220352-27-2Relevant articles and documents
Benzoazepine derivative as potent antagonists of the glycine binding site associated to the NMDA receptor
Di Fabio, Romano,Micheli, Fabrizio,Baraldi, Davide,Bertani, Barbara,Conti, Nadia,Dal Forno, Giovanna,Feriani, Aldo,Donati, Daniele,Marchioro, Carla,Messeri, Tommaso,Missio, Andrea,Pasquarello, Alessandra,Pentassuglia, Giorgio,Pizzi, Domenica A.,Provera, Stefano,Quaglia, Anna M.,Sabbatini, Fabio M.
, p. 723 - 738 (2003)
A series of benzoazepine derivatives, bearing suitable substituents at the C-3 position, was designed and evaluated by superimposition with the pharmacophore model of the glycine binding site. To fully explore the SAR of this class of compounds and to allow the preparation of new different compounds at the C-3 position, appropriate synthetic routes were set up. The benzoazepines were evaluated in terms of in vitro affinity using [ 3H]glycine binding assay and in vivo potency by inhibition of convulsions induced by N-methyl-D-aspartate (NMDA) in mice. This further analysis confirmed the preliminary results previously reported and that compound 27 is the most promising compound (Ki=32 nM, ED50=0.09 mg/kg, i.v.) in this series. Significant neuroprotective effect was observed after both pre- and post-ischaemia administration in the MCAo model. In particular, after post-ischaemia administration, it was found to be still effective when the administration was delayed up to 6 h after occlusion of the middle cerebral artery.
3-SUBSTITUTED 2-AMINO-INDOLE DERIVATIVES
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Page/Page column 109, (2016/04/04)
The present invention provides compounds of formula (I) (Formula (I)) and pharmaceutically acceptable salts thereof, wherein Q, X% X4,X5 X6, X7,R1, R2, R3 and R8 are as defined in the specification, processes for the preparation of such compounds, pharmaceutical compositions containing them and the use of such compounds in therapy.
EPOTHILONE DERIVATIVES, METHOD FOR PRODUCING SAME AND THEIR PHARMACEUTICAL USE
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, (2008/06/13)
This invention relates to the new epothilone derivatives of general formula I, 1in which substituents Y, Z R2a, R2b, R3, R4a, R4b, D—E, R5, R6, R7, R8 and X have the meanings that are indicated in more detail in the description. The new compounds interact with tubulin by stabilizing microtubuli that are formed. They are able to influence the cell-splitting in a phase-specific manner and are suitable for treating malignant tumors, for example, ovarian, stomach, colon, adeno-, breast, lung, head and neck carcinomas, malignant melanomas, acute lymphocytic and myelocytic leukemia. In addition, they are suitable for anti-angiogenesis therapy as well as for treatment of chronic inflammatory diseases (psoriasis, arthritis). To avoid uncontrolled proliferation of cells and for better compatibility of medical implants, they can be applied or introduced into polymer materials. The compounds according to the invention can be used alone or to achieve additive or synergistic actions in combination with other principles and classes of substances that can be used in tumor therapy.