Substituted benzimidazoles and their use as parp inhibitors

Details Substituted benzimidazoles and their use as parp inhibitors Substituted benzimidazoles and their use as parp inhibitors

C - Chemistry, Metallurgy

07

D

C07D 401/04 (2006.01) A61K 31/4184 (2006.01) A61K 31/454 (2006.01) A61K 31/496 (2006.01) A61P 9/00 (2006.01) A61P 25/00 (2006.01) C07D 235/30 (2006.01) C07D 401/14 (2006.01) C07D 403/04 (2006.01)

Patent

CA 2352554

The invention relates to compounds of general formula (1a) or (1b) wherein R1 and R4 are hydrogen or defined substituents, A is a saturated or monoethenoid heterocyclic ring with 4 to 8 members which contains one or two nitrogen atoms, wherein additionally one oxygen or sulfur atom can be present. Said ring can be further substituted. The invention also relates to their tautomer forms, possible enantiomer and diastereomer forms, their prodrugs, as well as possible physiologically acceptable salts. The invention also relates to the use of said compounds for treating diseases related to a pathologically increased activity of PARP.

L'invention concerne des composés de la formule générale 1a ou 1b. Dans ces formules, R1 et R4 désignent hydrogène ou des substituants déterminés, A désigne un composé hétérocyclique saturé ou monoéthénoïde, ayant entre 4 et 8 chaînons, qui contient un ou deux atomes d'azote, un atome d'oxygène ou de soufre qui peut en outre être substitué, pouvant de plus être intégré. L'invention concerne également les formes tautomères de ces composés, des formes énantiomères et diastéréomères possibles, leurs promédicaments, ainsi que des sels physiologiquement compatibles possibles. L'invention concerne par ailleurs l'utilisation de ces composés pour traiter des affections dans lesquelles la PARP manifeste des activités intensifiées au plan pathologique.

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