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1. 发明公开

EP0217286A1 Phenylalanine derivative and proteinase inhibitor 失效转让
标题翻译：苯丙氨酸和蛋白酶抑制剂。
公开(公告)号：EP0217286A1
公开(公告)日：1987-04-08
申请号：EP86113166.2
申请日：1986-09-24
申请人： Okamoto, Shosuke , SHOWA DENKO KABUSHIKI KAISHA
发明人： Okamoto, Shosuke , Okada, Yoshio , Okunomiya, Akiko , Naito, Taketoshi SHOWA DENKO K.K. , Kimura, Yoshio SHOWA DENKO K.K. , Yamada, Morihiko SHOWA DENKO K.K. , Ohno, Norio SHOWA DENKO K.K. , Katsuura, Yasuhiro SHOWA DENKO K.K. , Seki, Yumi SHOWA DENKO K.K.
IPC分类号： C07C233/57 , C07C233/63 , C07C257/00 , C07C311/30 , C07C311/35 , C07C323/31 , C07D207/16 , C07D211/16 , C07D211/32 , C07D211/58 , C07D211/62
CPC分类号： C07D213/30 , A61K38/00 , C07D211/16 , C07D211/32 , C07D211/62 , C07D213/40 , C07D213/643 , C07D213/75 , C07D239/42 , C07D295/185 , C07D307/14 , C07D401/12 , C07K5/06078
摘要： A phenylalanine derivative having the formula (I):
where R' and R 2 are independently hydrogen provided that both R' and R 2 are nof hydrogen at the same time;

