公开(公告)号：EP1660443B1

公开(公告)日：2009-03-04

申请号：EP04779938.2

申请日：2004-08-04

申请人： Schering Corporation ,  Pharmacopeia Drug Discovery, Inc.

发明人： CUMMING, Jared, N. ,  ISERLOH, Ulrich ,  STAMFORD, Andrew ,  STRICKLAND, Corey ,  VOIGT, Johannes, H. ,  WU, Yusheng ,  HUANG, Ying ,  XIA, Yan ,  CHACKALAMANNIL, Samuel ,  GUO, Tao ,  HOBBS, Douglas, W. ,  LE, Thuy, X., H. ,  LOWRIE, Jeffrey, F. ,  SAIONZ, Kurt, W. ,  BABU, Suresh, D.

IPC分类号： C07D201/00

CPC分类号： C07D243/08 ,  C07D205/04 ,  C07D207/08 ,  C07D207/09 ,  C07D207/12 ,  C07D207/26 ,  C07D209/52 ,  C07D211/26 ,  C07D211/46 ,  C07D217/18 ,  C07D233/32 ,  C07D241/04 ,  C07D241/08 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D409/06 ,  C07D409/12 ,  C07D413/06

摘要： Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R is-C(O)-N(R27 )(R28) or 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 cognitive or neurodegenerative diseases such as Alzheimer’s disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a β-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, and N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.

公开(公告)号：EP1999111A2

公开(公告)日：2008-12-10

申请号：EP07754070.6

申请日：2007-03-27

申请人： Schering Corporation

发明人： CHELLIAH, Mariappan, V. ,  CHACKALAMANNIL, Samuel ,  XIA, Yan

IPC分类号： C07D213/24 ,  A61K31/44 ,  A61P9/00 ,  A61P29/00

CPC分类号： C07D213/24 ,  C07D213/57 ,  C07D405/06

摘要： Monocyclic and bicyclic himbacine derivatives of the formula or a pharmaceutically acceptable salt or solvate of said compound wherein represents an optional double bond and wherein Gn, Jn, R3, R8, R9, R10, R11, R32, R33, B and Het are herein defined are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other agents is also claimed.

公开(公告)号：EP1937687A1

公开(公告)日：2008-07-02

申请号：EP06804036.9

申请日：2006-09-21

申请人： Schering Corporation

发明人： BOYLE, Craig, D. ,  CHACKALAMANNIL, Samuel ,  SHAH, Unmesh, G. ,  LACHOWICZ, Jean, E.

IPC分类号： C07D487/14 ,  A61K31/519 ,  A61P25/14 ,  A61P25/16

CPC分类号： C07D487/14

摘要： The compound having the structural formula I, or a pharmaceutically acceptable salt thereof, is disclosed, as well as its use in the treatment of central nervous system diseases, in particular Parkinson's disease, Extra Pyramidal Syndrome, restless legs syndrome and attention deficit hyperactivity disorder, pharmaceutical compositions comprising it, and combinations with other agents.

公开(公告)号：EP1745047A1

公开(公告)日：2007-01-24

申请号：EP05737774.9

申请日：2005-04-19

申请人： SCHERING CORPORATION

发明人： NEUSTADT, Bernard, R. ,  HAO, Jinsong ,  LIU, Hong ,  BOYLE, Craig, D. ,  CHACKALAMANNIL, Samuel ,  SHAH, Unmesh, G. ,  STAMFORD, Andrew ,  HARRIS, Joel, M.

IPC分类号： C07D487/14 ,  A61K31/505 ,  A61P25/28

CPC分类号： C07D487/14

摘要： Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, furanyl, thienyl, pyridyl, pyridyl N-oxide, oxazolyl or pyrrolyl, or cycloalkenyl R1, R2, R3, R4 and R5 are H, alkyl or alkoxyalkyl; and Z is optionally substituted aryl or heteroaryl are disclosed. Also disclosed is the use of compounds of formula I in the treatment of central nervous system diseases, in particular Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them.

公开(公告)号：EP1701953A1

公开(公告)日：2006-09-20

申请号：EP05705212.8

申请日：2005-01-07

申请人： SCHERING CORPORATION

发明人： THIRUVENGADAM, Tiruvettipuram, K. ,  WU, Wenxue ,  WANG, Tao ,  CHIU, John, S. ,  BOGDANOWICH-KNIPP, Susan ,  PAVLOVSKY, Anastasia ,  GREENLEE, William, J. ,  GRAZIANO, Michael, P. ,  KOSOGLOU, Teddy ,  CHINTALA, Madhu ,  CHACKALAMANNIL, Samuel

IPC分类号： C07D405/06 ,  C07D307/00 ,  C07D213/00

CPC分类号： C07D417/14 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D405/06 ,  C07D405/14 ,  C07D413/14

摘要： A crystalline polymorph of a bislulfate salt of a thrombin receptor antagonist compound, which exhibits a powder x-ray diffraction profile substantially the same as that shown in FIG. 1, or which exhibits a differential scanning calorimtery profile substantially the same as that shown in FIG. 3, and is represented by the formula for Compound 2: Chemical formula should be inserted here as it appears on the abstract in paper form. and processes for preparing Compound 2 are disclosed. Pharmaceutical compositions comprising the polymorph of the bisulfate salt and at least one excipient or carrier, and methods of using the polymorph of Compound 2 to treat a variety of physiological disorders, such as thrombosis, are also disclosed.

