209349-07-5

Upstream product

• 98-09-9 benzenesulfonyl chloride 
• 334824-88-3 N-[2-(4-fluoro-phenyl)-4-oxo-butyl]-N-methyl-benzenesulfonamide 
• 334824-79-2 N-[2-(4-fluoro-phenyl)-pent-4-enyl]-N-methyl-benzenesulfonamide 
• 235097-94-6 (S)-2-(4-fluorophenyl)pent-4-enoic acid,N-methyl amide 
• 810680-77-4 (S)-2-(4-fluorophenyl)pent-4-enoyl chloride 
• 494802-92-5 (S)-2-(4-fluorophenyl)-4-pentenoic acid 
• 235097-95-7 [(2S)-2-(4-fluorophenyl)pent-4-en-1-yl]methylamine 

Relevant academic research and scientific papers

Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 2: Structure-activity relationships for substituted 2-aryl-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-(piperidin-1-yl)butanes

(2S)-2-(3,4-Dichlorophenyl)-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-[spiro(2 ,3-dihydrobenzthiophene-3,4′-piperidin-1′yl)]butane S-oxide (3) has been identified as a potent CCR5 antagonist lead structure having an IC50 = 35 nM. Herein, we describe the structure-activity relationship studies directed toward the requirement for and optimization of the C-2 phenyl fragment. The phenyl was found to be important for CCR5 antagonism and substitution was limited to small moieties at the 3-position (13 and 16: X = H, 3-F, 3-Cl, 3-Me).

SPIRO-SUBSTITUTED AZACYCLES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY

The present invention is directed to spiro-substituted azacycles of the Formula 1: STR1 (wherein R 1, l, m, Q, W, X, Y, and Z are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.