C 1 -C 5 alkyl which may be substituted with hydroxy, hydroxycarbonyl, C 1 -C 4 alkoxycarbonyl, C 1 -C 4 alkyl- mercapto, C,-C4 alkoxy, carbamoyl, sulfamoyl, pyridyl, or phenyl which may further be substituted with nitro, C 1 -C 4 alkoxy, or halogen;
C 6 -C 3 cycloalkyl which may be substituted with hydroxy, C 1 -C 4 alkoxy, hydroxylcarbonyl, C 1 -C 4 alkoxycarbonyl, or C 1 -C 4 alkyl;
phenyl which may be substituted with halogen, nitro, trifluoromethyl, C,-C 4 alkoxy, C 1 -C 4 alkylmer- capto, C 1 -C 4 alkylcarbonyl, phenylcarbonyl, hydroxycarbonyl, C 1 -C 4 alkoxycarbonyl, carbamoyl, sulfamoyl, amidino, pyridylcarbonyl, or C 1 -C 6 alkyl which may further be substituted with C 1 -C 4 alkylcarbonyl, hydroxycarbonyl, or C 1 -C 4 alkoxycarbonyl;
pyridyl which may be substituted with halogen or C 1 -C 4 alkoxy;
pyrimidyl;
N-benzylazacyclohexyl; and
R' and R 2 may form with the nitrogen atom attached thereto a ring structure as morpholino; thiomorpholino; or piperidyl which may be substituted with phenylcarbonyl, benzyl, or C 1 -C 4 alkyl;
pyrrolidyl which may be substituted with hydroxycarbonyl or C 1 -C 4 alkoxycarbonyl; and
piperidine substituted with C 1 -C 4 alkyl, phenyl C 1 -C 4 alkyl, phenylcarbonyl, or C,-C 4 alkoxycarbonyl;
X is hydrogen; nitro; amino; or -OZ wherein Z is hydrogen: C 1 -C 4 alkyl; C 2 -C 4 alkenyl; benzyl which may be substituted with halogen, C 1 -C 4 alkyl, nitro, trifluoromethyl, hydroxycarbonyl, C 1 -C 4 alkoxycarbonyl, or cyano; phenylcarbonylmethyl, pyridylmethyl; phenyl which may be substituted with nitro or halogen; pyridyl or pyrimidyl which may be substituted with nitro; phenylsulfonyl which may be substituted with C 1 -C 4 alkyl; or benzyloxycarbonyl which may be substituted with halogen;
n is 4 to 10; and
the mark indicates that the configuration of the carbon may be either one of D-configuration, L-configuration and DL-configuration or a pharmaceutical 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：其中R1和R2独立地为氢，条件是R1和R2不同时为氢; 可以被羟基，羟基羰基，C 1 -C 4烷氧基羰基，C 1 -C 4烷基巯基，C 1 -C 4烷氧基，氨基甲酰基，氨磺酰基，吡啶基或可以进一步被硝基，C 1 -C 4烷氧基取代的苯基取代的C 1 -C 8烷基卤素; 可被羟基，C 1 -C 4烷氧基，羟基羰基，C 1 -C 4烷氧羰基或C 1 -C 4烷基取代的C 6 -C 8环烷基; 可以被卤素，硝基，三氟甲基，C 1 -C 4烷氧基C 1 -C 4烷基巯基，C 1 -C 4烷基羰基，苯基羰基，羟基羰基，C 1 -C 4烷氧基羰基，氨基甲酰基，氨磺酰基，脒基，吡啶基羰基或C 1 -C 6烷基取代的苯基，被C1-C4烷基羰基，羟基羰基或C1-C4烷氧基羰基取代; 可被卤素或C 1 -C 4烷氧基取代的吡啶基; 嘧啶; 的N- benzylazacyclohexyl; 并且R1和R2可以与其上连接的氮原子形成为环状结构作为吗啉代; 硫吗啉; 可被苯基羰基，苄基或C 1 -C 4烷基取代的哌嗪基; 可被羟基羰基或C 1 -C 4烷氧基羰基取代的吡咯烷基; 被C 1 -C 4烷基，苯基C 1 -C 4烷基，苯羰基或C 1 -C 4烷氧基羰基取代的哌啶子基; X是氢; 硝基; 氨基; 或-OZ，其中Z是氢; C 1 -C 4烷基; C 2 -C 4烯基; 可被卤素取代的苄基，C 1 -C 4烷基，硝基，三氟甲基，羟基羰基，C 1 -C 4烷氧基羰基或氰基; 苯基羰基; 吡啶; 可以被硝基或卤素取代的苯基; 可以被硝基取代的吡啶基或嘧啶基; 可被C 1 -C 4烷基取代的苯基磺酰基; 或可被卤素取代的苄氧基羰基; n为4〜10; 标记*表示碳的构型可以是D构型，L-构型和DL构型中的任一种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。

4. 发明公开

EP0183271A2 Lysin derivative and proteinase inhibitor 失效
标题翻译： Lysinderivat和蛋白酶抑制剂。
公开(公告)号：EP0183271A2
公开(公告)日：1986-06-04
申请号：EP85115142.3
申请日：1985-11-29
申请人： Okamoto, Shosuke , SHOWA DENKO KABUSHIKI KAISHA
发明人： Okamoto, Shosuke , Okada, Yoshio , Okunomiya, Akiko , Naito, Taketoshi SHOWA DENKO K.K. , Yamada, Morihiko SHOWA DENKO K.K. , Kimura, Yoshio SHOWA DENKO K.K. , Katsuura, Yasuhiro SHOWA DENKO K.K. , Suzuki, Hiroshi SHOWA DENKO K.K. , Ohno, Norio SHOWA DENKO K.K. , Seki, Yumi SHOWA DENKO K.K.
IPC分类号： C07C311/02 , C07C311/10 , C07K5/06 , C07K5/08 , C07D211/16 , C07D211/42 , C07D213/34 , C07D213/40 , C07D215/06 , C07D215/36 , C07D215/08
CPC分类号： C07D213/40 , A61K38/00 , C07C279/18 , C07C2601/14 , C07D211/16 , C07D211/22 , C07D211/42 , C07D211/60 , C07D211/62 , C07D213/34 , C07D215/08 , C07D215/36 , C07D215/42 , C07D295/185 , C07D295/192 , C07D307/91 , C07D311/16 , C07D405/12 , C07K5/06086
摘要： A lysine derivative having the general formula: A-Y-Lys- B (L-form) (A) wherein A represents

