Salt forms of [R-(R*,R*)]-2-(4-fluorophenyl)-β, δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic-acid

Patent metadata

Field	Value
Publication number	US-9637449-B2
Application number	US-201615061931-A
Country	US
Kind code	B2
Filing date	Mar 4, 2016
Priority date	May 5, 2004
Publication date	May 2, 2017
Grant date	May 2, 2017

Abstract

Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra 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, benign prostatic hyperplasia, and Alzheimer's Disease.

First claim

What is claimed is:

1. An atorvastatin 2-amino-2-methylpropan-1-ol having an x-ray powder diffraction pattern containing the following 2θ peaks measured using CuKα radiation: 4.2, 8.3, 16.0, 17.5, 18.3, 19.4, and 19.7, or a solid state 19 F nuclear magnetic resonance having the following chemical shifts measured in parts per million: −113.6 and −116.5.

2. An atorvastatin 2-amino-2-methylpropan-1-ol having an x-ray powder diffraction pattern containing the following 2θ peaks measured using CuK α radiation: 4.2, 6.0, 6.2, 8.3, 11.5, 12.5, 12.6, 16.0, 17.5, 18.3, 18.8, 19.4, 19.7, 21.3, 22.0, 22.8, 23.4, and 23.8.

3. An atorvastatin 2-amino-2-methylpropan-1-ol characterized by solid state 13 C nuclear magnetic resonance having the following chemical shifts expressed in parts per million: 179.8, 166.3, 163.3, 161.5, 161.2, 140.5, 139.5, 134.4, 132.3, 131.6, 129.8, 128.1, 126.1, 125.1, 122.2, 120.7, 116.4, 114.0, 113.4, 72.6, 71.4, 67.6, 66.3, 64.7, 64.4, 53.1, 46.9, 43.9, 43.5, 42.7, 39.7, 36.1, 26.8, 26.3, 24.3, 23.8, 23.1, 22.0, and 20.4.

4. An atorvastatin 2-amino-2-methlypropan-1-ol characterized by solid state 13 C nuclear magnetic resonance having the following chemical shifts expressed in parts per million: 179.8, 166.3, 163.3, 22.0, and 20.4.

Assignees

• Pfizer

Inventors

• Krzyzaniak Joseph Francis
• Leonard Jason Albert

Classifications

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P3/06

  Antihyperlipidemics · CPC title

• A61P25/28

  for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia · CPC title

• A61P15/08

  for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis · CPC title

• A61P19/10

  for osteoporosis · CPC title