公开(公告)号：EP2097387A2

公开(公告)日：2009-09-09

申请号：EP08714220.4

申请日：2008-02-20

申请人： Schering Corporation ,  Pharmacopeia, Inc.

发明人： ZHU, Zhaoning ,  MCKITTRICK, Brian ,  SUN, Zhong-Yue ,  YE, Yuanzan, C. ,  VOIGT, Johannes, H. ,  STRICKLAND, Corey ,  SMITH, Elizabeth, M. ,  STAMFORD, Andrew ,  GREENLEE, William, J. ,  MAZZOLA, JR., Robert, D. ,  CALDWELL, John ,  CUMMING, Jared, N. ,  WANG, Lingyan ,  WU, Yusheng ,  ISERLOH, Ulrich ,  LIU, Xiaoxiang ,  HUANG, Ying ,  LI, Guoqing ,  PAN, Jianping ,  MISIASZEK, Jeffrey, A. ,  GUO, Tao ,  LE, Thuy X. H. ,  SAIONZ, Kurt, W. ,  BABU, Suresh, D. ,  HUNTER, Rachael, C. ,  MORRIS, Michelle, L. ,  GU, Huizhong ,  QIAN, Gang ,  TADESSE, Dawit ,  LAI, Gaifa ,  DUO, Jingqi ,  QU, Chuanxing ,  SHAO, Yuefei

IPC分类号： C07D233/88 ,  C07D239/22 ,  C07D401/06 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D417/14 ,  C07D495/10 ,  C07D401/10 ,  C07D417/10 ,  A61K31/513 ,  A61P25/28

CPC分类号： C07D233/88 ,  A61K31/4168 ,  A61K31/4178 ,  C07D239/22 ,  C07D401/06 ,  C07D401/10 ,  C07D403/06 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D417/10 ,  C07D417/14 ,  C07D495/10

摘要： Disclosed are compounds of the formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, -C(=S)-, -S(O)-, -S(O)2-, -C(=O)-, -O-, -C(R6)(R7)-, -N(R5)- or -C(=N(R5))-; X is -O-, -N(R5)- or -C(R6)(R7)-; provided that when X is -O-, U is not -O-, -S(O)-, -S(O)2-, -C(=O)- or -C(=NR5)-; U is a bond, -S(O)-, -S(O)2-, -C(O)-, -O-, -P(O)(OR15)-, -C(=NR5)-, -(C(R6)(R7))b- or -N(R5)-; wherein b is 1 or 2; provided that when W is -S(O)-, -S(O)2-, -O-, or -N(R5)-, U is not -S(O)-, -S(O)2-, -O-, or -N(R5)-; provided that when X is -N(R5)- and W is -S(O)-, -S(O)2-, -O-, or -N(R5)-, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 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, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. 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：EP1838304A2

公开(公告)日：2007-10-03

申请号：EP05766007.8

申请日：2005-06-09

申请人： Schering Corporation ,  PHARMACOPEIA, INC.

发明人： ZHU, Zhaoning ,  MCKITTRICK, Brian ,  SUN, Zhong-Yue ,  YE, Yuanzan ,  VOIGT, Johannes H. ,  STRICKLAND, Corey ,  SMITH, Elizabeth M. ,  STAMFORD, Andrew ,  GREENLEE, William J. ,  MAZZOLA, Robert ,  CALDWELL, John ,  CUMMING, Jared ,  WANG, Lingyan ,  WU, Yusheng ,  ISERLOH, Ulrich ,  GUO, Tao ,  LE, Thuy X.H. ,  SAIONZ, Kurt W. ,  BABU, Suresh D. ,  HUNTER, Rachael C. ,  MORRIS, Michelle L. ,  GU, Huizhong ,  QIAN, Gang ,  TADESSE, Dawit

IPC分类号： A61K31/4168 ,  A61K31/4178 ,  C07D233/46 ,  C07D233/88 ,  C07D239/22 ,  C07D271/06 ,  C07D273/00 ,  C07D401/10 ,  C07D403/06 ,  C07D403/12 ,  C07D407/10 ,  C07D409/04 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  C07D417/06 ,  A61P9/00 ,  A61P25/00

CPC分类号： C07D233/88 ,  A61K31/4168 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/5377 ,  A61K31/655 ,  A61K45/06 ,  C07D233/46 ,  C07D233/70 ,  C07D235/02 ,  C07D239/22 ,  C07D239/70 ,  C07D271/07 ,  C07D273/00 ,  C07D295/15 ,  C07D401/04 ,  C07D401/06 ,  C07D401/08 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/08 ,  C07D403/10 ,  C07D403/12 ,  C07D405/06 ,  C07D405/10 ,  C07D405/14 ,  C07D407/06 ,  C07D409/04 ,  C07D409/06 ,  C07D409/10 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  C07D417/06 ,  Y02A50/411

摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, -C(-S)-, -S(O)-, -S(O)2-, -C(-O)-, -O-, -C(R6)(R7)-, -N(R5)- or -C(-N(R5))-; X is -O-, -N(R5)- or -C(R6)(R7)-; provided that when X is -O-, U is not -O-, -S(O)-, -S(O)2-, -C(-O)- or -C(-NR5)-; U is a bond, -S(O)-, -S(O)2-, -C(O)-, -O-, -P(O)(OR15)-, -C(-NR5)-, -(C(R6)(R7))b- or -N(R5)-; wherein b is 1 or 2; provided that when W is -S(O)-, -S(O)2-, -O-, or -N(R5)-, U is not -S(O)-, -S(O)2-, -O-, or -N(R5)-; provided that when X is -N(R5)- and W is -S(O)-, -S(O)2-, -O-, or -N(R5)-, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 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, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. 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 antagonist.

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：EP1747218A2

公开(公告)日：2007-01-31

申请号：EP05742268.5

申请日：2005-04-28

申请人： SCHERING CORPORATION

发明人： ZHU, Zhaoning ,  SUN, Zhong-Yue ,  YE, Yuanzan ,  MULLINS, Deborra E. ,  MCKITTRICK, Brian ,  STAMFORD, Andrew ,  GREENLEE, William, J.

IPC分类号： C07D417/12 ,  C07D487/04 ,  C07D513/04 ,  A61K31/428 ,  A61K31/541

CPC分类号： C07D487/04 ,  C07D417/12 ,  C07D513/04

摘要： The present invention discloses compounds, which are novel receptor antagonists for NPY Y1 as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such NPY Y1 receptor antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes. The compounds are represented by the structural Formula 1, Chemical formula should be inderted here as it appears on the abstract in paper form. a prodrug thereof, or any pharmaceutically acceptable salt, solvate, isomer or racemic mixture of the compound or said prodrug wherein R1 is heteroaryl, N-arylaminocarbonyl, N-heteroarylaminocarbonyl, benzimidazolyl or benzothiazolyl; R15 is present or not and if present is H, aryl, alkyl, arylalky or heteroarylalkyl; A is aryl, heteroaryl, cycloalkyl, cycloalkylidene, heterocycloalkylidene or heterocycloalkyl wherein said aryl, heteroaryl, cycloalkyl, cycloalkylidene, heterocycloalkylidene and heterocycloalkyl moieties may be substituted or unsubstituted; and B, L, X and R18 are defined herein.

公开(公告)号：EP2379566A2

公开(公告)日：2011-10-26

申请号：EP09775508.6

申请日：2009-12-18

申请人： Schering Corporation

发明人： ASBEROM, Theodros ,  ZHU, Zhaoning ,  CLADER, John, W. ,  SUN, Zhong-Yue ,  MANDAL, Mihirbaran ,  GALLO, Gioconda ,  LIU, Xiaoxiang

IPC分类号： C07D513/14 ,  C07D498/14 ,  A61K31/542 ,  A61K31/5365 ,  A61K31/4245 ,  A61P25/00

CPC分类号： C07D498/04 ,  C07D513/04

摘要： This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (Chemical formula should be inserted here as it appears on abstract in paper form). 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。 这些化合物具有化学式（化学式应该插入此处，因为它以摘要形式出现在纸上）。 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：EP2365976A1

公开(公告)日：2011-09-21

申请号：EP09760047.2

申请日：2009-11-12

申请人： Schering Corporation

发明人： ZHU, Zhaoning ,  GREENLEE, William J. ,  HUANG, Xianhai ,  QIN, Jun ,  LIU, Xiaoxiang ,  LI, Hongmei ,  ZHOU, Wei ,  PALANI, Anandan ,  ZHU, Xiaohong ,  VICAREL, Monica L. ,  MANDAL, Mihirbaran ,  SUN, Zhong-Yue ,  BENNETT, Chad E. ,  MCCRACKEN, Troy M. ,  GALLO, Gioconda

IPC分类号： C07D471/04 ,  C07D498/04 ,  A61K31/5395 ,  A61P25/28

CPC分类号： C07D471/04 ,  C07D498/04

摘要： In its many embodiments, the present invention provides a novel class of heterocyclic compounds of Group A or Group, as defined herein, 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.

