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    • 4. 发明专利
    • Reverse amide compounds as protein deacetylase inhibitors and methods of use thereof
    • NZ601655A
    • 2014-10-31
    • NZ60165511
    • 2011-01-21
    • ACETYLON PHARMACEUTICALS INC
    • VAN DUZER JOHN HBRADNER JAMES ELLIOTTMAZITSCHEK RALPHOGIER WALTERXIE DEJIANYU NANHUANG GUOXIANG
    • C07D239/42A61K31/505A61P25/00A61P35/00C07C233/78
    • Disclosed herein are reverse amide compounds of formula (I), wherein the substituents are as defined within the specification, processes for their preparation, compositions comprising said compounds and uses thereof. Said compounds are useful as protein deacetylase inhibitors (HDAC), particularly HDAC6, as such is useful in the treatment of lung cancer, colon cancer, breast cancer, prostate cancer, liver cancer, pancreas cancer, brain cancer, kidney cancer, ovarian cancer, stomach cancer, skin cancer, bone cancer, gastric cancer, breast cancer, pancreatic cancer, glioma, gliobastoma, hepatocellular carcinoma, papillary renal carcinoma, head and neck squamous cell carcinoma, leukemias, lymphomas, myelomas, solid tumors, Wilson’s disease, spinocerebellar ataxia, prion disease, Parkinson’s disease, Huntington’s disease, amy trophic 15 lateral sclerosis, amyloidosis, Alzheimer’s disease, Alexander’s disease, alcoholic liver disease, cystic fibrosis, Pick’s Disease, spinal muscular dystrophy or Lewy body dementia. Particularly preferred compounds include: 2-(diphenylamino)-N-(7-(hydroxyamino)-7-oxoheptyl)pyrimidine-5-carboxamide; N-(7-(hydroxyamino)-7-oxoheptyl)-4-(phenyl(pyridin-2-yl)amino)benzamide; 4-((2-cyanophenyl)(methyl)amino)-N-(7-(hydroxyamino)-7-oxoheptyl)-N-methylbenzamide; 2-(2,6-dimethylphenylamino)-N-(7-(hydroxyamino)-7-oxoheptyl)-N-methylpyrimidine-5-carboxamide; 3-(2,6-dimethylphenylamino)-N-(7-(hydroxyamino)-7-oxoheptyl)benzamide; 4-((2,6-dimethylphenyl)(pyrimidin-2-yl)amino)-N-(7-(hydroxyamino)-7-oxoheptyl)-N-methylbenzamide; 4-(ethoxydiphenylmethyl)-N-(7-(hydroxyamino)-7-oxoheptyl)benzamide.