Non-covalent inhibitors of urokinase and blood vessel formation

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 5/062 (2006.01) A61K 38/05 (2006.01) C07K 5/06 (2006.01) C07K 5/078 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2387002

Novel compounds having activity as non-covalent inhibitors of urokinase and having activity in reducing or inhibiting blood vessel formation are provided. These compounds have P1 a group having an amidino or guanidino moiety or derivative thereof. These compounds are useful in vitro for monitoring plasminogen activator levels and in vivo in treatment of conditions which are ameliorated by inhibition of or decreased activity of urokinase and in treating pathologic conditions wherein blood vessel formation is related to a pathologic condition.

L'invention concerne de nouveaux composés présentant une activité d'inhibiteurs non covalents de l'urokinase ainsi qu'une activité de réduction ou d'inhibition de la formation de vaisseaux sanguins. Ces composés comportent en P1 un groupe portant un fragment amidino ou guanidino ou un dérivé de ce fragment. Ces composés servent au contrôle in vivo de niveaux d'activateurs de plasminogène, au traitement in vivo d'affections pouvant être traitées par inhibition ou réduction de l'activité de l'urokinase, ainsi qu'au traitement d'affections pathologiques dans lesquelles la formation de vaisseaux sanguins est liée à une affection pathologique.

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