| 摘要 |
3-Amidino-N-sulphonyl-phenylalanine derivatives (I) are new. 3-Amidino-N-sulphonyl-phenylalanine derivatives (I) in L- or D-form or as racemates and their addition salts are new. R<1> = (a) OH; alkoxy; cycloalkoxy; aralkoxy; benzyl; or phenylethyl; (b) NR<4>R<5>; (c) piperidyl, 2-, 3- or 4-(1-4C alkyl or OH)-piperidyl or a group of formula (i) or (ii) each optionally fused with an aromatic or cycloaliphatic ring; and a CH2 group in formula (i) or (ii) is optionally substituted with OH, COOH, alkyl or aralkyl; (d) N<4>-R<7>-piperazin-1-yl; (e) CO-X; (f) aralkyl optionally ring-substituted with halo, alkyl, alkoxy, OH or NO2; (g) CONR'R"; CSNR'R"; or CH2-CONR'R"; (h) SO2Y; (i) cycloalkyl optionally substituted with OH or oxo; (j) optionally substituted heteroaryl or C-bonded heterocycloaliphatic group; or (k) (CH2)q-X<1>; R<2> = alkyl; optionally substituted aryl or heteroaryl; or a camphor group; R<3> = H or alkyl; n = 0 or 1; R<4>, R<5> = both H or both alkyl; or R<4> = H and R<5> = alkyl, optionally substituted aralkyl, cycloalkylalkyl, optionally substituted NH2, aryl or heteroaryl; m = 1 or 2; R<6> = defined as R<1> in (a), (b) or (d); p and r = 1 or 2, but p + r = 2 or 3; R<7> = alkyl; optionally substituted aryl; saturated or unsaturated alkylcarbonyl, alkoxycarbonyl or alkoxy; or optionally substituted phenoxy or benzyloxycarbonyl; X = H or optionally substituted alkyl, aryl, heteroaryl or cycloalkyl; R', R" = both H or both alkyl; or R' = H and R" = alkyl, aryl, phenyl; or NR'R" forms a ring; Y = optionally substituted alkyl, aryl or heteroaryl; or NRaRb; Ra, Rb = H or alkyl; q = 1-8; X<1> = OH; alkoxy; aralkoxy; aryloxy; hydroxy-alkoxy; acyloxy; halo; NMe2, NEt2; NPr2; or a N-bonded ring. The full definitions are given in the DEFINITIONS (Full Definitions) Field
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