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    N.sup.2 -dansyl-L-arginine derivatives, and the pharmaceutically acceptable acid addition salts thereof
    41.
    发明授权
    N.sup.2 -dansyl-L-arginine derivatives, and the pharmaceutically acceptable acid addition salts thereof 失效

    公开(公告)号：US3978045A

    公开(公告)日：1976-08-31

    申请号：US496939

    申请日：1974-08-13

    申请人： Shosuke Okamoto ,  Ryoji Kikumoto ,  Yoshikuni Tamao ,  Shinji Tonomura ,  Kazuo Ohkubo

    发明人： Shosuke Okamoto ,  Ryoji Kikumoto ,  Yoshikuni Tamao ,  Shinji Tonomura ,  Kazuo Ohkubo

    IPC分类号： C07D307/12 ,  C07D225/02

    CPC分类号： C07D307/12

    摘要： N.sup.2 -dansyl-L-arginine esters and amides having the formula ##SPC1##Or the acid addition salts thereof with a pharmaceutically acceptable acid, wherein R is selected from the group consisting of(1) alkoxy, alkenyloxy, alkynyloxy, and cycloalkoxy, respectively, containing not more than 10 carbon atoms, aralkyloxy of not more than 15 carbon atoms, tetrahydrofurfuryloxy, and alkoxy of not more than 10 carbon atoms substituted with an alkoxy group of not more than 10 carbon atoms, halogen or nitro; ##EQU1## wherein R.sub.1 and R.sub.2 are members selected from the group consisting of hydrogen, alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, alkenyl, and alkyl, wherein said member has no more than 10 carbon atoms, and wherein said alkyl may be substituted with a member selected from the group consisting of alkoxy, alkoxycarbonyl, arylcarbamoyl, acyl, acyloxy, N,N-polymethylenecarbamoyl, respectively, containing not more than 10 carbon atoms, and carboxyl; and ##EQU2## wherein Z is a divalent group containing up to 10 carbon atoms, which consists of more than one group selected from the group consiting of methylene --CH.sub.2, monosubstituted methylene ##EQU3## wherein R.sub.3 is selected from the group consisting of alkyl, acyl, alkoxy, and alkoxycarbonyl, respectively, containing not more than 10 carbon atoms, and carbonyl, and disubstituted methylene ##EQU4## wherein R.sub.4 and R.sub.5 are alkyl groups of not more than 10 carbon atoms,And which may further contain at least one member selected from the group consisting of oxy--O--, thio --S--, cycloalkylene of not more than 10 carbon atoms, imino ##EQU5## alkyl substituted imino ##EQU6## wherein R.sub.6 is an alkyl group of not more than 10 carbon atoms, acyl substituted imino ##EQU7## wherein R.sub.7 is an alkyl group of not more than 10 carbon atoms, phenylene ##SPC2## and carbonyl ##EQU8## which completes the ##EQU9## ring together with the said methylene, mono-substituted methylene or disubstituted methylene.

    N.sup.2 -naphthalenesulfonyl-L-arginine derivatives, and the pharmaceutically acceptable acid addition salts thereof
    42.
    发明授权
    N.sup.2 -naphthalenesulfonyl-L-arginine derivatives, and the pharmaceutically acceptable acid addition salts thereof 失效

    公开(公告)号：US4062963A

    公开(公告)日：1977-12-13

    申请号：US671435

    申请日：1976-03-29

    申请人： Shosuke Okamoto ,  Ryoji Kikumoto ,  Kazuo Ohkubo ,  Shinji Tonomura ,  Yoshikuni Tamao

    发明人： Shosuke Okamoto ,  Ryoji Kikumoto ,  Kazuo Ohkubo ,  Shinji Tonomura ,  Yoshikuni Tamao

