Substituted benzofurans and benzothiophenes, methods of making and methods of use as integrin antagonists

摘要

The present invention relates to novel substituted benzofurans and benzothiophenes compounds that are antagonists of alpha V (alphav) integrins, for example alpha_vbeta₃ and alpha_vbeta₅ integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by alpha_vbeta₃ and alpha_vbeta₅ integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, 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 and k are defined herein.