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. 03, 2019
Filed:
Oct. 14, 2016
Applicant:
Pharmaleads, Paris, FR;
Inventors:
Herve Poras, Villepreux, FR;
Loic Lefebvre, Canteleu, FR;
Xinjun Zhao, Dalian, CN;
Luca Gamberoni, Comerio Va, IT;
Sabrina De Rosa, Cervignano del Friuli Ud, IT;
Rosario Velardi, Udine Ud, IT;
Assignee:
PHARMALEADS, Paris, FR;
Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07C 323/25 (2006.01); C07C 319/02 (2006.01); C07C 319/22 (2006.01); C07C 319/24 (2006.01); C07C 319/28 (2006.01); C07C 327/32 (2006.01); B01J 19/18 (2006.01); C07D 215/26 (2006.01); C07C 323/40 (2006.01);
U.S. Cl.
CPC ...
C07C 323/25 (2013.01); B01J 19/1862 (2013.01); C07C 319/02 (2013.01); C07C 319/22 (2013.01); C07C 319/24 (2013.01); C07C 319/28 (2013.01); C07C 327/32 (2013.01); C07D 215/26 (2013.01); B01J 2219/0004 (2013.01); B01J 2219/00029 (2013.01); C07B 2200/07 (2013.01); C07C 323/40 (2013.01);
Abstract
The present invention relates to an industrial process for the preparation of (5S,10S)-10-benzyl-16-methyl-11,14,18-trioxo-15,17,19-trioxa-2,7,8-trithia-12-azahenicosan-5-aminium (E)-3-carboxyacrylate salt of following formula (I): wherein X is fumarate. This process comprises the following successive key steps: a kinetic resolution, formation of disulfide compound, peptide coupling, and anion exchange reaction to obtain the desired product of formula (I).