公开(公告)号：EP1140909B1

公开(公告)日：2005-07-06

申请号：EP99965906.3

申请日：1999-12-22

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

发明人： COOPER, Alan, B. ,  DOLL, Ronald, J. ,  FERREIRA, Johan, A. ,  GANGULY, Ashit ,  GIRIJAVALLABHAN, Viyyoor, M. ,  TAVERAS, Arthur, G. ,  CHAO, Jianping ,  BALDWIN, John, J. ,  HUANG, Chia-Yu ,  LI, Ge

IPC分类号： C07D403/12 ,  C07D401/14 ,  C07D241/04 ,  A61K31/496 ,  A61P35/00

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D241/04 ,  C07D249/08 ,  C07D401/14 ,  C07D403/12

摘要： Novel compounds and pharmaceutical compositions are disclosed which are inhibitors of the enzyme, farnesyl-protein transferase. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering the novel aminooxyamide compound to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human.

公开(公告)号：EP1664092B1

公开(公告)日：2011-02-02

申请号：EP04784827.0

申请日：2004-09-23

申请人： Schering Corporation

发明人： VENKATRAMAN, Srikanth ,  NJOROGE, F., George ,  WU, Wanli ,  GIRIJAVALLABHAN, Viyyoor, M. ,  MCKITTRICK, Brian ,  SU, Jing ,  VELAZQUEZ, Francisco ,  PINTO, Patrick, A.

IPC分类号： C07K5/12 ,  C07D245/00 ,  A61K38/12

CPC分类号： C07D245/04 ,  A61K31/33 ,  A61K38/12 ,  A61K38/21 ,  A61K38/212 ,  C04B35/632 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D487/04 ,  C07D513/04 ,  C07K5/0217 ,  C07K5/0802 ,  A61K2300/00

摘要： The present invention discloses novel compounds which have HCV protease inhibitory activity as well as pharmaceutical compositions comprising such compounds and methods of using them to treat disorders associated with the HCV protease. The novel compounds typically include a 15-20 member macrocycle and have the general structure of structural Formula (1): wherein Z', L', M', R1, X and D are defined herein.

公开(公告)号：EP1660477B1

公开(公告)日：2008-12-10

申请号：EP04779960.6

申请日：2004-08-04

申请人： Schering Corporation

发明人： ZHU, Hugh, Y. ,  COOPER, Alan, B. ,  DESAI, Jagdish, A. ,  WANG, James, J-S. ,  RANE, Dinanath, F. ,  DOLL, Ronald, J. ,  NJOROGE, F., George ,  GIRIJAVALLABHAN, Viyyoor, M.

IPC分类号： C07D401/06 ,  C07D401/14 ,  A61K31/415 ,  A61P35/00

CPC分类号： C07D401/06

摘要： Disclosed are novel tricyclic compounds of the formula (I) and a pharmaceutically acceptable salts or solvates thereof. The compounds are useful for inhibiting farnesyl protein transferase. Also disclosed are pharmaceutical compositions comprising the compounds of formula (I). Also disclosed are uses of the compounds of formula (I) for the manufacture of a medicament for the treatment of cancer.

公开(公告)号：EP1543008B1

公开(公告)日：2007-11-07

申请号：EP03754658.7

申请日：2003-09-19

申请人： Schering Corporation

发明人： PARUCH, Kamil ,  GUZI, Timothy, J. ,  DWYER, Michael, P. ,  DOLL, Ronald, J. ,  GIRIJAVALLABHAN, Viyyoor, M. ,  MALLAMS, Alan, K.

IPC分类号： C07D487/04 ,  A61K31/495 ,  A61P35/00

CPC分类号： C07D487/04

摘要： In its many embodiments, the present invention provides a novel class of imidazo[1,2-a]pyrazine compounds of formula (III) as inhibitors of cyclin dependent kinases, 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 CDKs using such compounds or pharmaceutical compositions.

公开(公告)号：EP1797111A1

公开(公告)日：2007-06-20

申请号：EP05790914.5

申请日：2005-08-25

申请人： SCHERING CORPORATION

发明人： SANNIGRAHI, Mousumi ,  NJOROGE, F., George ,  GIRIJAVALLABHAN, Viyyoor, M.

IPC分类号： C07K5/08 ,  A61K38/06 ,  A61P31/22

CPC分类号： C07K5/0808 ,  A61K38/00 ,  C07K5/0217

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：EP1572299A1

公开(公告)日：2005-09-14

申请号：EP03790505.6

申请日：2003-12-15

申请人： SCHERING CORPORATION

发明人： GUZI, Timothy, J. ,  LIU, Yi-Tsung ,  DOLL, Ronald, J. ,  SAKSENA, Anil ,  GIRIJAVALLABHAN, Viyyoor, M. ,  PACHTER, Jonathan, A.

