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：EP1601669B1

公开(公告)日：2008-12-24

申请号：EP04716913.1

申请日：2004-03-03

申请人： Schering Corporation

发明人： BURNETT, Duane, A. ,  CLADER, John, W.

IPC分类号： C07D405/12 ,  C07D405/14 ,  A61K31/397 ,  A61P3/06

CPC分类号： C07D405/12 ,  C07D405/14 ,  Y10S930/28

摘要： The present invention provides substituted azetidinone compounds of formula (I), formulations and processes for preparing the same which can be useful for treating vascular conditions such as atherosclerosis or hypercholesterolemia, diabetes, obesity, stroke, demyelination and lowering plasma levels of sterols and/or stanols in a subject.

公开(公告)号：EP1532147B1

公开(公告)日：2006-08-02

申请号：EP03762050.7

申请日：2003-06-26

申请人： SCHERING CORPORATION

发明人： BURNETT, Duane, A. ,  WU, Wen-Lian ,  SASIKUMAR, Thavalakulam, K. ,  DOMALSKI, Martin, S.

IPC分类号： C07D471/10 ,  A61K31/438 ,  A61P3/04

CPC分类号： C07D471/10

摘要： The present invention discloses compounds according to formula 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：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：EP1601669A1

公开(公告)日：2005-12-07

申请号：EP04716913.1

申请日：2004-03-03

申请人： SCHERING CORPORATION

发明人： BURNETT, Duane, A. ,  CLADER, John, W.

IPC分类号： C07D405/12 ,  C07D405/14 ,  A61K31/397 ,  A61P3/06

CPC分类号： C07D405/12 ,  C07D405/14 ,  Y10S930/28

摘要： The present invention provides substituted azetidinone compounds of formula (I), formulations and processes for preparing the same which can be useful for treating vascular conditions such as atherosclerosis or hypercholesterolemia, diabetes, obesity, stroke, demyelination and lowering plasma levels of sterols and/or stanols in a subject.

摘要翻译： 本发明提供了式（I）的取代的氮杂环丁酮化合物，制备该制剂的制剂和方法，其可用于治疗血管疾病如动脉粥样硬化或高胆固醇血症，糖尿病，肥胖症，中风，脱髓鞘和降低甾醇的血浆水平和/或 一个科目中的stanols。

公开(公告)号：EP0720599B1

公开(公告)日：1999-05-19

申请号：EP94928563.9

申请日：1994-09-14

申请人： SCHERING CORPORATION

发明人： ROSENBLUM, Stuart, B. ,  DUGAR, Sundeep ,  BURNETT, Duane, A. ,  CLADER, John, W. ,  MCKITTRICK, Brian, A.

IPC分类号： C07D205/08 ,  A61K31/395

CPC分类号： C07D205/08 ,  A61K9/2018 ,  A61K9/4858 ,  A61K31/21 ,  A61K31/35 ,  A61K31/395 ,  A61K31/40 ,  A61K45/06 ,  Y02P20/55 ,  Y10S514/824 ,  A61K2300/00

摘要： Hydroxy-substd. azetidinone derivs. of formula (I) and their salts are new. Ar1,Ar2 = aryl (opt. substd. by 1-5 gps. R4); Ar3 = aryl (opt. substd. by 1-5 gps. R5); X, Y, Z = CH2, CH(1-6C alkyl) or C(di(1-6C alkyl); R, R2 = OR6, OCOR6, OCOOR9 or OCONR6R7; R1, R3 = H, 1-6C alkyl or aryl; q, r = 0 or 1; m, n, p = 0-4, provided that i) at least one of q and r is 1, and the sum of m, n q and r is 1-6, and ii) when p is 0 and r is 1, the sum of m, q and n is 1-5; R4 = 1-6C alkyl, OR6, OCOR6, OCOR9, O(CH2)sOR6, OCONR6R7, NR6R7, NR6COR7, NR6COOR9, NR9, NR6CONR7R8, NR6CONR7R8, NR6SO2R9, COOR6, CONR6R7, COR6, SO2NR6R7, S(O)tR9, O(CH2)uCOOR6, O(CH2)uCONR6R7, lower alkylCOOR6, CH=CH-COOR6, CF3, CN, NO2 or halogen; R5 = OR6, OCOR6, O(CO)R9, O(CH2)vOR6, -O(CO)NR6R7, NR6R7, NR6COR7, NR6COOR9, NR6COOR9, NR6CONR7R8, NR6SO2R9, COOR6, CONR6R7, COR6, SO2NR6R7, S(O)tR9, -O(CH2)uCOOR6, O(CH2)uCONR6R7, lower alkylCOOR6 or -CH=CH-COOR6; s = 1-5; t = 0-2; u = 1-10; v = 1-5; R6, R7, R8 = H, 1-6C alkyl (opt.substd. with aryl) or aryl; and R9 = 1-6C alkyl (opt. substd. with aryl) or aryl.

