N.sup.2 -alkoxynaphthalenesulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof
AssigneeMitsubishi Chemical Industries Limited
InventorsShosuke Okamoto, Ryoji Kikumoto, Kazuo Ohkubo, Tohru Tezuka, Shinji Tonomura, Yoshikuni Tamao, Akiko Hijikata
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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.
Claims7
N.sup.2 -alkoxynaphthalenesulfonyl-L-argininamides having the formula (I):
- ##STR40## 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.3 -C.sub.10 cycloalkyl or C.sub.4 -C.sub.10 cycloalkylalkyl;
- 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 and 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 patient a pharmaceutically effective amount of an N.sup.2 -alkoxynaphthalenesulfonyl-L-argininamide having the formula (I):
- ##STR41## or a 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 C.sub.3 -C.sub.10 cycloalkyl or C.sub.4 -C.sub.10 cycloalkylalkyl;
- 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 and C.sub.7 -C.sub.12 aralkyl;
- and n is an integer of 1, 2 or 3.
Dependencies are inferred from the claim text.