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1. 发明专利

AT409065T 未知
公开(公告)号：AT409065T
公开(公告)日：2008-10-15
申请号：AT03790505
申请日：2003-12-15
申请人： SCHERING CORP
发明人： GUZI TIMOTHY , LIU YI-TSUNG , DOLL RONALD , SAKSENA ANIL , GIRIJAVALLABHAN VIYYOOR , PACHTER JONATHAN
IPC分类号： A61P5/28 , A61K31/4545 , A61K31/473 , A61K31/496 , A61P35/00 , C07D401/14
摘要： In its many embodiments, the present invention provides a novel class of compounds as inhibitors of type 3 17beta-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 17beta-hydroxysteroid dehydrogenase using such compounds or pharmaceutical compositions.

2. 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

3. 发明专利

AT378336T 未知
公开(公告)号：AT378336T
公开(公告)日：2007-11-15
申请号：AT03786514
申请日：2003-09-17
申请人： SCHERING CORP
发明人： DWYER MICHAEL , GUZI TIMOTHY , PARUCH KAMIL , DOLL RONALD , KEERTIKAR KARTIK , GIRIJAVALLABHAN VIYYOOR
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
摘要： In its many embodiments, the present invention provides a novel class of imidazo[1,2-a]pyridine compounds 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.

5. 发明专利

AT364608T 未知
公开(公告)号：AT364608T
公开(公告)日：2007-07-15
申请号：AT03749317
申请日：2003-09-03
申请人： SCHERING CORP , PHARMACOPEIA DRUG DISCOVERY
发明人： GUZI TIMOTHY , PARUCH KAMIL , DWYER MICHAEL , DOLL RONALD , GIRIJAVALLABHAN VIYYOOR , DILLARD LAWRENCE , TRAN VINH , HE ZHEN MIN , JAMES RAY , PARK HAENGSOON
IPC分类号： C07D487/04 , A61K31/519 , A61P25/00 , A61P35/00
摘要： In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds 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.

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

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.

9. 发明专利

HK1036279A1 Farnesyl protein transferase inhibitors. 未知
公开(公告)号：HK1036279A1
公开(公告)日：2001-12-28
申请号：HK01107119
申请日：2001-10-11
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 , C07D , A61K , A61P
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.

10. 发明专利

TR200101755T2 未知
公开(公告)号：TR200101755T2
公开(公告)日：2001-09-21
申请号：TR200101755
申请日：1999-12-16
申请人： SCHERING CORP
发明人： TAVERAS ARTHUR G , DOLL RONALD J , COOPER ALAN B , FERREIRA JOHAN A , GUZI TIMOTHY , MALLAMS ALAN K , RANE DINANATH F , GIRIJAVALLABHAN VIYYOOR M , AFONSO ADRIANO , AKI CYNTHIA J , CHAO JIANPING , ALVAREZ CARMEN , KELLY JOSEPH M , LALWANI TARIK , DESAI JAGDISH A , WANG JAMES J S , WEINSTEIN JAY
IPC分类号： A61K31/496 , A61P35/00 , A61P35/02 , A61P43/00 , C07D401/12 , C07D401/14 , C07D403/12 , C07D521/00 , C07D413/14 , A61K31/445 , A61K31/44 , A61K31/55
摘要： Disclosed are compounds of formula (1.0) wherein R represents an imidazole ring; R represents a carbamate, urea, amide or sulfonamide group; R represents H when the alkyl chain between the amide group and the R imidazole group is substituted, or R represents a substituent such aa arylalkyl, heteroarylalkyl or cycloalkyl; and the remaining substituents are as defined herein. Also disclosed are compounds wherein R is H, and the alkyl chain between the amide group and the R imidazole group is unsubstituted. Also disclosed is a method of treating cancer and a method of inhibiting farnesyl protein transferase using the disclosed compounds.

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