864655-26-5

Upstream product

• 79099-07-3 N-tert-butyloxycarbonylpiperidin-4-one 
• 156-87-6 propan-1-ol-3-amine 

Downstream Products

• 1216859-23-2 tert-butyl 4-(2-oxo-1,3-oxazinan-3-yl)piperidine-1-carboxylate 
• 280141-27-7 4-[(4-nitro-phenoxycarbonyl)-(3-oxo-propyl)-amino]-piperidine-1-carboxylic acid tert-butyl ester 

Relevant academic research and scientific papers

BICYCLIC AZA COMPOUNDS AS MUSCARINIC M1 RECEPTOR AGONISTS.

This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula 1, or a salt thereof, wherein Q, R1 , R2, R3 and R4 are as defined herein.

Potent CCR4 antagonists: Synthesis, evaluation, and docking study of 2,4-diaminoquinazolines

A series of CC chemokine receptor-4 (CCR4) antagonists were examined in a previous report in an attempt to improve metabolic stability in human liver microsomes. In this study, the cycloheptylamine moiety of N-cycloheptyl-6,7-dimethoxy-2-(4-pyrrolidin-1-ylpiperidin-1-yl)quinazolin-4-amine 1 was replaced with the p-chloroaniline moiety, and the resulting compound, N-(4-chlorophenyl)-6,7-dimethoxy-2-(4-pyrrolidin-1-ylpiperidin-1-yl)quinazolin-4-amine (8c), retained its potency ([35S]GTPγS-binding inhibition and CCL22-induced chemotaxis in humans/mice). Based on the structure-activity relationships (SAR), a homology model was constructed for CCR4 to explain the binding mode of 8c. Overall, there was good agreement between the docking pose of the CCR4 homology model and the human [35S]GTPγS assay results. Administration of 8c in a murine model of acute dermatitis showed anti-inflammatory activity (oxazolone-induced contact hypersensitivity test).

INHIBITORS OF MONOAMINE UPTAKE

N,N-disubstituted 4-amino-piperidines of the general Formula (I) are inhibitors of the uptake of serotonin and/or norepinephrine and/or dopamine. As such, they may be useful for the treatment of disorders of the central and/or peripheral nervous system.

Preparation of oxime dual NK1/NK2 antagonists with reduced NK3 affinity

By employing a stereosimplification approach, a thorough SAR exploration of the piperidine region of Sch 206272 was possible through a practical and efficient synthesis of substituted cyclic ureas. This SAR study led to the identification of a benzimidazolinone series of compounds which display single digit nanomolar NK1/NK2 affinity and near micromolar binding for the NK3 receptor.