公开(公告)号：EP0938483B1

公开(公告)日：2003-02-26

申请号：EP97936296.9

申请日：1997-08-06

申请人： SCHERING CORPORATION

发明人： LOWE, Derek, B. ,  CHANG, Wei, K. ,  KOZLOWSKI, Joseph, A. ,  BERGER, Joel, G. ,  McQUADE, Robert ,  BARNETT, Allen ,  SHERLOCK, Margaret ,  TOM, Wing ,  DUGAR, Sundeep ,  CHEN, Lian-Yong ,  CLADER, John, W. ,  CHACKALAMANNIL, Samuel ,  WANG, Yuguang ,  McCOMBIE, Stuart, W. ,  TAGAT, Jayaram, R. ,  VICE, Susan, F. ,  VACCARO, Wayne, D. ,  GREEN, Michael, J. ,  BROWNE, Margaret, E. ,  BOYLE, Craig, D. ,  JOSIEN, Hubert, B. ,  ASBEROM, Theodros

IPC分类号： C07D405/00 ,  A61K31/00

CPC分类号： C07D405/14 ,  C07C2601/14 ,  C07D211/24 ,  C07D211/32 ,  C07D239/34 ,  C07D257/04 ,  C07D295/03 ,  C07D295/088 ,  C07D295/092 ,  C07D295/096 ,  C07D295/112 ,  C07D295/116 ,  C07D295/125 ,  C07D295/13 ,  C07D295/135 ,  C07D295/145 ,  C07D295/15 ,  C07D405/12 ,  C07D409/14

摘要： Di-N-substituted piperazine or 1,4 di-substituted piperidine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) wherein R, R?1, R2, R3, R4, R21, R27, R28¿, X, Y and Z as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula with acetylcholinesterase inhibitors.

摘要翻译： 根据式I的二-N-取代哌嗪或1,4-二取代哌啶化合物（包括所有异构体，盐，酯和溶剂合物），其中R，R 1，R 2，R 3，R 4，R 21，R 27，R 28，X ，Y和Z如本文所定义的是可用于治疗认知障碍如阿尔茨海默氏病的毒蕈碱拮抗剂。 还公开了药物组合物和制备方法。 还公开了上式化合物与乙酰胆碱酯酶抑制剂的协同组合。

公开(公告)号：EP0912534B1

公开(公告)日：2002-09-25

申请号：EP97931281.6

申请日：1997-06-26

申请人： SCHERING CORPORATION

发明人： KOZLOWSKI, Joseph, A. ,  LOWE, Derek, B. ,  CHANG, Wei, K. ,  DUGAR, Sundeep

IPC分类号： C07D295/096 ,  C07D311/68 ,  C07D213/643 ,  C07D405/12 ,  A61K31/495 ,  A61K31/44 ,  A61K31/35

CPC分类号： C07D317/62 ,  C07B2200/07 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2602/12 ,  C07D211/58 ,  C07D239/34 ,  C07D295/088 ,  C07D295/096 ,  C07D311/68 ,  C07D317/58

摘要： Di-N-substituted piperazine or 1,4-di-substituted piperidine compounds in accordance with formula (I) (including all isomers, salts, esters, and solvates), wherein Q, n, R, R?1, R2, R3, R4, R21, R27, R28¿, X, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations with acetylcholinesterase inhibitors of compounds capable of enhancing acetylcholine release and having the above formula.

摘要翻译： 根据式（I）的二-N-取代哌嗪或1,4-二取代哌啶化合物（包括所有异构体，盐，酯和溶剂合物），其中Q，n，R，R 1， R 2，R 3，R 4，R 21，R 27，R 28，X和Z如本文所定义，是可用于治疗认知障碍如阿尔茨海默氏病的毒蕈碱性拮抗剂。 还公开了药物组合物和制备方法。 还公开了与能够增强乙酰胆碱释放并具有上式的化合物的乙酰胆碱酯酶抑制剂的协同组合。

