Crystalline forms of [r-(r*,r*)]-2-(4-fluorophenyl)-beta,...

Details Crystalline forms of [r-(r*,r*)]-2-(4-fluorophenyl)-beta,... Crystalline forms of [r-(r*,r*)]-2-(4-fluorophenyl)-beta,...

C - Chemistry, Metallurgy

07

D

C07D 207/34 (2006.01) A61K 31/40 (2006.01) A61P 3/06 (2006.01) A61P 19/10 (2006.01) A61P 25/28 (2006.01)

Patent

CA 2450111

Novel crystalline forms of [R-(R*,R*)]-2-(4-fluorophenyl)-.beta., .DELTA.;- dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1- heptanoic acid hemi calcium salt atorvastatin designated Form V, Form VI, Form VII, Form VIII, Form IX, Form X, Form XI, Form XII, Form XIII, Form XIV, Form XV, Form XVI, Form XVII, Form XVIII, and Form XIX are characterized by their X- ray powder diffraction, solid-state NMR, and/or Raman spectroscopy are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, and Alzheimer's disease.

L'invention concerne des nouvelles formes cristallines de sel hémicalcique d'acide [R-(R*,R*)]-2-(4-fluorophényl)-.beta.,.delta.-dihydroxy-5-(1-méthyléthyl)-3-phényl-4-[(phénylamino)carbonyl]-1H-pyrrole-1-heptanoïque (atorvastatine), appelées Forme V, Forme VI, Forme VII, Forme VIII, Forme IX, Forme X, Forme XI, Forme XII, Forme XIII, Forme XIV, Forme XV, Forme XVI, Forme XVII, Forme XVIII et Forme XIX. Ces formes sont caractérisées par leur diffraction des rayons X sur poudre, leur NMR en phase solide et/ou leur spectroscopie Raman. L'invention concerne également des procédés de préparation et une composition pharmaceutique de ces formes, lesquelles sont utiles comme agents destinés à traiter l'hyperlipidémie, l'hypercholestérolémie, l'ostéoporose et la maladie d'Alzheimer.

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