50424-28-7Relevant articles and documents
Quinazoline and phthalazine derivatives as novel melatonin receptor ligands analogues of agomelatine
Bolteau, Rapha?l,Descamps, Florian,Ettaoussi, Mohamed,Caignard, Daniel H.,Delagrange, Philippe,Melnyk, Patricia,Yous, Sa?d
, (2020/01/30)
For further development of successors of Agomelatine through modulation of its pharmacokinetic properties, we report herein the design, synthesis and pharmacological results of a new family of melatonin receptor ligands. Issued from the introduction of quinazoline and phthalazine scaffolds carrying an ethyl amide lateral chain and a methoxy group as bioisosteric ligands analogues of previously developed Agomelatine. The biological activity of the prepared analogues was compared with that of Agomelatine. Quinazoline and phthalazine rings proved to be a versatile scaffold for easy feasible MT1 and MT2 ligands. Potent agonists with sub-micromolar binding affinity were obtained. However, the presence of two nitrogen atoms resulted in compounds with lower affinity for both MT1 and MT2, in comparison with the parent compound, balanced by the exhibition of good pharmacokinetic properties.
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.