Astellas Pharma Gmbh

Yamanouchi Pharmaceutical Company Ltd.

Takeshi Shigenaga

Fukushi Hirayama

Yuji Koga

Keizo Sugasawa

Tsukasa Ishihara

Norio Seki

Hiroyuki Koshio

Yuzo Matsumoto

Souichirou Kawazoe

Ryota Shiraki

Shunichiro Hachiya

Takeshi Kadokura

To provide a compound which has an anticoagulation action based upon inhibition of activated blood coagulation factor X and is useful as an anticoagulant or an agent for prevention and treatment of diseases caused by thrombus or embolus. A diazepan derivative such as 4-[(3-carbamimidoylphenylamino)methyl]-3-[4-(4-methyl-1,4-diazepan-1-yl)benzoylamino]benzoic acid and 3-hydroxy-4'-methoxy-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzanilide or a salt thereof is an effective ingredient.

Diazepan derivatives or salts thereof

There are provided compounds having an anticoagulant action on the basis of inhibition of activated blood coagulation factor X and being useful as anticoagulants or preventive/therapeutic agents for diseases induced by thrombosis or embolism. Effective ingredients are the compounds such as 4'-bromo-2&#x2032;-[(5-chloro-2-pyridyl) carbamoyl]-6&#x2032;-&#x3b2;-D-galactopyranosyloxy-1-isopropylpiperidine-4-carboxanilide, 2&#x2032;-(2-acetamido-2-deoxy-&#x3b2;-D-glucopyranosyloxy)-4&#x2032;-bromo-6&#x2032;-[(5-chloro-2-pyridyl)carbamoyl]-1-isopropylpiperidine-4-carboxanilide, etc. or salts thereof.

Substituted benzene derivatives or salts thereof

There are provided compounds having an anticoagulant action on the basis of inhibition of activated blood coagulation factor X and being useful as anticoagulants or preventive/therapeutic agents for diseases induced by thrombosis or embolism. Effective ingredients are the compounds such as 4'-bromo-2&#x2032;-[(5-chloro-2-pyridyl)carbamoyl]-6&#x2032;-&#x3b2;-D-galactopyranosyloxy-1-isopropylpiperidine-4-carboxanilide, 2&#x2032;-(2-acetamido-2-deoxy-&#x3b2;-D-glucopyranosyloxy)-4&#x2032;-bromo-6&#x2032;-[(5-chloro-2-pyridyl)carbamoyl]-1-isopropylpiperidine-4-carboxanilide, etc. or salts thereof.

To provide a compound which has an anticoagulation action based upon inhibition of activated blood coagulation factor X and is useful as an anticoagulant or an agent for prevention and treatment of diseases caused by thrombus or embolus. A diazepan derivative such as 4-&lsqb;(3-carbamimidoylphenylamino)methyl&rsqb;-3-&lsqb;4-(4-METHYL-1,4-diazepan-1-yl)benzoylamino&rsqb;benzoic acid and 3-hydroxy-4&prime;-methoxy-2-&lcub;&lsqb;4-(4-methyl-1,4-diazepan-1-yl)benzoyl&rsqb;amino&rcub;benzanilide or a salt thereof is an effective ingredient.

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Tsukuba, Japan

Takeshi Shigenaga