Substituted benzofurans and benzothiophenes, methods of...

C - Chemistry – Metallurgy – 07 – D

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C07D 409/12 (2006.01) A61K 31/443 (2006.01) A61K 31/4436 (2006.01) A61P 19/10 (2006.01) A61P 29/00 (2006.01) A61P 35/00 (2006.01) C07D 405/12 (2006.01)

Patent

CA 2445629

The present invention relates to novel substituted benzofurans and benzothiophenes compounds that are antagonists of alpha V(.alpha.v) integrins, for example agr;v.beta.3 and .alpha.v.beta.5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by .alpha.v6beta;5 integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneraion, diabetic retinopathy, and rheumatoid arthritis. The compounds have the general formula (I), where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, m, n, i, j an ka are defined herein.

L'invention concerne de nouveaux composés de benzofurannes et de benzothiophènes substitués qui sont des antagonistes des intégrines alpha V(.alpha.v), par exemple des intégrines .alpha.¿v?.beta.¿3? et .alpha.¿v?.beta.¿5?, leurs sels acceptables sur le plan pharmaceutique, et des compositions pharmaceutiques de celles-ci. Ces composés peuvent être utilisés dans le traitement de cas pathologiques par le biais d'intégrines .alpha.¿v?.beta.¿3? et .alpha.¿v?.beta.¿5?, et d'états tels que la croissance tumorale, la métastase, la resténose, l'ostéoporose, l'inflammation, la dégénérescence maculaire, la rétinopathie diabétique, et la polyarthrite rhumatoïde. Ces composés sont représentés par la formule (I), dans laquelle R?1¿, R?2¿, R?3¿, R?4¿, R?5¿, R?6¿, R?7¿, R?8¿, R?9¿, R?10¿, R?11¿, R?12¿, R?13¿, R?14¿, m, n, i, j et k sont définis.

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