167484-79-9

Upstream product

• 164328-62-5 [(2S)-2-(3,4-dichloro-phenyl)-4-oxo-butyl]-methyl-carbamic acid tert-butyl ester 
• 167483-88-7 1'-(3-((S)-(3,4-dichlorophenyl))-4-(methylamino)butyl)-1-methanesulfonyl-spiro(indoline-3,4'-piperidine) 
• 167483-86-5 [2-(3,4-dichloro-phenyl)-pent-4-enyl]-methyl-carbamic acid tert-butyl ester 
• 147643-61-6 (S)-2-(3,4-dichlorophenyl)pent-4-enoic acid N-methyl amide 
• 156300-01-5 (S)-N-methyl-(2-(3,4-dichlorophenyl)pent-4-enyl)amine 
• 147643-57-0 (2S)-2-(3,4-dichlorophenyl)pent-4-enoic acid 
• 156300-02-6 (S)-2-(3,4-dichlorophenyl)pent-4-enoyl chloride 

Downstream Products

• 167484-85-7 1'-(3-((S)-(3,4-dichlorophenyl))-4-(N-(t-butoxycarbonyl)(methylamino))butyl)-spiro(2,3-dihydrobenzothiophene-3,4'-piperidine)-1,1-dioxide 
• 209349-60-0 1'-(3-((S)-(3,4-Dichlorophenyl))-4-(N-(quinoline-8-sulfonyl) (methylamino))-butyl)-spiro(2.3-dihydrobenzothiophene-3,4'-piperidine) 

Relevant academic research and scientific papers

Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 1: Discovery and initial structure-activity relationships for 1-amino-2-phenyl-4-(piperidin-1-yl) butanes

Screening of the Merck sample collection for compounds with CCR5 receptor binding afforded (2S)-2-(3,4-dichlorophenyl)-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-[spiro(2 ,3-dihydrobenzthiophene-3,4′-piperidin-1′-yl)]butane S-oxide (4) as a potent lead structure having an IC50 binding affinity of 35 nM. Herein, we describe the discovery of this lead structure and our initial structure-activity relationship studies directed toward the requirement for and optimization of the 1-amino fragment.

Spiro-substituted azacycles as neurokinin antagonists

Disclosed are spiro-substituted azacycles of formula I are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, and asthma. In particular compounds of formula I are shown to be neurokinin antagonists.

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.