Sanofi

Genzyme Corporation

Gernot Zech

Melitta Just

Gerhard Hessler

Tilo Weiss

Marc Nazaré

Elisabeth Defossa

Kurt Ritter

Jochen Goerlitzer

Sven Ruf

Marc Nazare

Werngard Czechtizky

Maria Mendez-Perez

Joerg Czech

Valérie Fossey

Nils Rackelmann

Markus Kohlmann

Angelina Besse

The present disclosure relates to isoxazolidines and their use as receptor-interacting protein kinase 1 inhibitors, for example in the treatment of diseases and disorders mediated by RIP kinase 1.

Isoxazolidines as RIPK1 inhibitors and use thereof

The present invention relates to compounds of the formula I, in which R; R; R; R; R; R; Z; A; B; E; X; Q; J; 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 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.

Quinoline-carboxamide derivatives as P2Y12 antagonists

The present invention relates to compounds of the formula I, whereinR1; R2; Z; A; B; D; Q; J; 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 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.

Pyrazole-carboxamide derivatives as P2Y12 antagonists

The present invention relates to compounds of the formula I, wherein

Heterocyclic pyrazole-carboxamidesas P2Y12 antagonists

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Frankfurt am Main, Germany

Gernot Zech