Daiichi Pharmaceutical Co., Ltd.

Daiichi Sankyo Company, Limited

Akiyoshi Mochizuki

Tsutomu Nagata

Satoshi Komoriya

Noriyasu Haginoya

Syozo Kobayashi

Toshiharu Yoshino

Makoto Ono

Hiroyuki Naito

Masayuki Ito

Hideyuki Kanno

Kenji Yoshikawa

Kouichi Uoto

Masatoshi Nagamochi

Takayasu Nagahara

Toshiharu Ohta

Yumi Nakamoto

Haruhiko Horino

Masanori Suzuki

An object of the present invention is to provide a novel compound which has a potent inhibitory effect on FXa and exhibits an excellent antithrombotic effect when orally administered. The present invention provides a compound represented by the following general formula (1): wherein Rand Reach independently represent a hydrogen atom, a hydroxy group, an alkyl group or an alkoxy group; Qrepresents a saturated or unsaturated bicyclic or tricyclic fused hydrocarbon group which may be substituted, a saturated or unsaturated bicyclic or tricyclic fused heterocyclic group which may be substituted, or the like; Qrepresents a single bond, a straight-chained or branched alkylene group having 1 to 6 carbon atoms, a straight-chained or branched alkenylene group having 2 to 6 carbon atoms, or the like; Rand Reach represent an alkyl group, or the like; m and n each represent an integer from 0 to 3; Qrepresents an aryl group; and Tand Teach represent a carbonyl group or the like, and a medicine containing the compound.

Triamine derivative

A compound represented by formula (1):Q-Q-T-N(R)-Q-N(R)-T-Q&#x2003;&#x2003;(1)[wherein Rand Rare hydrogen atoms or the like; Qis a saturated or unsaturated, 5- or 6-membered cyclic hydrocarbon group which may be substituted, or the like; Qis a single bond or the like; Qrepresents the following group: (wherein Qis an alkylene group having 1 to 8 carbon atoms, or the like); and Tand Tare carbonyl groups or the like], a salt thereof, a solvate thereof, or an N-oxide thereof. The compound is useful as an agent for preventing and/or treating cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger's disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after artificial valve or joint replacement, thrombus formation and reocclusion after angioplasty, systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing.

Diamine derivatives

A compound represented by the general formula (1):Q-Q-T-N(R)-Q-N(R)-T-Q&#x2003;&#x2003;(1)wherein Rand Rare hydrogen atoms or the like; Qis a saturated or unsaturated, 5- or 6-membered cyclic hydrocarbon group which may be substituted, or the like; Qis a single bond or the like; Qis a group in which Qis an alkylene group having 1 to 8 carbon atoms, or the like; and Tand Tare carbonyl groups or the like; a salt thereof, a solvate thereof, or an N-oxide thereof. The compound is useful as an agent for preventing and/or treating cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger's disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after valve or joint replacement, thrombus formation and reocclusion after angioplasty, systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing.

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.

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Tokyo, Japan

Akiyoshi Mochizuki