公开(公告)号：EP1940828A2

公开(公告)日：2008-07-09

申请号：EP06817385.5

申请日：2006-10-25

申请人： Schering Corporation

发明人： ZHU, Zhaoning ,  STAMFORD, Andrew, W. ,  MCKITTRICK, Brian

IPC分类号： C07D409/04 ,  C07D487/04 ,  C07D498/04 ,  A61K31/395 ,  A61P9/00 ,  A61P25/28 ,  A61P31/18 ,  A61P33/02

CPC分类号： C07D409/04 ,  C07D487/04

摘要： Disclosed are compounds of the formula I Chemical formula should be inserted here as it appears on the abstract in paper form. or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Ar, R1, R2, R3, R4 and R5 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.

公开(公告)号：EP1934227A1

公开(公告)日：2008-06-25

申请号：EP06803715.9

申请日：2006-09-15

申请人： Schering Corporation

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

IPC分类号： C07D487/14 ,  A61K31/519 ,  A61P25/00

CPC分类号： C07D487/14

摘要： Compounds having the structural formula (I) or a pharmaceutically acceptable salt thereof, wherein R is R1-isoxazolyl, R1-oxadiazolyl, R1-dihydrofuranyl, R1-pyrazolyl, R1-imidazolyl, R1-pyrazinyl or R1-pyrimidinyl; R1 is 1 , 2 or 3 substituents selected from H, alkyl, alkoxy and halo; Z is optionally substituted-aryl, or optionally substituted-heteroaryl; are disclosed, as well as their use in the treatment of central nervous system diseases, in particular Parkinson's disease and Extra Pyramidal Syndrome, pharmaceutical compositions comprising them, and combinations with other agents.

公开(公告)号：EP1896477A1

公开(公告)日：2008-03-12

申请号：EP06784753.3

申请日：2006-06-12

申请人： Schering Corporation

发明人： ZHU, Zhaoning ,  MCKITTRICK, Brian ,  STAMFORD, Andrew, W. ,  HUANG, Ying ,  SMITH, Elizabeth, M.

IPC分类号： C07D487/04 ,  C07D498/04 ,  A61P9/00 ,  A61P25/00 ,  A61P25/28 ,  A61P31/18 ,  A61K31/395

CPC分类号： C07D487/04

摘要： Disclosed are compounds of the formula (I) Chemical formula should be inserted here as it appears on the abstract in paper form or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein U, W, R, R1, R2, R3 and R4 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula (I). Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula (I) in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.

摘要翻译： 公开的是式（I）化合物化学式应当以其在摘要中出现的纸形式或其立体异构体，互变异构体或药学上可接受的盐或溶剂化物插入本文，其中U，W，R，R1，R2，R3 和R4如说明书中所定义; 和包含式（I）化合物的药物组合物。 还公开了抑制天冬氨酰蛋白酶的方法，特别是治疗心血管疾病，认知和神经退行性疾病的方法。 还公开了使用式（I）化合物与胆碱酯酶抑制剂或毒蕈碱m1激动剂或m2拮抗剂联合治疗认知或神经退行性疾病的方法。

公开(公告)号：EP1891021A1

公开(公告)日：2008-02-27

申请号：EP06772934.3

申请日：2006-06-12

申请人： Schering Corporation ,  PHARMACOPEIA, INC.

发明人： ZHU, Zhaoning ,  MCKITTRICK, Brian ,  STAMFORD, Andrew, W. ,  LE, Thuy, X.H. ,  GUO, Tao

IPC分类号： C07D239/70 ,  C07D491/10 ,  C07D495/10 ,  C07D471/10 ,  C07D487/10

CPC分类号： C07D471/10 ,  C07D239/70 ,  C07D487/10 ,  C07D491/10 ,  C07D495/10

摘要： Disclosed are certain substituted spiro iminopyrimidinones and other compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein U, W, A, R, R1, R2, R6a and R7, are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of using such compounds and compositions to inhibit aspartyl protease, and to treat a variety of disease and indications including (but not limited) to cardiovascular disease and cognitive and neurodegenerative disease. The compounds of the present invention are disclosed for use alone or in combination with one or more additional active ingredients such as cholinesterase inhibitors and a muscarinic m1 agonist and/or m2 antagonists.

摘要翻译： 本文公开了式I化合物或其立体异构体，互变异构体或药学上可接受的盐或溶剂合物，其中U，W，A，R，R1，R2，R6a和R7如说明书中所定义; 以及包含式I化合物的药物组合物。还公开了抑制天冬氨酰蛋白酶的方法，特别是治疗心血管疾病，认知和神经退行性疾病的方法。 还公开了使用式I化合物与胆碱酯酶抑制剂或毒蕈碱m1激动剂或m2拮抗剂组合治疗认知或神经退行性疾病的方法。

公开(公告)号：EP1819684A1

公开(公告)日：2007-08-22

申请号：EP05852503.1

申请日：2005-12-01

申请人： SCHERING CORPORATION

发明人： GILBERT, Eric, J. ,  MILLER, Michael, W. ,  SCOTT, Jack, D. ,  STAMFORD, Andrew, W. ,  GREENLEE, William, J. ,  WEINSTEIN, Jay

IPC分类号： C07D241/04 ,  A61K31/495 ,  A61K31/496 ,  A61P3/00

CPC分类号： C07D241/04 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/08 ,  C07D405/12 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/06 ,  C07D413/12 ,  C07D417/06 ,  C07D417/10

摘要： Compounds of Formula (I): Chemical formula should be inserted here as it appears on the abstract in paper form. or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1 receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.

