New anhydro-statin-phosphono:pyrrolidine(s) and -piperidine(s) - useful as antiviral cpds. in human and animal medicine, active against e.g. HIV

摘要

Pyrrolidine and piperidine-substd. pseudopeptide derivs. of formula (I) and their physiologically acceptable salts are new. W = H, or a typical amino protecting gp., opt. branched 1-6C alkyl or alkenyl (each opt. substd. by 6-10C aryl), R3CO-, R5R4NCO- or R6SO2-; R3 = H, CF3, opt. branched 1-8C alkoxy, 1-18C alkyl (opt. substd. with 6-10C aryl or pyridyl), 6-10C aryl (opt. substd. by halogen, CF3, CF3O or opt. branched 1-8C alkyl), 3-7C cycloalkyl, indolyl, pyridyl, morpholino, piperazinyl, R8YCH2CH(R7)-, R9COOCH(R7)-, R10S(O)mNHCH(R7)-, T-NH(CH2)p-, (v), (R7CH2)2 or (R11)2PO(CH2)sCH(R7)-; R7 = Ph or naphthyl; R8, R10 and R10 = each opt. branched 1-17C alkyl (opt. substd. with Ph or naphthyl) or 6-10C aryl (opt. substd. with 1-4C alkyl); m = 0, 1 or 2; T = morpholino or cyclohexyl; p = 1, 2 or 3; Y and Y' = each CO or SO2; t = 0-1; R11 = opt. different OH or 1-8C alkoxy; s = 1 or 2; R4 and R5 = each H, 6-10C aryl (opt. substd. by opt. branched 1-6C alkyl or halogen), 3-7C cycloalkyl or opt. branched 1-18C alkyl (opt. substd. by pyridyl; R6 = opt. branched 1-8C alkyl; A, B (and D) = a bond or a gp. of formula (i)-(iv) n and n1 = each 1 or 2; r = 0 or 1; z = 0 or 1; R12 = H or opt. branched 1-8 alkyl; R13 = 3-8C cycloalkyl, 6-10C aryl, H or opt. branched 1-8C alkyl, 5-6 membered heterocycle or indolyl in which the corresp. NH functions are opt. protected by 1-6C alkyl); R15 and R15 = each H, opt. branched 1-8C alkyl or Ph; R16 = OH, benzyloxy, 1-6C alkoxy or -NR14R15; R1 = 3-8C cycloalkyl, opt. branched 1-10C alkyl or alkenyl n = 1-2; R2 = -PO(R11)z1-COR17 or -CONR4R5; R17 = opt. branched 1-8C alkoxy opt. substd. by Ph. USE/ADVANTAGE - (I) can be used as antiviral agents in human and animal medicine. (I) are esp. effective against retroviruses. (34pp Dwg.No.0/0)