N.sup.2 -alkoxynaphthalenesulfonyl-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
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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.
Claims12
An N.sup.2 -alkoxynaphthalenesulfonyl-L-argininamide having the formula:
- ##STR33## 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 hydrogen or C.sub.1 - C.sub.10 alkyl;
- R.sub.3 is -- COOR.sub.4 wherein R.sub.4 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;
- R.sub.2 can be substituted at the 2, 3, 4, 5 or 6 -- position;
- and R.sub.3 is substituted at the 2 or 3 -- position.
A method for inhibiting activity and suppressing activation of thrombin in vivo, which comprises administering to a patient a pharmceutically effective amount of an N.sup.2 -alkoxynaphthalenesulfonyl-L-argininamide having the formula:
- ##STR36## 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 hydrogen or C.sub.1 - C.sub.10 alkyl;
- R.sub.3 is --COOR.sub.4 wherein R.sub.4 is selected from the grou 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;
- R.sub.2 can be substituted at the 2, 3, 4, 5 or 6 -- position;
- and R.sub.3 is substituted at the 2 or 3 position.
Dependencies are inferred from the claim text.