公开(公告)号：JPS5283655A

公开(公告)日：1977-07-12

申请号：JP25476

申请日：1976-01-01

Applicant: MITSUBISHI CHEM IND ,  OKAMOTO SHOSUKE

Inventor： OKAMOTO SHIYOUSUKE ,  KIKUMOTO RIYOUJI ,  TAMAO YOSHIKUNI ,  OOKUBO KAZUO ,  TEZUKA TOORU ,  TONOMURA SHINJI ,  HIJIKATA AKIKO

IPC: A61K31/325 ,  A61K31/335 ,  A61K31/357 ,  A61P7/00 ,  A61P7/02 ,  C07D307/91 ,  C07D311/14 ,  C07D311/58 ,  C07D311/80 ,  C07D311/82 ,  C07D319/18 ,  C07D319/24 ,  C07D321/10 ,  C07D405/12

Abstract: PURPOSE:N -Substituted-L-argininamides of the formula I [R is a chain or cyclic amino group, etc. (e.g. alkylamino, benzylamino, piperidino, morpholino, etc.); and R' is 6-chromanyl, coumarinyl, 1,4-benzodioxan-6-yl,2-dibenzofuranyl, etc.], and their acid salts. For example, 4-ethyl-1-(N -6-courmarinesulfonyl)-L-arginyl)-piperidine may be cited.

公开(公告)号：JPS5246059A

公开(公告)日：1977-04-12

申请号：JP12117375

申请日：1975-10-07

Applicant: MITSUBISHI CHEM IND ,  OKAMOTO SHOSUKE

Inventor： OKAMOTO AKISUKE ,  KIKUMOTO RIYOUJI ,  TAMAO YOSHIKUNI ,  OOKUBO KAZUO ,  TEZUKA TOORU ,  TONOMURA SHINJI ,  HIJIKATA AKIKO

IPC: A61K31/18 ,  A61K31/22 ,  A61P7/02 ,  C07C67/00 ,  C07C301/00 ,  C07C303/40 ,  C07C311/29

Abstract: PURPOSE:The title compound, useful as thrombosis remedy having the action of antithrombin, is prepared by the esterification of N -naphthalenesulfonylarginines.

公开(公告)号：JPS5219653A

公开(公告)日：1977-02-15

申请号：JP9641775

申请日：1975-08-08

Applicant: MITSUBISHI CHEM IND ,  OKAMOTO SHOSUKE

Inventor： OKAMOTO SHIYOUSUKE ,  KIKUMOTO RIYOUJI ,  TAMAO YOSHIKUNI ,  OOKUBO KAZUO ,  TEZUKA TOORU ,  TONOMURA SHINJI ,  HIJIKATA AKIKO

IPC: C07D317/70 ,  A61K31/335 ,  A61K31/357 ,  A61P7/02 ,  C07D307/78 ,  C07D307/91 ,  C07D311/02 ,  C07D311/58 ,  C07D311/80 ,  C07D311/82 ,  C07D319/14 ,  C07D319/18 ,  C07D319/24 ,  C07D321/10 ,  C07D405/12 ,  C07K1/113 ,  C07K5/06 ,  C07K14/81

Abstract: PURPOSE:Preparation of title compounds useful as anticoagulants having powerful activity upon thrombin.

公开(公告)号：JPS5283665A

公开(公告)日：1977-07-12

申请号：JP24976

申请日：1976-01-01

Applicant: MITSUBISHI CHEM IND ,  OKAMOTO SHOSUKE

Inventor： OKAMOTO SHIYOUSUKE ,  KIKUMOTO RIYOUJI ,  TAMAO YOSHIKUNI ,  OOKUBO KAZUO ,  TEZUKA TOORU ,  TONOMURA SHINJI ,  HIJIKATA AKIKO

IPC: C07D311/08 ,  A61K31/37 ,  A61K31/443 ,  A61K31/445 ,  A61K31/495 ,  A61K31/535 ,  A61P7/02 ,  C07D211/16 ,  C07D295/18 ,  C07D405/12 ,  C07D413/12

Abstract: PURPOSE:NG-Substituted-N -coumarinsulfonylargininamides of the formula I [one of X and Y is a protective group of a guanidino group, and the other is H or a protective group of the guanidino group; R is-NR1R2 (R1 and R2 are H, alkyl, aralkyl, etc.) or a cyclic amino group (e.g. 1-polymethyleneiminyl, 3oxazolidinyl, morpholino, etc.); and R' is H or alkyl], and their acid salts. For example, 4-ethyl-1-(NG-nitro-N -(6-coumarinsulfonyl)-L-arginyl) piperidine may be cited.