or
wherein X and X' independently represent hydrogen, halogen, alkyl, cycloalkyl, alkoxy, aryloxy, dialkylamino, alkylcarbonyl amino, arylcarbonyl amino, and n, is an integer of 3 to 6, n 2 is an integer of 1 to 3, and n 3 is an integer of 0 to 3; Y represents S0 2 or CO; -Lys- represents
B represents NR 1 R 2 , NZW, or tetrahydroquinolyl, wherein R' and R 2 independently represents hydrogen provided that both R' and R 2 cannot be hydrogen at the same time; alkyl substituted with carboxyl, alkoxycarbonyl, phenyl, hydroxyphenyl, or benzoyl; cycloalkyl which may be substituted with arylcarbonyl; cycloalkyl-alkyl which may be substituted with carboxyl, arylcarbonyl, or aralkyloxycar- bonyi; phenyl which may be substituted with halogen, nitro, cyano, trifluoromethyl, alkyl, alkoxy, alkoxycarbonyl, alkoxycarbonylalkyl, phenylalkyl which may be further substituted with dialkylamino, alkylcarbonyl, phenylalkenyl which may be further substituted with dialkylamino, phenoxy, pheny-Icarbonyl which may be further substituted with an amino, dialkylamino, alkoxycarbonyl, or nitro group, pyridylmethyl, phenyl hydroxyalkyl, alkylsulfonyl, or alkoxycarbonyl alkylcarbonyl, coumaryl which may be substituted with alkyl; quinolyl; adamantyl; norbornyl; or tetrahydronaphthyl; and
W is hydrogen; hydroxyl; carboxyl; aminocarbonyl; alkyl; alkoxy carbonyl; phenyl; phenylalkyl which may be substituted with dialkylamino; or phenylcarbonyl which may be substituted with alkoxycarbonyl; or tetrahydroquinolyl; and or the pharmaceutically acceptable salt thereof. This lysine derivative is effective as a proteinase inhibitor.
摘要翻译：具有以下通式的赖氨酸衍生物：AY-Lys-B（L型）（A）其中A表示，其中X和Xmin独立地表示氢，卤素，烷基，环烷基，烷氧基，芳氧基，二烷基氨基，烷基羰基氨基，芳基羰基氨基，n1为3〜6的整数，n2为1〜3的整数，n3为0〜3的整数。 Y表示SO2或CO; -Lys-表示 B表示NR 1 R 2，NZW或四氢喹啉基，其中R 1和R 2独立地表示氢，条件是R 1和R 2都不能为氢气同时; 被羧基取代的烷基，烷氧基羰基，苯基，羟基苯基或苯甲酰基; 可被芳基羰基取代的环烷基; 可被羧基，芳基羰基或芳烷氧基羰基取代的环烷基 - 烷基; 可以被卤素，硝基，氰基，三氟甲基，烷基，烷氧基，烷氧基羰基，烷氧基羰基，可以进一步被二烷基氨基取代的苯基烷基，烷基羰基，可被二烷基氨基进一步取代的苯基烯基，苯氧基，可以进一步取代的苯基羰基氨基，二烷基氨基，烷氧基羰基或硝基，吡啶基甲基，苯基羟基烷基，烷基磺酰基或烷氧基羰基烷基羰基，可被烷基取代的芳香芳基; 喹啉; 金刚; 冰片; 或四氢萘基; 并且Z是 - （CH 2）m1 @ H（CH 2）m m或 - （CH 2）m1 - （CH 2）m 2; W是氢，羟基; 羧基; 羰基; 烷基; 烷氧基羰基; 苯基; 可被二烷基氨基取代的苯基烷基; 或可被烷氧基羰基取代的苯基羰基; 或四氢喹啉基; 和m1 + m2 = 3或4或其药学上可接受的盐。该赖氨酸衍生物作为蛋白酶抑制剂是有效的。

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