Urokinase inhibitors

Details Urokinase inhibitors Urokinase inhibitors

C - Chemistry, Metallurgy

07

K

C07K 5/062 (2006.01) A61K 38/05 (2006.01) A61P 35/00 (2006.01) C07C 281/06 (2006.01) C07K 5/06 (2006.01) G01N 33/68 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2411981

The invention relates to a highly active, highly specific urokinase inhibitor which is suitable for therapeutic applications and can be synthesized in an extremely simple manner. Surprisingly, it was found that amidino benzylamine derivatives, especially 4-amidino-benzylamine, with two bonded amino acids represent a new group of highly active and very selective uPA inhibitors. The urokinase inhibitors can be used in medical applications, e.g. in the treatment of malign tumors such as in cases of metastatic spread.

L'invention concerne un agent apte à des utilisations thérapeutiques, inhibiteur à haute activité et à haute spécificité de l'urokinase et dont la synthèse est la plus simple possible. On a découvert de façon surprenante que des dérivés de l'amidino-benzylamine, notamment 4-amidino-benzylamine, constituent, avec deux acides aminés liés, un nouveau groupe d'inhibiteurs uPA hautement actifs et très sélectifs. Les inhibiteurs de l'urokinase sont utilisés dans des applications médicales, par exemple dans le traitement de tumeurs malignes et de la formation de métastases.

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