New benzamide derivatives useful as cysteine protease inhibitors for treating neurodegenerative diseases, neuronal damage, stroke, cranial trauma, Alzheimer's disease, etc.

摘要

Benzamide derivatives (I) are new. Benzamide derivatives of formula (I) and their tautomers, isomers and salts are new: R<1> = 1-6C alkyl optionally monosubstituted by Ar, cyclohexyl, indolyl or SMe; Ar = phenyl optionally substituted by 1-2 R<4> groups; R<4> = H, 1-4C alkyl, 1-4C alkoxy, OH, halogen, CN, COOH, 2-5C alkoxycarbonyl or 2-5C alkanoylamino; R<2> = N(R<5>)COR<6> or N(R<5>)SO2R<6>; R<3> = halogen, 1-6C alkyl, 2-5C alkanoylamino, 1-4C alkylsulfonylamino, NO2, 1-4C alkoxy, CN, COOH, CONH2, 2-5C alkoxycarbonyl, 1-4C alkylsulfonyl, phenylsulfonyl, 1-4C alkylsulfamoyl, SO2NH2 or NH2; A = aryl or heteroaryl, e.g. naphthyl, quinolyl, quinoxalinyl, benzimidazolyl, benzothienyl, quinazolinyl, phenyl, thienyl, imidazolyl, pyridyl, pyrimidinyl or pyridazinyl, all optionally substituted by R<9> and 0-2 R<8> groups; B = a bond; (CH2)m, (CH2)mQ(CH2)o, CH=CH, ethynylene, COCH=CH or NHCOCH=CH; Q = O, S, SO, SO2, CO, NHCO, CONH, NHSO2 or SO2NH; or A-B = a group of formula (i)-(iv): R<5> = H or 1-4C alkyl; R<6> = H, phenyl, naphthyl, or 1-6C alkyl optionally substituted by Ar; R<8> = H, 1-4C alkyl, 1-4C alkoxy, OH, halogen, CF3, NO2, NH2, CN, COOH, 2-5C alkoxycarbonyl, 2-5C alkanoylamino, phenyl, benzamido, 1-4C alkylsulfonylamino, phenylsulfonylamino, 1-4C alkylsulfonyl, pyridyl or phenylsulfonyl; R<9> = H or (CH2)pR<12>; R<12> = pyrrolidinyl, morpholinyl, piperidyl, homopiperazinyl, NR<10>R<13> or 4-R<10>-1-piperazinyl; R<10> = 1-6C alkyl optionally substituted by Ar'; Ar' = phenyl optionally substituted by 1-2 R<11> groups; R<11> = H, 1-4C alkyl, 1-4C alkoxy, OH, halogen, CF3, NO2, NH2, CN, COOH, 2-5C alkoxycarbonyl, 2-5C alkanoylamino, 1-4C alkylsulfonylamino or 1-4C alkylsulfonyl; R<13> = H or 1-6C alkyl; n = 0-2; m, q (sic; o and p are not defined) = 0-4.