N.sup.2 alkoxynaphthylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof
AssigneesMitsubishi Chemical Industries Limited, Shosuke Okamoto
InventorsShosuke Okamoto, Akiko Hijikata, Ryoji Kikumoto, Yoshikuni Tamao, Kazuo Ohkubo, Tohru Tezuka, Shinji Tonomura
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Abstract
N.sup.2 -alkoxynaphthylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis in mammals.
Claims4
N.sup.2 -alkoxynaphthylsulfonyl-L-argininamides having the formula:
- ##STR66## and the pharmaceutically acceptable salts thereof, wherein R.sub.1 is naphthyl substituted with at least one C.sub.1 -C.sub.5 alkoxy;
- R.sub.2 is piperidino substituted with --COOR.sub.3 wherein R.sub.3 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.6 -C.sub.10 aryl, C.sub.7 -C.sub.12 aralkyl and 5-indanyl, said substituted piperidino being optionally substituted with one or more substituents which, alike or different, are selected from the group consisting of C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxy, phenyl, alkoxycarbonyl or carboxy;
- and the --COOR.sub.3 radical is at the 2 or 3-position of the piperidine radical.
A method for inhibiting activity and suppressing activation of thrombin in vivo, which comprises introducing into a mammal a pharmaceutically effective amount of an N.sup.2 -alkoxynaphthylsulfonyl-L-argininamide having the formula:
- ##STR68## or the pharmaceutically acceptable salt thereof, wherein R.sub.1 is naphthyl substituted with at least one C.sub.1 -C.sub.5 alkoxy;
- R.sub.2 is piperidino substituted with --COOR.sub.3 wherein R.sub.3 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.6 -C.sub.10 aryl, C.sub.7 -C.sub.12 aralkyl and 5-indanyl, said substituted piperidino being optionally substituted with one or more substituents, which, alike or different, are selected from the group consisting of C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxy, phenyl, alkoxycarbonyl or carboxy;
- and the --COOR.sub.3 radical is at the 2 or 3-position of the piperidino radical.
Dependencies are inferred from the claim text.