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1. 发明公开

EP0298135A1 Phenylalanine derivative and proteinase inhibitor 失效
标题翻译：苯丙氨酸蛋白酶抑制剂冯蛋白酶。
公开(公告)号：EP0298135A1
公开(公告)日：1989-01-11
申请号：EP87104691.8
申请日：1987-03-30
申请人： Okamoto, Shosuke , SHOWA DENKO KABUSHIKI KAISHA
发明人： Okamoto, Shosuke , Okada, Yoshio , Okunomiya, Akiko , Naito, Taketoshi , Kimura, Yoshio , Yamada, Morihiko , Ohno, Norio , Katsuura, Yasuhiro , Nojima, Hiroshi , Shishikura, Takashi
IPC分类号： C07C273/04 , C07C233/76 , C07C233/81 , C07C257/00 , C07D213/32 , C07D213/40 , C07D213/75 , C07D295/182
CPC分类号： C07D213/40 , A61K38/00 , C07C279/14 , C07C279/18 , C07D211/32 , C07D213/75 , C07K5/06078
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 R¹ and R² are, independently, (a) hydrogen, provided that both R¹ and R² 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) R¹ and R² 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.
摘要翻译：具有式（I）的苯丙氨酸衍生物： X表示氢，（b）羟基，（c）硝基或（d）可被苯基取代的C 1 -C 4烷氧基; Y表示，其中R 1和R 2独立地为（a）氢，条件是R 1和R 2不同时为氢; （b）苯基，其可被（i）苯基羰基取代，（ii）C 1 -C 4烷基羰基，（iii）可以被C 1 -C 4烷氧基羰基或羟基羰基进一步取代的C 1 -C 4烷基，（iv）C 2 -C 5 烯基，其可以进一步被C 1 -C 4烷氧基羰基取代，（v）三氟甲基; （c）可被C 1 -C 4烷氧基取代的吡啶基; （d）可被（i）羟基，（ⅱ）C 1 -C 4烷氧基羰基，（ⅲ）吡啶基或（ⅳ）苯基取代的C 1 -C 4烷基，其可进一步被C 1 -C 4烷基氨基羰基取代; （e）可被C 1 -C 4烷基取代的C 5 -C 7环烷基; 或（f）R 1和R 2可以与其连接的氮原子形成，（i）可被苯基羰基取代的哌啶子基或可以被C 1 -C 4烷氧基羰基取代的（ⅱ）吡咯烷基; 或其药学上可接受的盐。该苯丙氨酸衍生物作为蛋白酶抑制剂是有效的。

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