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.

Date of Patent:
Oct. 02, 2018

Filed:

Mar. 30, 2016
Applicant:

Hovione Scientia Limited, Cork, IE;

Inventors:

Zita Mendes, Lisbon, PT;

Constança Cacela, Lisbon, PT;

Ana Carina Constantino, Charneca da Caparica, PT;

Bruno Santos, Odivelas, PT;

Assignee:
Attorneys:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
C07D 453/02 (2006.01); A61P 11/08 (2006.01); A61K 9/00 (2006.01); A61K 31/439 (2006.01); A61K 47/26 (2006.01); B01D 9/00 (2006.01);
U.S. Cl.
CPC ...
C07D 453/02 (2013.01); A61K 9/0075 (2013.01); A61K 31/439 (2013.01); A61K 47/26 (2013.01); A61P 11/08 (2018.01); B01D 9/005 (2013.01); B01D 9/0027 (2013.01); C07B 2200/13 (2013.01);
Abstract

A process for preparing (3R)-3-[2-Hydroxy(di-2-thienyl)acetoxy]-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide (aclidinium bromide) comprises reacting 2-hydroxy-2,2-dithien-2-ylacetic acid 1-azabicyclo[2.2.2]oct-3(R) yl methyl ester and 3-phenoxypropyl bromide, wherein the reaction takes place in a solvent or mixture of solvents selected from the group of amides and/or the group of solvents with a sulfoxide group. Also provided is a crystalline aclidinium bromide characterized by a powder XRPD pattern having peaks at 7.7±0.2° 2θ, 10.4±0.2° 2θ, 13.2±0.2° 2θ, 13.8±0.2° 2θ, 19.9±0.2° 2θ, 20.3±0.2° 2θ, 20.8±0.2° 2θ, 24.2±0.2° 2θ, 25.7±0.2° 2θ, 26.1±0.2° 2θ, 29.2±0.2° 2θ, 30.8±0.2° 2θ. A pharmaceutical composition comprises aclidinium bromide according to the invention and a pharmaceutically acceptable excipient.


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