New dipeptide 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-(homo)piperazinylcarbonylacyl dipeptide derivatives (I) are new. Dipeptide derivatives of formula (I) and their salts are new: R<3> = a group of formula (i) or (ii): n = 2 or 3; 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 (iii) or (iv): or (c) CH2-W-CH2; W = a bond, O, S, NR<6>, CR<4>R<5> or 3-7C cycloalkylidene; R<6> = 1-6C alkyl or phenyl(1-3C)alkyl; R<4>, R<5> = H, 1-6C alkyl or phenyl; B = Arg, Lys, Ser, His, Pro, Ala, Val, Phe, Phe(p-CN), Phe(p-C(NH)NH2), Asn, Asp, Gly or Orn in L or D configuration, optionally with protected side chains; D = Tyr, Phe, Cha, His, Cys, Thr, Ser, Asp, Glu, Tyr(3,5-di-Br), Phe(p-F), Phe(p-Cl), Phe(p-NO2), phenylglycine, 2-thienylalanine, cyclohexylalanine, homophenylalanine or N-methyl-phenylalanine, in L or D configuration, optionally with protected side chains. An Independent claim is also included for carboxylic acids of formula (II):