New amino acid derivatives useful as neuropeptide Y agonists and/or antagonists for treating cardiovascular disorders, coronary, cerebral or renal vasospasms, obesity, bulimia and asthma

摘要

N-Carbamylacyl amino acid derivatives (I) are new. Amino acid derivatives of formula (I) and their salts are new: R1, R2 = H, 1-6C alkyl (optionally mono- or disubstituted by Ar, piperidinyl, pyrrolidinyl, morpholino, perhydroazepinyl, NH2, 1-6C alkylamino or di(1-6C alkyl)amino) or Ar, or NR1R2 = morpholino or a group of formula (i): n = 2 or 3; Ar = phenyl optionally mono- or disubstituted by halogen, NO2, 1-3C alkoxy or CF3; R3 = H, 1-6C alkyl (optionally mono- or disubstituted by di(1-6C alkyl)amino, 3-6C cycloalkyl, Ar or methylenedioxyphenyl), 3-7C cyloalkyl, Ar, amidino, N1,N2-dicyclohexylamidino or a group of formula (ii) or (iii): Q, U = CH2, CO or NH, provided that Q and U can be the same only when they are CH2; A = (a) a 3- to 6-membered (un)saturated optionally bridged ring that may contain an O, S or N atom and is linked to the carbonyl groups through two adjacent C atoms; (b) a group of formula (iv) or (v): or (c) CH2-W-CH2; W = a bond, O, S, NR6, CR4R5 or 3-7C cycloalkylidene; R6 = 1-6C alkyl or phenyl(1-3C)alkyl; R4, R5 = H, 1-6C alkyl or phenyl; B = Arg, homo-Arg, His or Orn in L or D configuration, optionally with protected side chains; G = 1-4C alkoxy, NH2, NHR, 4-methyl-1-piperazinyl, NH(CH2)xR' or a group of formula (vi): R = 1-4C alkyl optionally substituted by phenyl or p-aminophenyl; x = 2 or 3; R' = OH, 1-4C alkoxy or 4-diphenylmethyl-1-piperazinyl; E = 2-6C alkylene (optionally substituted by phenyl) or o-, m- or p-phenylenedimethylene; X, Y = CH2, CHPh or NPh, or X-Y = o-phenylene. An Independent claim is also included for compounds of formula (IIa): R3 = a group of formula (ii) or (iii).