N-alkyl-taurourodeoxycholic acids and their therapeutically acti

Details N-alkyl-taurourodeoxycholic acids and their therapeutically acti N-alkyl-taurourodeoxycholic acids and their therapeutically acti

1994-02-15

1996-03-19

Kestler, Kimberly J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Cyclopentanohydrophenanthrene ring system doai

552554, A61K 31575, C07J 900

Patent

active

055004210

ABSTRACT:
The invention discloses N-alkyl-tauroursodeoxycholic acids and their pharmaceutically acceptable salts of the formula ##STR1## wherein R is a C.sub.2 -C.sub.4 alkyl group and R.sub.1 is hydrogen, an alkali metal, an alkaline earth metal or a radical of a basic amino acid.
The compounds are prepared by reacting a mixed anhydride of ursodeoxycholic acid and alkyltaurine followed by percolation through two columns respectively containing a strong cationic resin in H.sup.+ form and a weakly anionic resin OH.sup.- form. The compounds are useful for the treatment of hepatic diseases.

REFERENCES:
patent: 3580936 (1971-05-01), Pattchett et al.
patent: 3622669 (1971-11-01), Patchett et al.
patent: 4104285 (1978-08-01), Gallo-Torres et al.
patent: 4565810 (1986-01-01), Castagnola et al.
patent: 4892868 (1990-01-01), Castagnola et al.
patent: 5122520 (1992-06-01), Azria et al.
Schmassmann et al "Prevention of Ursodeoxycholate . . . " Hepatology, vol. 11, No. 6, 1990, pp. 989-996.
Batta et al "Substrate Specificity of Cholylglycine . . . " Journal of Biological Chemistry, vol. 259, No. 24, 1984, pp. 15035-15039.

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