871556-32-0Relevant academic research and scientific papers
Structure-activity relationship studies and discovery of a potent transient receptor potential vanilloid (TRPV1) antagonist 4-[3-chloro-5-[(1 S)-1,2-dihydroxyethyl]-2-pyridyl]-N-[5-(trifluoromethyl)-2-pyridyl]-3, 6-dihydro-2 H-pyridine-1-carboxamide (V116517) as a clinical candidate for pain management
Tafesse, Laykea,Kanemasa, Toshiyuki,Kurose, Noriyuki,Yu, Jianming,Asaki, Toshiyuki,Wu, Gang,Iwamoto, Yuka,Yamaguchi, Yoshitaka,Ni, Chiyou,Engel, John,Tsuno, Naoki,Patel, Aniket,Zhou, Xiaoming,Shintani, Takuya,Brown, Kevin,Hasegawa, Tsuyoshi,Shet, Manjunath,Iso, Yasuyoshi,Kato, Akira,Kyle, Donald J.
, p. 6781 - 6794 (2014)
A series of novel tetrahydropyridinecarboxamide TRPV1 antagonists were prepared and evaluated in an effort to optimize properties of previously described lead compounds from piperazinecarboxamide series. The compounds were evaluated for their ability to block capsaicin and acid-induced calcium influx in CHO cells expressing human TRPV1. The most potent of these TRPV1 antagonists were further characterized in pharmacokinetic, efficacy, and body temperature studies. On the basis of its pharmacokinetic, in vivo efficacy, safety, and toxicological properties, compound 37 was selected for further evaluation in human clinical trials.
NOVEL HETEROCYCLYL COMPOUNDS
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Page/Page column 32, (2010/02/17)
The invention is concerned with novel heterocyclyl compounds of formula (I) wherein A, X, Y1, Y2, Y3, R3, R4, R5, R6, R7, R8, R9, R10, m, n and p are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor and can be used as medicaments.
