NOVEL FORMS OF [R-(R*,R*)]-2-(4-FLUOROPHENYL)-beta,delta-DIHYDROXY-5-(1-METHYLETHYL)-3-PHENYL-4-[(PHENYLAMINO)CARBONYL]-1H-PYRROLE-1-HEPTANOIC ACID MAGNESIUM
AssigneePfizer Inc.
InventorsJason A. Leonard, Janathan M. Miller
Life of this patent
Estimating the term…
Abstract
Novel forms of atorvastatin magnesium salt designated Form A, Form B, Form C, Form D, Form E, and Form F, pharmaceutical compositions containing such compounds, methods for their preparation and methods utilizing the compounds for treatment of hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia (BPH) and Alzheimer's disease are described.
Claims15
A Form A atorvastatin magnesium having an X-ray powder diffraction containing the following 2θ values measured using CuKa radiation:
- 9.3, 14.3, and 18.4.
A Form A atorvastatin magnesium having a solid state NMR shift selected from the group consisting of:
- A) a 13Cshift containing the values:
- 118.7, 124.4, 140.3, and 141.7 ppm;
- and
- B) an 19F shift containing the values:
- −108.4, and −112.6 ppm.
A Form B atorvastatin magnesium having an X-ray powder diffraction containing the following 2θ values measured using CuKa radiation:
- 6.1, 8.0, 10.9, 19.8, and 23.0.
A Form B atorvastatin magnesium having a solid state NMR shift selected from the group consisting of:
- A) a 13C shift containing values:
- 118.3, 125.4, 126.8, 132.2, and 133.8 ppm;
- and
- B) an 19F shift containing value:
- −115.7 ppm.
A Form C atorvastatin magnesium having an X-ray diffraction containing the following 2θ values measured using CuKa radiation:
- 5.2, 6.6, and 12.3.
A Form C atorvastatin magnesium having a solid state NMR shift selected from the group consisting of:
- A) a 13Cshift containing the values:
- 129.2, 133.3, and 139.1 ppm;
- and
- B) an 19F shift containing the values:
- −109.6, and −113.0 ppm.
A Form D atorvastatin magnesium having an X-ray diffraction containing the following 2θ values measured using CuKa radiation:
- 7.7, 20.5, and 24.2.
A Form D atorvastatin magnesium having a solid state NMR shift selected from the group consisting of:
- A) a 13Cshift containing the values:
- 132.6, 134.4, 136.9, and 138.6 ppm;
- and
- B) an 19F shift containing the values:
- −110.0, −111.7, −114.7, and −119.8 ppm.
(canceled)
(canceled)
A Form F atorvastatin magnesium having an X-ray diffraction containing the following 2θ values measured using CuKa radiation:
- 8.7, 10.1, 11.7, and 16.1.
A Form F atorvastatin magnesium having a solid state NMR shift selected from the group consisting of:
- A) a 13Cshift containing the values:
- 128.5, 130.4, and 138.2 ppm;
- and
- B) an 19F shift containing the values:
- −114.7, −118.8, −119.8, and −122.3 ppm.
A pharmaceutical composition comprising atorvastatin magnesium selected from the group consisting of Form A, Form B, Form C, Form D, and Form F;
- and at least one pharmaceutically acceptable excipient, diluent, or carrier.
A method for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, or Alzheimer's disease comprising administering to a patient suffering therefrom a therapeutically effective amount of atorvastatin magnesium selected from the group consisting of Form A, Form B, Form C, Form D, Form E, and Form F.
A method for preparing Form A, Form B, Form C, Form D, Form E, and Form F atorvastatin magnesium comprising forming atorvastatin magnesium under conditions which yield Forms A, B, C, D, E, and F atorvastatin magnesium.
Dependencies are inferred from the claim text.