公开(公告)号：EP1492772A1

公开(公告)日：2005-01-05

申请号：EP03711214.1

申请日：2003-02-25

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

发明人： ZHU, Hugh, Y. ,  NJOROGE, F., George ,  COOPER, Alan, B. ,  GUZI, Timothy, J. ,  RANE, Dinanath, F. ,  MINOR, Keith, P. ,  DOLL, Ronald, J. ,  GIRIJAVALLABHAN, Viyyoor, Moopil ,  SANTHANAM, Bama ,  PINTO, Patrick, A. ,  VIBULBHAN, Bancha ,  KEERTIKAR, Kartik, M. ,  ALVAREZ, Carmen, S. ,  BALDWIN, John, J. ,  LI, Ge ,  HUANG, Chia-Yu ,  JAMES, Ray, A. ,  BISHOP, W., Robert ,  WANG, James J-S ,  Desai, Jagdish A

IPC分类号： C07D221/16 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14 ,  C07D521/00 ,  A61K31/47 ,  A61K31/50 ,  A61K31/444 ,  A61K31/445 ,  A61K31/495 ,  A61K31/496 ,  A61K31/505 ,  A61P35/00

CPC分类号： C07D231/12 ,  C07D221/16 ,  C07D233/56 ,  C07D249/08 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14

摘要： Disclosed are novel tricyclic compounds represented by the formula (1.0) and a pharmaceutically acceptable salt or solvate thereof. The compounds are useful for inhibiting farnesyl protein transferase. Also disclosed are pharmaceutical compositions comprising compounds of formula 1.0. Also disclosed are methods of treating cancer using the compounds of formula 1.0.

公开(公告)号：EP1313725B1

公开(公告)日：2007-04-11

申请号：EP01968188.1

申请日：2001-08-28

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

发明人： NJOROGE, F., George ,  VIBULBHAN, Bancha ,  COOPER, Alan, B. ,  GUZI, Timothy ,  RANE, Dinanath, F. ,  MINOR, Keith, P. ,  DOLL, Ronald, J. ,  GIRIJAVALLABHAN, Viyyoor, Moopil ,  SANTHANAM, Bama ,  PINTO, Patrick, A. ,  ZHU, Hugh, Y. ,  KEERTIKAR, Kartik, M. ,  ALVAREZ, Carmen, S. ,  BALDWIN, John, J. ,  LI, Ge ,  HUANG, Chia-Yu ,  JAMES, Ray, A. ,  BISHOP, Robert, W. ,  WANG, James ,  DESAI, Jagdish, A.

IPC分类号： C07D401/06 ,  C07D401/04 ,  C07D401/14 ,  C07D221/16 ,  A61K31/435 ,  A61P35/00

CPC分类号： C07D231/12 ,  C07D221/16 ,  C07D233/56 ,  C07D249/08 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14

摘要： The present invention discloses novel tricyclic compounds represented by the formula (1.0), a prodrug thereof, or a pharmaceutically acceptable salt or solvate of the compound or of said prodrug useful for inhibiting farnesyl protein transferase. Also disclosed are pharmaceutical compositions comprising such compounds their preparation as well as methods of using them to treat proliferative diseases such as cancer.

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：EP1140904B1

公开(公告)日：2005-04-20

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：EP0989983B1

公开(公告)日：2004-08-11

申请号：EP98928886.5

申请日：1998-06-15

申请人： SCHERING CORPORATION ,  PHARMACOPEIA, INC.

发明人： COOPER, Alan, B. ,  DOLL, Ronald, J. ,  GIRIJAVALLABHAN, Viyyoor, M. ,  GANGULY, Ashit ,  READER, John, C. ,  BALDWIN, John, J. ,  HUANG, Chia-yu

IPC分类号： C07D401/14 ,  A61K31/55 ,  C07D401/04 ,  A61K31/495 ,  A61K31/44

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D405/14

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：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。

公开(公告)号：EP0931077A1

公开(公告)日：1999-07-28

申请号：EP97941476.0

申请日：1997-09-11

申请人： SCHERING CORPORATION

发明人： RANE, Dinanath, F. ,  COOPER, Alan, B. ,  MALLAMS, Alan, K. ,  DOLL, Ronald, J. ,  NJOROGE, F., George ,  TAVERAS, Arthur, G.

IPC分类号： A61K31 ,  A61P35 ,  C07D401

CPC分类号： C07D401/14

摘要： Novel tricyclic compounds of formula (1.0) or a pharmaceutically acceptable salt or solvate thereof, wherein: one of a, b, c and d represents N or NR9 wherein R?9 is O-, -CH¿3 or -(CH2)nCO2H wherein n is 1 to 3, and the remaining a, b, c and d groups represent CR?1 or CR2¿; or each of a, b, c, and d are independently selected from CR?1 or CR2¿; each R1 and each R2 is independently selected from H, halo, -CF¿3?, -OR?10, -COR10, -SR10¿, -S(O)¿tR?11 (wherein t is 0, 1 or 2), -SCN, -N(R10)2, -NR?10R11, -NO¿2, -OC(O)R10, -CO2R10, -OCO¿2R?11, -CN, -NHC(O)R10, -NHSO¿2R?10, -CONHR10, -CONHCH¿2?CH2OH, -NR?10COOR11, -SR11C(O)OR11, -SR11N(R75)¿2; y is 0 (zero) or 1; n is 0, 1, 2, 3, 4, 5 or 6; T is -CO-; -SO-; -SO2-; or -CR30R31; Z represents alkyl, aryl, aralkyl, heteroalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl, heterocycloalkylalkyl, -OR?40, -SR40, 1C-R40R42¿, (i), (ii), -NR40R42, (iii). 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 tricyclic 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：EP2483263A1

公开(公告)日：2012-08-08

申请号：EP10821040.2

申请日：2010-09-20

申请人： Schering Corporation

发明人： ZHU, Hugh, Y. ,  DESAI, Jagdish, A. ,  COOPER, Alan, B. ,  DOLL, Ronald, J.

IPC分类号： C07D403/00

CPC分类号： C07D417/14 ,  C07D401/10 ,  C07D401/14

摘要： Disclosed are the ERK inhibitors of formula 1.0: (Formula (A1)), and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine ring that can have a bridge or a fused ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula A1.