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NEW CCR2 RECEPTOR ANTAGONISTS AND USES THEREOF

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of Formula (I) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H108N – PubChem

 

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Isoindolinone derivatives, production and use thereof

A compound of the formula STR1 wherein X is hydrogen, halogen or nitro; Ar is phenyl or naphthyridinyl which may optionally be substituted; and either one of Z 1 and Z 2 is hydrogen and the other is lower alkanoyloxy or hydroxy, each of Z 1 and Z 2 is lower alkoxy, or Z 1 and Z 2 combinedly represent hydroxyimino, oxo or a group of the formula: STR2 in which Y is oxygen or sulfur and A is a branched or unbranched lower alkylene chain; and a salt thereof, act on the central nervous system but are weak in adverse effects such as hypnotic and muscle relaxant effects.

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H447N – PubChem

 

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A convenient synthesis of functionalized 8- and 9-aza-1-oxaspiro[5.5]undecanes

2-Hydroxy-8-(or 9-)aza-1-oxaspiro[5.5]undec-3-en-5-ones derived from their corresponding 2-furfuryl alcohols were used as key intermediates for the convenient synthesis of several novel 8- and 9-aza-1-oxaspiro[5.5]undecane derivatives.

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Piperidine – Wikipedia,
Piperidine | C5H459N – PubChem

 

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Synthesis of alpha,beta-Unsaturated Carbonyl-Based Compounds, Oxime and Oxime Ether Analogs as Potential Anticancer Agents for Overcoming Cancer Multidrug Resistance by Modulation of Efflux Pumps in Tumor Cells

Sixty-nine novel alpha,beta-unsaturated carbonyl based compounds, including cyclohexanone, tetralone, oxime, and oxime ether analogs, were synthesized. The antiproliferative activity determined by using seven different human cancer cell lines provided a structure-activity relationship. Compound 8ag exhibited high antiproliferative activity against Panc-1, PaCa-2, A-549, and PC-3 cell lines, with IC50 value of 0.02 muM, comparable to the positive control Erlotinib. The ten most active antiproliferative compounds were assessed for mechanistic effects on BRAFV600E, EGFR TK kinases, and tubulin polymerization, and were investigated in vitro to reverse efflux-mediated resistance developed by cancer cells. Compound 8af exhibited the most potent BRAFV600E inhibitory activity with an IC50 value of 0.9 muM. Oxime analog 7o displayed the most potent EGFR TK inhibitory activity with an IC50 of 0.07 muM, which was analogous to the positive control. Some analogs including 7f, 8af, and 8ag showed a dual role as anticancer and MDR reversal agents.

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Piperidine – Wikipedia,
Piperidine | C5H211N – PubChem

 

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Synthesis and characterization of Co3O4 immobilized on dipeptide-functionalized silica-coated magnetite nanoparticles as a catalyst for the selective aerobic oxidation of alcohols

Synthesis and characterization of a new silica-coated magnetite nanocatalyst are described. This catalyst was prepared through a multistep procedure consisting of surface modification, functionalization with the product of an Ugi multicomponent reaction, and immobilization of Co3O4 on silica-coated magnetite nanoparticles. The prepared nanocatalyst was characterized using various techniques such as Fourier-transform infrared and energy-dispersive X-ray spectroscopies, thermal and elemental analyses, X-ray diffraction, and field-emission scanning and transmission electron microscopies. The catalyst showed high catalytic activity for the aerobic oxidation of alcohols in acetonitrile as the solvent at mild temperatures and reusability for five repeated runs without loss of its activity.

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H201N – PubChem