公开(公告)号：JPS5283654A

公开(公告)日：1977-07-12

申请号：JP25076

申请日：1976-01-01

Applicant: MITSUBISHI CHEM IND ,  OKAMOTO SHOSUKE

Inventor： OKAMOTO SHIYOUSUKE ,  KIKUMOTO RIYOUJI ,  TAMAO YOSHIKUNI ,  OOKUBO KAZUO ,  TEZUKA TOORU ,  TONOMURA SHINJI ,  HIJIKATA AKIKO

IPC: C07D319/18 ,  A61K31/335 ,  A61K31/357 ,  A61P7/00 ,  C07D307/91 ,  C07D311/80 ,  C07D311/82 ,  C07D321/10 ,  C07D405/12

Abstract: PURPOSE:NG-Substituted-N -substituted-argininamides of the formula I [one of X and Y is a protective group of a guanidino group, and the other is H or a protective group of the guanidino group; R is a chain or cyclic amino group, etc. (e.g. piperidino, alkylamino, etc.); and R' is 6-chromanyl, 1,4-benzodioxan-6-y1, 2dibenzofuranyl, etc.], and their acid salts. For example, 4-ethyl-1-(NG-nitro-N (1,4-benzodioxane-6-sulfonyl)-L-arginine) piperidine may be cited.

公开(公告)号：JPS5283648A

公开(公告)日：1977-07-12

申请号：JP24176

申请日：1976-01-01

Applicant: MITSUBISHI CHEM IND ,  OKAMOTO SHOSUKE

Inventor： OKAMOTO SHIYOUSUKE ,  KIKUMOTO RIYOUJI ,  TAMAO YOSHIKUNI ,  OOKUBO KAZUO ,  TEZUKA TOORU ,  TONOMURA SHINJI ,  HIJIKATA AKIKO

IPC: C07D295/18 ,  A61K31/17 ,  A61K31/18 ,  A61K31/395 ,  A61K31/435 ,  A61K31/495 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/54 ,  A61P7/02 ,  C07C67/00 ,  C07C301/00 ,  C07C311/18 ,  C07C311/19 ,  C07D209/44 ,  C07D211/00 ,  C07D211/16 ,  C07D211/32 ,  C07D211/46 ,  C07D211/62 ,  C07D215/08 ,  C07D217/06 ,  C07D221/04 ,  C07D223/04 ,  C07D225/02 ,  C07D233/00 ,  C07D295/00

Abstract: PURPOSE:NG-Substituted-N -(5,6,7,8-tetrahydro-1,2-naphthylenesulfonyl) argininamides of the formula I [X and Y are protective groups of a guanidino group (one of them may be H); R is a group of the formula II (R1 and R2 are H, C1-10 alkyl, etc.) or the formula III(Z is a bivalent group in which 20 or less of groups of methylene, mono-substituted methylene, oxy, thio, etc. are bonding); R' is 5,6,7,8-tetrahydro-1-naphthyl, etc.], or their acid salts. For example, NGnitro-N -(5,6,7,8-tetrahydro-1-naphthalenesulfonyl)-N-benzyl-N-met hyl-L-argininamide may be cited.

公开(公告)号：JPS5283647A

公开(公告)日：1977-07-12

申请号：JP25576

申请日：1976-01-01

Applicant: MITSUBISHI CHEM IND ,  OKAMOTO SHOSUKE

Inventor： OKAMOTO SHIYOUSUKE ,  KIKUMOTO RIYOUJI ,  TAMAO YOSHIKUNI ,  OOKUBO KAZUO ,  TEZUKA TOORU ,  TONOMURA SHINJI ,  HIJIKATA AKIKO

IPC: C07D295/18 ,  A61K31/18 ,  A61K31/335 ,  A61K31/357 ,  A61K31/395 ,  A61P7/02 ,  C07C67/00 ,  C07C301/00 ,  C07C311/19 ,  C07C311/29 ,  C07D207/02 ,  C07D209/44 ,  C07D211/00 ,  C07D211/16 ,  C07D211/32 ,  C07D211/46 ,  C07D211/62 ,  C07D223/04 ,  C07D225/02 ,  C07D241/04 ,  C07D295/00 ,  C07D319/16 ,  C07D319/22

Abstract: PURPOSE:N -Naphthalenesulfonyl-L-arginine derivatives of the formula I [R is a group of the formula II (R1 is C1-10 alkyl, etc.), the formula III(R2 and R3 are H, C1-10 alkyl, etc.), or the formula IV (Z is a bivalent group in which 20 or less of groups of methylene, mono-substituted methylene, oxy, thio, etc. are bonding); and R' is a group of the formula V (R'' and R''' are C1-10 alkyl; and in the case R'' and R''' are bonding, -R''-R'''- is C1-10 alkylene)] and their acid salts. For example, N -(6,7-dimethoxy-2-naphthalenesulfonyl)-L-arginine propyl ester may be cited.

