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1. 发明申请

WO2005014577A9 NOVEL FARNESYL PROTEIN TRANSFERASE INHIBITORS AS ANTITUMOR AGENTS 审中-公开
标题翻译：新型蛋氨酸转运酶抑制剂作为抗菌剂
公开(公告)号：WO2005014577A9
公开(公告)日：2006-03-23
申请号：PCT/US2004025042
申请日：2004-08-04
申请人： SCHERING CORP , 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
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： A61P35/00 , C07D401/06 , A61K31/415 , C07D401/14
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.
摘要翻译：公开了式（I）的新型三环化合物及其药学上可接受的盐或溶剂化物。该化合物可用于抑制法呢基蛋白转移酶。还公开了包含式（I）化合物的药物组合物。还公开了式（I）化合物在制备用于治疗癌症的药物中的用途。

2. 发明专利

NZ534809A Farnesyl protein transferase inhibitors as antitumor agents 未知
公开(公告)号：NZ534809A
公开(公告)日：2007-12-21
申请号：NZ53480903
申请日：2003-02-25
申请人： SCHERING CORP , PHARMACOPEIA 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： A61K31/496 , A61K45/00 , A61P35/00 , A61P43/00 , C07D221/16 , C07D401/04 , C07D401/06 , C07D401/14 , C07D521/00 , C07D401/12 , C07D405/14 , C07D409/14 , C07D417/14 , A61K31/47 , A61K31/50 , A61K31/444 , A61K31/445 , A61K31/495 , A61K31/505
摘要： Disclosed is a compound of formula 1.0, wherein: one of a, b, c and d represents N or N+O-, and the remaining a, b, c and d groups represent carbon, wherein each carbon has an R1 or R2 group bound to said carbon; or each of a, b, c and d is carbon, wherein each carbon has an R1 or R2 group bound to said carbon; the dotted line represents optional bonds; X represents N or CH when the optional bond (to C11) is absent, and represents C when the optional bond (to C11) is present; at least one of A and B is: a substituent û(CH2)pû(C(R30)(R31))pûR9 wherein R30 and R31 are the same or different, and each p is independently selected; provided that for each ûC(R30)(R31)û group when one of R30 or R31 is selected from the group consisting of ûOH, =O, ûOR9a, ûNH2, ûNHR9a, ûN(R9a)2, ûN3, ûNHR9b and ûN(R9a)R9b, then the remaining R30 or R31 is selected from the group consisting of: H, alkyl, aryl and aralkyl; or a substituent û(CH2)pûC(R30)(R31)ûC(R32)(R33)ûR9 wherein R30 and R31 are the same or different; provided that when one of R30 or R31 is selected from the group consisting of ûOH, =O, ûOR9a, ûNH2, ûNHR9a, ûN(R9a)2, ûN3, ûNHR9b and ûN(R9a)R9b, then the remaining R30 or R31 is selected from the group consisting of: H, alkyl, aryl and aralkyl; and provided that when one of R31 or R32 is selected from the group consisting of ûOH, =O, ûOR9a, ûNH2, ûNHR9a, ûN(R9a)2, ûN3, ûNHR9b and ûN(R9a)R9b, then the remaining R31 or R32 is selected from the group consisting of: H, alkyl, aryl and aralkyl; and wherein at least one of R30 to R33 is selected from the group consisting of ûOR9a, ûNH2, ûNHR9a, ûN(R9a)2, ûN3, ûNHR9b and ûN(R9a)R9b; p is 0, 1, 2, 3 or 4; and the remaining substituents are as defined in the specification. The compounds are farnesyl protein transferase inhibitors useful as antitumour agents.

3. 发明专利

ES2284686T3 COMPUESTOS ANTITUMORALES TRICICLICOS QUE SON INHIBIDORES DE LA PROTEINA TRANSFERASA DE FARNESILO. 未知
公开(公告)号：ES2284686T3
公开(公告)日：2007-11-16
申请号：ES01968188
申请日：2001-08-28
申请人： SCHERING CORP , PHARMACOPEIA INC
发明人： NJOROGE F GEORGE , VIBULBHAN BANCHA , COOPER ALAN B , GUZI TIMOTHY , RANE DINANATH F , MINOR KEITH P
IPC分类号： C07D233/61 , A61K31/435 , C07D401/06 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/5513 , A61K45/00 , A61P35/00 , A61P43/00 , C07D221/16 , C07D401/04 , C07D401/10 , C07D401/14 , C07D405/06 , C07D409/06 , C07D409/12 , C07D413/06 , C07D413/12 , C07D521/00
摘要： Un compuesto de la **fórmula**, o una sal aceptable para uso farmacéutico, o solvato, de dicho compuesto, donde: uno de a, b, c y d representa N o N+O-, y los grupos restantes a, b, c y d representan carbono, donde cada carbono tiene un grupo R1 o R2 enlazado a dicho carbono; o cada a, b, c y d es carbono, donde cada carbono tiene un grupo R1 o R2 enlazado a dicho carbono; las líneas de puntos (---) representan enlaces opcionales; X representa N o CH cuando el enlace opcional está ausente, y representa C cuando el enlace opcional está presente; cuando se presenta el enlace opcional entre el átomo de carbono 5 y el átomo de carbono 6, entonces hay solo un sustituyente A enlazado al átomo de carbono 5, y hay solo un sustituyente B enlazado al átomo de carbono 6, y A o B es diferente de H; cuando no se presenta el enlace opcional entre el átomo de carbono 5 y el átomo de carbono 6, entonces hay dos sustituyentes A enlazados al átomo de carbono 5, y hay dos sustituyentes B enlazados al átomo decarbono 6, y donde por lo menos uno de los dos sustituyentes A o uno de los dos sustituyentes B es H, y donde por lo menos uno de los dos sustituyentes A o uno de los dos sustituyentes B es diferente de H; donde cada sustituyente A y B se seleccionan de modo independiente de: (1) -H; (2) -R9; (3) -R9-C(O)-R9; (4) -R9-CO2-R9a; (5) -C(O)NHR9; (6) -C(O)NH-CH2-C(O)-NH2; (7) -C(O)NHR26; (8) -(CH2)p(R9)2, donde cada R9 es igual o diferente; (9) -(CH2)pC(O)R9; (10) -(CH2)pC(O)R27a; (11) -(CH2)pC(O)N(R9)2, donde cada R9 es igual o diferente; (12) -(CH2)pC(O)NH(R9); (13) -(CH2)pNHC(O)R50; (14) -(CH2)pNHC(O)2R50; (15) -(CH2)pN(C(O)R27a)2, donde cada R27a es igual o diferente; (16) -(CH2)pNR51C(O)R27, o R51 y R27 tomados junto con los átomos a los cuales están enlazados forman un anillo heterocicloalquilo que consiste en 5 ó 6 miembros, siempre que cuando R51 y R27 forman un anillo, R51 no sea H; (17) -(CH2)pNR51C(O)NR27, o R51 y R27 tomados junto con los átomos a los cuales están enlazados forman unanillo heterocicloalquilo que consiste en 5 ó 6 miembros, siempre que cuando R51 y R27 forman un anillo, R51 no sea H; (18) -(CH2)pNR51C(O)N(R27a)2, donde cada R27a es igual o diferente; (19) -(CH2)pNHSO2N(R51)2, donde cada R51 es igual o diferente; (20) -(CH2)pNHCO2R50; (21) -(CH2)pCO2R51; (22) -NHR9

