Daiichi Pharmaceutical Co., Ltd.

Takayasu Nagahara

Yukio Yokoyama

Naoaki Kanaya

Kazue Inamura

Masayuki Ito

Satoshi Komoriya

Noriyasu Haginoya

Tsutomu Nagata

Akiyoshi Mochizuki

Syozo Kobayashi

Haruhiko Horino

Masanori Suzuki

Toshiharu Yoshino

Sulfonyl derivatives

Sulfonyl derivatives represented by general formula (I), salts of the same, and solvates of both: and application of them as drugs: &lsqb;wherein R is hydrogen, hydroxyl, nitro or the like; R and R are each independently hydrogen, halogeno or the like; R and R are each dependently hydrogen, halogeno or the like; Q is an optionally substituted saturated or unsaturated 5- or 6-membered cyclic hydrocarbon group or the like; Q is a single bond, oxygen or the like; Q is, e.g., a group represented by formula (a): T is carbonyl or the like; and X and X are each independently methylidyne or nitrogen&rsqb;. These compounds exhibit potent Fxa inhibiting activities and serve as excellent anticoagulants which speedily exert satisfactory and persistent anti-thrombotic effects through oral administration and little cause adverse effects.

An anticoagulant agent which comprises, as an active ingredient, an aromatic amidine derivative represented by the following general formula (1) or a salt thereof: ##STR1## wherein the group represented by ##STR2## is a group selected from indolyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, naphthyl, tetrahydronaphthyl and indanyl; X is a single bond, an oxygen atom, a sulfur atom or a carbonyl group; and Y is a saturated or unsaturated 5- or 6-membered heterocyclic moiety or cyclic hydrocarbon moiety optionally having a substituent group, an amino group optionally having a substituent group or an aminoalkyl group optionally having a substituent group. The inventive compound has a high anticoagulant capacity based on its excellent FXa inhibition activity.

Aromatic amidine derivatives and salts thereof

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Tokyo, Japan

Takayasu Nagahara