PHENYLALANINE DERIVATIVES AND PROTEINASE INHIBITION

摘要

A phenylalanine derivative having the formula (I): X represents hydrogen, (b) hydroxy, (c) nitro, or (d) C1-C4 alkyloxy which may be substituted with phenyl; Y represents wherein R<1> and R<2> are, independently, (a) hydrogen, provided that both R<1> and R<2> are not hydrogen at the same time; (b) phenyl, which may be substituted with (i) phenylcarbonyl, (ii) C1-C4 alkylcarbonyl, (iii) C1-C4 alkyl, which may be further substituted with C1-C4 alkoxycarbonyl or hydroxycarbonyl, (iv) C2-C5 alkenyl, which may further be substituted with C1-C4 alkoxycarbonyl, (v) trifluoromethyl; (c) pyridyl, which may be substituted with C1-C4 alkoxy; (d) C1-C4 alkyl, which may be substituted with (i) hydroxy, (ii) C1-C4 alkoxycarbonyl, (iii) pyridyl, or (iv) phenyl, which may be further substituted with C1-C4 alkylaminocarbonyl; (e) C5-C7 cycloalkyl, which may be substituted with C1-C4 alkyl; or (f) R<1> and R<2> may form, with the nitrogen atom attached thereto, (i) piperidino, which may be substituted with phenylcarbonyl or (ii) pyrrolidyl, which may be substituted with C1-C4 alkoxycarbonyl; or a pharmaceutically acceptable salt thereof. This phenylalanine derivative is effective as a proteinase inhibitor.