Pyrrole derivatives as p2y12 antagonists

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 403/06 (2006.01) A61K 31/454 (2006.01) A61K 31/496 (2006.01) C07D 401/06 (2006.01) C07D 405/14 (2006.01)

Patent

CA 2690243

The present invention relates to compounds of the formula (I), in which R1; R2; R3; R4; R5; R6; R7; R8; R9; R10; R11; R12; R13; A; B, D and E have the meanings indicated indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable e.g. for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

La présente invention concerne des composés de formule (I), dans laquelle R1; R2; R3; R4; R5; R6; R7; R8; R9; R10; R11; R12; R13; A; B; D et E ont les significations indiquées dans les revendications. Les composés de formule (I) sont des composés pharmacologiquement actifs importants. Ils présentent un effet antiagrégation plaquettaire fort, et donc également un effet antithrombotique, et conviennent par exemple pour le traitement et la prophylaxie des troubles cardio-vasculaires comme les maladies thromboemboliques ou les resténoses. Les composés sont des antagonistes réversibles du récepteur plaquettaire de l'ADP P2Y12, et peuvent généralement être appliqués dans des conditions dans lesquelles une activation non désirée du récepteur plaquettaire de l'ADP P2Y12 est présente ou pour des traitements ou préventions pour lesquels l'inhibition du récepteur plaquettaire de l'ADP P2Y12 est prévue. L'invention concerne de plus les procédés de préparation des composés de formule (I), leur utilisation, en particulier en tant qu'ingrédients actifs dans les préparations pharmaceutiques, et les procédés de préparation des préparations pharmaceutiques les contenant.

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