| 摘要 |
The invention relates to novel aspartyl dipeptide of formula (I): R1-NHC1H(CH2COOH)CO-X-NH-C2R2R3R4 (I) wherein R1 is a hydrogen atom or a hydrocarbon group having from 1 to 13 carbon atoms; R2 and R3 are each, independently, an alkyl group having from 1 to 3 carbon atoms, or C2, R2 and R3 together form a cycloalkyl group having from 3 to 6 carbon atoms, or R2 is a hydrogen atom and R3 is an alkylthioalkyl group having from 2 to 7 carbon atoms, an alkyl-sulfinylalkyl group having from 2 to 7 carbon atoms, an alkylsulfonylalkyl group having from 2 to 7 carbon atoms or an alkoxycarbonylmethyl group having from 2 to 7 carbon atoms; R4 is a phenyl group; a benzyl group; a cyclohexyl group; a cyclohexylmethyl group; a phenyl group substituted at the 2-, 3- or 4-position with a substituent selected from the group consisting of F, Cl, Br, I, a hydroxyl group, an alkoxy group having from 1 to 6 carbon atoms, a cyano group, a nitro group, an acetyl group, an amino group and an acetylamino group; a phenyl group substituted at the position 2- and 3-positions or in the 3- and 4-positions with a substituent selected from the group consisting of a methylenedioxy group, a trimethylene group and a tetramethylene group, a 2-, 3- or 4-pyridyl group; a 2- or 3-furyl group; or a 2- or 3-thienyl group; X is an .alpha.-amino acid residue selected from the group consisting of D-alanine, D-.alpha.-aminobutyric acid, D-norvaline, D-valine, D-norleucine, D-leucine, D-isoleucine, D-alloisoleucine, D-t-leucine, D-serine, D-O-methylserine, D-threonine, D-O-methylthreonine, D-allothreonine, D-O-methylallothreonine, D-S-methyl-cysteine, D-methionine, D-phenyl-glycine, D-furylglycine and L-furylglycine, or X is a residue of a cyclic or acyclic .alpha.,.alpha.-dialkylamino acid having from 3 to 6 carbon atoms; the configuration at the C1-position is (S); the configuration at the C2-position is (R) or (S) when at least two of R2, R3 and R4 are different; and physiologically acceptable salts thereof. |
