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

机译:新的二肽衍生物可用作神经肽Y激动剂和/或拮抗剂,可用于治疗心血管疾病,冠状动脉,脑或肾血管痉挛,肥胖症,贪食症和哮喘

摘要

N-Carbamylacyl dipeptide derivatives (I) are new: Peptide derivatives of formula (I) and their salts are new: R1 = a group of formula (i): n = 1-6, preferably 1-4; Ar = phenyl (optionally mono- or disubstituted by halogen or CF3) or naphthyl; 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 (ii) or (iii): or (c) CH2-W-CH2; W = a bond, O, S, NR6, CR4R5 or 3-7C cycloalkylidene; R4, R5 = H, 1-6C alkyl or phenyl; R6 = 1-6C alkyl or phenyl(1-3C)alkyl; 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, homo-phenylalanine or N-methyl-phenylalanine, in L or D configuration, optionally with protected side chains. Independent claims are also included for the following: a) amines of formula (II) and (b) carboxylic acids of formula (III):
机译:N-氨基甲酰基二肽衍生物(I)是新的:式(I)的肽衍生物及其盐是新的:R 1 =式(i)的基团:n = 1-6,优选1-4。 Ar =苯基(可选被卤素或CF3单或二取代)或萘基; A =(a)可含有O,S或N原子并通过两个相邻的C原子与羰基连接的3至6元(不饱和)任选桥连的环; (b)式(ii)或(iii)的基团:或(c)CH 2 -W-CH 2; W =键,O,S,NR 6,CR 4 R 5或3-7C亚环烷基; R 4,R 5 = H,1〜6C的烷基或苯基。 R 6 = 1-6C烷基或苯基(1-3C)烷基; B =呈L或D构型的Arg,Lys,Ser,His,Pro,Ala,Val,Phe,Phe(p-CN),Phe(pC(NH)NH2),Asn,Asp,Gly或Orn,可选带保护侧链D = Tyr,Phe,Cha,His,Cys,Thr,Ser,Asp,Glu,Tyr(3,5-di-Br),Phe(pF),Phe(p-Cl),Phe(p-NO2), L或D构型的苯甘氨酸,2-噻吩丙氨酸,环己基丙氨酸,高苯丙氨酸或N-甲基苯丙氨酸,可选带有受保护的侧链。还包括以下方面的独立权利要求:a)式(II)的胺和(b)式(III)的羧酸:

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