WO 2012130821, BENZOIC ACID SALT OF OTAMIXABAN (SANOFI)

Otamixaban (INN) is a direct factor Xa inhibitor,[1] currently being developed by the French pharmaceutical company Sanofi-Aventis as a treatment for acute coronary syndrome.

Methyl (2R,3R)-2-{3-[amino(imino)methyl]benzyl}-3-{[4-(1-oxidopyridin-4-yl)benzoyl]amino}butanoate

Guertin KR, Choi YM (2007). “The discovery of the Factor Xa inhibitor otamixaban: from lead identification to clinical development”Curr. Med. Chem. 14 (23): 2471–81.doi:10.2174/092986707782023659PMID 17979700.

Methyl (2R,3R)-2-{3-[amino(imino)methyl]benzyl}-3-{[4-(1 -oxidopyridin-4-yl)benzoyl]amino}butanoate, (CAS number 193153-04-7) has the International Nonproprietary Name Otamixaban

The present invention (WO2012130821) 4TH OCT 2012, BENZOIC ACID SALT OF OTAMIXABAN, SANOFI relates to a benzoic acid salt of methyl (2R,3R)-2-{3-[amino(imino)methyl]benzyl}-3-{[4-(1 -oxidopyridin-4-yl)benzoyl]amino}butanoate, and to a benzoic acid salt of methyl (2R,3R)-2-{3-[amino(imino)methyl]benzyl}-3-{[4-(1 -oxidopyridin-4-yl)benzoyl]amino}butanoate which is in a crystalline form or in at least partially crystalline form, as well as a process for the preparation of the same, methods of using such salt to treat subjects suffering from conditions which can be ameliorated by the administration of an inhibitor of Factor Xa and shows the structure illustrated in Formula I:

 

 

The benzoic acid salt of methyl (2R,3R)-2-{3-[amino(imino)methyl]benzyl}-3-{[4-(1 -oxidopyridin-4-yl)benzoyl]amino}butanoate according to claims 1 to 5 for use in the treatment of acute myocardial infarction, non-ST elevation myocardial infarction, unstable angina, thromboembolism, acute vessel closure associated with thrombolytic therapy, percutaneous transluminal coronary angioplasty, transient ischemic attacks, stroke, intermittent claudication, and restenosis.

http://patentscope.wipo.int/search/en/detail.jsf?docId=WO2012130821&recNum=1&docAn=EP2012055364&queryString=WO:2012130821%20&maxRec=1

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