I). Also disclosed are pharmaceutical compositions comprising the compounds of Formula (I). Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula (I). Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula (I) in combination with a H1 receptor antagonist.