公开(公告)号：EP1934227B1

公开(公告)日：2011-12-21

申请号：EP06803715.9

申请日：2006-09-15

申请人： Schering Corporation

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

IPC分类号： C07D487/14 ,  A61K31/519 ,  A61P25/00

CPC分类号： C07D487/14

摘要： Compounds having the structural formula (I) or a pharmaceutically acceptable salt thereof, wherein R is R1-isoxazolyl, R1-oxadiazolyl, R1-dihydrofuranyl, R1-pyrazolyl, R1-imidazolyl, R1-pyrazinyl or R1-pyrimidinyl; R1 is 1 , 2 or 3 substituents selected from H, alkyl, alkoxy and halo; Z is optionally substituted-aryl, or optionally substituted-heteroaryl; are disclosed, as well as their use in the treatment of central nervous system diseases, in particular Parkinson's disease and Extra Pyramidal Syndrome, pharmaceutical compositions comprising them, and combinations with other agents.

公开(公告)号：EP2328897A1

公开(公告)日：2011-06-08

申请号：EP09790449.4

申请日：2009-07-15

申请人： Schering Corporation

发明人： NEELAMKAVIL, Santhosh, Francis ,  BOYLE, Craig, D. ,  HARRIS, Joel, M. ,  STAMFORD, Andrew, W. ,  HAO, Jinsong ,  NEUSTADT, Bernardt, R. ,  CHACKALAMANNIL, Samuel ,  XIA, Yan ,  GREENLEE, William, J.

IPC分类号： C07D473/30 ,  C07D473/34 ,  C07D487/04 ,  A61K31/52 ,  A61K31/519 ,  A61P3/00 ,  A61P9/00

CPC分类号： C07D487/04 ,  C07D473/30 ,  C07D473/34

摘要： The present invention relates to Bicyclic Heterocycle Derivatives of Formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein-coupled receptor (GPCR) in a patient.

公开(公告)号：EP2288613A1

公开(公告)日：2011-03-02

申请号：EP09734237.2

申请日：2009-04-21

申请人： Schering Corporation

发明人： STAMFORD, Andrew, W. ,  ZHU, Zhaoning ,  MANDAL, Mihirbaran ,  WU, Yusheng ,  CUMMING, Jared, N. ,  LIU, Xiaoxiang ,  LI, Guoqing ,  ISERLOH, Ulrich

IPC分类号： C07D487/04 ,  A61P25/28 ,  A61K31/519

CPC分类号： C07D487/04

摘要： In its many embodiments, the present invention provides provides certain 2-imino-3-methyl pyrrolo pyrimidone compounds, including compounds Formula (II): and include tautomers, steroisomers, or pharmaceutically acceptable salts or solvates of said compounds, stereoisomers, or said tautomers, wherein R
2 , R
3 , R
4 , R
5 , R
6 , R
7 , R
8 , and R
9 are each selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds, and methods for their preparation and use in treating pathologies associated with amyloid beta (Aβ) protein, including Alzheimer's Disease, are also disclosed.

公开(公告)号：EP2262811A1

公开(公告)日：2010-12-22

申请号：EP09716584.9

申请日：2009-03-03

申请人： Schering Corporation

发明人： HARRIS, Joel, M. ,  NEUSTADT, Bernard, R. ,  HAO, Jinsong ,  STAMFORD, Andrew, W.

IPC分类号： C07D487/14 ,  A61K31/519 ,  A61P25/16 ,  C07D487/04

CPC分类号： C07D487/14 ,  C07D487/04

摘要： Compounds of the Formula I wherein R
1 and R
2 together with the carbon atoms to which they are bonded optionally form a further heteroaromatic ring of the formula (II) as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof are adenosine A2a receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease.

公开(公告)号：EP1940828B1

公开(公告)日：2010-08-18

申请号：EP06817385.5

申请日：2006-10-25

申请人： Schering Corporation

发明人： ZHU, Zhaoning ,  STAMFORD, Andrew, W. ,  MCKITTRICK, Brian

IPC分类号： C07D409/04 ,  C07D487/04 ,  C07D498/04 ,  A61K31/395 ,  A61P9/00 ,  A61P25/28 ,  A61P31/18 ,  A61P33/02

CPC分类号： C07D409/04 ,  C07D487/04

摘要： Disclosed are compounds of the formula I Chemical formula should be inserted here as it appears on the abstract in paper form. or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Ar, R1, R2, R3, R4 and R5 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.

摘要翻译： 所公开的是式I化合物，化学式应插入此处，因为它以摘要形式出现在纸上。 或其立体异构体，互变异构体或药学上可接受的盐或溶剂化物，其中Ar，R1，R2，R3，R4和R5如说明书中所定义; 以及包含式I化合物的药物组合物。还公开了抑制天冬氨酰蛋白酶的方法，特别是治疗心血管疾病，认知和神经退行性疾病的方法。 还公开了使用式I化合物与胆碱酯酶抑制剂或毒蕈碱m1激动剂或m2拮抗剂组合治疗认知或神经退行性疾病的方法。