N.sup.2 -Alkoxynaphthalenesulfonyl-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 -alkoxynaphthalenesulfonyl-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, and are prepared by reacting N.sup.2 -alkoxynaphthalenesulfonyl-L-arginyl halide with a secondary amine.
Claims4
N.sup.2 -alkoxynaphthalenesulfonyl-L-argininamides having the formula:
- ##STR55## 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 C.sub.7 -C.sub.15 aralkyl;
- R.sub.3 is C.sub.1 -C.sub.10 alkyl, C.sub.6 -C.sub.10 aryl or C.sub.7 -C.sub.12 aralkyl;
- and n is an integer of 1, 2 or 3.
A method for inhibiting activity and suppressing activation of thrombin in vivo, which comprises administering to a mammal a pharmaceutically effective amount of an N.sup.2 -alkoxynaphthalenesulfonyl-L-argininamide having the formula:
- ##STR56## or 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 C.sub.7 -C.sub.15 aralkyl;
- R.sub.3 is C.sub.1 -C.sub.10 alkyl, C.sub.6 -C.sub.10 aryl or C.sub.7 -C.sub.12 aralkyl;
- and n is an integer of 1, 2 or 3.
Dependencies are inferred from the claim text.