| 摘要 |
<p>Acetic acid derivatives of formula H2N(NH)C-X-Y-CO-Z-CH(Q1)COOQ2 (I), their hydrates, solvates and salts. In (I), Q1 = H, CH3 or phenyl. Q2 = H, phenyl-alkyl or physiologically-cleavable alkyl. X = 1,4-phenylene, 2,5- or 3,6-pyridylene or 1,4-piperidylene, which is bound to Y via the 4-C atom. Y = -(CH2)n-CONH-CH(Q3)-(CH2)m- (where n = 0-2 and m = 1-3); -CONH-CH2-CH(Q4)-, -(CH2)2-NHCO-CH2-, -NHCO-(CH2)3-, or a group of formula (a), (b) or (c). In the formulae, Q3 = H, CH3, phenyl, COOH, -COO-alkyl, -CONH-(CH2)2-COOH or -CONH-(CH2)2-COO-alkyl. Q4 = H, CH3 or phenyl. Z = 1,4-piperazinyl, 1,4-piperidinyl (which is bound to the CO group via the 1-N atom) or a group of formula -NH-CH(R1)- or -NH-CH(COR2). R1 = H, CH3, phenyl or COO-alkyl. R2 = an alpha-amino carboxylic acid linked via the amino group (or its ester or amide) or a group of formula -NH-(CH2)2-Ar, -CO2R2, an optionally mono- or dialkylated -CONH2 group, or a pyrrolidinoyl or piperidinoyl. Ar = phenyl optionally substituted by alkyl, alkoxy, -COOH, -CO-alkyl, -O(CH2)p-COOH (p = 1-4), O(CH2)p-COO-alkyl, -CONH2, -CONH-alkyl, -CO(alkyl)2, pyrrolidinoyl or piperidinoyl.</p> |
