Phosphoric acid salt of an integrin receptor antagonist

Details Phosphoric acid salt of an integrin receptor antagonist Phosphoric acid salt of an integrin receptor antagonist

C - Chemistry, Metallurgy

07

D

C07D 487/04 (2006.01) A61K 31/55 (2006.01) A61P 19/10 (2006.01) C07D 471/04 (2006.01) C07D 487/02 (2006.01)

Patent

CA 2424117

The phosphoric acid salt of 3-(2-methoxy-pyrimidin-5-yl)-5-oxo-9-(6,7,8,9- tetrahydro-5H-pyrido[2,3-b]azepin-2-yl)-nonanoic acid is a potent antagonist of the integrin .alpha..nu..beta.3 receptor and is useful for the prevention and/or treatment of osteoporosis and vascular restenosis, as well as conditions associated with excessive angiogenesis, such as macular degeneration, diabetic retinopathy, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth. The invention also relates to a process for the preparation of the novel salt as well as pharmaceutical compositions and methods of use.

le sel d'acide phosphorique d'acide 3-(2-méthoxy-pyrimidin-5-yl)-5-oxo-9-(6,7,8,9-tétrahydro-5H-pyrido[2,3-b]azépin-2-yl) nonanoïque, qui est un antagoniste puissant du récepteur .alpha..nu..beta.3 de l'intégrine, convient bien pour la prévention et/ou le traitement de l'ostéoporose et des la resténose vasculaire ainsi que d'états liés à une angiogenèse excessive tels que la dégénérescence maculaire, la rétinopathie diabétique, l'athérosclérose, l'arthrite inflammatoire, le cancer, et la métastatisation de tumeurs. L'invention concerne également une technique de préparation de ce nouveau sel ainsi que des compositions pharmaceutiques et des méthodes d'utilisation.

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