Substituted dihydropyrano indole-3,4-dione derivatives and...

C - Chemistry – Metallurgy – 07 – D

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C07D 491/052 (2006.01) A61K 31/407 (2006.01)

Patent

CA 2509242

Compounds of formula (I) and (II) are provided wherein: X is an alkali metal or a basic amine moiety; R1 is alkyl, cycloalkyl, -CH2-cycloalkyl, pyridinyl, - CH2-pyridinyl, phenyl or benzyl, the rings of these groups being optionally substituted; R2 is H, halogen, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, -CH2- cycloalkyl, -NH2, or -NO2; R3 is phenyl, benzyl, benzyloxy, pyridinyl, or -CH2- pyridinyl, with the rings of these groups being optionally substituted; or a pharmaceutically acceptable salt or ester form thereof, as well as pharmaceutical compositions and methods using these compounds as inhibitors of plasminogen activator inhibitor-1 (PAI-1) and as therapeutic compositions for treating conditions resulting from fibrinolytic disorders such as deep vein thrombosis and coronary heart disease, and pulmonary fibrosis.

L'invention concerne des composés de formule (I) et (II). Dans ces formules, X désigne un métal alcalin ou une fraction amine basique; R¿1? désigne alkyle, cycloalkyle, cycloalkyl-CH¿2?-, pyridinyle, pyridinyl-CH¿2?-, phényle ou benzyle, les anneaux de ces groupes étant éventuellement substitués; R¿2? désigne H, halogène, alkyle, perfluoroalkyle, alcoxy, cycloalkyle, cycloalkyl-C¿2?-, -NH¿2?, ou -N0¿2?; R¿3? désigne phényle, benzyle, benzyloxy, pyridinyle, ou pyridinyl-CH¿2?-, les anneaux de ces groupes étant éventuellement substitués ; ou un sel ou un ester pharmaceutiquement acceptable de ceux-ci, ainsi que des compositions pharmaceutiques et des méthodes d'utilisation de ces composés en tant qu'inhibiteurs d'un inhibiteur 1 d'activateur du plasminogène (PAI-1), et en tant que compositions thérapeutiques permettant de traiter les troubles résultant de troubles fibrinolytiques, notamment une thrombose veineuse profonde, une coronaropathie et une fibrose pulmonaire.

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