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.:
Date of Patent:
Mar. 30, 2010
Filed:
Mar. 28, 2006
Thomas Bader, Zürich, CH;
Hans-ulrich Bichsel, Hörhausen, CH;
Bruno Gilomen, Zürich, CH;
Imelda Meyer-wilmes, Haag, CH;
Mark Sundermeier, Dusseldorf, DE;
Thomas Bader, Zürich, CH;
Hans-Ulrich Bichsel, Hörhausen, CH;
Bruno Gilomen, Zürich, CH;
Imelda Meyer-Wilmes, Haag, CH;
Mark Sundermeier, Dusseldorf, DE;
Azad Pharmaceutical Ingredients, AG, Schaffhausen, CH;
Universität Zürich, Zürich, CH;
Abstract
The present invention provides a novel polymorphic form of olopatadine hydrochloride ([(Z)-3-(dimethylamino)propylidene]-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid hydrochloride), a selective histamine H1-receptor antagonist that is used for the treatment of ocular symptoms of seasonal allergic conjunctivitis. The present invention also provides novel methods for producing olopatadine on a large scale, and in a manner that is cost effective, provides a low level of impurities and eliminates the need to use the costly and dangerous base, butyllithium, which is used in prior art reactions for making olopatadine. The present invention further provides novel processes for carrying out a large scale production of 3-dimethylaminopropyltriphenylphosphonium bromide and its corresponding hydrobromide salt, which are employed in the production of olopatadine, and pharmaceutically acceptable salts of olopatadine.