Method of treating cancer using FPT inhibitors and antineoplastic agents
申请人:Schering Corporation
公开号:US20040006087A1
公开(公告)日:2004-01-08
Disclosed is a method of treating cancer in a patient in need of such treatment comprising administering a therapeutically effective amount of an FPT inhibitor and therapeutically effective amounts of one or more antineoplastic agents. Methods of treating non small cell lung cancer, squamous cell cancer of the head and neck, CML, AML, non-Hodgkin's lymphoma and multiple myeloma are disclosed.
17 Beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases
申请人:SCHERING CORPORATION
公开号:US20040138226A1
公开(公告)日:2004-07-15
In its many embodiments, the present invention provides a novel class of compounds as inhibitors of type 3 17&bgr;-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 17&bgr;-hydroxysteroid dehydrogenase using such compounds or pharmaceutical compositions.
Disclosed are compounds of the formula:
1
wherein R
13
represents an imidazole ring; R
14
represents a carbamate, urea, amide or sulfonamide group; R
8
represents H when the alkyl chain between the amide group and the R
13
imidazole group is substituted, or R
8
represents a substituent such as arylalkyl, heteroarylalkyl or cycloalkyl; and the remaining substituents are as defined herein.
Also disclosed are compounds wherein R
8
is H, and the alkyl chain between the amide group and the R
13
imidazole group is unsubstituted.
Also disclosed is a method of treating cancer and a method of inhibiting farnesyl protein transferase using the disclosed compounds.
本发明公开了以下式子的化合物
1
其中 R
13
代表咪唑环
14
代表氨基甲酸酯、脲、酰胺或磺酰胺基团; R
8
代表 H,当酰胺基团与 R
13
咪唑基团之间的烷基链被取代时,R 8 代表 H,或 R
8
代表取代基,如芳基烷基、杂芳基烷基或环烷基;其余取代基如本文所定义。
还公开了一些化合物,其中 R
8
为 H,且酰胺基团与 R
13
咪唑基团之间的烷基链未被取代。
还公开了一种治疗癌症的方法和一种使用所公开化合物抑制法呢基蛋白转移酶的方法。
NOVEL INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE
申请人:Schering Corporation
公开号:EP1140909B1
公开(公告)日:2005-07-06
TRICYCLIC ANTITUMOR COMPOUNDS BEING FARNESYL PROTEIN TRANSFERASE INHIBITORS