公开(公告)号：EP1481000B1

公开(公告)日：2010-06-02

申请号：EP03731956.3

申请日：2003-01-16

申请人： Schering Corporation ,  DENDREON CORPORATION

发明人： SAKSENA, Anil, K. ,  GIRIJAVALLABHN, Viyyoor, M. ,  LOVEY, Raymond, G. ,  JAO, Edwin ,  BENNETT, Frank ,  MC CORMICK, Jinping, L. ,  WANG, Haiyan ,  PIKE, Russell, E. ,  BOGEN, Stephane, L. ,  CHAN, Tin-Yau ,  LIU, Yi-Tsung ,  ZHU, Zhaoning ,  NJOROGE, George, F. ,  ARASAPPAN, Ashok ,  PAREKH, Tejal ,  GANGULY, Ashit, K. ,  CHEN, Kevin, X. ,  VENKATRAMAN, Srikanth ,  VACCARO, Henry, A. ,  PINTO, Patrick A. ,  SANTHANAM, Bama ,  KEMP, Scott Jeffrey ,  LEVY, Odile Esther ,  LIM-WILBY, Marguerita ,  TAMURA, Susan Y. ,  WU, Wanli ,  HENDRATA, Siska ,  HUANG, Yuhua ,  WONG, Jesse K. ,  NAIR, Latha G.

IPC分类号： C07K5/062 ,  C07K5/065 ,  A61K38/55

CPC分类号： C07K5/0804 ,  A61K38/00 ,  C07K5/0202 ,  C07K5/0812 ,  C07K5/0827 ,  C07K7/02

摘要： The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

公开(公告)号：EP1385870B1

公开(公告)日：2010-03-17

申请号：EP01954764.5

申请日：2001-07-19

申请人： Schering Corporation ,  DENDREON CORPORATION

发明人： SAKSENA, Anil, K. ,  GIRIJAVALLABHAN, Viyyoor, Moopil ,  LOVEY, Raymond, G. ,  JAO, Edwin, E. ,  BENNETT, Frank ,  MC CORMICK, Jinping, L. ,  WANG, Haiyan ,  PIKE, Russell, E. ,  BOGEN, Stephane, L. ,  CHAN, Tin-Yau ,  LIU, Yi-Tsung ,  ZHU, Zhaoning ,  NJOROGE, F., George ,  ARASAPPAN, Ashok ,  PAREKH, Tejal, N. ,  GANGULY, Ashit, K. ,  CHEN, Kevin, X. ,  VENKATRAMAN, Srikanth ,  VACCARO, Henry, A. ,  PINTO, Patrick A. ,  SANTHANAM, Bama ,  WU, Wanli ,  HENDRATA, Siska ,  HUANG, Yuhua ,  KEMP, Scott Jeffrey ,  LEVY, Odile Esther ,  LIM-WILBY, Marguerita ,  TAMURA, Susan Y.

IPC分类号： C07K1/00

CPC分类号： C07K5/0202 ,  A61K38/00 ,  C07K5/0812 ,  C07K5/0827 ,  C07K7/02

摘要： The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

公开(公告)号：EP1481000A2

公开(公告)日：2004-12-01

申请号：EP03731956.3

申请日：2003-01-16

申请人： SCHERING CORPORATION ,  DENDREON CORPORATION

发明人： SAKSENA, Anil, K. ,  GIRIJAVALLABHN, Viyyoor, M. ,  LOVEY, Raymond, G. ,  JAO, Edwin ,  BENNETT, Frank ,  MC CORMICK, Jinping, L. ,  WANG, Haiyan ,  PIKE, Russell, E. ,  BOGEN, Stephane, L. ,  CHAN, Tin-Yau ,  LIU, Yi-Tsung ,  ZHU, Zhaoning ,  NJOROGE, George, F. ,  ARASAPPAN, Ashok ,  PAREKH, Tejal ,  GANGULY, Ashit, K. ,  CHEN, Kevin, X. ,  VENKATRAMAN, Srikanth ,  VACCARO, Henry, A. ,  PINTO, Patrick A. ,  SANTHANAM, Bama ,  KEMP, Scott Jeffrey ,  LEVY, Odile Esther ,  LIM-WILBY, Marguerita ,  TAMURA, Susan Y. ,  WU, Wanli ,  HENDRATA, Siska ,  HUANG, Yuhua ,  WONG, Jesse K. ,  NAIR, Latha G.

IPC分类号： C07K5/062 ,  C07K5/065 ,  A61K38/55

CPC分类号： C07K5/0804 ,  A61K38/00 ,  C07K5/0202 ,  C07K5/0812 ,  C07K5/0827 ,  C07K7/02

摘要： The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

公开(公告)号：EP1948638B1

公开(公告)日：2011-08-03

申请号：EP06789659.7

申请日：2006-08-10

申请人： Schering Corporation

发明人： ZHU, Zhaoning ,  MAZZOLA, Robert, D. ,  YU, Wensheng ,  KOZLOWSKI, Joseph, A.

