Novel 4-aminopyridazines, processes for their production as...

C - Chemistry – Metallurgy – 07 – D

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C07D 237/22 (2006.01) A61K 31/495 (2006.01) A61K 31/53 (2006.01) C07D 237/20 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01) C07D 413/12 (2006.01) C07D 417/12 (2006.01)

Patent

CA 2198366

The invention concerns novel 4-aminopyridazines of general formula, (I), in which R1 means the group R2-SO2-O- or R2-SO2-NR3, wherein R2 means a cycloalkyl group, an unsubstituted or substituted aryl or heteroaryl group, R3 means a hydrogen atom, an alkyl or alkyloxyalkyl group, which can be unsubstituted or substituted one or more times by hydroxy groups, wherein the hydroxy groups can be substituted by alkyl, hydroxyalkyl, alkyloxyalkyl, hydroxyalkyloxyalkyl or alkylcarbonyl groups and wherein two vicinal hydroxy groups can each be linked by alkylidene groups, as well as hydrates, solvates and physiologically compatible salts thereof. The invention further concerns the optically active forms, racemates and diastereomer mixtures of these compounds, a method of preparing them and drugs containing these compounds and having a thrombin-inhibiting effect.

L'invention a pour objet de nouvelles amino-4 pyridazines, de formule générale (I), dans laquelle R?1¿ désigne le groupe R?2¿-SO¿2?-O- ou R?2¿-SO¿2?-NR?3¿, où R?2¿ désigne un reste cycloalkyle, un reste aryle ou hétéro-aryle non substitué ou substitué, R?3¿ désigne un atome d'hydrogène, un groupe alkyle ou alkyloxyalkyle pouvant être non substitué ou substitué une ou plusieurs fois par des groupes hydroxy, lesdits groupes hydroxy pouvant être substitués par des groupes alkyle, hydroxyalkyle, alkyloxyalkyle, hydroxyalkyloxyalkyle ou alkylcarbonyle et deux groupes hydroxy voisins pouvant être reliés par des groupes alkylidène, ainsi que les hydrates, solvates et les sels physiologiquement compatibles de ces composés. L'invention a également pour objet les formes optiquement actives, les racémates et les mélanges diastéréomères de ces composés, leur procédé de production, ainsi que les médicaments contenant ces composés, à effet inhibiteur de la thrombine.

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