公开(公告)号：EP1436298A1

公开(公告)日：2004-07-14

申请号：EP02801732.5

申请日：2002-10-16

申请人： SCHERING CORPORATION

发明人： CHACKALAMANNIL, Samuel ,  CHELLIAH, Mariappan, V. ,  CLASBY, Martin, C. ,  XIA, Yan

IPC分类号： C07D491/04 ,  A61K31/445 ,  A61K31/34 ,  A61P29/00 ,  A61P19/02 ,  A61P9/00

CPC分类号： C07D491/04 ,  C07D493/04 ,  C07D495/04

摘要： Heterocyclic-substituted tricyclics of the formula (I) or a pharmaceutically acceptable salts thereof, wherein: n1 and n2 are independently 0-2; Het is an optionally substituted mono-, bi- or tricyclic heteroaromatic group; B is alkyl or optionally substituted alkenyl; R22 is -COR23 or a carboxy, sulfinyl, sulfonyl, sulfonamide or amino acid derivative; R23 is haloalkyl; alkenyl; haloalkenyl; alkynyl; optionally substituted cycloalkyl; cycloalkyl-alkyl; aryl; arylalkyl; heteroaryl; heterocycloalkyl; or -COOH and/or -SO¿3?H substituted alkyl; R?1, R2, R3, R9, R10 and R11¿ are as defined in the specification; are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds.

摘要翻译： 式（I）的杂环取代的三环或其药学上可接受的盐，其中：n1和n2独立地为0-2; Het是任选取代的单环，双环或三环杂芳族基团; B是烷基或任选取代的链烯基; R22是-COR23或羧基，亚磺酰基，磺酰基，磺酰胺或氨基酸衍生物; R23是卤代烷基; 烯基; 卤代链; 炔基; 任选取代的环烷基 环烷基 - 烷基; 芳基; 芳; 杂; 杂环; 或-COOH和/或-SO 3 H取代的烷基; R 1，R 2，R 3，R 9，R 10和R 11如说明书中所定义; 以及含有它们的药物组合物以及通过施用所述化合物治疗与血栓形成，动脉粥样硬化，再狭窄，高血压，心绞痛，心律失常，心力衰竭和癌症相关的疾病的方法。

公开(公告)号：EP1036072B1

公开(公告)日：2004-05-06

申请号：EP98958039.4

申请日：1998-11-23

申请人： SCHERING CORPORATION

发明人： CHACKALAMANNIL, Samuel ,  ASBEROM, Theodros ,  XIA, Yan ,  DOLLER, Dario ,  CLASBY, Martin, C. ,  CZARNIECKI, Michael, F.

IPC分类号： C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D405/12 ,  C07D417/06 ,  C07D401/06 ,  C07D491/04 ,  C07D471/04 ,  C07D493/10 ,  A61K31/44 ,  A61K31/47

CPC分类号： C07D401/06 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D417/06 ,  C07D471/04 ,  C07D491/04 ,  C07D493/10

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：EP1283839A1

公开(公告)日：2003-02-19

申请号：EP01945991.6

申请日：2001-05-24

申请人： SCHERING CORPORATION

发明人： NEUSTADT, Bernard, R. ,  LINDO, Neil, A. ,  GREENLEE, William, J. ,  TULSHIAN, Deen ,  SILVERMAN, Lisa, S. ,  XIA, Yan ,  BOYLE, Craig, D. ,  CHACKALAMANNIL, Samuel

IPC分类号： C07D487/14 ,  A61K31/505 ,  A61P25/28

CPC分类号： C07D487/14

摘要： Compounds having the structural formula (I) or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or -C(O)CH2-;Y is -N(R2)CH2CH2N(R3)-, -OCH¿2?CH2N(R?2¿)-, -O-, -S-, -CH¿2?S-, -(CH2)2-NH-, or optionally substituted,(Ia), m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R?6¿-C(O)-, R6-SO2-, R6-OC(O)-, R7-N(R8)-C(O)-, R7-N(R8)-C(S)-, phenyl-CH(OH)-, or phenyl-C(=NOR2)-; or when Q is CH, (Ib),phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R?2, R3, R6, R7, and R8¿ are as defined in the specification are disclosed, their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them; also disclosed are a processes for preparing intermediates useful for preparing compounds of formula (I).

公开(公告)号：EP0767794B1

公开(公告)日：2000-02-02

申请号：EP95924573.9

申请日：1995-06-19

申请人： SCHERING CORPORATION

发明人： MCKITTRICK, Brian, A. ,  CZARNIECKI, Michael, F. ,  CHACKALAMANNIL, Samuel ,  CHUNG, Shin ,  DEFREES, Shawn ,  STAMFORD, Andrew, W.

IPC分类号： C07F9/30 ,  A61K31/66 ,  C07F9/572 ,  C07F9/6558

CPC分类号： C07F9/65583 ,  C07F9/303 ,  C07F9/5728