IPC分类号： C07D401/12 ,  A61K31/4709 ,  A61P29/00

CPC分类号： C07D401/12

摘要： This invention relates to compounds of the Formula (I): Chemical formula should be inserted here as it appears on the abstract in paper form. or a pharmaceutically acceptable salt, solvate or isomer thereof, wherein n, M, V, T, W, X, U, R1 and R2 are as disclosed in the present specification, and which compounds are useful for the treatment of diseases or conditions mediated by MMPs, TNF- or combinations thereof.

摘要翻译： 本发明涉及式（I）的化合物：化学式应当在摘要中以纸的形式出现在此处。 或其药学上可接受的盐，溶剂化物或异构体，其中n，M，V，T，W，X，U，R 1和R 2如本说明书中所公开的，并且所述化合物可用于治疗介导的疾病或病症 通过MMPs，TNF-或其组合。

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：EP2229381A1

公开(公告)日：2010-09-22

申请号：EP08856462.0

申请日：2008-12-04

申请人： Schering Corporation

发明人： HUANG, Xianhai ,  PALANI, Anandan ,  QIN, Jun ,  ASLANIAN, Robert, G. ,  ZHU, Zhaoning ,  GREENLEE, William, J. ,  JOSIEN, Hubert ,  ZHOU, Wei ,  ZHU, Xiaohong ,  BENNETT, Chad, E. ,  PISSARNITSKI, Dmitri ,  MANDAL, Mihirbaran ,  DHONDI, Pawan ,  MCCRACKEN, Troy ,  BARA, Thomas ,  ZHAO, Zhiqiang ,  BURNETT, Duane ,  CLADER, John

IPC分类号： C07D403/10 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04 ,  A61K31/4738 ,  A61P25/28

CPC分类号： C07D471/04 ,  C07D403/10 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

摘要： This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I) wherein R2 is a fused bicyclic ring of the formula (II). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's disease using the compounds of formula (I).

摘要翻译： 本发明提供了γ分泌酶调节剂的新化合物。 该化合物具有式（I），其中R 2是式（II）的稠合双环。 还公开了使用式（I）化合物调节γ分泌酶活性的方法和治疗阿尔茨海默病的方法。

公开(公告)号：EP2217604A1

公开(公告)日：2010-08-18

申请号：EP08848226.0

申请日：2008-11-03

申请人： Schering Corporation

发明人： GREENLEE, William J. ,  ZHU, Zhaoning ,  ASBEROM, Theodros ,  HUANG, Xianhai ,  JOSIEN, Hubert B.

IPC分类号： C07D487/10 ,  C07D487/20 ,  C07D493/20 ,  C07D495/20 ,  C07D498/10 ,  C07D498/20 ,  C07D498/22 ,  C07F7/08 ,  C07F9/6571

CPC分类号： C07D498/10 ,  C07D487/10 ,  C07D487/20 ,  C07D493/20 ,  C07D495/20 ,  C07D498/20 ,  C07D498/22 ,  C07F7/0812 ,  C07F9/657181

摘要： This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).

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。

公开(公告)号：EP2164852A2

公开(公告)日：2010-03-24

申请号：EP08767901.5

申请日：2008-05-28

申请人： Schering Corporation

发明人： ZHU, Zhaoning ,  GREENLEE, William, J. ,  SUN, Zhong-Yue ,  GALLO, Gioconda ,  XU, Ruo ,  HUANG, Xianhai ,  ZHU, Xiaohong

IPC分类号： C07D498/04 ,  C07D413/10 ,  A61K31/4355 ,  A61K31/5365 ,  A61K31/421 ,  A61P25/28

CPC分类号： C07D498/04 ,  C07D413/10

摘要： In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.

公开(公告)号：EP2061771A1

公开(公告)日：2009-05-27

申请号：EP07862713.0

申请日：2007-12-10

申请人： Schering Corporation

发明人： ZHU, Zhaoning ,  STAMFORD, Andrew ,  LI, Guoqing ,  MANDAL, Mihirbaran

IPC分类号： C07D239/70 ,  C07D471/04 ,  C07D487/04 ,  C07D493/04 ,  C07D513/04 ,  A61K31/517 ,  A61K31/519

CPC分类号： C07D239/70 ,  C07D471/04 ,  C07D487/04 ,  C07D493/04 ,  C07D513/04

摘要： Disclosed are compounds of Formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof or wherein R1, R2, R3, R4, R6, R7, R14, W, V, X, Y, A and b are as described above in the specification. Also disclosed is a method of inhibiting aspartyl protease, methods of treating cardiovascular diseases, cognitive diseases, neurodegenerative diseases, and other biological processes and indications. Combination treatments and compositions are also disclosed.