Synthetic conjugated bile acid and method of use thereof
Patent 5079240 Issued on January 7, 1992. Estimated Expiration Date: 
March 15, 2010. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.
March 15, 2010. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.Patent References 3846411 3852440 3859437 3910888 Quantitative evaluation of enteric microbial overgrowth Labelled bile acids Investigating body function Process for purifying iodinated bile acid conjugates Method and reagents for measuring the level of conjugated bile acids Pharmaceutical composition of prolonged action containing bile acids InventorApplicationNo. 493902 filed on 03/15/1990US Classes:514/182, Oxygen single bonded to a ring carbon of the cyclopentanohydrophenanthrene ring system514/867, DIARRHEA514/877GALLSTONEExaminersPrimary: Rose, Shep K.Attorney, Agent or FirmForeign Patent References
International ClassA61K 031/56AbstractA method is described for the replacement of bile acid in the biliary tract during conditions of bile acid deficiency which comprises administering an effective amount of a synthetic bile acid comprising the reaction product of a natural bile acid and an N-alkyl amino acid. A critical element of the invention is the presence of the N-methyl amino acid as the conjugating moiety for the synthetic bile acid. Such does not occur in nature, and is a key factor in the ability of the compounds of this invention to be efficacious in the treatment method of the invention.Also described is a bile acid replacement composition which comprises the reaction product of a natural bile acid and an N-alkyl amino acid. The N-alkyl amino acid is an N-alkyl glycine, more preferably N-methyl glycine; the natural bile acid is cholic acid; and in the exemplified embodiment the compound is the N-acyl reaction product of N-methyl glycine and cholic acid, i.e., cholylsarcosine.Potential clinical uses of the compounds of this invention as natural bile acid replacements include use when natural bile acid secretion into the small intestine is decreased or when normally secreted bile acids are deconjugated by bacterial overgrowth.Other References
Field of SearchOxygen single bonded to a ring carbon of the cyclopentanohydrophenanthrene ring systemOxygen bonded directly at the 12-position (e.g., cholic acids, desoxycholic acids, dehydrocholic acids, etc.) Halogen, nitrogen, or sulfur containing (e.g., glycocholic acids, taurocholic acids, etc.) Oxygen bonded directly at the 6- or 7-position (e.g., chenodeoxycholic acids, ursodeoxycholic acids, etc.) Exactly one oxygen bonded directly to the cyclopentanohydrophenanthrene ring system (e.g., 3-hydroxycholanic acids, lithocholic acids, etc.) Carbon bonded directly at the 17 beta-position of the cyclopentanohydrophenanthrene ring system is a member of an acyclic chain of three or four uninterruped carbons, (e.g., diketobisnorcholenic acids, etc.) | |
