IP Library Granted Patent US 9,790,177
Granted Patent B2
US 9,790,177 · App. 15/285,037 · Granted Oct 17, 2017

Forms of [R-(R*,R*)]-2-(4-fluorophenyl)-beta, gamma-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid calcium salt (2:1)

Inventors: George Michael Laurence (West Lafayette, IN); Aeri Park (Lansdale, PA); Timothy Andrew Woods (Edinburgh, IN)
Assignee: Warner-Lambert Company LLC
C07D207/34
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Quick Facts
Patent No.
US 9,790,177
App. No.
15/285,037
Granted
Oct 17, 2017
Kind
B2
Abstract

Novel forms of [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-Dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1-H-pyrrole-1-heptanoic acid hemi calcium salt designated Form XX, Form XXI, Form XXII, Form XXIII, Form XXIV, Forms XXV, Form XXVI, Form XXVII, Form XXVIII, Form XXIX, and Form XXX 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, benign prostatic hyperplasia (BPH) and Alzheimer's disease.

Claims (10)

1. A Form XXV atorvastatin calcium having an X-ray powder diffraction containing the following 2θ values measured using CuKa radiation: 3.1, 5.2, 7.4, 8.7, 10.4, 12.7, 16.6, 18.1, 19.2, 20.0, 20.7, 23.2, and 24.4.

2. A Form XXVI atorvastatin calcium having an X-ray powder diffraction containing the following 2θ values measured using CuKa radiation: 3.7, 8.4, 9.0, 17.1, 17.7, 18.7, 20.1, 22.3, and 23.0.

3. A Form XXV atorvastatin calcium having an X-ray powder diffraction containing the following 2θ values measured using CuKa radiation: 7.4, 8.7, 19.2, and 20.0, and a solid state 19 F nuclear magnetic resonance having the following chemical shifts expressed in parts per million: −113.2, −116.3, and −118.4.

4. A Form XXV atorvastatin calcium having an X-ray powder diffraction containing the following 2θ values measured using CuKa radiation: 3.1, 5.2, 6.4, 7.4, 7.9, 8.7, 10.4, 12.0, 12.7, 16.6, 18.1, 19.2, 20.0, 20.7, 22.8, 23.2, 24.4, 25.6, 26.5, and 29.3.

5. A Form XXVI atorvastatin calcium having an X-ray powder diffraction containing the following 2θ values measured using CuKa radiation: 3.7, 7.3, 8.4, 9.0, 12.2, 16.0, 17.1, 17.7, 18.7, 20.1, 20.7, 22.3, 23.0, 25.2, and 28.7.

6. A Form XXV atorvastatin calcium having an X-ray powder diffraction containing the following 2θ values measured using CuKa radiation: 3.1, 5.2, 7.4, 8.7, 23.2, and 24.4.

7. A Form XXVI atorvastatin calcium having an X-ray powder diffraction containing the following 2θ values measured using CuKa radiation: 3.7, 8.4, 9.0, 17.1, 18.7, 20.1, and 23.0.

8. A Form XXV atorvastatin calcium characterized by Raman spectroscopy having the following peaks expressed in cm −1 : 138, 224, 245, 300, 422, 495, 617, 644, 697, 726, 825, 859, 901, 1001, 1034, 1058, 1112, 1159, 1181, 1243, 1320, 1368, 1397, 1412, 1477, 1528, 1604, 1654, 2257, 2933, and 3063.

9. A Form XXV atorvastatin calcium having a solid state 13 C nuclear magnetic resonance having the following chemical shifts expressed in parts per million: 186.3, 185.0, 182.5, 177.0, 167.0, 166.2, 162.8, 160.9, 138.6, 136.1, 133.4, 129.2, 128.5, 126.0, 124.0, 121.5, 120.7, 118.0, 116.8, 116.0, 69.9, 68.0, 46.4, 43.3, 40.9, 25.7, 25.2, 21.3, 20.0, and 0.6.

10. A Form XXV atorvastatin calcium having a solid state 19 F nuclear magnetic resonance having the following chemical shifts expressed in parts per million: −113.2, −116.3, and −118.4.

Assignments (2)
CHANGE OF NAME Recorded Oct 31, 2022
From: UPJOHN US 1 LLC
To: VIATRIS SPECIALTY LLC.
Reel/Frame 061808/0420 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 6, 2020
From: WARNER-LAMBERT COMPANY LLC
To: UPJOHN US 1 LLC
Reel/Frame 054293/0956 →
Continuity (7)
Division 14924011 · Oct 27, 2015
Division 14520742 · Oct 22, 2014
Division 14021151 · Sep 9, 2013
Division 13214559 · Aug 22, 2011
Division 11572333
Provisional Application 60589485 · Jul 20, 2004
Related Publication 20170022156A1 · Jan 26, 2017