Bile acid derivatives, processes for their preparation, and...

Details Bile acid derivatives, processes for their preparation, and... Bile acid derivatives, processes for their preparation, and...

C - Chemistry, Metallurgy

07

J

167/191, 260/62,

C07J 9/00 (2006.01) A61K 31/56 (2006.01) A61K 31/66 (2006.01) A61K 38/05 (2006.01) C07D 213/26 (2006.01) C07D 213/56 (2006.01) C07D 213/81 (2006.01) C07J 17/00 (2006.01) C07J 31/00 (2006.01) C07J 41/00 (2006.01) C07J 43/00 (2006.01) C07J 51/00 (2006.01) C07K 5/06 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2025294

Bile acid derivatives of the formula I W - X - G in which G ie a bile acid radical, W is an active com- pound moiety of a medicament and X is a bonding member between a bile acid radical and active compound moiety, are outstandingly suitable for introducing active com- pounds into the enterohepatic circulation. The compounds I are absorbed and pass into the bloodstream. It is possible in this way, using the natural reabsorption of the bile acids, to achieve improved absorption of non- absorbable or poorly absorbable pharmaceuticals. W may be, for example, a peptide, an antibiotic, an antiviral substance, an anticancer agent, a hepatoprotec- tive agent, an antihyperlipidemic, a diuretic, a hypoten- sive, a renin inhibitor, a substance for the treatment of cirrhosis of the liver or a substance for the treatment of diabetes. G is a bile acid radical in the form of the free natural or chemically modified acids, the esters and amides, the salt forms and forms derivatized on alcohol groups. X is a large number of intermediate members or, alterna- tively, a bond.

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