182181-36-8Relevant academic research and scientific papers
CHEMOKINE RECEPTOR ANTAGONISTS AND METHODS OF USE THEREOF
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Paragraph 1604; 0605, (2016/02/21)
Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: or physiologically acceptable salt thereof.
NOVEL COMPOUNDS
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Page/Page column 21, (2009/01/24)
The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof for treating diseases and conditions mediated by positive allosteric modulation of the G- protein coupled metabotropic subtype 5 receptor (mGluR5), such as neur
Design, synthesis, in vitro, and in vivo characterization of phenylpiperazines and pyridinylpiperazines as potent and selective antagonists of the melanocortin-4 receptor
Tran, Joe A.,Jiang, Wanlong,Tucci, Fabio C.,Fleck, Beth A.,Wen, Jenny,Sai, Yang,Madan, Ajay,Ta, Kung Chen,Markison, Stacy,Foster, Alan C.,Hoare, Sam R.,Marks, Daniel,Harman, John,Chen, Caroline W.,Arellano, Melissa,Marinkovic, Dragan,Bozigian, Haig,Saunders, John,Chen, Chen
, p. 6356 - 6366 (2008/03/30)
Benzylamine and pyridinemethylamine derivatives were synthesized and characterized as potent and selective antagonists of the melanocortin-4 receptor (MC4R). These compounds were also profiled in rodents for their pharmacokinetic properties. Two compounds with diversified profiles in chemical structure, pharmacological activities, and pharmacokinetics, 10 and 12b, showed efficacy in an established murine cachexia model. For example, 12b had a Ki value of 3.4 nM at MC4R, was more than 200-fold selective over MC3R, and had a good pharmacokinetic profile in mice, including high brain penetration. Moreover, 12b was able to stimulate food intake in the tumor-bearing mice and reverse their lean body mass loss. Our results provided further evidence that a potent and selective MC4R antagonist with appropriate pharmacokinetic properties might potentially be useful for the treatment of cancer cachexia.
Chemokine receptor antagonists and methods of use thereof
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, (2008/06/13)
Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: formula (1) or physiologically acceptable salt thereof.
IMIDAZO[1,2-A]PYRIDINES FOR THE TREATMENT OF CNS AND CARDIAC DISEASES
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, (2008/06/13)
The present invention relates to imidazo[1,2-a]pyridine compounds of formula (1) STR1 which are dopamine D-4 antagonists and useful as anti-psychotic agents.
