WENDT MICHAEL D,DING HONG,KUNZER AARON R,SOUERS ANDREW J,HEXAMER LAURA,SONG XIAOHONG,SULLIVAN GERARD M,ELMORE STEVEN W,TAO ZHI-FU
申请号:
NZ70394110
公开号:
NZ703941A
申请日:
2010.01.15
申请国别(地区):
NZ
年份:
2016
代理人:
摘要:
Disclosed are benzamide compounds with a substituted sulfonyl group on the amide and substituted heteroalkyl group at the 4 position of the benzamideof formula (I) where the substituents are as disclosed in the specification. Examples of these compounds are: 4-(4-{ [2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl} piperazin-1-yl)-2-(1H-indol-5-yloxy)-N-(isoquinolin-5-ylsulfonyl)benzamide; 4-{ 4-[(4’-chlorobiphenyl-2-yl)methyl]piperazin-1-yl} -N-[(2-chloropyridin-3-yl)sulfonyl]benzamide; and 4-{ 4-[(4’-chlorobiphenyl-2-yl)methyl]piperazin-1-yl} -N-({ 5-[ethyl(trifluoroacetyl)amino]-1-naphthyl} sulfonyl)benzamide. The compounds inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein. Also disclosed is a composition comprising one of the compounds and the use of one of the compounds for the manufacture of a medicament for treating bladder cancer, brain cancer, breast cancer, bone marrow cancer, cervical cancer, chronic lymphocytic leukaemia, colorectal cancer, oesophageal cancer, hepatocellular cancer, lymphoblastic leukaemia, follicular lymphoma, a lymphoid malignancy of T-cell or B-cell origin, melanoma, myelogenous leukaemia, myeloma, oral cancer, ovarian cancer, non-small cell lung cancer, prostate cancer, small cell lung cancer or spleen cancer.