Fatty acid derivatives of bile acids and bile acid derivatives

C - Chemistry – Metallurgy – 07 – J

Patent

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C07J 41/00 (2006.01) A61K 31/575 (2006.01) A61P 1/00 (2006.01) A61P 9/10 (2006.01) C07J 9/00 (2006.01)

Patent

CA 2325933

The present invention relates to bile acid or bile salt fatty acid conjugates (hereinafter called "BAFAC"), to their use in dissolving cholesterol gallstones in bile, preventing their occurrence or recurrence, to their use in reducing or preventing arteriosclerosis and to methods for the treatment of said diseases. The conjugates are of the formula W - X - G in which G is a bile acid or bile salt radical, W stands for one or two saturated fatty acid radicals and X is either a direct bond or a bonding member between said bile acid or bile salt and fatty acid(s). The conjugation is advantageously performed at a position selected among the 3, 6, 7, 12 and 24 positions of the bile acid or bile salt nucleus. The fatty acids are preferably saturated fatty acids having (14 - 22) carbon atoms.

La présente invention concerne des conjugués d'acide biliaire ou d'acides gras de sels biliaires, l'utilisation de ces derniers pour dissoudre dans de la bile les lithiases biliaires à cholestérol, empêcher leur apparition ou leur réapparition, et leur utilisation en vue de réduire ou de prévenir l'artériosclérose ainsi que des procédés de traitement de ces maladies. Les conjugués sont représentés par la formule W - X - G dans laquelle G représente un acide biliaire ou un radical de sel biliaire, W représente un ou deux radicaux d'acides gras saturés et X représente soit une liaison directe soit un élément de liaison situé entre l'acide biliaire ou le sel biliaire et le ou les acides gras. La conjugaison est, pour un meilleur résultat, effectuée à un endroit sélectionné entre les positions 3, 6, 7, 12 et 24 du noyau d'acide biliaire ou de sel biliaire. Les acides gras sont de préférence des acides gras saturés comprenant de 14 à 22 atomes de carbone.

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