Polymorphic forms of olopatadine hydrochloride and methods for producing olopatadine and salts thereof
US7687646B2 · kind B2 · utility
Assignees
Inventors
Key dates
| Filing date | Mar 28, 2006 |
| Grant date | Mar 30, 2010 |
| Priority date | — |
| Expiry date | Nov 17, 2027 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07F9/5442
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.