Bile acid derivatives, processes for their preparation, and use as pharmaceuticals

US5668126A · kind A · utility

Assignee

• Hoechst GmbH · DE

Inventors

• Werner Kramer · Schwandorf, DE
• Gunther Wess · Niederrodenbach, DE

Key dates

• Filing date: Jun 7, 1995
• Grant date: Sep 16, 1997
• Expiry date: Jun 7, 2015

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K38/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Bile acid derivatives of the formula I EQU W--X--G in which G is a bile acid radical, W is an active compound 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 compounds 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 hepatoprotective agent, an antihyperlipidemic, a diuretic, a hypotensive, 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, alternatively, a bond.