C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 471/04 (2006.01) C07D 213/64 (2006.01) C07D 221/00 (2006.01)
Patent
CA 2389999
A novel process is provided for the preparation of imidazolidinone .alpha.v.beta.3/.alpha.v.beta.5 integrin antagonists, and the useful intermediates obtained therein. These compounds are antagonists of .alpha.v.beta.3/.alpha.v.beta.5 integrin receptors and thus useful for inhibiting bone resorption and treating and preventing osteoporosis. Also disclosed is 3-{2-oxo-3-[3-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)- propyl]imidazolidin-1-yl}-3(S)-(6-methoxy-pyridin-3-yl)-propionic acid in the form of a hemihydrate.
L'invention concerne un nouveau procédé de préparation d'antagonistes d'intégrine .alpha.v.beta.3/.alpha.v.beta.5 d'imidazolidinone, et les intermédiaires utiles obtenus dans ces derniers. Ces composés sont des antagonistes de récepteurs d'intégrine .alpha.v.beta.3/.alpha.v.beta.5, et sont ainsi utiles pour inhiber la résorption osseuse, traiter et prévenir l'ostéoporose. L'invention concerne également 3-{2-oxo-3-[3-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-propyl]imidazolidin-1-yl}-3(S)-(6-methoxy-pyridin-3-yl)-acide propionique sous forme de semi-hydrate.
Jensen Mark S.
Palucki Michael
Rivera Nelo R.
Wang Yaling
Wells Kenneth M.
Merck & Co. Inc.
Merck Sharp & Dohme Corp.
Norton Rose Or S.e.n.c.r.l. S.r.l./llp
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