公开(公告)号：EP1667679B1

公开(公告)日：2009-06-03

申请号：EP04789487.8

申请日：2004-09-30

申请人： Schering Corporation

发明人： SASIKUMAR, Thavalakulamgara, K. ,  BURNETT, Duane, A.

IPC分类号： A61K31/4184 ,  C07D235/30 ,  C07D403/12 ,  A61P3/04

CPC分类号： C04B35/632 ,  C07D235/30 ,  C07D401/12 ,  C07D403/12

摘要： The present invention discloses compounds of formula I formula I wherein Ar, Z, m, n, p, R1 and R8 are herein defined, said compounds being 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：EP2178882A1

公开(公告)日：2010-04-28

申请号：EP08794506.9

申请日：2008-07-15

申请人： Schering Corporation

发明人： SASIKUMAR, Thavalakulamgara, K. ,  BURNETT, Duane, A. ,  ASBEROM, Theodros ,  WU, Wen-Lian ,  LI, Hongmei ,  XU, Ruo ,  JOSIEN, Hubert, B.

IPC分类号： C07D491/04 ,  C07D493/04 ,  C07D513/04 ,  C07D513/14 ,  A61K31/542 ,  A61K31/54 ,  A61K31/519 ,  A61K31/35

CPC分类号： C07D493/04 ,  C07D491/04 ,  C07D513/04 ,  C07D513/14

摘要： Disclosed are novel gamma secretase inhibitors of the formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, wherein L1, n, X, Ar, Y, Z, Q, and Q1 are as defined herein. Also disclosed are methods for inhibiting gamma secretase, methods for treating Azheimer's disease, methods of treating one or more neurodegenerative diseases, and methods of inhibiting the deposition of amyloid protein (e.g., amyloid beta protein) in, on or around neurological tissue (e.g., the brain) using the compounds of formula 1.0.

公开(公告)号：EP1667679A1

公开(公告)日：2006-06-14

申请号：EP04789487.8

申请日：2004-09-30

申请人： SCHERING CORPORATION

发明人： SASIKUMAR, Thavalakulamgara, K. ,  BURNETT, Duane, A.

IPC分类号： A61K31/4184 ,  C07D235/30 ,  C07D403/12 ,  A61P3/04

CPC分类号： C04B35/632 ,  C07D235/30 ,  C07D401/12 ,  C07D403/12

摘要： The present invention discloses compounds of formula I formula I wherein Ar, Z, m, n, p, R1 and R8 are herein defined, said compounds being 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：EP1664022A1

公开(公告)日：2006-06-07

申请号：EP04782252.3

申请日：2004-08-26

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

发明人： BURNETT, Duane, A. ,  WU, Wen-Lian ,  SASIKUMAR, Thavalakulamgara, K. ,  GREENLEE, William, J. ,  CAPLEN, Mary, Ann ,  GUO, Tao ,  HUNTER, Rachael

IPC分类号： C07D401/12 ,  C07D401/06 ,  A61K31/454 ,  A61P3/04 ,  A61P3/10

CPC分类号： C04B35/632 ,  C07D401/06 ,  C07D401/12

摘要： The present invention discloses compounds of formula (I); wherein Ar, Y, m, n, R1 and R4 are herein defined, said compounds being 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：EP1664022B1

公开(公告)日：2011-06-15

申请号：EP04782252.3

申请日：2004-08-26

申请人： Schering Corporation ,  Pharmacopeia, LLC

发明人： BURNETT, Duane, A. ,  WU, Wen-Lian ,  SASIKUMAR, Thavalakulamgara, K. ,  GREENLEE, William, J. ,  CAPLEN, Mary, Ann ,  GUO, Tao ,  HUNTER, Rachael

IPC分类号： C07D401/12 ,  C07D401/06 ,  A61K31/454 ,  A61P3/04 ,  A61P3/10

CPC分类号： C04B35/632 ,  C07D401/06 ,  C07D401/12

摘要： The present invention discloses compounds of formula (I); wherein Ar, Y, m, n, R1 and R4 are herein defined, said compounds being 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：EP1601664B1

公开(公告)日：2008-04-30

申请号：EP04715072.7

申请日：2004-02-26

申请人： Schering Corporation

发明人： SASIKUMAR, Thavalakulamgara, K. ,  WU, Wen-Lian ,  BURNETT, Duane, A. ,  QIANG, Li

IPC分类号： C07D401/04 ,  A61K31/165 ,  C07D417/14 ,  C07D401/14

CPC分类号： C07D401/04 ,  A61K45/06 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14

摘要： The present invention discloses compounds which are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In other aspects, the invention is directed to 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. Compounds of the invention generally have the structure: F (1) where the substituents are as defined herein.

公开(公告)号：EP1765829A1

公开(公告)日：2007-03-28

申请号：EP05761566.8

申请日：2005-06-14

申请人： SCHERING CORPORATION

发明人： MATASI, Julius, J. ,  TULSHIAN, Deen ,  BURNETT, Duane, A. ,  WU, Wen-Lian ,  KORAKAS, Peter ,  SILVERMAN, Lisa, S. ,  SASIKUMAR, Thavalakulamgara, K. ,  QIANG, Li ,  DOMALSKI, Martin, S.

IPC分类号： C07D495/14 ,  C07D491/14 ,  C07D495/04 ,  C07D471/14 ,  A61K31/519 ,  A61P25/00 ,  C07D333/00 ,  C07D239/00 ,  C07D221/00 ,  C07D307/00

CPC分类号： C07D471/14 ,  C07D491/14 ,  C07D495/04 ,  C07D495/14 ,  C09B57/00

摘要： In its many embodiments, the present invention provides tricyclic compounds of Formula (I) (wherein J1-J4, X, and R1-R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.

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：EP1765829B1

公开(公告)日：2010-07-07

申请号：EP05761566.8

申请日：2005-06-14

申请人： Schering Corporation

发明人： MATASI, Julius, J. ,  TULSHIAN, Deen ,  BURNETT, Duane, A. ,  WU, Wen-Lian ,  KORAKAS, Peter ,  SILVERMAN, Lisa, S. ,  SASIKUMAR, Thavalakulamgara, K. ,  QIANG, Li ,  DOMALSKI, Martin, S.

IPC分类号： C07D495/14 ,  C07D491/14 ,  C07D495/04 ,  C07D471/14 ,  A61K31/519 ,  A61P25/00

CPC分类号： C07D471/14 ,  C07D491/14 ,  C07D495/04 ,  C07D495/14 ,  C09B57/00

摘要： In its many embodiments, the present invention provides tricyclic compounds of Formula (I) (wherein J1-J4, X, and R1-R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.

公开(公告)号：EP1773822B1

公开(公告)日：2009-06-17

申请号：EP05773671.2

申请日：2005-07-14

申请人： Schering Corporation

发明人： SU, Jing ,  MCKITTRICK, Brian ,  TANG, Haiqun ,  SASIKUMAR, Thavalakulamgara, K. ,  QIANG, Li

IPC分类号： C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D487/08

CPC分类号： C07D487/08 ,  C07D277/26 ,  C07D277/28 ,  C07D333/20 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14

摘要： The present invention discloses compounds of formula (I) wherein m, n, p, R1, R2 and X, are herein defined, said compounds being 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.