N.sup.2 -naphthalenesulfonyl-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 -naphthalenesulfonyl-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.
Claims11
N.sup.2 -naphthalenesulfonyl-L-arginamides having the formula (I):
- ##STR50## and the pharmaceutically acceptable salts thereof, wherein R.sub.1 is selected from the group consisting of naphthyl, 5,6,7,8-tetrahydronaphthyl and naphthyl substituted with at least one substituent selected from the group consisting of halo, hydroxy, C.sub.1 -C.sub.10 alkyl and C.sub.2 -C.sub.20 dialkylamino;
- R.sub.2 is selected from the group consisting of C.sub.2 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkoxyalkyl, C.sub.2 -C.sub.10 alkylthioalkyl, C.sub.7 -C.sub.15 aralkyl, C.sub.3 -C.sub.10 cycloalkyl and C.sub.4 -C.sub.10 cycloalkylalkyl;
- R.sub.3 is hydrogen;
- and n is an integer of 1, 2 or 3.
A method of inhibiting activity and suppressing activation of thrombin in vivo, which comprises administering to a mammal, a pharmaceutically effective amount of an N.sup.2 -naphthalenesulfonyl-L-argininamide having the formula (I):
- ##STR51## or the pharmaceutically acceptable salts thereof, wherein R.sub.1 is selected from the group consisting of naphthyl, 5,6,7,8-tetrahydronaphthyl and naphthyl substituted with at least one substituent selected from the group consisting of halo, hydroxy, C.sub.1 -C.sub.10 alkyl and C.sub.2 -C.sub.20 dialkylamino;
- R.sub.2 is selected from the group consisting of C.sub.2 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkoxyalkyl, C.sub.2 -C.sub.10 alkylthioalkyl, C.sub.7 -C.sub.15 aralkyl, C.sub.3 -C.sub.10 cycloalkyl and C.sub.4 -C.sub.10 cycloalkylalkyl;
- R.sub.3 is hydrogen;
- and n is an integer of 1, 2 or 3.
Dependencies are inferred from the claim text.