    IPC分类号： A61K38/00 ,  C07D211/16 ,  C07D211/32 ,  C07D211/46 ,  C07D211/60 ,  C07D211/90 ,  C07D295/185 ,  A61K31/445

    CPC分类号： C07D295/185 ,  C07D211/16 ,  C07D211/32 ,  C07D211/46 ,  C07D211/60 ,  C07D211/90 ,  A61K38/00 ,  Y10S514/822

    摘要： N.sup.2 -naphthalenesulfonyl-L-arginine esters and amides having the formula ##STR1## or the acid addition salts thereof with a pharmaceutically acceptable acid, wherein R is selected from the class consisting of (1) alkoxy, alkenyloxy, cycloalkoxy and halogenated alkoxy, respectively containing not more than 10 carbon atoms, aralkyloxy of not more than 15 carbon atoms, and alkoxy of not more than 10 carbon atoms substituted with an alkoxy group of not more than 10 carbon atoms; ##STR2## wherein R.sub.1 and R.sub.2 are members selected from the class consisting of hydrogen, alkyl, aryl, alkenyl and cycloalkyl, respectively containing not more than 10 carbon atoms, and aralkyl and cycloalkylalkyl, respectively containing not more than 15 carbon atoms, and substituted alkyl containing not more than 20 carbon atoms, said substituent being selected from the class consisting of alkoxy, alkoxycarbonyl, acyl, acyloxy, arylcarbamoyl and N,N-polymethylenecarbamoyl, respectively containing not more than 10 carbon atoms, and carboxy; and ##STR3## wherein Z is a divalent group containing up to 10 carbon atoms, which consists of more than one group selected from the class consisting of methylene --CH.sub.2 --, monosubstituted methylene ##STR4## wherein R.sub.3 is selected from the class consisting of alkyl, acyl, alkoxy and alkoxycarbonyl, respectively containing not more than 10 carbon atoms, and carbamoyl, and disubstituted methylene ##STR5## wherein R.sub.4 and R.sub.5 are alkyl groups of not more than 10 carbon atoms, and which may further contain at least one member selected from the class consisting of oxy-O-, thio -S-, cycloalkylene of not more than 10 carbon atoms, imino ##STR6## alkyl-substituted imino ##STR7## wherein R.sup.6 is an alkyl group of not more than 10 carbon atoms, acyl-substituted imino ##STR8## wherein R.sub.7 is an alkyl group of not more than 10 carbon atoms, and phenylene ##STR9## which may be arranged in any order and complete the ##STR10## ring together with the said methylene, monosubstituted methylene or disubstituted methylene, and R' is a member selected from the class consisting of 1-naphthyl substituted 2-, 3-, 4-, 6-, 7- or 8-dialkylamino, respectively, containing not more than 20 carbon atoms, and 1-naphthyl substituted with 5-dialkylamino containing 3-20 carbon atoms, 2-naphthyl substituted dialkylamino containing not more than 20 carbon atoms.

    N.sup.2 -dansyl-L-arginine derivatives, and the pharmaceutically acceptable acid addition salts thereof
    44.
    发明授权
    N.sup.2 -dansyl-L-arginine derivatives, and the pharmaceutically acceptable acid addition salts thereof 失效

    公开(公告)号：US4670420A

    公开(公告)日：1987-06-02

    申请号：US118096

    申请日：1980-02-04

    申请人： Shosuke Okamoto ,  Ryoji Kikumoto ,  Yoshikuni Tamao ,  Shinji Tonomura ,  Kazuo Ohkubo

    发明人： Shosuke Okamoto ,  Ryoji Kikumoto ,  Yoshikuni Tamao ,  Shinji Tonomura ,  Kazuo Ohkubo

    IPC分类号： C07D207/16 ,  C07D211/16 ,  C07D211/32 ,  C07D211/62 ,  C07D215/08 ,  C07D265/30 ,  C07D295/185 ,  C07D307/12 ,  C07C143/80 ,  A61K37/02

