797804-60-5Relevant academic research and scientific papers
Development of a potent and selective FLT3 kinase inhibitor by systematic expansion of a non-selective fragment-screening hit
Nakano, Hirofumi,Hasegawa, Tsukasa,Imamura, Riyo,Saito, Nae,Kojima, Hirotatsu,Okabe, Takayoshi,Nagano, Tetsuo
, p. 2370 - 2374 (2016/04/20)
A non-selective inhibitor (1) of FMS-like tyrosine kinase-3 (FLT3) was identified by fragment screening and systematically modified to afford a potent and selective inhibitor 26. We confirmed that 26 inhibited the growth of FLT-3-activated human acute myeloid leukemia cell line MV4-11. Our design strategy enabled rapid development of a novel type of FLT3 inhibitor from the hit fragment in the absence of target-structural information.
Indazole-derivatives as factor Xa inhibitors
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Page 63, (2008/06/13)
The present invention relates to compounds of the formulae I and Ib wherein R0 ; R1 ; R2 ;Q; V, G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formulae I and Ib, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
