公开(公告)号：EP2389369A1

公开(公告)日：2011-11-30

申请号：EP10704242.6

申请日：2010-01-21

申请人： Schering Corporation

发明人： JOSIEN, Hubert, B. ,  CLADER, John, W. ,  STAMFORD, Andrew ,  GREENLEE, William, J. ,  MAYER, Michael, John ,  DAVIS, Jason, L. ,  HSIA, Ming Min ,  WAN, Shuangyi

IPC分类号： C07D277/34 ,  C07D417/04 ,  A61K31/426 ,  A61K31/427 ,  A61P3/00

CPC分类号： C07D417/04 ,  C07D277/34

摘要： This invention provides for certain pentafluorosulpholane-containing compounds of the formula or a pharmaceutically acceptable salt, ester, solvate or prodrug thereof, wherein the variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.

公开(公告)号：EP1492765B1

公开(公告)日：2011-07-06

申请号：EP02759233.6

申请日：2002-08-01

申请人： Schering Corporation

发明人： ASBEROM, Theodros ,  GUZIK, Henry, S. ,  JOSIEN, Hubert, B. ,  PISSARNITSKI, Dmitri, A.

IPC分类号： C07D201/00

CPC分类号： C07D231/12 ,  C07D215/58 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D471/04 ,  C07D487/04

摘要： This invention discloses novel gamma secretase inhibitors of the formula:(Chemical formula should be inserted here as it appears on abstract in paper form)wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, -X(CO)Y, -(CR32)1-4X(CO)Y; each R3A is independently H or alkyl; X is -O-, -NH, or -N-alkyl; and Y is -NR6R7, or -N(R3)(CH2)2-6NR6R7. Also disclosed is a method of treating Alzheimer s Disease.

公开(公告)号：EP1663975A1

公开(公告)日：2006-06-07

申请号：EP04784148.1

申请日：2004-09-15

申请人： SCHERING CORPORATION ,  Pharmacopeia Drug Discovery, Inc.

发明人： PISSARNITSKI, Dmitri, A. ,  JOSIEN, Hubert, B. ,  SMITH, Elizabeth, M. ,  CLADER, John, W. ,  ASBEROM, Theodros ,  GUO, Tao ,  HOBBS, Douglas, W.

IPC分类号： C07D211/96 ,  C07D401/12 ,  C07D409/12 ,  C07D207/48 ,  C07D403/12 ,  A61K31/44 ,  A61P25/28

CPC分类号： C07D401/14 ,  C07D207/08 ,  C07D211/96 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D451/06 ,  C07D471/04 ,  C07D471/10 ,  C07D491/10

摘要： This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, -XC(O)Y, alkylene-XC(O)Y, cycloalkylene-X-C(O)-Y, -CH-X-C(O)-NR3-Y or -CH-X-C(O)-Y, wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.

公开(公告)号：EP1175401B1

公开(公告)日：2005-07-20

申请号：EP00926486.2

申请日：2000-05-01

申请人： SCHERING CORPORATION

发明人： BAROUDY, Bahige, M. ,  CLADER, John, W. ,  JOSIEN, Hubert, B. ,  MCCOMBIE, Stuart, W. ,  MCKITTRICK, Brian, A. ,  MILLER, Michael, W. ,  NEUSTADT, Bernard, R. ,  PALANI, Anandan ,  SMITH, Elizabeth, M. ,  STEENSMA, Ruo ,  TAGAT, Jayaram, R. ,  VICE, Susan, F. ,  LAUGHLIN, Mark, A. ,  GILBERT, Eric ,  LABROLI, Marc, A.

IPC分类号： C07D211/58 ,  C07D401/06 ,  C07D405/12 ,  C07D401/10 ,  C07D413/06 ,  C07D409/06 ,  A61K31/496 ,  A61P31/12 ,  A61P19/00

CPC分类号： C07D409/06 ,  A61K31/496 ,  C07D211/58 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D405/12 ,  C07D413/06

摘要： The use of CCR5 antagonists of formula (I) or a pharmaceutically acceptable salt thereof, wherein: R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R?4, R5 and R7¿ are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.

