Phosphinic acid amides as matrix metalloprotease inhibitors

C - Chemistry – Metallurgy – 07 – F

Patent

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Details

C07F 9/36 (2006.01) C07F 9/44 (2006.01) C07F 9/58 (2006.01) C07F 9/6553 (2006.01)

Patent

CA 2264254

The invention provides compounds which are useful as inhibitors of matrix matalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to a compound having a structure according to formula (I) wherein R1, R2, R3 and R4 are described in the claims, a stereoisomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable alkoxyamide, ester acyloxyamide, imide or derivative thereof. Also disclosed are compounds, pharmaceutical compositions and methods of treating diseases characterized by matrix metalloprotease activity using these compounds or the pharmaceutical compositions containing them.

La présente invention concerne des composés convenant comme inhibiteurs de métalloprotéases de matrices et qui sont efficaces dans le traitement d'états caractérisés par une activité excessive de ces enzymes. L'invention concerne en l'occurrence, non seulement un composé dont la structure est représentée par la formule générale (I) et dans laquelle R¿1?, R¿2?, R¿3? et R¿4? sont tels que décrits par les revendications, mais aussi l'un de ses stéréoisomères ou énantiomères, l'un de ses sels pharmaceutiquement admis, ou encore l'un de ses alcoxylamides biohydrolysables, l'un de ses esters alcoxylamides, l'un de ses imides ou l'un de leurs dérivés. L'invention concerne également des composés, des compositions pharmaceutiques et des thérapies dirigées contre des affections caractérisées par une activité de métalloprotéase de matrices, lesquelles thérapies impliquent l'utilisation de ces composés ou de compositions pharmaceutiques contenant ces composés.

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