| 摘要 |
N-Carbamylacyl dipeptide derivatives (I) are new. Peptide derivatives of formula (I) and their salts are new: R<1>, R<2> = H, 1-6C alkyl (optionally mono- or disubstituted by phenyl, mono- or dihalophenyl, pyrrolidinyl, morpholino, perhydroazepinyl, NH2, 1-6C alkylamino or di(1-6C alkyl)amino), phenyl or mono- or dihalophenyl, or R<1> = H; and R<2> = a group of formula (i) or (ii): or NR<1>R<2> = morpholino or a group of formula (iii): n = 2 or 3; R<3> = H, 1-6C alkyl (optionally mono- or disubstituted by di(1-6C alkyl)amino, 3-6C cycloalkyl, phenyl, mono- or dihalophenyl, nitrophenyl or methylenedioxyphenyl), 3-7C cycloalkyl, phenyl, mono- or dihalophenyl, nitrophenyl, amidino or N1,N2-dicyclohexylamidino; 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, NR<6>, CR<4>R<5> or 3-7C cycloalkylidene; R<4>, R<5> = H, 1-6C alkyl or phenyl; R<6> = 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, Orn or an amino acid residue of formula (vi): 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.
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