公开(公告)号：JPS5283645A

公开(公告)日：1977-07-12

申请号：JP24876

申请日：1976-01-01

Applicant: MITSUBISHI CHEM IND ,  OKAMOTO SHOSUKE

Inventor： OKAMOTO SHIYOUSUKE ,  KIKUMOTO RIYOUJI ,  TAMAO YOSHIKUNI ,  OOKUBO KAZUO ,  TEZUKA TOORU ,  TONOMURA SHINJI ,  HIJIKATA AKIKO

IPC: C07D295/18 ,  A61K31/17 ,  A61K31/18 ,  A61K31/395 ,  A61K31/435 ,  A61K31/495 ,  A61K31/535 ,  A61K31/5375 ,  A61P7/02 ,  C07C67/00 ,  C07C301/00 ,  C07C311/18 ,  C07C311/42 ,  C07D209/44 ,  C07D211/00 ,  C07D211/16 ,  C07D211/32 ,  C07D211/46 ,  C07D211/62 ,  C07D215/08 ,  C07D217/06 ,  C07D223/04 ,  C07D223/14 ,  C07D225/02 ,  C07D241/02 ,  C07D265/28 ,  C07D279/12

Abstract: PURPOSE:NG-Substituted-N -naphthalenesulfonylargininamides of the formula I [X and Y are protective groups of a guanidino group (one of them may be H); R is a group of the formula II (R1 and R2 are H, C1-10 alkyl, etc.) or the formula III(Z is a bivalent group in which 20 or less of groups of methylene, mono-substituted methylene, oxy, thio, etc. are bonding); and R' is 1-naphthyl or 2-naphthyl], or their acid salts. For example, 4-ethyl-1-(NG-nitro-N -(1-naphthalenesulfonyl)L-arginyl) piperidine may be cited.

公开(公告)号：JPS5242863A

公开(公告)日：1977-04-04

申请号：JP11852575

申请日：1975-10-01

Applicant: MITSUBISHI CHEM IND ,  OKAMOTO SHOSUKE

Inventor： OKAMOTO SHIYOUSUKE ,  KIKUMOTO RIYOUJI ,  TAMAO YOSHIKUNI ,  OOKUBO KAZUO ,  TEZUKA TOORU ,  TONOMURA SHINJI ,  HIJIKATA AKIKO

IPC: A61K31/18 ,  A61K31/395 ,  A61P7/02 ,  C07C15/24 ,  C07C67/00 ,  C07C301/00 ,  C07C303/38 ,  C07C311/29 ,  C07D209/44 ,  C07D211/16 ,  C07D211/32 ,  C07D211/46 ,  C07D211/62 ,  C07D405/12

Abstract: PURPOSE:The title compounds, having preventive action for coagulation of blooad and the action for anti-trombin, are prepared by the reaction of arginine esters of their amides with substituted naphthalenesulfonylhalogenides.

公开(公告)号：JPS5223057A

公开(公告)日：1977-02-21

申请号：JP9836875

申请日：1975-08-13

Applicant: MITSUBISHI CHEM IND ,  OKAMOTO SHOSUKE

Inventor： OKAMOTO SHIYOUSUKE ,  KIKUMOTO RIYOUJI ,  TAMAO YOSHIKUNI ,  OOKUBO KAZUO ,  TEZUKA TOORU ,  TONOMURA SHINJI ,  HIJIKATA AKIKO

IPC: C07D295/18 ,  A61K31/18 ,  A61K31/215 ,  A61K31/275 ,  A61K31/33 ,  A61P7/02 ,  C07C67/00 ,  C07C301/00 ,  C07C303/40 ,  C07C311/41 ,  C07C311/42 ,  C07D207/16 ,  C07D209/02 ,  C07D209/44 ,  C07D209/72 ,  C07D211/16 ,  C07D211/32 ,  C07D211/36 ,  C07D211/46 ,  C07D211/62 ,  C07D215/00 ,  C07D215/08 ,  C07D265/30 ,  C07D295/00

Abstract: PURPOSE:Simple preparation of N -naphthalenesulfonyl alginamides, useful as retarder of thrombin (a protease), in good yield.