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:
Sep. 23, 2014
Filed:
Mar. 25, 2010
Applicants:
Ehud Marom, Kfar Saba, IL;
Michael Mizhiritskii, Rehovot, IL;
Shai Rubnov, Tel Aviv, IL;
Inventors:
Assignee:
Mapi Pharma Ltd., Ness Ziona, IL;
Primary Examiner:
Int. Cl.
CPC ...
C07D 401/04 (2006.01); A61K 31/506 (2006.01); A61P 19/02 (2006.01); C07D 239/62 (2006.01); C07C 275/24 (2006.01); C07D 403/04 (2006.01); A61K 31/513 (2006.01); C07D 239/545 (2006.01); C07C 275/50 (2006.01);
U.S. Cl.
CPC ...
A61K 31/513 (2013.01); C07D 239/62 (2013.01); C07C 275/24 (2013.01); C07D 403/04 (2013.01); C07D 239/545 (2013.01); C07C 275/50 (2013.01);
Abstract
The present invention is based on the discovery of a process for preparing pyrimidin-dione compounds, especially alogliptin and its derivatives, which comprises the reaction of a urea derivative of formula (VIII) with a malonic acid or its derivatives to form intermediates of formulae (VII) or (VII-A), which are subsequently converted to a compound of formula (II) upon introduction of a leaving group X. Compound (II) then reacts with an amine to form compound (I), which is optionally converted to its salts of formula (IV).