Gemfibrozil oxime derivative and its use as FXR antagonist

An alcohol solvent and drug technology, applied in the field of FXR antagonist, its preparation, gemfibrozil oxime derivatives, can solve the problem of not being able to improve the plasma lipid density of hypercholesterolemic patients and the like
CN106478452AActive Publication Date: 2017-03-08SHANGHAI INST OF PHARMA IND +1
3 Cites 0 Cited by

Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
SHANGHAI INST OF PHARMA IND
Publication Date
2017-03-08

Smart Images

  • Figure 1
    Figure 1
  • Figure 2
    Figure 2
  • Figure 3
    Figure 3
Patent Text Reader

Abstract

The invention relates to a gemfibrozil oxime derivative and its use as an FXR antagonist. The invention provides a compound shown in the formula (I) or its pharmaceutically acceptable salt and a preparation method thereof. In the formula, R1 represents hydrogen, hydroxyl, methyl, methoxyl, halogen, or a nitro group, R2 represents hydrogen, hydroxyl, methyl, trifluoromethyl or halogen, R3 represents hydrogen, hydroxyl, methyl, methoxyl, halogen or a nitro group, R4 represents hydrogen or methyl, R5 represents hydrogen or methyl, R6 represents hydrogen or methyl, and X represents NH, O or S. In addition, the compound shown in the formula (I) or its pharmaceutically acceptable salt has pharmacological effects of reducing blood fat and is a FXR antagonist.
Need to check novelty before this filing date? Find Prior Art

Description

technical field

[0001] The invention belongs to the field of new drug design and synthesis, and in particular relates to a gemfibrozil oxime derivative, its preparation method and its application as an FXR antagonist. Background technique

[0002] Cardiovascular and cerebrovascular diseases are currently one of the most serious diseases that endanger human life and health. They are common and frequently-occurring diseases of middle-aged and elderly people, and rank first in morbidity and mortality in many countries. Atherosclerosis is the basis of many cardiovascular and cerebrovascular diseases. A large number of experimental and clinical data prove that atherosclerosis is closely related to abnormal blood lipid metabolism. Therefore, blood lipid regulation has become an important field in the current research of this type of new drug.

[0003] Through prospective, random and controlled clinical studies, it has been proved that some statins can reduce the occurrence of ath...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More