    CPC分类号： C07D265/30 ,  C07D207/16 ,  C07D211/16 ,  C07D211/32 ,  C07D211/62 ,  C07D215/08 ,  C07D295/185 ,  C07D307/12

    摘要： N.sup.2 -dansyl-L-arginine esters and amides having the formula ##STR1## or the acid addition salts thereof with a pharmaceutically acceptable acid, wherein R is selected from the group consisting of (1) alkoxy, alkenyloxy, alkynyloxy, and cycloalkoxy, respectively, containing not more than 10 carbon atoms, aralkyl of not more than 15 carbon atoms, tetrahydrofurfuryloxy, and alkoxy of not more than 10 carbon atoms substituted with an alkoxy group of not more than 10 carbon atoms, halogen or nitro; (2) ##STR2## wherein R.sub.1 and R.sub.2 are members selected from the group consisting of hydrogen, alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, alkenyl, and alkyl, wherein said member has no more than 10 carbon atoms, and wherein said alkyl may be substituted with a member selected from the group consisting of alkoxy, alkoxycarbonyl, arylcarbamoyl, acyl, acyloxy, N,N-polymethylenecarbamoyl, respectively, containing not more than 10 carbon atoms, and carboxyl; and (2) ##STR3## wherein Z is a divalent group containing up to 10 carbon atoms, which consists of more than one group selected from the group consisting of methylene --CH.sub.2, monosubstituted methylene ##STR4## wherein R.sub.3 is selected from the group consisting of alkyl, acyl, alkoxy, and alkoxycarbonyl, respectively, containing not more than 10 carbon atoms, and carbamoyl, and disubstituted methylene ##STR5## wherein R.sub.4 R.sub.5 are alkyl groups of not more than 10 carbon atoms, and which may further contain at least one member selected from the group consisting of oxy--O--, thio --S--, cycloalkylene of not more than 10 carbon atoms, imino ##STR6## alkyl substituted imino ##STR7## wherein R.sub.6 is an alkyl group of not more than 10 carbon atoms, acyl substituted imino ##STR8## wherein R.sub.7 is an alkyl group of not more than 10 carbon atoms, phenylene ##STR9## and carbonyl ##STR10## which completes the ring together with the said methylene, mono-substituted methylene or disubstituted methylene.

    N.sup.2 -Naphthalenesulfonyl-L-arginine derivatives, and the pharmaceutically acceptable acid addition salts thereof
    47.
    发明授权
    N.sup.2 -Naphthalenesulfonyl-L-arginine derivatives, and the pharmaceutically acceptable acid addition salts thereof 失效
    N {HU 2 {B-萘磺酰基-L-精氨酸衍生物及其药学上可接受的酸加成盐

    公开(公告)号：US4069329A

    公开(公告)日：1978-01-17

    申请号：US760740

    申请日：1977-01-19

    申请人： Shosuke Okamoto ,  Ryoji Kikumoto ,  Yoshikuno Tamao ,  Kazuo Ohkubo ,  Shinji Tonomura

    发明人： Shosuke Okamoto ,  Ryoji Kikumoto ,  Yoshikuno Tamao ,  Kazuo Ohkubo ,  Shinji Tonomura

    IPC分类号： A61K38/00 ,  C07D211/16 ,  C07D211/32 ,  C07D211/46 ,  C07D211/90 ,  C07D295/185 ,  A61K31/445

    CPC分类号： C07D295/185 ,  C07D211/16 ,  C07D211/32 ,  C07D211/46 ,  C07D211/90 ,  A61K38/00 ,  Y10S514/822

    摘要： N.sup.2 -naphthalenesulfonyl-L-arginine esters and amides having the formula ##STR1## or the acid addition salts thereof with a pharmaceutically acceptable acid, wherein R is selected from the class consisting of (1) alkoxy, alkenyloxy, cycloalkoxy and halogenated alkoxy, aralkyloxy, and alkoxy substituted with an alkoxy group; ##STR2## wherein R.sub.1 and R.sub.2 are members selected from the class consisting of hydrogen, alkyl, aryl, alkenyl and cycloalkyl, and aralkyl and cycloalkylalkyl, and substituted alkyl, said substituent being selected from the class consisting of alkoxy, alkoxycarbonyl, acyl, acyloxy, arylcarbamoyl and N,N-polymethylenecarbamoyl, and carboxy; and ##STR3## wherein Z is a divalent group containing up to 10 carbon atoms, which consists of more than one group selected from the class consisting of methylene, monosubstituted methylene; and disubstituted methylene, and which may further contain at least one member selected from the class consisting of oxy-O-, thio --S--, cycloalkylene, imino, alkyl-substituted imino, acyl-substituted imino, and phenylene, which may be arranged in any order and complete the ##STR4## ring together with the said methylene, monosubstituted methylene or disubstituted methylene, and R' is a member selected from the class consisting of 1-naphthyl substituted 2-, 3-, 4-, 6-, 7- or 8-dialkylamino, respectively, containing not more than 20 carbon atoms, and 1-naphthyl substituted with 5-dialkylamino containing 3 - 20 carbon atoms, 2-naphthyl substituted dialkylamino containing not more than 20 carbon atoms.

