609772-03-4

Upstream product

• 722-92-9 2-(4-aminophenyl)-1,1,1,3,3,3-hexafluoro-2-propanol 
• 407-25-0 trifluoroacetic anhydride 
• 75-90-1 2,2,2-Trifluoroacetaldehyde 
• 70430-20-5 2,2,2-trifluoro-N-[4-(2,2,2-trifluoro-1-hydroxy-1-trifluoromethyl-ethyl)-phenyl]-acetamide 

Downstream Products

• 872690-56-7 2-{4-[benzyl-(2,2,2-trifluoro-ethyl)-amino]-phenyl}-1,1,1,3,3,3-hexafluoro-propan-2-ol 
• 629621-69-8 dimethyl 2-((2,2,2-trifluoroethyl){4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)-ethyl]phenyl}amino)malonate 

Relevant academic research and scientific papers

Discovery and optimization of a series of sulfonamide inverse agonists for the retinoic acid receptor-related orphan receptor-α

Background: Despite a massive industry endeavor to develop RORγ-modulators for autoimmune disorders, there has been no indication of efforts to target the close family member RORα for similar indications. This may be due to the misconception that RORα is

Structure-based design of substituted hexafluoroisopropanol- arylsulfonamides as modulators of RORc

The structure-activity relationships of T0901317 analogs were explored as RORc inverse agonists using the principles of property- and structure-based drug design. An X-ray co-crystal structure of T0901317 and RORc was obtained and provided molecular insight into why T0901317 functioned as an inverse agonist of RORc; whereas, the same ligand functioned as an agonist of FXR, LXR, and PXR. The structural data was also used to design inhibitors with improved RORc biochemical and cellular activities. The improved inhibitors possessed enhanced selectivity profiles (rationalized using the X-ray crystallographic data) against other nuclear receptors.

Synthesis and evaluation of anilinohexafluoroisopropanols as activators/modulators of LXRα and β

A series of branched and unbranched anilinohexafluoroisopropanols related to the known sulfonamide T0901317 were prepared and evaluated as activators/modulators of both LXRα and LXRβ. A structure-activity relationship was established and compounds with high potency on both the receptors were identified. Many compounds showed a tendency toward selectivity for LXRβ versus LXRα. Several analogues were evaluated for effects on plasma lipoprotein levels in mice. A few of these significantly raised HDL-cholesterol levels in plasma but showed markedly different effects on liver triglyceride content, suggesting that this series may yield candidates with improved efficacy/safety profiles compared to existing molecules.

Novel hexafluoroisopropanol derivatives

The invention is concerned with novel hexafluoroisopropanol derivatives of formula (I) wherein R1 to R6, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. The

ANILINO LIVER X-RECEPTOR MODULATORS

The present invention is directed to selective LXR modulators, small molecule compounds corresponding to Formula I and is further directed to a process of treating a condition in a mammal that is modulated by LXR using a therapeutically effective dose of a compound of Formula I.