Beijing Chenguang Tongchuang Pharmaceutical Research Institute Co., Ltd.

Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.l.c. China

Institute of Pharmacology and Toxicology Academy of Military Medical Sciences Pla China

Changbin Guo

Wei Li

Liang Ma

Song Li

Wu Zhong

Junhai Xiao

Zhong Wu

Shaolin Huang

Qingjuan Yang

Pengfei Song

Jingwang Fan

Xiaosong Mao

Xiancheng Jiang

The invention relates to a prodrug compound of levosimendan as shown by the formula below, and solvates, hydrates, N-oxides, stereoisomers, and pharmaceutically acceptable salts thereof, wherein each of Ra and Rb is selected from hydrogen or C1-C6 alkyl; Rp is selected from a basic group containing N atom or an acidic group containing carboxyl group, phosphate group, sulfate group, and sulfonate group. The prodrug compound overcomes the defects of levosimendan such as poor water solubility, and has an ideal pharmacokinetic profile and excellent prospects for medicament development. 

Prodrug compound of levosimendan, preparation method and use thereof

The present invention relates to 2,4,5-trisubstituted thiazole compounds of formula (I) or all possible isomers, prodrugs, pharmaceutically acceptable salts, solvates or hydrates thereof for the inhibition of plasma PLTP activity and/or plasma CETP activity, wherein the substituents are as defined in the specification; a process for the preparation of the compounds of formula (I); a pharmaceutical composition comprising the compound of formula (I) and its use for the preparation of a medicament for treatment and/or prevention of diseases associated with the increased plasma PLTP activity and/or the increased plasma CETP activity in a mammal, such as atherosclerosis, cardiovascular diseases and peripheral vascular diseases, etc. 

Trisubstituted thiazole compounds, preparations methods, pharmaceutical compositions and medicals uses thereof

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Beijing, China

Changbin Guo