207405-67-2

Upstream product

• 100-46-9 benzylamine 
• 185099-67-6 Boc-tropinone 
• 185099-67-6 N-Boc-nortropinone 

Downstream Products

• 716359-02-3 endo-tert-butyl (1R,5S)-3-[(2-amino-4-fluorophenyl)amino]-8-azabicyclo[3.2.1]octane-8-carboxylate 
• 716359-00-1 endo-tert-butyl (1R,5S)-3-{[2-amino-4-(methylsulfonyl)phenyl]amino}-8-azabicyclo[3.2.1]octane-8-carboxylate 
• 716359-01-2 endo-tert-butyl (1R,5S)-3-[(4-fluoro-2-nifrophenyl)amino]-8-azabicyclo[3.2.1]octane-8-carboxylate 
• 716358-99-5 endo-tert-butyl (1R,5S)-3-{[4-(methylsulfonyl)-2-nitrophenyl]amino}-8-azabicyclo[3.2.1]octane-8-carboxylate 
• 280762-27-8 C₁₄H₁₇N₃ 
• 280762-13-2 endo-tert-butyl 3-[(2-aminophenyl)amino]-8-azabicyclo[3.2.1]octane-8-carboxylate 
• 280762-06-3 endo-tert-butyl 3-[(2-nitrophenyl)amino]-8-azabicyclo[3.2.1]octane-8-carboxylate 
• 207405-68-3 tert-butyl 3-endo-amino-8-azabicyclo[3.2.1]octane-8-carboxylate 

Relevant academic research and scientific papers

1-(3-AMINOPROPYL) SUBSTITUTED CYCLIC AMINE COMPOUNDS, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITIONS AND USES THEREOF

Provided are 1-(3-aminopropyl) substituted cyclic amine compounds as represented by formula (I), pharmaceutically acceptable salts, enantiomers, diastereoisomers, racemates and mixtures thereof, and a method of synthesizing said 1-(3-aminopropyl) substituted cyclic amine compounds by using aromatic heterocyclic formaldehyde as raw material. Said compounds can be used as CCR 5 antagonist for the treatment of HIV infection.

Discovery of bioavailable 4,4-disubstituted piperidines as potent ligands of the chemokine receptor 5 and inhibitors of the human immunodeficiency virus-1

We describe robust chemical approaches toward putative CCR5 scaffolds designed in our laboratories. Evaluation of analogues in the 125I-[MIP-1β] binding and Ba-L-HOS antiviral assays resulted in the discovery of 64 and 68 in the 4,4-disubstitited piperidine class H, both potent CCR5 ligands (pIC50 = 8.30 and 9.00, respectively) and HIV-1 inhibitors (pIC50 = 7.80 and 7.84, respectively, in Ba-L-HOS assay). In addition, 64 and 68 were bioavailable in rodents, establishing them as lead molecules for further optimization toward CCR5 clinical candidates.

PIPERAZINO DERIVATIVES AS NEUROKININ ANTAGONISTS

The invention relates to compounds of formula (I) wherein Z, Rc, y, m, u, Ar2, n, X, Rc', l and Ar2 are as described herein. These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.

Chemical compounds

The present invention provides compounds of formula (I) wherein R1 and R2 are as defined hereinabove. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors. Modulators of the CCR5 receptor may be useful in the treatment of various inflammatory diseases and conditions, and in the treatment of infection by HIV and genetically related retroviruses.