Shanghai Institute of Pharmaceutical Industry

Qun Hao

Weicheng Zhou

Zhengyan Cai

Yuchen Sheng

Mingyu Shi

Zhenhua Shi

Qingning Liang

A kind of quinoline compounds as formula A, pharmaceutical accepted solvates, optical isomers or polymorphisms thereof. The intermediates of formula D. in which, R, Rand Ris independently H, halo or the subustitents of formula H, in which, R is H, halo, C&#x2dc;Calkyl, C&#x2dc;Calkoxyl. The preparation methods and the uses for the manufacture of a medicament of inhibiting the HMG CoA reductase and treating the diseases relating to the high blood fat. Compared with the fluvastatin, rosuvatatin, pitavastatin disclosed in the prior arts, present quinoline compounds have better activity of inhibiting HMG CoA reductase. Present quinoline compounds can be used for treating the diseases relating to the high blood fat.

Quinoline compounds, intermediates, preparation methods and uses thereof

The present invention discloses a quinoline compound represented by the formula A or pharmaceutically acceptable solvate, optical isomer or polymorph thereof, wherein X is S or O; M is H, Na, NH4or Ca; each of R, Rand Ris independently H, halogen, the group represented by formula D or formula E; R is H, halogen, C1&#x2dc;C4 alkyl or C1&#x2dc;C4 alkoxy.  The present invention also discloses its pharmaceutical composition and the preparation method thereof and application in manufacturing a medicament for inhibiting HMG-CoA reductase or for the treatment and prophylaxis of the diseases which can be treated effectively by inhibiting HMG-CoA reductase. The quinloline compound and pharmaceutical composition thereof of the present invention have an excellent lipid reduction effect in vivo and can be applied for treatment of a hyperlipidemia-related disease.

Quinoline compound and pharmaceutical composition, preparation method and uses thereof

Growing community of inventors

Shanghai, China

Qun Hao