Synthetic bile acid compositions and methods

Abstract

Bile acids and related compositions and methods of synthesis and use. More specifically, deoxycholic acid and related compositions, said compositions being free of all moieties of animal origin and free of pyrogenic moieties.

1 . A compound that is deoxycholic acid (DCA) or a pharmaceutically acceptable salt thereof: 
       
         
           
           
               
               
           
         
       
       wherein said compound is not isolated from a mammalian or microbial organism naturally producing DCA. 
     
     
         2 . A composition comprising a compound of  claim 1  and pharmaceutically acceptable excipient. 
     
     
         3 . The composition of  claim 2  further comprising at least one additional active ingredient selected from the group consisting of a neuropeptide Y (NPY) receptor antagonist and a fat selective pro-apoptotic peptide. 
     
     
         4 . The composition of  claim 3 , wherein said neuropeptide Y (NPY) receptor antagonist is selected from the group consisting of BIBP-3226, neuropeptide Y5 antagonist (the Amgen NPY receptor antagonists), BIBO-3304 (the Boehringer Ingleheim NPY receptor antagonist), BMS-192548 (the Bristol-Myers Squibb NPY receptor antagonist), AR-H040922 (the Bristol-Myers Squibb NPY receptor antagonist), LY-357897 (the Eli Lilly NPY receptor antagonist), the Esteve NPY-Y5 receptor antagonist, 1229U91 (the GlaxoSmithKline NPY receptor antagonists), GW438014S (the GlaxoSmithKline NPY receptor antagonists), JNJ-5207787 (the Johnson & Johnson NPY receptor antagonist), Lu-AA-44608 (the Lundbeck NPY receptor antagonist), MK-0557 (the Merck NPY receptor antagonist), NGD-95-1 (the Neurgogen NPY receptor antagonist), NLX-E201 (the Neurologix NPY receptor antagonist), CGP-71683 (the Novartis NPY receptor antagonist), PD-160170 (the Pfizer NPY receptor antagonists), SR-120819A (the Sanofi Aventis NPY receptor antagonists), BLIE0246 (the Sanofi Aventis NPY receptor antagonists), S.A.0204 (the Sanofi Aventis NPY receptor antagonists), S-2367 (the Shiongli NPY receptor antagonist), dihydropyridine NPY receptor antagonists, dihydropyridine derivative NPY receptor antagonists, bicyclic compound NPY receptor antagonists, carbazole NPY receptor antagonist, and tricyclic compounds NPY receptor antagonists. 
     
     
         5 . The composition of  claim 3 , wherein the fat selective pro-apoptotic peptide is CKGGRAKDC peptide that homes to white fat vasculature. 
     
     
         6 . A method for removal of fat deposits from selected locations in a mammal comprising administering to the mammal in need thereof a therapeutically effective amount of DCA or a pharmaceutically acceptable salt thereof: 
       
         
           
           
               
               
           
         
       
       wherein said compound is not isolated from a mammalian or microbial organism naturally producing DCA. 
     
     
         7 . The method of  claim 6  further comprising administering to the mammal at least one additional active ingredient selected from the group consisting of a neuropeptide Y (NPY) receptor antagonist and a fat selective pro-apoptotic peptide. 
     
     
         8 . The method of  claim 7 , wherein said neuropeptide Y (NPY) receptor antagonist is selected from the group consisting of BIBP-3226, neuropeptide Y5 antagonist (the Amgen NPY receptor antagonists), BIBO-3304 (the Boehringer Ingleheim NPY receptor antagonist), BMS-192548 (the Bristol-Myers Squibb NPY receptor antagonist), AR-H040922 (the Bristol-Myers Squibb NPY receptor antagonist), LY-357897 (the Eli Lilly NPY receptor antagonist), the Esteve NPY-Y5 receptor antagonist, 1229U91 (the GlaxoSmithKline NPY receptor antagonists), GW438014S (the GlaxoSmithKline NPY receptor antagonists), JNJ-5207787 (the Johnson & Johnson NPY receptor antagonist), Lu-AA-44608 (the Lundbeck NPY receptor antagonist), MK-0557 (the Merck NPY receptor antagonist), NGD-95-1 (the Neurgogen NPY receptor antagonist), NLX-E201 (the Neurologix NPY receptor antagonist), CGP-71683 (the Novartis NPY receptor antagonist), PD-160170 (the Pfizer NPY receptor antagonists), SR-120819A (the Sanofi Aventis NPY receptor antagonists), BLIE0246 (the Sanofi Aventis NPY receptor antagonists), S.A.0204 (the Sanofi Aventis NPY receptor antagonists), S-2367 (the Shiongli NPY receptor antagonist), dihydropyridine NPY receptor antagonists, dihydropyridine derivative NPY receptor antagonists, bicyclic compound NPY receptor antagonists, carbazole NPY receptor antagonist, and tricyclic compounds NPY receptor antagonists. 
     
     
         9 . The method of  claim 7 , wherein fat selective pro-apoptotic peptide is CKGGRAKDC peptide that homes to white fat vasculature.