摘要翻译： 在其许多实施方案中，本发明提供了一类如本文所定义的A类或组的杂环化合物作为γ分泌酶的调节剂，制备所述化合物的方法，含有一种或多种这类化合物的药物组合物，制备药物的方法 包含一种或多种此类化合物的制剂，以及使用此类化合物或药物组合物治疗，预防，抑制或改善与中枢神经系统相关的一种或多种疾病的方法。

公开(公告)号：EP1343807A2

公开(公告)日：2003-09-17

申请号：EP01986126.9

申请日：2001-12-10

申请人： SCHERING CORPORATION

发明人： ZHU, Zhaoning ,  SUN, Zhong-Yue ,  VENKATRAMAN, Srikanth ,  NJOROGE, F. George, ,  ARASAPPAN, Ashok ,  MALCOLM, Bruce A. ,  GIRIJAVALLABHAN, Viyyoor M. ,  LOVEY, Raymond G. ,  CHEN, Kevin X.

IPC分类号： C07K1/00

CPC分类号： C07K5/0202 ,  A61K38/00 ,  C07K14/811

摘要： The present invention is directed to certain diaryl amide compounds as NS3-Serine protease inhibitors of hepatitis C virus. A particularly preferred compound is of the formula (I).

公开(公告)号：EP1343807B1

公开(公告)日：2009-04-29

申请号：EP01986126.9

申请日：2001-12-10

申请人： Schering Corporation

发明人： ZHU, Zhaoning ,  SUN, Zhong-Yue ,  VENKATRAMAN, Srikanth ,  NJOROGE, F. George, ,  ARASAPPAN, Ashok ,  MALCOLM, Bruce A. ,  GIRIJAVALLABHAN, Viyyoor M. ,  LOVEY, Raymond G. ,  CHEN, Kevin X.

IPC分类号： C07K14/81 ,  C07K5/08 ,  A61K38/00 ,  A61P31/12

CPC分类号： C07K5/0202 ,  A61K38/00 ,  C07K14/811

摘要： The present invention is directed to certain diaryl amide compounds as NS3-Serine protease inhibitors of hepatitis C virus. A particularly preferred compound is of the formula (I).

摘要翻译： 本发明涉及某些二芳基酰胺化合物作为丙型肝炎病毒的NS3-丝氨酸蛋白酶抑制剂。 特别优选的化合物是式（I）的化合物。

公开(公告)号：EP2032542A2

公开(公告)日：2009-03-11

申请号：EP07795971.6

申请日：2007-06-07

申请人： Schering Corporation

发明人： WU, Yusheng ,  ISERLOH, Ulrich ,  CUMMING, Jared ,  LIU, Xiaoxiang ,  MAZZOLA, Robert, D. ,  SUN, Zhong-Yue ,  HUANG, Ying ,  STAMFORD, Andrew ,  MCKITTRICK, Brian ,  ZHU, Zhaoning

IPC分类号： C07D239/20 ,  C07D401/04 ,  C07D401/10 ,  C07D403/04 ,  C07D405/04 ,  C07D409/14 ,  C07D411/04 ,  C07D417/14 ,  C07D495/20 ,  A61K31/513 ,  A61P25/28

CPC分类号： C07D239/20 ,  C07D401/04 ,  C07D401/10 ,  C07D403/04 ,  C07D405/04 ,  C07D409/14 ,  C07D411/04 ,  C07D417/04 ,  C07D417/14 ,  C07D495/20

摘要： Disclosed are compounds of formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, U, W, X, R1, R2, R6, R7, R30 and R31 are as described above in the specification. 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，U，W，X，R 1，R 2，R 6，R 7，R 30和R 31如上文在说明书中所述。 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：EP1699455A1

公开(公告)日：2006-09-13

申请号：EP04813947.1

申请日：2004-12-13

申请人： SCHERING CORPORATION ,  Pharmacopeia Drug Discovery, Inc.

发明人： ZHU, Zhaoning ,  MCKITTRICK, Brian ,  SUN, Zhong-Yue ,  YE, Yuanzan, C. ,  STRICKLAND, Corey ,  SMITH, Elizabeth, M. ,  STAMFORD, Andrew ,  GREENLEE, William, J. ,  WU, Yusheng ,  ISERLOH, Ulrich ,  MAZZOLA, Robert ,  CALDWELL, John ,  CUMMING, Jared ,  WANG, Lingyan ,  GUO, Tao ,  LE, Thuy, X. H. ,  SAIONZ, Kurt, W. ,  BABU, Suresh, D. ,  VOIGT, Johannes H. ,  HUNTER, Rachael C.

IPC分类号： A61K31/4168 ,  A61K31/4178 ,  C07D233/88 ,  C07D239/22 ,  C07D271/06 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/10 ,  C07D403/14 ,  C07D405/06 ,  C07D405/14 ,  C07D407/14

CPC分类号： C07D233/88 ,  C07D235/02 ,  C07D239/22 ,  C07D271/07 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D409/06 ,  C07D409/10 ,  C07D409/14 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

摘要： Disclosed are compounds of the formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. 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 antagonist.