125117-98-8Relevant articles and documents
Discovery of novel pyridyl carboxamides as potent CCR5 antagonists and optimization of their pharmacokinetic profile in rats
Duan, Maosheng,Kazmierski, Wieslaw M.,Chong, Pek Y.,DeAnda, Felix,Edelstein, Mark,Ferris, Rob,Peckham, Jennifer,Wheelan, Pat,Xiong, Zhiping,Zhang, Huichang,Nishizawa, Rena,Takaoka, Yoshikazu
scheme or table, p. 6470 - 6475 (2011/11/29)
A novel series of pyridyl carboxamide-based CCR5 inhibitors was designed, synthesized, and demonstrated to be highly potent against HIV-1 infection in both HOS and PBL assays. Attempts to evaluate this series of compounds in a rat PK model revealed its instability in rat plasma. A hypothesis for this liability was proposed, and strategies to overcome this issue were pursued, leading to discovery of highly potent 40 and 41, which featured dramatically improved rat PK profiles. 2011 Elsevier Ltd. All rights reserved.
Arylaminoaryl-alkyl-substituted imidazolidine-2,4-diones, process for preparing them, medicaments comprising these compounds, and their use
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Page/Page column 58, (2009/09/07)
This invention relates to arylaminoaryl-alkyl-substituted imidazolidone-2,4-diones of formula (I) and also to their physiologically tolerated salts: Wherein R, R′, R1 to R10, A, D, E, G, L and p are as defined herein. The invention also relates to processes for preparing them, pharmaceutical compositions comprising them and their therapeutic use. The compounds are suitable, for example, as anti-obesity drugs and for treating cardiometabolic syndrome.