440634-06-0Relevant articles and documents
3-substituted-1,5-benzodiazepine compound and pharmaceutical application thereof
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, (2019/11/20)
The invention belongs to the technical field of medicine, and relates to a 3-substituted-1,5-benzodiazepine compound with a general molecular formula of a formula I and application of the 3-substituted-1,5-benzodiazepine compound to medicine. The 3-substituted-1,5-benzodiazepine compound can selectively inhibit the activity of glycogen synthase kinase-3beta (GSK 3beta) and can be used for the preparation of the medicine for preventing and/or treating diseases with abnormal pathological characteristics of the GSK 3beta, wherein the diseases includes cancer, neurological diseases, metabolic syndromes and the like. (Please see the specification for the formula.)
Design, synthesis, and biological evaluation of 1,5-benzothiazepine-4-one derivatives targeting factor VIIa/tissue factor
Ayral, Erwan,Gloanec, Philippe,Berge, Gilbert,de Nanteuil, Guillaume,Mennecier, Philippe,Rupin, Alain,Verbeuren, Tony J.,Fulcrand, Pierre,Martinez, Jean,Hernandez, Jean-Francois
supporting information; scheme or table, p. 1386 - 1391 (2009/10/15)
The 1,5-benzothiazepine-4-one scaffold was earlier shown to provide efficient protease inhibitors. In this contribution, we describe its use in the design of factor VIIa/tissue factor inhibitors. A series containing a scaffold non-substituted on its aryl part led to compound 20 with an IC50 of 2.16 μM. Following molecular modelling studies of this compound, a second series was prepared, which necessitated the synthesis of protected 7- or 8-substituted 1,5-benzothiazepine-4-one derivatives.