6. 发明专利

ZA200601052B Novel farnesyl protein transferase inhibitors as antitumor agents 未知
公开(公告)号：ZA200601052B
公开(公告)日：2007-05-30
申请号：ZA200601052
申请日：2006-02-06
申请人： SCHERING CORP
发明人： ZHU HUGH Y , DESAI JAGDISH A , RANE DINANATH F , GEORGE NJOROGE F , COOPER ALAN B , WANG JAMES J-S , DOLL RONALD J , GIRIJAVALLABHAN VIYYOOR M
IPC分类号： A61K20090101 , A61P20090101 , C07D20090101

7. 发明专利

NZ524246A Tricyclic antitumor compounds being farnesyl protein transferase inhibitors useful for treating cancer 未知
公开(公告)号：NZ524246A
公开(公告)日：2004-11-26
申请号：NZ52424601
申请日：2001-08-28
申请人： SCHERING CORP , PHARMACOPEIA 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： A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/5513 , A61K45/00 , A61P35/00 , C07D233/61 , A61P43/00 , C07D221/16 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D405/06 , C07D409/06 , C07D409/12 , C07D413/06 , C07D413/12 , C07D521/00 , A61K31/435
摘要： Tricyclic compounds represented by the formula (1.0), and their pharmaceutically acceptable salt or solvate that are useful for inhibiting farnesyl protein transferase are disclosed, wherein the variables shown in the formula (1.0) are as described in the specification. Also disclosed are pharmaceutical compositions comprising such compounds their preparation as well as methods of using them to treat proliferative diseases such as lung cancer, head and neck cancer, bladder cancer, breast cancer, prostate cancer and myeloid leukemia.

8. 发明专利

ES2194986T3 未知
公开(公告)号：ES2194986T3
公开(公告)日：2003-12-01
申请号：ES96911440
申请日：1996-04-03
申请人： SCHERING CORP , PHARMACOPEIA INC
发明人： DOLL RONALD J , MALLAMS ALAN K , AFONSO ADRIANO , RANE DINANATH F , NJOROGE F GEORGE , ROSSMAN RANDALL A
IPC分类号： A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4465 , A61K31/451 , A61K31/495 , A61K31/496 , A61K31/535 , A61P35/00 , A61P43/00 , C07D211/34 , C07D211/38 , C07D211/50 , C07D213/56 , C07D213/89 , C07D241/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/06 , C07D413/06 , C07D417/12 , A61K31/44 , C07D295/12 , C07D417/06

9. 发明专利

AT220400T 未知
公开(公告)号：AT220400T
公开(公告)日：2002-07-15
申请号：AT96911439
申请日：1996-04-03
申请人： SCHERING CORP
发明人： DOLL RONALD J , MALLAMS ALAN K , AFONSO ADRIANO , RANE DINANATH F , NJOROGE F GEORGE , ROSSMAN RANDALL R
IPC分类号： A61K31/55 , A61P35/00 , C07D401/12 , C07D403/06 , C07D471/04
摘要： Novel compounds of Formula (1.0) are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering a compound of the formula to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being.

10. 发明专利

CZ20011900A3 Substance, treatment method and pharmaceutical preparation in which the substance is comprised as well as use thereof for inhibition of farnesyl protein transferase 未知
公开(公告)号：CZ20011900A3
公开(公告)日：2002-02-13
申请号：CZ20011900
申请日：1999-12-16
申请人： SCHERING CORP
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： A61K31/496 , A61K31/5377 , A61K31/541 , A61P35/00 , A61P43/00 , C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D521/00 , C07D403/14 , A61K31/4545
摘要： Disclosed are compounds of formula (1.0), wherein R represents a cyclic moiety to which is bound an imodazolylalkyl group; R 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.

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