    摘要翻译： 具有式“IMAGE”1的N 2 - 萘磺酰基-L-精氨酸酯和酰胺或其药学上可接受的酸的酸加成盐，其中R选自（1）烷氧基，烯氧基，环烷氧基和卤代烷氧基， 芳烷氧基和被烷氧基取代的烷氧基; （2）其中R1和R2是选自氢，烷基，芳基，烯基和环烷基，芳烷基和环烷基烷基和取代烷基的成员，所述取代基选自烷氧基，烷氧基羰基， 酰基，酰氧基，芳基氨基甲酰基和N，N-聚亚甲基氨基甲酰基和羧基; （3）其中Z是含有至多10个碳原子的二价基团，其由多于一个选自亚甲基，单取代的亚甲基的基团组成; 和二取代的亚甲基，并且其还可以含有选自氧基-O-，硫代-S-，亚环烷基，亚氨基，烷基取代的亚氨基，酰基取代的亚氨基和亚苯基中的至少一种，其可以被布置 以任何顺序并与所述亚甲基，单取代的亚甲基或二取代的亚甲基一起完成环，R'是选自1-，3-，4-，6-， 分别含有不超过20个碳原子的7-或8-二烷基氨基，以及含有3-20个碳原子的5-二烷基氨基取代的1-萘基，含有不超过20个碳原子的2-萘基取代的二烷基氨基。

    N.sup.2 -Naphthalenesulfonyl-L-arginine derivatives, and the pharmaceutically acceptable acid addition salts thereof
    48.
    发明授权
    N.sup.2 -Naphthalenesulfonyl-L-arginine derivatives, and the pharmaceutically acceptable acid addition salts thereof 失效
    N {HU 2 {B-萘磺酰基-L-精氨酸衍生物及其药学上可接受的酸加成盐

    公开(公告)号：US4168307A

    公开(公告)日：1979-09-18

    申请号：US844181

    申请日：1977-10-21

    申请人： Shosuke Okamoto ,  Ryoji Kikumoto ,  Yoshikuno Tamao ,  Kazuo Ohkubo ,  Shinji Tonomura

    发明人： Shosuke Okamoto ,  Ryoji Kikumoto ,  Yoshikuno Tamao ,  Kazuo Ohkubo ,  Shinji Tonomura

    IPC分类号： A61K38/00 ,  C07D211/16 ,  C07D211/32 ,  C07D211/46 ,  C07D211/60 ,  C07D211/90 ,  C07D295/185 ,  A61K31/445

    CPC分类号： C07D295/185 ,  C07D211/16 ,  C07D211/32 ,  C07D211/46 ,  C07D211/60 ,  C07D211/90 ,  A61K38/00

    摘要： N.sup.2 -naphthalenesulfonyl-L-arginine amides having the formula ##STR1## or the acid addition salts thereof with a pharmaceutically acceptable acid wherein R.sub.1 is alkenyl of not more than 10 carbon atoms, or substituted alkyl containing not more than 20 carbon atoms wherein said substituent is a member selected from the class consisting of alkoxy, alkoxycarbonyl, arylcarbamoyl acyl, acyloxy, N,N-polymethylenecarbamoyl and carboxy, and R.sub.2 is aryl, cycloalkyl, aralkyl or cycloalkylalkyl, respectively containing not more than 15 carbon atoms and R' is 1-naphthyl substituted with a member selected from the class consisting of 2-dialkylamino, 3-dialkylamino, 4-dialkylamino, 6-dialkylamino, 7-dialkylamino, 8-dialkylamino, respectively containing not more than 20 carbon atoms, and 5-dialkylamino containing 3-20 carbon atoms; or 2-naphthyl substituted with dialkylamino containing not more than 20 carbon atoms.

    摘要翻译： 具有式“IMAGE”的N 2 - 萘磺酰基-L-精氨酸酰胺或其酸加成盐与其药物上可接受的酸（其中R 1为不大于10个碳原子的链烯基）或取代的不超过20个碳原子的烷基，其中所述取代基 是选自烷氧基，烷氧基羰基，芳基氨基甲酰基酰基，酰氧基，N，N-多亚甲基氨基甲酰基和羧基的成员，R2是分别含有不超过15个碳原子和R'为1的芳基，环烷基，芳烷基或环烷基烷基 - 被选自分别含有不超过20个碳原子的2-二烷基氨基，3-二烷基氨基，4-二烷基氨基，6-二烷基氨基，7-二烷基氨基，8-二烷基氨基，和含有 3-20个碳原子; 或由不多于20个碳原子的二烷基氨基取代的2-萘基。

