Kowa Company Limited

Manac Incorporated

Shinji Ina

Noriaki Gomi

Junichi Sakata

Takahiro Yamazaki

Koji Ezaki

Katsuhiro Sakamoto

Kenjirou Yamana

Yoshio Kaneko

Provided is a method of manufacturing a high quality phosphonocrotonic acid derivative. The present invention is a method of manufacturing a compound represented by the following Formula (3) by reacting a compound represented by the following Formula (1) with a compound represented by the following Formula (2), which comprises a treatment process using an acid or base. [in the formula, Rrepresents a Clinear or branched alkyl group that may be substituted by a Caryl group, a Clinear or branched alkenyl group that may be substituted by a Caryl group, a Clinear or branched alkynyl group that may be substituted by a Caryl group, or a Caryl group, Rrepresents a hydrogen atom, or a Clinear or branched alkyl group that may be substituted by a Caryl group, Rrepresents a Clinear or branched alkyl group, a Caryl group, or a halogen atom, and X represents a halogen atom, and multiple Rs may be the same or different]. 

Method for manufacturing phosphonocrotonic acid derivative

To find a compound having a tissue fibrinosis-inhibitory activity and a fibrinolytic activity, and to provide a novel compound that is useful for preventing and/or treating tissue fibrinosis diseases (pulmonary fibrosis, renal fibrosis etc.), diseases caused by pathological blood clots such as ischemic heart diseases (myocardial infarction, angina), intraatrial thrombus, pulmonary embolism, deep venous thrombosis, disseminated intravascular coagulation, ischemic cerebral diseases (cerebral infarction, cerebral bleeding) and arteriosclerosis and the like. To provide a pharmaceutical drug comprising a 5-phenyl-3-pyridazinone derivative represented by the following general formula (I): and an optical isomer thereof, or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof, useful for preventing and/or treating disease conditions or symptoms mediated by plasminogen activator inhibitor-1.

5-phenyl-3-pyridazinone derivative

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Ageo, Japan

Shinji Ina