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:
Feb. 12, 2013

Filed:

Apr. 24, 2008
Applicants:

Stefan Welzig, Vienna, AT;

Jan Rothenburger, Oslip, AT;

Beate Kälz, Steinbrunn, AT;

József Gungl, Sopron, HU;

Klaus Gerdes, Vienna, AT;

Federico Gaeta, Mountain View, CA (US);

Inventors:

Stefan Welzig, Vienna, AT;

Jan Rothenburger, Oslip, AT;

Beate Kälz, Steinbrunn, AT;

József Gungl, Sopron, HU;

Klaus Gerdes, Vienna, AT;

Federico Gaeta, Mountain View, CA (US);

Assignee:
Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D 295/107 (2006.01);
U.S. Cl.
CPC ...
Abstract

The invention relates to a method for producing highly pure 2,4'-dimethyl-3-piperidino-propiophenone (tolperisone) (formula I) and the pharmaceutically acceptable salts, hydrochlorides, and hydrates thereof. The method allows the content of the undesired byproduct 2-methyl-1-(4-methylphenyl) propenone (4-MMPPO) to be kept significantly lower than in previously known methods. The invention further relates to active substance formulations which contain tolperisone and are suitable, among other things, for producing combination preparations used for treating patients suffering from Alzheimer's disease. The invention also relates to topical formulations, controlled release (CR) formulations, and transdermal therapeutic systems, such as active substance patches, which contain less than 50 ppm, preferably less than 10 ppm, more preferably less than 7 ppm, and most preferably less than 3 ppm or 0 ppm (i.e. less than the detectable amount) of the undesired byproduct 2-methyl-1-(4-methylphenyl) propenone (4-MMPPO) in relation to 100 percent by weight of active substance.


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