IPC分类号： A61P5/28 ,  A61P35/00 ,  A61K31/496 ,  A61K31/4545 ,  C07D401/14

CPC分类号： C07D401/14 ,  A61K31/435 ,  A61K31/495 ,  A61K31/56 ,  A61K45/06 ,  C07D211/16 ,  C07D241/04 ,  C07D241/08 ,  C07D401/04 ,  C07D401/06 ,  A61K2300/00

摘要： The present invention provides a novel class of compounds of formula (I): as inhibitors of type 3 17β-hydroxysteroid dehydrogenase, 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 type 3 17β-hydroxysteroid dehydrogenase using such compounds or pharmaceutical compositions.

公开(公告)号：EP1337522A1

公开(公告)日：2003-08-27

申请号：EP01985496.7

申请日：2001-11-27

申请人： Schering Corporation

发明人： NJOROGE, F., George ,  VIBULBHAN, Bancha ,  GIRIJAVALLABHAN, Viyyoor, M. ,  SHI, Xiongwei

IPC分类号： C07D401/04 ,  C07D401/14 ,  A61K31/473 ,  A61P35/00

CPC分类号： C07D401/04 ,  C07D401/14

摘要： The present invention describes compounds useful for the inhibition of Farnesyl Protein Transferase. This invention also discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with FPT.

公开(公告)号：EP1282632A1

公开(公告)日：2003-02-12

申请号：EP01928662.4

申请日：2001-04-18

申请人： SCHERING CORPORATION

发明人： GANGULY, Ashit, K. ,  MCCORMICK, Jinping ,  LOVEY, Raymond, G. ,  BENNETT, Frank ,  SAKSENA, Anil, K. ,  GIRIJAVALLABHAN, Viyyoor, M.

IPC分类号： C07H19/056 ,  A61K31/7056 ,  A61P31/12

CPC分类号： C07H19/056 ,  Y10S514/894

摘要： Ribavirin derivatives represented by the formula (II), pharmaceutical compositions containing them as well as the use of the ribavirin derivatives represented by the formula (II) for the preparation of a medicament for the treatment of susceptible viral infections, for example, chronic hepatitis C infections administrating, the ribavirin derivatives being represented by formula (II) are disclosed.

公开(公告)号：EP1140904A1

公开(公告)日：2001-10-10

申请号：EP99967139.9

申请日：1999-12-16

申请人： SCHERING CORPORATION

发明人： GUZI, Timothy ,  RANE, Dinanath, F. ,  MALLAMS, Alan, K. ,  COOPER, Alan, B. ,  DOLL, Ronald, J. ,  GIRIJAVALLABHAN, Viyyoor, M. ,  TAVERAS, Arthur, G. ,  STRICKLAND, Corey ,  KELLY, Joseph, M. ,  CHAO, Jianping

IPC分类号： C07D401/14 ,  A61K31/497 ,  A61K31/44 ,  A61P43/00

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/04 ,  C07D401/14

摘要： Disclosed are compounds of formula (1.0), wherein R8 represents a cyclic moiety to which is bound an imodazolylalkyl group; R9 represents a carbamate, urea, amide or sulfonamide group; and the remaining substituents are as defined herein. Also disclosed is a method of treating cancer and a method of inhibiting farnesyl protein transferase using the disclosed compounds.

公开(公告)号：EP0993454A1

公开(公告)日：2000-04-19

申请号：EP98926277.9

申请日：1998-06-15

申请人： SCHERING CORPORATION

发明人： COOPER, Alan, B. ,  DOLL, Ronald, J. ,  SAKSENA, Anil, K. ,  GIRIJAVALLABHAN, Viyyoor, M.

IPC分类号： C07D401/04 ,  C07D401/14 ,  A61K31/435

CPC分类号： C07D401/04 ,  C07D401/14

摘要： Novel compounds of formula (1.0) or a pharmaceutically acceptable salt or solvate thereof, wherein: a represents N or NO?-; R1 and R3¿ are the same or different and each represents halo; R?2 and R4¿ are the same or different and each is selected from H and halo, provided that at least one of R?2 and R4¿ is H; T is a substituent selected from SO¿2? R or (A); Z is O or S; n is zero or an integer from 1 to 6; R is alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, heterocycloalkyl, or N(R?5)¿2; R5 is H, alkyl, aryl, heteroaryl or cycloalkyl. Also disclosed are methods of inhibiting farnesyl protein transferase and methods for treating tumor cells.

摘要翻译： 式（1.0）的新型化合物或其药学上可接受的盐或溶剂合物，其中：a代表N或NO 2 - ; R1和R3'相同或不同，各自代表卤素; R 2和R 4'相同或不同，且各自选自H和卤素，条件是R 2'和R 4'中的至少一个是H; T是选自SO 2的取代基。 R或（A）; Z是O或S; n是零或1至6的整数; R是烷基，芳基，芳基烷基，杂芳基，杂芳基烷基，环烷基，杂环烷基或N（R 5）2; R5是H，烷基，芳基，杂芳基或环烷基。 还公开了抑制法尼基蛋白转移酶的方法和治疗肿瘤细胞的方法。