The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Patent No.:

US 9056814 B1

PDF
Full Text
Expired
Date of Patent:
Jun. 16, 2015

Filed:

Jun. 24, 2011
Applicants:

Soren Ebdrup, Roskilde, DK;

Kim Troensegaard Nielsen, Jyllinge, DK;

Tanja Maria Greve, Birkerød, DK;

Inventors:

Soren Ebdrup, Roskilde, DK;

Kim Troensegaard Nielsen, Jyllinge, DK;

Tanja Maria Greve, Birkerød, DK;

Assignee:

LEO PHARMA A/S, Ballerup, DK;

Attorney:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
C07C 43/20 (2006.01); A61K 31/075 (2006.01); C07C 217/74 (2006.01); C07C 213/10 (2006.01); A61K 31/196 (2006.01); A61K 31/592 (2006.01); A61K 31/593 (2006.01);
U.S. Cl.
CPC ...
C07C 217/74 (2013.01); C07C 213/10 (2013.01); C07C 2101/08 (2013.01); A61K 31/196 (2013.01); A61K 31/592 (2013.01); A61K 31/593 (2013.01);
Abstract

The present invention relates to the crystalline, polymorphic Form C of the calcimimetic compound {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid, to methods of preparation thereof, to methods of characterization thereof by single crystal X-Ray crystallography (XRC), X-Ray Powder diffractometry, attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy, Solid State NMR spectroscopy and Differential Scanning Calorimetry (DSC), and to its use. The invention also relates to the preparation of Form C by crystallization from a saturated solution of {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid in the presence of crystallization seeds of Form C, or alternatively by conversion of an amorphous starting material into the different crystalline polymorphic Form X by crystallization of {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid, followed by a solid solution transformation thereof into the desired polymorphic Form C.


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