    Phenylalanine derivative and proteinase inhibitor
    50.
    发明授权
    Phenylalanine derivative and proteinase inhibitor 失效

    公开(公告)号：US4895842A

    公开(公告)日：1990-01-23

    申请号：US912480

    申请日：1986-09-29

    申请人： Shosuke Okamoto ,  Yoshio Okada ,  Akiko Okunomiya ,  Taketoshi Naito ,  Yoshio Kimura ,  Morihiko Yamada ,  Norio Ohno ,  Yasuhiro Katsuura ,  Yumi Seki

    发明人： Shosuke Okamoto ,  Yoshio Okada ,  Akiko Okunomiya ,  Taketoshi Naito ,  Yoshio Kimura ,  Morihiko Yamada ,  Norio Ohno ,  Yasuhiro Katsuura ,  Yumi Seki

    IPC分类号： A61K38/00 ,  C07D211/16 ,  C07D211/32 ,  C07D211/62 ,  C07D213/30 ,  C07D213/40 ,  C07D213/64 ,  C07D213/643 ,  C07D213/75 ,  C07D239/42 ,  C07D295/185 ,  C07D307/14 ,  C07D401/12 ,  C07K5/065

    CPC分类号： C07D213/30 ,  C07D211/16 ,  C07D211/32 ,  C07D211/62 ,  C07D213/40 ,  C07D213/643 ,  C07D213/75 ,  C07D239/42 ,  C07D295/185 ,  C07D307/14 ,  C07D401/12 ,  C07K5/06078 ,  A61K38/00

    摘要： A phenylalanine derivative having the formula (I): ##STR1## where R.sup.1 and R.sup.2 are independently hydrogen provided that both R.sup.1 and R.sup.2 are not hydrogen at the same time;C.sub.1 -C.sub.8 alkyl which may be substituted with hydroxy, hydroxycarbonyl, C.sub.1 -C.sub.4 alkoxycarbonyl, C.sub.1 -C.sub.4 alkylmercapto, C.sub.1 -C.sub.4 alkoxy, carbamoyl, sulfamoyl, pyridyl, or phenyl which may further be substituted with nitro, C.sub.1 -C.sub.4 alkoxy, or halogen;C.sub.6 -C.sub.8 cycloalkyl which may be substituted with hydroxy, C.sub.1 -C.sub.4 alkoxy, hydroxylcarbonyl, C.sub.1 -C.sub.4 alkoxycarbonyl, or C.sub.1 -C.sub.4 alkyl;phenyl which may be substituted with halogen, nitro, trifluoromethyl, C.sub.1 -C.sub.4 alkoxy C.sub.1 C.sub.4 alkylmercapto, C.sub.1 -C.sub.4 alkylcarbonyl, phenylcarbonyl, hydroxycarbonyl, C.sub.1 -C.sub.4 alkoxycarbonyl, carbamoyl, sulfamoyl, amidino, pyridylcarbonyl, or C.sub.1 -C.sub.6 alkyl which may further be substituted with C.sub.1 -C.sub.4 alkylcarbonyl, hydroxycarbonyl, or C.sub.1 -C.sub.4 alkoxycarbonyl;pyridyl which may be substituted with halogen or C.sub.1 -C.sub.4 alkoxy;pyrimidyl;N-benzylazacyclohexyl; andR.sup.1 and R.sup.2 may form with the nitrogen atom attached thereto a ring structure as morpholino; thiomorpholino; piperazino which may be substituted with phenylcarbonyl, benzyl, or C.sub.1 -C.sub.4 alkyl;pyrrolidyl which may be substituted with hydroxycarbonyl or C.sub.1 -C.sub.4 alkoxycarbonyl; andpiperidino substituted with C.sub.1 -C.sub.4 alkyl, phenyl C.sub.1 -C.sub.4 alkyl, phenycarbonyl, or C.sub.1 -C.sub.4 alkoxycarbonyl;X is hydrogen; nitro; amino; or --OZ wherein Z is hydrogen; C.sub.1 -C.sub.4 alkyl; C.sub.2 -C.sub.4 alkenyl; benzyl which may be substituted with halogen, C.sub.1 -C.sub.4 alkyl, nitro, trifluoromethyl, hydroxycarbonyl, C.sub.1 -C.sub.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.sub.1 -C.sub.4 alkyl; or benzyloxycarbonyl which may be substituted with halogen;n is 4 to 10; andthe 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.