Substituted indoles and their use as integrin antagonists

Details Substituted indoles and their use as integrin antagonists Substituted indoles and their use as integrin antagonists

C - Chemistry, Metallurgy

07

D

C07D 209/04 (2006.01) A61K 31/404 (2006.01) A61K 31/405 (2006.01) A61K 31/4178 (2006.01) A61K 31/4375 (2006.01) A61K 31/4402 (2006.01) A61K 31/4439 (2006.01) A61K 31/444 (2006.01) C07D 209/08 (2006.01) C07D 213/74 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 403/06 (2006.01) C07D 403/12 (2006.01) C07D 405/02 (2006.01) C07D 417/12 (2006.01) C07D 471/04 (2006.01) C07D 498/04 (2006.01)

Patent

CA 2436130

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

La présente invention concerne de nouveaux composés indole substitué qui sont des antagonistes des intégrines alpha V (.alpha.v), par exemple des intégrines .alpha.¿v?.beta.¿3? et .alpha.¿v?.beta.¿5?, des sels de ceux-ci répondant aux normes pharmaceutiques et des compositions pharmaceutiques constituées de ces composés. On peut utiliser ces composés pour le traitement d'états pathologiques induits par des intégrines .alpha.¿v?.beta.¿3? et .alpha.¿v?.beta.¿5?, notamment des pathologies comme la croissance tumorale, la présence de métastases, la resténose, l'ostéoporose, l'inflammation, la dégénérescence maculaire, la rétinopathie diabétique et l'arthrite rhumatoïde. Ces composés sont représentés par la formule générale (IV) 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¿, D, X, W, a, m, n, I, j, k et v sont tels que définis dans les spécifications.

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