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

Patent metadata

Field	Value
Publication number	US-9309195-B2
Application number	US-201514716361-A
Country	US
Kind code	B2
Filing date	May 19, 2015
Priority date	May 5, 2004
Publication date	Apr 12, 2016
Grant date	Apr 12, 2016

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 olamine having an x-ray powder diffraction pattern containing the following 2θ peaks measured using CuKα radiation: 8.5, 9.8, 17.4, 18.6, 20.9, 22.5, and 24.1, or a solid state 19F nuclear magnetic resonance having the following chemical shifts measured in parts per million: −118.7.

2. An atorvastatin olamine having an x-ray powder diffraction pattern containing the following 2θ peaks measured using CuK α radiation: 8.5, 9.8, 11.4, 12.0, 16.3, 17.4, 18.6, 19.6, 20.1, 20.9, 21.4, 22.0, 22.5, 22.8, 23.5, 24.1, 25.1, 25.9, 26.2, 27.8, 28.8, 29.6, 31.7, and 37.7.

3. An atorvastatin olamine characterized by solid state 13 C nuclear magnetic resonance having the following chemical shifts expressed in parts per million: 182.0, 178.9, 165.4, 161.6, 159.5, 137.4, 134.8, 133.8, 131.0, 128.7, 128.0, 127.0, 123.1, 122.6, 121.9, 120.9, 120.1, 117.3, 115.6, 114.3, 66.5, 66.0, 65.2, 58.5, 58.2, 51.1, 47.8, 46.0, 43.9, 42.4, 41.3, 40.6, 39.8, 25.7, 23.1, 21.1, and 20.7.

4. An atorvastatin olamine characterized by solid state 13 C nuclear magnetic resonance having the following chemical shifts expressed in parts per million: 182.0, 178.9, 165.4, 161.6, 159.5, 25.7, 23.1, 21.1, and 20.7.

Assignees

• Pfizer

Inventors

• Krzyzaniak Joseph Francis
• Leonard Jason Albert

Classifications

• A61P3/06

  Antihyperlipidemics · CPC title

• A61P43/00

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