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.
Claims10
An N.sup.2 -[naphthalenesulfonyl-L-argininamides] Napthalenesulfonyl-L-argininamide compound having the formula (I):
- ##STR35## or a pharmaceutically acceptable salt 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, nitro, cyano, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxy and C.sub.2 -C.sub.20 dialkylamino;
- R.sub.2 is selected from the group consisting of furfuryl, 3-furylmethyl tetrahydrofurfuryl and tetrahydro-3-furylmethyl;
- R.sub.3 is hydrogen or C.sub.1 -C.sub.5 alkyl;
- R.sub.4 is selected from the group consisting of hydrogen, 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 0, 1 or 2.
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-compound having the formula (I):
- ##STR36## or the pharmaceutically acceptable salt thereof, wherein R.sub.1 is selected from a 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, nitro, cyano, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxy and C.sub.2 -C.sub.20 dialkylamino;
- R.sub.2 is selected from the group consisting of furfuryl, 3-furylmethyl, tetrahydrofurfuryl and tetrahydro-3-furylmethyl;
- R.sub.3 is hydrogen or C.sub.1 -C.sub.5 alkyl;
- R.sub.4 is selected from the group consisting of hydrogen, 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 0, 1 or 2.
Dependencies are inferred from the claim text.