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US 4,070,457 AGranted
N.sup.2 -naphthalenesulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof
AssigneesMitsubishi Chemical Industries Limited, Shosuke Okamoto
InventorsShosuke Okamoto, Ryoji Kikumoto, Kazuo Ohkubo, Tohru Tezuka, Shinji Tonomura, Yoshikuni Tamao, Akiko Hijikata
Life of this patent
Estimating the term…
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.
Claims4
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 and C.sub.1 -C.sub.10 alkyl;
- 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 selected from the group consisting of C.sub.1 -C.sub.10 alkyl, C.sub.7 -C.sub.12 aralkyl and C.sub.6 -C.sub.10 aryl;
- and n is an integer of 1,2 or 3.
1 more element
A method of inhibiting activity and suppressing activation of thrombin in vivo, which comprises administering to a patient 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 and C.sub.1 -C.sub.10 alkyl 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 selected from the group consisting of C.sub.1 -C.sub.10 alkyl, C.sub.7 -C.sub.12 aralkyl and C.sub.6 -C.sub.10 aryl;
- and n is an integer of 1, 2 or 3.
Dependencies are inferred from the claim text.