942232-53-3Relevant academic research and scientific papers
Optimization of 1,3,4-benzotriazepine-based CCK2 antagonists to obtain potent, orally active inhibitors of gastrin-mediated gastric acid secretion
McDonald, Iain M.,Black, James W.,Buck, Ildiko M.,Dunstone, David J.,Griffin, Eric P.,Harper, Elaine A.,Hull, Robert A. D.,Kalindjian, S. Barret,Lilley, Elliot J.,Linney, Ian D.,Pether, Michael J.,Roberts, Sonia P.,Shaxted, Mark E.,Spencer, John,Steel, Katherine I. M.,Sykes, David A.,Walker, Martin K.,Watt, Gillian F.,Wright, Laurence,Wright, Paul T.,Xun, Wei
, p. 3101 - 3112 (2008/02/09)
Starting from a novel, achiral 1,3,4-benzotriazepine-based CCK2 receptor antagonist, a process of optimization has afforded further compounds of this type that maintain the nanomolar affinity for recombinant, human CCK2 receptors and high selectivity over
Anti-tumor compounds
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, (2008/06/13)
The invention relates to quinazoline derivatives, or pharmaceutically-acceptable salts thereof, which possess anti-tumour activity; to processes for their manufacture; and to pharmaceutical compositions containing them. The invention provides a quinazoline of the formula: STR1 wherein R1 includes hydrogen, amino and alkyl or alkoxy each of up to 4 carbon atoms; R2 includes hydrogen, alkyl, hydroxyalkyl and halogenoalkyl each of up to 4 carbon atoms; R3 is hydrogen or alkyl or up to 3 carbon atoms; Ar is phenylene or heterocyclene; L is a group of the formula --CO.NH--, --NH.CO--, --CO.NR4 --, --NR4.CO--, --CH=CH-- or --CO.O--, wherein R4 is alkyl of up to 4 carbon atoms; and Y is a branched alkyl group bearing substituents Y2 and Y3 the definition of each independently including hydroxy, cyano, aryl and heteroaryl, and the definition of Y3 also optionally including sulpho, N-phenylsulphonylcarbamoyl and 5-tetrazolyl; or a pharmaceutically-acceptable salt thereof.
