US2011152509A1PendingUtilityA1

Compositions of polysaccharides derived from heparin, their preparation and pharmaceutical compositions containing them

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Assignee: AVENTIS PHARMA SAPriority: Jul 21, 2000Filed: Aug 25, 2010Published: Jun 23, 2011
Est. expiryJul 21, 2020(expired)· nominal 20-yr term from priority
Inventors:Christelle PecquetElisabeth PerrinChristian Viskov
C08B 37/0078A61K 31/727C08B 37/0075
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Claims

Abstract

Alkali and alkali-earth metal salts of polysaccharides derived from heparin, their method of preparation and the pharmaceutical compositions containing them.

Claims

exact text as granted — not AI-modified
1 . A composition comprising at least one alkali or alkaline-earth metal salt of at least one sulphated polysaccaride of heparin, said at least one alkali or alkaline-earth metal salt of at least one sulphated polysaccaride of heparin having
 a mean molecular weight in the range from 1500 to 3000 daltons;   an anti-Xa activity in the range from 94 to 150 IU/mg;   an anti-IIa activity in the range up to 10 IU/mg;   and an anti-Xa activity:anti-IIa activity ratio greater than 10:1.   
     
     
         2 . A composition comprising at least one alkali or alkaline-earth metal salt of at least one sulphated polysaccaride of heparin in which the alkali or alkaline-earth metal salt of at least one sulphated polysaccaride of heparin has 2 to 26 saccharide units and has a 4,5-unsaturated glucuronic acid 2-O-sulphate unit at least one end. 
     
     
         3 . A composition according to  claim 1  in which the alkali or alkaline-earth metal salt of at least one sulphated polysaccaride of heparin has 2 to 26 saccharide units and has a 4,5-unsaturated glucuronic acid 2-O-sulphate unit at least one end. 
     
     
         4 . A composition according to  claim 2  having anti-Xa activity in the range of 125 to 150 IU/mg. 
     
     
         5 . A composition according to  claim 2  having a mean molecular weight in the range of 2000 to 3000 daltons. 
     
     
         6 . A composition according to  claim 2  having anti-Xa activity in the range of 140 to 150 IU/mg and a mean molecular weight in the range of 2000 to 3000 daltons. 
     
     
         7 . A composition according to  claim 2 , in which the at least one alkali or alkaline-earth metal salt is a sodium, potassium, calcium or magnesium salt. 
     
     
         8 . A composition according to  claim 2 , having an anti-IIa activity in the range of up to 5 IU/mg. 
     
     
         9 . A composition according to  claim 2 , having an anti-Xa activity:anti-IIa activity ratio greater than 25. 
     
     
         10 . The method of preparing at least one alkali or alkaline-earth metal salt of at least one sulphated polysaccaride of heparin comprising:
 depolymerizing a quaternary ammonium salt of the benzyl ester of heparin in an organic medium with a base with a pKa greater than 20;   converting the quaternary ammonium salt of the benzyl ester of the depolymerized heparin to a sodium salt;   saponifying the ester; and   optionally purifying the product.   
     
     
         11 . The method according to  claim 10 , in which the at least one alkali or alkaline-earth metal salt of at least one sulphated polysaccharide of heparin has a mean molecular weight in the range of 1500 to 3000 daltons. 
     
     
         12 . The method according to  claim 10 , in which the at least one alkali or alkaline-earth metal salt of at least one sulphated polysaccharide of heparin has an anti-Xa activity in the range of 94 to 150 IU/mg. 
     
     
         13 . The method according to  claim 10 , in which the at least one alkali or alkaline-earth metal salt of at least one sulphated polysaccharide of heparin has an anti-IIa activity in the range of up to 10 IU/mg. 
     
     
         14 . The method according to  claim 10 , in which the at least one alkali or alkaline-earth metal salt of at least one sulphated polysaccharide of heparin has an anti-Xa activity:anti-IIa activity ratio greater than 10:1. 
     
     
         15 . The method according to  claim 10 , in which the at least one alkali or alkaline-earth metal salt of at least one sulphated polysaccharide of heparin comprises 2 to 26 saccharide units and has a 4,5-unsaturated glucuronic acid 2-O-sulphate unit at least one end. 
     
     
         16 . The method according to  claim 10 , in which the quaternary ammonium salt of the benzyl ester of heparin is a benzethonium, cetylpyridinium, or cetyltrimethylammonium salt. 
     
     
         17 . The method according to  claim 10 , in which the base with a pKa greater than 20 is chosen from 1,5,7-triazabicyclo-[4.4.0]-dec-5-ene, 2-tert-butylimino-2-diethylamino-1,3-dimethylperhydro-1,3,2-diaza-phosphorine, a base of guanidine, and a base of phosphazene. 
     
     
         18 . The method according to  claim 17 , in which the base of guanidine comprises: 
       
         
           
           
               
               
           
         
       
       where R 1  is hydrogen or alkyl, and where R 2 , R 3 , R 4 . and R 5 , which are identical or different, and each is a C 1 -C 6  alkyl. 
     
     
         19 . The method according to  claim 18 , where R 1  is hydrogen, and R 2 , R 3 , R 4  and R 5  are each methyl. 
     
     
         20 . The method according to  claim 17 , in which the base of phosphazene comprises: 
       
         
           
           
               
               
           
         
       
       where R 1  to R 7  are identical or different, and each is a C 1 -C 6  alkyl. 
     
     
         21 - 46 . (canceled)

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