92900-79-3Relevant academic research and scientific papers
HEPARANASE INHIBITORS AND USE THEREOF
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Paragraph 0144; 0181, (2018/07/05)
The invention relates to functionalized quinazoline compounds, pharmaceutical compositions comprising such compounds, and the use of such compounds as heparanase inhibitors for the treatment of diseases or conditions related to heparanse activity.
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).
2-(β-Arylethylamino)- and 4-(β-Arylethylamino)quinazolines as Phosphodiesterase Inhibitors
Millen, J.,Riley, T. N.,Waters, I. W.,Hamrick, M. E.
, p. 12 - 17 (2007/10/02)
The existence of several forms of cAMP phosphodiesterase having different kinetic characteristics suggests the feasibility of developing tissue-selective inhibitors of this enzyme.This observation is of particular importance in the development of therapeutic agents for the management of reversible obstructive airways disorders.The present report describes the design, synthesis and pharmacological characterization of a series of 6,7-dimethoxyquinazoline derivatives having β-arylethylamine substituents at the 2- or 4- positions.The quinazoline nucleus is intended to confer a high degree of inhibitory activity for phosphodiesterase while the β-arylethylamine moieties are designed to provide selectivity for adrenergically innervated tissue.The target compounds of this study, 6 and 7 were prepared via β-arylethylamine displacement of chloride from an appropriate chloroquinazoline intermediate.The resulting products were evaluated for their ability to relax guinea pig tracheal smooth muscle and as inhibitors of phosphodiesterase.