公开(公告)号：EP2435424A1

公开(公告)日：2012-04-04

申请号：EP10721906.5

申请日：2010-05-28

申请人： Schering Corporation

发明人： ZENG, Qingbei ,  CHEN, Kevin, X. ,  ANILKUMAR, Gopinadhan, N. ,  ROSENBLUM, Stuart, B. ,  KOZLOWSKI, Joseph, A. ,  NJOROGE, F., George

IPC分类号： C07D403/14 ,  A61P31/12 ,  A61K31/4184

CPC分类号： C07D403/14

摘要： The present invention relates to novel Linked Tricyclic Aryl Compounds, compositions comprising at least one Linked Tricyclic Compound, and methods of using Linked Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient. in one aspect, the present invention provides Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein: Non-limiting examples of the Compounds of Formula (II) include compound 56

公开(公告)号：EP2355825A2

公开(公告)日：2011-08-17

申请号：EP09752068.8

申请日：2009-11-09

申请人： Schering Corporation

发明人： TONG, Ling ,  LAVEY, Brian, J. ,  SHANKAR, Bandarpalle, B. ,  KIM, Seong-Heon ,  YU, Wensheng ,  KOZLOWSKI, Joseph, A. ,  WONG, Michael, K.C. ,  CHEN, Lei ,  ZHOU, Guowei ,  RIZVI, Razia, K. ,  FELTZ, Robert ,  KOSINSKI, Aneta, Maria ,  YANG, De-Yi ,  DAI, Chaoyang ,  FIRE, Luke ,  GIRIJAVALLABHAN, Vinay, M. ,  LI, Dansu ,  POPOVICI-MULLER, Janeta ,  RICHARD, Judson, E. ,  ROSNER, Kristin, E. ,  SIDDIQUI, M., Arshad ,  YANG, Liping

IPC分类号： A61K31/4741

CPC分类号： C07D498/04 ,  C07D513/00 ,  C07D519/00

摘要： This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.

摘要翻译： 本发明涉及式（I）的化合物：（化学式应插入此处，如出现在纸上的摘要中）（I）或其药学上可接受的盐，其可用于治疗介导的疾病或病症 由MMPs，ADAMs，TACE，聚集蛋白聚糖酶，TNF-或其组合。

公开(公告)号：EP1778676B1

公开(公告)日：2010-08-25

申请号：EP05771446.1

申请日：2005-07-13

申请人： Schering Corporation

发明人： YU, Wensheng ,  TONG, Ling ,  CHEN, Lei ,  KOZLOWSKI, Joseph, A. ,  LAVEY, Brian, J. ,  SHIH, Neng-Yang ,  MADISON, Vincent, S. ,  ZHOU, Guowei ,  ORTH, Peter ,  GUO, Zhuyan ,  WONG, Michael, K. C. ,  YANG, De-Yi ,  KIM, Seong, Heon ,  SHANKAR, Bandarpalle

IPC分类号： C07D403/06 ,  C07D417/14 ,  C07D401/14 ,  C07D409/14 ,  C07D413/14 ,  A61P43/00 ,  A61P29/00 ,  A61K31/4178

CPC分类号： C07D401/14 ,  C07D403/06 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

摘要： This invention relates to compounds of Formula (1) or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF- or combinations thereof.

公开(公告)号：EP1996577A1

公开(公告)日：2008-12-03

申请号：EP07753453.5

申请日：2007-03-19

申请人： Schering Corporation ,  PHARMACOPEIA, INC.

发明人： ROSENBLUM, Stuart, B. ,  KOZLOWSKI, Joseph, A. ,  SHIH, Neng-Yang ,  MCGUINNESS, Brian, F. ,  HOBBS, Douglas, W.

IPC分类号： C07D401/14 ,  C07D413/14 ,  A61K31/497 ,  A61P29/00 ,  A61P37/06

CPC分类号： C07D401/14 ,  C07D413/14

摘要： The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: or a pharmaceutically acceptable salt, solvate or ester thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, zenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.

