865239-03-8

Upstream product

• 55041-27-5 3,3-bis[4-hydroxy-3-methylphenyl]pentane 
• 23735-43-5 (S)-1-O-tosyl-2,3-O-isopropylideneglycerol 
• 850917-98-5 C₂₂H₃₀O₄ 
• 77-76-9 2,2-dimethoxy-propane 

Downstream Products

• 1258316-04-9 C₃₇H₄₈O₅ 
• 1258316-06-1 C₃₈H₅₀O₅ 
• 1258316-08-3 C₃₉H₅₂O₅ 
• 1258316-10-7 C₄₀H₅₄O₅ 
• 1258316-14-1 C₄₁H₅₀O₅ 
• 1258315-98-8 C₃₆H₄₇NO₅ 
• 1258316-12-9 C₃₇H₅₀O₅ 
• 1258315-99-9 C₃₇H₄₇NO₇ 

Relevant academic research and scientific papers

Novel selective anti-androgens with a diphenylpentane skeleton

We have proposed a multi-template approach for drug development, focusing on similar fold structures of proteins, and have effectively generated lead compounds for several drug targets. Modification of these polypharmacological lead compounds is then needed to generate target-selective compounds. In the work presented here, we aimed at separation of the anti-androgen activity and vitamin D activity of previously identified diphenylpentane lead compounds. Based on the determined X-ray crystal structures of androgen receptor and vitamin D receptor, bulky substituents were introduced at the t-butyl group in the lead compounds 2 and 3. As a result of this structural development, we obtained 16c, which exhibits more potent anti-androgen activity (IC 50: 0.13 μM) than clinically used anti-androgen bicalutamide (IC50: 0.67 μM) with 30-fold selectivity over vitamin D activity. This result indicates that lead compounds obtained via the multi-template approach can indeed be structurally modified to generate target-selective compounds.

BISPHENYL COMPOUNDS USEFUL AS VITAMIN D3 RECEPTOR AGONISTS

The present invention discloses bisphenyl compounds of the formula (I): wherein R1, R2, R3, R4, R5, R6, X, Y, W are defined herein after. These compounds are useful as pharmaceuticals.