公开(公告)号：EP0596015A1

公开(公告)日：1994-05-11

申请号：EP92916790.0

申请日：1992-07-21

申请人： SCHERING CORPORATION

发明人： BURNETT, Duane, A. ,  CLADER, John, W. ,  THIRUVENGADAM, Tiruvettipuram, K. ,  TANN, Chou-Hong ,  LEE, Junning ,  MC ALLISTER, Timothy ,  COLON, Cesar ,  BARTON, Derek, H., R. ,  BRESLOW, Ronald ,  DUGAR, Sundeep ,  VACCARO, Wayne

IPC分类号： A61K31 ,  A61P3 ,  A61P9 ,  C07D205 ,  C07D401 ,  C07D403 ,  C07D405 ,  C07D409 ,  C07D413 ,  C07F7

CPC分类号： C07D401/04 ,  C07D205/08 ,  C07D205/085 ,  C07D403/04 ,  C07D405/04 ,  C07D405/10 ,  C07D409/04 ,  C07F7/0812 ,  C07F7/186 ,  C07F7/1892

摘要： Nouveaux composés de la formule (I), où A représente -CH=CH-B; -C=CB; -(CH2)pXB, où p vaut entre 0 et 2 et X représente une liaison, -NH-, ou -S(O)0-2-; hétéroaryle éventuellement substitué ou hétéroaryle à fusion benzoïque; -C(O)-B; ou (Ia), où k vaut entre 1 et 2; D représente B'-(CH2)mC(O)-, où m vaut entre1 et 5; B'-(CH2)q-, où q vaut entre 2 et 6; B'-(CH2)eZ-(CH2)r-, où Z représente -O-, -C(O)-, phénylène, -NR8- ou -S(O)0-2-, e vaut entre 0 et 5 et r vaut entre 1 et 5, pourvu que la somme de e et r soit comprise entre 1 et 6; B'-(alcénylène)-; B'-(alcadiénylène)-; B'-(CH2)tZ-(alcénylène), où t vaut entre 0 et 3, pourvu que la somme de t et du nombre d'atomes de carbone dans la chaîne alcénylène soit comprise entre 2 et 6; B'(CH2)fV-(CH2)g-, où V représente cycloalkylène, f vaut entre 1 et 5 et g vaut entre 0 et 5, pourvu que la somme de f et g soit comprise entre 1 et 6; B'-(CH2)tV-(alcénylène) ou B-(alcénylène)-V-(CH2)t-, pourvu que la somme de t et du nombre d'atomes de carbone dans la chaîne alcénylène soit comprise entre 2 et 6; B'-(CH2)aZ-(CH2)bV-(CH2)d-, où a, b et d valent entre 0 et 6, pourvu que la somme de a, b et d soit comprise entre 0 et 6; T-(CH2)s-, où T représente cycloalkyle et s vaut entre 1 et 6; naphtylméthyle ou hétéroarylméthyle éventuellement substitué; B représente phényle éventuellement substitué; B' représente naphtyle, hétéroaryle éventuellement substitué ou phényle éventuellement substitué; R représente hydrogène, fluoro, alkyle, alcényle, alcynyle ou B-(CH2)h-, où h vaut entre 0 et 3; R4 représente indanyle, benzofuranyle, tetrahydronaphtyle, pyridyle, pyrazinyle, pyrimidinyle, quinolyle ou phényle éventuellement substitué. On décrit également l'utilisation de ces composés comme agents d'hypocholestérolémie, ainsi que des composés de la formule (II), où R20 représente phényle éventuellement substitué, naphtyle éventuellement substitué, hétéroaryle éventuellement substitué ou hétéroaryle à fusion benzoïque éventuellement substitué, R21, R22 et R23 sont indépendamment

公开(公告)号：EP2061792A2

公开(公告)日：2009-05-27

申请号：EP07838185.2

申请日：2007-09-13

申请人： Schering Corporation

发明人： ASLANIAN, Robert, G. ,  BENNETT, Chad, E. ,  BURNETT, Duane, A. ,  CHAN, Tin-Yau ,  KISELGOF, Eugenia, Y. ,  KNUTSON, Chad, E. ,  HARRIS, Joel, M. ,  MC KITTRICK, Brian, A. ,  PALANI, Anandan ,  SMITH, Elizabeth, M. ,  VACCARO, Henry, M. ,  XIAO, Dong ,  KIM, Hyunjin, M.

IPC分类号： C07D471/10 ,  A61K31/438 ,  A61P3/00

CPC分类号： C07D471/10

摘要： The present invention relates to Azetidinone Derivatives, compositions comprising an Azetidinone Derivative and methods for treating or preventing a disorder of lipid metabolism, pain, diabetes, a vascular condition, demyelination or nonalcoholic fatty liver disease, comprising administering to a patient an effective amount of an Azetidinone Derivative.

公开(公告)号：EP1928885A1

公开(公告)日：2008-06-11

申请号：EP06801600.5

申请日：2006-10-16

申请人： Schering Corporation

发明人： BENNETT, Chad, E. ,  GREENLEE, William, J. ,  KNUTSON, Chad, E. ,  BURNETT, Duane, A.

IPC分类号： C07D495/14 ,  A61P25/00 ,  A61P13/00 ,  A61P25/06 ,  A61P25/22 ,  A61P25/04

CPC分类号： C07D487/22 ,  C07D495/14

摘要： In its many embodiments, the present invention provides tricyclic compounds of formula (I) (wherein J1-J3, X, Z, and R1, R3, and R4 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.