公开(公告)号：EP1973901A1

公开(公告)日：2008-10-01

申请号：EP07716634.6

申请日：2007-01-16

申请人： Schering Corporation

发明人： LAVEY, Brian, J. ,  KOZLOWSKI, Joseph, A. ,  ZHOU, Guowei ,  TONG, Ling ,  YU, Wensheng ,  WONG, Michael, K.C. ,  SHANKAR, Bandarpalle, B. ,  SHIH, Neng-Yang ,  SIDDIQUI, M., Arshad ,  ROSNER, Kristin, E. ,  DAI, Chaoyang ,  POPOVICI-MULLER, Janeta ,  GIRIJAVALLABHAN, Vinay, M. ,  LI, Dansu ,  RIZVI, Razia ,  CHEN, Lei ,  YANG, De-yi ,  FELTZ, Robert ,  KIM, Seong-heon

IPC分类号： C07D403/14 ,  A61K31/4178 ,  A61P29/00

CPC分类号： C07D403/14 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D473/00

摘要： This invention relates to compounds of the Formula: (I); or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-α or combinations thereof.

公开(公告)号：EP1848710A2

公开(公告)日：2007-10-31

申请号：EP06735000.9

申请日：2006-02-14

申请人： Schering Corporation ,  PHARMACOPEIA, INC.

发明人： KIM, Seong, Heon ,  ANILKUMAR, Gopinadhan, N. ,  WONG, Michael, K. C. ,  ZENG, Qingbei ,  ROSENBLUM, Stuart, B. ,  KOZLOWSKI, Joseph, A. ,  SHAO, Yuefei ,  MC GUINNESS, Brian, F. ,  HOBBS, Douglas, W.

IPC分类号： C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  A61K31/445 ,  A61K31/495

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

摘要： The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1 or a pharmaceutically acceptable salt, solvate or ester thereof, wherein the various moieties are defined herein. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non limiting example(s) include, psoriasis), autoimmune diseases (non limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g , tuberculoid leprosy), fixed drug eruptions, cutaneous delayed type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.

公开(公告)号：EP1768667A1

公开(公告)日：2007-04-04

申请号：EP05766578.8

申请日：2005-06-21

申请人： SCHERING CORPORATION

发明人： SHANKAR, Bandarpalle, B. ,  GILBERT, Eric ,  RIZVI, Razia, K. ,  HUANG, Chunli ,  KOZLOWSKI, Joseph, A. ,  MCCOMBIE, Stuart ,  SHIH, Neng-Yang

IPC分类号： A61K31/438 ,  C07D209/52 ,  C07D221/20 ,  C07D401/12 ,  C07D471/08 ,  A61P29/00

CPC分类号： C07D221/20 ,  C07D209/52 ,  C07D401/12 ,  C07D471/08

摘要： Compounds of Formula (I) and/or pharmaceutically acceptable salts, solvates or prodrugs thereof, or pharmaceutical compositions containing such compounds exhibit anti-inflammatory and immunomodulatory activity, and can be effective asCB2 receptor ligands in treating cancer and inflammatory, immunomodulatory or respiratory diseases or conditions.

公开(公告)号：EP1565431A1

公开(公告)日：2005-08-24

申请号：EP03789933.3

申请日：2003-11-21

申请人： SCHERING CORPORATION

发明人： TONG, Ling ,  CHEN, Lei ,  SHANKAR, Bandarpalle, B. ,  KOZLOWSKI, Joseph, A. ,  SHIH, Neng-Yang

IPC分类号： C07C317/32 ,  C07C323/49 ,  C07C323/31 ,  C07C323/41 ,  C07D213/70 ,  C07D401/12 ,  A61K31/10 ,  A61P11/00 ,  A61P35/00 ,  A61P29/00 ,  A61P37/00

CPC分类号： C07D401/12 ,  C07C317/32 ,  C07C323/31 ,  C07C323/41 ,  C07C323/49 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2602/08 ,  C07D213/71

摘要： A compound of the formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein:R1, R2, L1, L2, M1, M2, n, p, q, A, D, X, Y and Z are as described in the specification; pharmaceutical compositions thereof, methods of making said pharmaceutical compositions; and methods of use thereof.