864291-95-2Relevant academic research and scientific papers
TRPV4 ANTAGONISTS
-
Page/Page column 34-35, (2011/10/13)
The present invention relates to quinoline analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.
TRPV4 ANTAGONISTS
-
Page/Page column 38-39, (2011/10/13)
The present invention relates to quinoline analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.
Discovery of potent CCR4 antagonists: Synthesis and structure-activity relationship study of 2,4-diaminoquinazolines
Yokoyama, Kazuhiro,Ishikawa, Noriko,Igarashi, Susumu,Kawano, Noriyuki,Hattori, Kazuyuki,Miyazaki, Takahiro,Ogino, Shin-ichi,Matsumoto, Yuzo,Takeuchi, Makoto,Ohta, Mitsuaki
, p. 7021 - 7032 (2008/12/22)
A new series of quinazolines that function as CCR4 antagonists were discovered during the screening of our corporate compound libraries. Subsequent compound optimization elucidated the structure-activity relationships and led the identification of 2-(1,4′-bipiperidine-1′-yl)-N-cycloheptyl-6,7-dimethoxyquinazolin-4-amine 14a, which showed potent inhibition in the [35S]GTPγS-binding assay (IC50 = 18 nM). This compound also inhibited the chemotaxis of human and mouse CCR4-expressing cells (IC50 = 140 nM, 39 nM).