公开(公告)号：EP1370528B1

公开(公告)日：2005-06-08

申请号：EP02709850.8

申请日：2002-03-20

申请人： SCHERING CORPORATION

发明人： CLADER, John, W. ,  JOSIEN, Hubert, B. ,  PALANI, Anandan ,  CHAN, Tin-Yau

IPC分类号： C07D211/26 ,  A61K31/445 ,  C07D241/04 ,  A61P3/04

CPC分类号： C07D295/215 ,  A61K45/06 ,  C07D211/26 ,  C07D211/28 ,  C07D211/34 ,  C07D211/58 ,  C07D211/96 ,  C07D211/98 ,  C07D295/155 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14

摘要： The present invention discloses compounds of the formula (I) which are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

公开(公告)号：EP2435416A2

公开(公告)日：2012-04-04

申请号：EP08768856.0

申请日：2008-07-01

申请人： Schering Corporation

发明人： WU, Wen-lian ,  BARA, Thomas, A. ,  BURNETT, Duane, A. ,  CLADER, John, W. ,  DOMALSKI, Martin S. ,  JIN, Yan ,  JOSIEN, Hubert, B. ,  LI, Hongmei ,  LIANG, Xian ,  PISSARNITSKI, Dmitri, A. ,  SASIKUMAR, Thavalakulamgara, K. ,  WONG, Jesse, K. ,  XU, Ruo ,  ZHAO, Zhiqiang ,  MCNAMARA, Paul

IPC分类号： C07D311/78 ,  C07D407/12 ,  C07D493/04 ,  A61K31/35 ,  A61K31/352 ,  A61P25/28

CPC分类号： C07D493/04 ,  C07D311/78 ,  C07D407/12

摘要： Disclosed are novel gamma secretase inhibitors of the formula. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease. Also disclosed are processes for preparing alkenes in one reaction step using a mixture of an aldehyde (or ketone) and an alkyl substituted with two electron withdrawing groups, and reacting the mixture with: (a) a sulfonyl halide (e.g., a sulfonyl chloride) and a basic tertiary amine, or, (b) a sulfonyl anhydride and a basic amine, or (c) an aryl-C(O)-halide and a basic tertiary amine, or (d) an aryl-C(O)-O-C(O)-aryl and a basic tertiary amine, or (e) an heteroaryl-C(O)-halide and a basic tertiary amine, or (f) a heteroaryl-C(O)-O-C(O)-heteroaryl and a basic tertiary amine.

摘要翻译： 公开了下式的新型γ分泌酶抑制剂。 还公开了抑制γ-分泌酶的方法，治疗神经退行性疾病的方法以及治疗阿尔茨海默氏病的方法。 还公开了使用醛（或酮）和被两个吸电子基团取代的烷基的混合物在一个反应​​步骤中制备烯烃的方法，并使该混合物与以下物质反应：（a）磺酰卤（例如磺酰氯） （b）磺酰基酸酐和碱性胺，或（c）芳基-C（O） - 卤化物和碱性叔胺，或（d）芳基-C（O） - OC（O） - 芳基和碱性叔胺，或（e）杂芳基-C（O） - 卤化物和碱性叔胺，或（f）杂芳基-C（O）-OC（O） - 杂芳基和 一种碱性叔胺。

公开(公告)号：EP2389368A1

公开(公告)日：2011-11-30

申请号：EP10703379.7

申请日：2010-01-21

申请人： Schering Corporation

发明人： JOSIEN, Hubert, B. ,  CLADER, John, W. ,  GREENLEE, William, J. ,  MAYER, Michael, John ,  DAVIS, Jason, L. ,  WAN, Shuangyi

IPC分类号： C07D263/44 ,  C07D277/34 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  A61K31/421 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/502 ,  A61P3/10

CPC分类号： C07D417/14 ,  C07D263/44 ,  C07D277/34 ,  C07D417/04 ,  C07D417/12

摘要： This invention provides for certain bridged and fused compounds of the formula G-L-AI or a pharmaceutically acceptable salt, ester of solvate thereof wherein: A is and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.

