50424-28-7Relevant articles and documents
Intramolecular Ring-Opening of Oxetanes: Access to Functionalised Hydroxymethyl 2,3-Dihydroimidazo[1,2- c ]quinazolines
Bagal, Sharan K.,Bodnarchuk, Michael S.,King, Thomas A.,Luo, Xuehong,McKerrecher, Darren,Steward, Oliver R.,Wang, Peng
supporting information, p. 502 - 506 (2020/03/13)
An intramolecular oxetane ring-opening was developed, affording novel 2-(hydroxymethyl)-2,3-dihydroimidazo[1,2- c ]quinazolines from N -(3-methyloxetan-3-yl)quinazolin-4-amines under mild conditions. The resulting medicinally relevant tricyclic scaffolds were synthesised in good yields with diverse substituents. Moreover, reaction optimisation led to the development of a one-pot procedure.
IDENTIFICATION AND USE OF ERK5 INHIBITORS
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Page/Page column 51; 91, (2019/10/01)
The present invention covers heterocyclic compounds of general formula (I) in which T, U, Y, Z, R1 and R3 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer disorders, as a sole agent or in combination with other active ingredients.
Synthesis and biological evaluation of novel quinazoline-4-piperidinesulfamide derivatives as inhibitors of NPP1
Forcellini, Elsa,Boutin, Sophie,Lefebvre, Carole-Anne,Shayhidin, Elnur Elyar,Boulanger, Marie-Chloé,Rhéaume, Gabrielle,Barbeau, Xavier,Lagüe, Patrick,Mathieu, Patrick,Paquin, Jean-Fran?ois
, p. 130 - 149 (2018/02/14)
The ecto-nucleotide pyrophosphatase/phosphodiesterase-1 (NPP1) was recently shown to promote mineralization of the aortic valve, hence, its inhibition represents a significant target. A quinazoline-4-piperidine sulfamide compound (QPS1) has been described as a specific and non-competitive inhibitor of NPP1. We report herein the synthesis and in vitro inhibition studies of novel quinazoline-4-piperidine sulfamide analogues using QPS1 as the lead compound. Of the 26 derivatives prepared, four compounds were found to have Ki 105 nM against human NPP1.