Invention Grant
US07687646B2 Polymorphic forms of olopatadine hydrochloride and methods for producing olopatadine and salts thereof
有权
盐酸奥洛他定的多形态形式及其制备奥洛他定及其盐的方法
- Patent Title: Polymorphic forms of olopatadine hydrochloride and methods for producing olopatadine and salts thereof
- Patent Title (中): 盐酸奥洛他定的多形态形式及其制备奥洛他定及其盐的方法
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Application No.: US11392098Application Date: 2006-03-28
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Publication No.: US07687646B2Publication Date: 2010-03-30
- Inventor: Thomas Bader , Hans-Ulrich Bichsel , Bruno Gilomen , Imelda Meyer-Wilmes , Mark Sundermeier
- Applicant: Thomas Bader , Hans-Ulrich Bichsel , Bruno Gilomen , Imelda Meyer-Wilmes , Mark Sundermeier
- Applicant Address: CH Schaffhausen CH Zürich
- Assignee: Azad Pharmaceutical Ingredients, AG,Universität Zürich
- Current Assignee: Azad Pharmaceutical Ingredients, AG,Universität Zürich
- Current Assignee Address: CH Schaffhausen CH Zürich
- Agency: Locke, Lord, Bissell & Liddell LLP
- Agent Roberta L. Hastreiter; Scott B. Feder
- Main IPC: C07D313/10
- IPC: C07D313/10

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.
Public/Granted literature
- US20070232814A1 Polymorphic forms of olopatadine hydrochloride and methods for producing olopatadine and salts thereof Public/Granted day:2007-10-04
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