公开(公告)号：EP2389226A1

公开(公告)日：2011-11-30

申请号：EP10703543.8

申请日：2010-01-21

申请人： Schering Corporation

发明人： JOSIEN, Hubert, B. ,  CLADER, John, W. ,  GREENLEE, William, J. ,  MAYER, Michael, John ,  HERR, Robert, Jason ,  DAVIS, Jason, L. ,  DENG, Kai ,  HSIA, Ming Min ,  WAN, Shuangyi

IPC分类号： A61P3/10 ,  A61K31/435 ,  A61K31/427 ,  C07D417/12 ,  C07D417/14 ,  C07D215/233 ,  C07D217/24

CPC分类号： C07D417/12 ,  C07D215/233 ,  C07D417/14

摘要： This invention provides for certain bridged and fused heterocyclic compounds of the formula ( I ) or a pharmaceutically acceptable salt, ester solvate or prodrug thereof wherein: L is: ( II ) and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.

公开(公告)号：EP2185522A1

公开(公告)日：2010-05-19

申请号：EP08795013.5

申请日：2008-08-04

申请人： Schering Corporation

发明人： ZHU, Zhaoning ,  GREENLEE, William, J. ,  CALDWELL, John, P. ,  MAZZOLA, Robert, D. ,  MCKITTRICK, Brian ,  BENNETT, Chad, E. ,  HUANG, Xianhai ,  JOSIEN, Hubert, B. ,  BURNETT, Duane, A.

IPC分类号： C07D217/24 ,  C07D487/04 ,  C07D498/04

CPC分类号： C07D487/04 ,  C07D217/24 ,  C07D498/04

摘要： In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, 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 diseases associated with the central nervous system using such compounds or pharmaceutical compositions.

摘要翻译： 在其许多实施方案中，本发明提供了一类作为γ分泌酶调节剂的新型杂环化合物，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的药物制剂的方法以及方法 使用这些化合物或药物组合物治疗，预防，抑制或改善一种或多种与中枢神经系统有关的疾病。

公开(公告)号：EP1976843A2

公开(公告)日：2008-10-08

申请号：EP07716750.0

申请日：2007-01-18

申请人： Schering Corporation

发明人： ASBEROM, Theodros ,  BARA, Thomas ,  BENNETT, Chad, E. ,  BURNETT, Duane, A. ,  CAPLEN, Mary Ann ,  CLADER, John, W. ,  COLE, David, J. ,  DOMALSKI, Martin, S. ,  JOSIEN, Hubert, B. ,  KNUTSON, Chad, E. ,  LI, Hongmei ,  MCBRIAR, Mark, D. ,  PISSARNITSKI, Dmitri, A. ,  QIANG, Li ,  RAJAGOPALAN, Murali ,  SASIKUMAR, Thavalakulamgar, K. ,  SU, Jing ,  TANG, Haiqun ,  WU, Wen-Lian ,  XU, Ruo ,  ZHAO, Zhiqiang

IPC分类号： C07D311/22 ,  C07D311/80 ,  C07D311/92 ,  C07D311/94 ,  C07D313/08 ,  C07D335/06

CPC分类号： C07D311/22 ,  C07C317/14 ,  C07C317/20 ,  C07C317/44 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2602/12 ,  C07D311/80 ,  C07D311/92 ,  C07D311/94 ,  C07D313/08 ,  C07D335/06 ,  C07D405/12 ,  C07D409/12 ,  C07D491/04 ,  C07D493/04

摘要： This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.