255820-47-4

Upstream product

• 94651-33-9 2-(trifluoromethoxy)benzaldehyde 

Downstream Products

• 1103500-32-8 methyl 5-cyclopropyl-3-(2-(trifluoromethoxy)phenyl)isoxazole-4-carboxylate 
• 543713-03-7 N-hydroxy-2-(trifluoromethoxy)benzimidonyl chloride 
• 946427-86-7 4-(bromomethyl)-5-cyclopropyl-3-(2-(trifluoromethoxy)phenyl)isoxazole 

Relevant academic research and scientific papers

Discovery of BMS-986318, a Potent Nonbile Acid FXR Agonist for the Treatment of Nonalcoholic Steatohepatitis

Herein we report the discovery and preclinical biological evaluation of 6-(2-(5-cyclopropyl-3-(3,5-dichloropyridin-4-yl)isoxazol-4-yl)-7-azaspiro[3.5]non-1-en-7-yl)-4-(trifluoromethyl)quinoline-2-carboxylic acid, compound 1 (BMS-986318), a nonbile acid farnesoid X receptor (FXR) agonist. Compound 1 exhibits potent in vitro and in vivo activation of FXR, has a suitable ADME profile, and demonstrates efficacy in the mouse bile duct ligation model of liver cholestasis and fibrosis. The overall profile of compound 1 supports its continued evaluation.

Isoxazole FXR receptor agonist as well as preparation method and medical application thereof

The invention belongs to the field of medicinal chemistry, and particularly relates to an isoxazole FXR receptor agonist and a preparation method and medical application thereof. The invention relates to a compound as shown in a formula (I), and pharmaceutically acceptable salts and isotope markers thereof. The compound as shown in the formula (I), the pharmaceutically acceptable salts and the isotope markers thereof have FXR receptor agonist activity and can be applied to preparation of drugs for treating or preventing hyperlipidemia, atherosclerosis, non-alcoholic steatohepatitis and type II diabetes mellitus.

COMPOSITIONS AND METHODS FOR TREATING LIVER DISORDERS

The present disclosure is directed to FXR agonists, pharmaceutical compositions thereof, and methods of using the same for preventing, treating, or ameliorating fatty liver diseases such as steatosis, non-alcoholic fatty liver disease, and non-alcoholic steatohepatitis, either alone or in combination with thyroid receptor agonists.

LACTAM COMPOUND AS FXR RECEPTOR AGONIST

Disclosed is a compound as shown in formula (I), an optical isomer thereof or a pharmaceutically acceptable salt thereof, and the present invention relates to the use of same in the preparation of a drug for treating FXR-related diseases.

Discovery and Optimization of Non-bile Acid FXR Agonists as Preclinical Candidates for the Treatment of Nonalcoholic Steatohepatitis

Farnesoid X receptor (FXR) plays a key role in bile acid homeostasis, inflammation, fibrosis, and metabolism of lipid and glucose and becomes a promising therapeutic target for nonalcoholic steatohepatitis (NASH) or other FXR-dependent diseases. The phase III trial results of obeticholic acid demonstrate that the FXR agonists emerge as a promising intervention in patients with NASH and fibrosis, but this bile acid-derived FXR agonist brings severe pruritus and an elevated risk of cardiovascular disease for patients. Herein, we reported our efforts in the discovery of a series of non-bile acid FXR agonists, and 36 compounds were designed and synthesized based on the structure-based drug design and structural optimization strategies. Particularly, compound 42 is a highly potent and selective FXR agonist, along with good pharmacokinetic profiles, high liver distribution, and preferable in vivo efficacy, indicating that it is a potential candidate for the treatment of NASH or other FXR-dependent diseases.

ISOXAZOLE DERIVATIVES AND PREPARATION PROCESS THEREOF

The present invention relates to an isoxazole derivative compound of Formula (1) useful as a substance for treating respiratory viral infectious disease caused by coronavirus, in particular, Middle East respiratory syndrome-coronavirus (MERS-CoV); a pharm

COMPOUNDS FOR MODULATING FXR

Provided herein are compounds of Formula (I), a stereoisomer, enantiomer or a pharmaceutically acceptable salt thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesoid X receptors (FXR).

NITROGENOUS TRICYCLIC COMPOUNDS AND USES THEREOF IN MEDICINE

The present invention relates to nitrogenous tricyclic compounds and uses thereof in medicine, in particular, the present invention discloses a novel nitrogenous tricyclic compound used as an FXR active regulator and a stereoisomer, a geometrical isomer,

AN ISOXAZOLE DERIVATIVES AS NUCLEAR RECEPTOR AGONISTS AND USED THEREOF

The present invention relates to isoxazole derivatives, including pharmaceutical compositions and for the preparation of isoxazole derivatives. And more particularly the present invention provided a pharmaceutical composition of isoxazole derivatives for activation of Farnesoid X receptor(FXR, NR1H4).

PHENYL-ISOXAZOL DERIVATIVES AND PREPARATION PROCESS THEREOF

Disclosed are a phenyl-isoxazol derivative compound, which is useful as a treatment material for virus infection, especially, infection of an influenza virus, or its pharmaceutically acceptable derivative, a preparation method thereof, and an illness treatment pharmaceutical composition including the compound as an active ingredient.