220772-52-1

Upstream product

• 41979-39-9 4-piperidone hydrochloride 
• 102-47-6 3,4-Dichlorophenylmethyl chloride 
• 41661-47-6 piperidin-4-one 
• 18880-04-1 3,4-dichlorobenzyl bromide 

Downstream Products

• 220772-53-2 ethyl [1-(3,4-dichlorobenzyl)piperidin-4-ylidene]acetate 
• 861390-37-6 [1'-(3,4-dichloro-benzyl)-4'-methyl-[1,4']bipiperidinyl-3-ylmethyl]-carbamic acid tert-butyl ester 
• 185434-43-9 ethyl [1-(3,4-dichlorobenzyl)piperidin-4-yl]acetate 
• 220772-56-5 1(RS)-[1-(3,4-dichlorobenzyl)piperidin-4-ylmethyl]-2-methylpropylamine 
• 220772-55-4 1-[1-(3,4-dichlorobenzyl)piperidin-4-yl]-3-methyl-2-butanone 
• 220772-54-3 1(RS)-[1-(3,4-dichlorobenzyl)piperidin-4-ylmethyl]-2-methylpropanol 
• 328084-04-4 1-(3,4-dichlorobenzyl)-4-(methylamino)piperidine 
• 328083-81-4 tert-butyl 2-{[1-(3,4-dichlorobenzyl)-4-piperidinyl]amino}ethylcarbamate 
• 328084-02-2 (2-{[1-(3,4-Dichloro-benzyl)-piperidin-4-yl]-methyl-amino}-ethyl)-carbamic acid tert-butyl ester 
• 328083-67-6 N'-[1-(3,4-dichlorobenzyl)-4-piperidinyl]-2-[4-(trifluoromethoxy)phenoxy]acetohydrazide 

Relevant academic research and scientific papers

The synthesis of substituted bipiperidine amide compounds as CCR3 ligands: Antagonists versus agonists

Structure-activity relationship study of bipiperidine amide 1 has identified the reverse bipiperidine amide 4a as a CC chemokine-3 (CCR3) receptor antagonist. Optimization of the structure-activity relationship of compound 4a has resulted in the identification of a CCR3 antagonist 4i as well as a CCR3 agonist 13.

Substituted piperidine compounds useful as modulators of chemokine receptor activity

The invention provides compounds of formula (I) wherein R1, R2, R3, R6, Z, Q, m, n, X1, X2, X3, X4 and T are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy, especially for the treatment of chemokine receptor related diseases and conditions

Design and synthesis of novel CCR3 antagonists

As part of our investigation into the development of potent CCR3 antagonists, a series of piperidine analogues was designed and prepared. Exploration of the piperidine core examined both the basicity and the location of a nitrogen, as well as conformational variants. The bicyclo-piperidine 24c was found to be the most potent inhibitor of CCR3 with an IC50 of 0.0082 μM in the binding assay and 0.0024 μM in the chemotaxis assay.

Cyclic amine derivatives-CCR-3 receptor antagonists

This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonist, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.

Cyclic amine derivatives- CCR-3 receptor antagonists

This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.

Allosteric modulation of the adenosine A1 receptor. Synthesis and biological evaluation of novel 2-amino-3-benzoylthiophenes as allosteric enhancers of agonist binding

Novel allosteric enhancers of agonist binding to the rat adenosine A1 receptor are described. The lead compound for the new series was PD 81,723 ((2-amino-4,5-dimethyl-3-thienyl)[3-(trifluoromethyl)phenyl]methanone), a compound previously reported by Bruns and co-workers (Mol. Pharmacol. 1990, 38, 950-958). The 4,5-dimethyl group and the benzoyl moiety were targets for further modifications, leading to series of 4,5-dialkyl (12a-g), of tetrahydrobenzo (12h-u), and of tetrahydropyridine (13a-g) derivatives. A number of compounds, in particular 12b, 12e, 12j, 12n, and 12u, proved superior to PD 81,723. Their EC50 values for enhancing the binding of the adenosine A1 receptor agonist N6-cyclopentyladenosine to the receptor were lower, and/or their antagonistic activity on the adenosine A1 receptor was shown to be diminished.