Tyrosine alkoxyguanidines as integrin inhibitors

C - Chemistry – Metallurgy – 07 – C

Patent

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C07C 311/03 (2006.01) A61K 31/18 (2006.01) A61K 31/381 (2006.01) A61K 31/4164 (2006.01) A61K 31/4245 (2006.01) C07C 311/06 (2006.01) C07C 311/10 (2006.01) C07C 311/13 (2006.01) C07C 311/15 (2006.01) C07C 311/19 (2006.01) C07C 311/29 (2006.01) C07C 311/42 (2006.01) C07C 311/46 (2006.01) C07C 317/14 (2006.01) C07D 209/48 (2006.01) C07D 231/18 (2006.01) C07D 233/84 (2006.01) C07D 271/12 (2006.01) C07D 277/36 (2006.01) C07D 277/54 (2006.01) C07D 311/70 (2006.01) C07D 333/34 (2006.01) C07D 333/62 (2006.01) C07D

Patent

CA 2362372

The present invention relates to novel tyrosine alkoxyguanidine compounds that are inhibitors 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 the treatment of pathological conditions mediated by .alpha.v.beta.3 and .alpha.v.beta.5 integrins, including conditions such as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. The compounds have general formula (IV), where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, m and n are defined herein.

L'invention concerne des composés de tyrosine alcoxyguanidine inhibant les intégrines alpha V (.alpha.v), par exemple .alpha.v.beta.3 et .alpha.v.beta.5, y compris leurs sels pharmaceutiquement acceptables, et des compositions pharmaceutiques correspondantes. Les composés peuvent être utilisés dans le traitement des états pathologiques dont la médiation est assurée par les intégrines .alpha.v.beta.3 et .alpha.v.beta.5, y compris la croissance tumorale, la métastase, la resténose, l'ostéoporose, l'inflammation, la dégénérescence maculaire, la rétinopathie diabétique et la polyarthrite rhumatoïde. Les composés sont représentés par la formule générale (IV). Dans ladite formule, R?1¿, R?2¿, R?3¿, R?4¿, R?5¿, R?6¿, R?7¿, R?8¿, R?9¿, R?10¿, R?11¿, m et n sont tels que définis dans le corps de l'invention.

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