Amide derivatives of natural bile acids, prepared by conjugating 3b amine derivatives of bile acids with acid chlorides, succinic anhydride or glutamic anhydride

Amide derivatives of natural bile acids which are substituted in the 3-position on ring A are claimed. Amide derivatives of bile acids which are substituted in the 3-position on ring A and are of the following formula are claimed: Independent claims are also included for the preparation of these com...

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Hauptverfasser: ANTELO QUEIJO ALVARO, TRILLO NOVO JUAN VENTURA, SOTO TELLINI VICTOR HUGO, MEJILDE DEL RIO FRANCISCO, VAZQUEZ TATO JOSE, ALVAREZ ALCALDE MERCEDES
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Sprache:eng ; spa
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Zusammenfassung:Amide derivatives of natural bile acids which are substituted in the 3-position on ring A are claimed. Amide derivatives of bile acids which are substituted in the 3-position on ring A and are of the following formula are claimed: Independent claims are also included for the preparation of these compounds by the conjugation of 3b-amine derivatives of natural bile acids such as cholic acid, deoxycholic acid, ursodeoxycholic acid or chenodeoxycholic acid with acid chloride derivatives of acids chosen from 3,3-dimethylbutanoic acid, 1-adamantane carboxylic acid, 2-decahydronaphthalene carboxylic acid, 4-tert.-butylbenzoic acid, 1-pyrene carboxylic acid, 1H-2-indole carboxylic acid, 2-naphthalene carboxylic acid, 5-isopropyl-2-methyl cyclohexane carboxylic acid, 2-phenanthrene carboxylic acid, terephthalic acid and 4-nitrobenzoic acid, or by the conjugation of 3b-amine derivatives of natural bile acids with succinic anhydride or glutamic anhydride. The resulting compounds are obtained in their acid form or as sodium or potassium salts. Amide derivatives of natural bile acids which are substituted in the 3-position on ring A are claimed. Amide derivatives of bile acids which are substituted in the 3-position on ring A and are of the following formula are claimed: Independent claims are also included for the preparation of these compounds by the conjugation of 3b-amine derivatives of natural bile acids such as cholic acid, deoxycholic acid, ursodeoxycholic acid or chenodeoxycholic acid with acid chloride derivatives of acids chosen from 3,3-dimethylbutanoic acid, 1-adamantane carboxylic acid, 2-decahydronaphthalene carboxylic acid, 4-tert.-butylbenzoic acid, 1-pyrene carboxylic acid, 1H-2-indole carboxylic acid, 2-naphthalene carboxylic acid, 5-isopropyl-2-methyl cyclohexane carboxylic acid, 2-phenanthrene carboxylic acid, terephthalic acid and 4-nitrobenzoic acid, or by the conjugation of 3b-amine derivatives of natural bile acids with succinic anhydride or glutamic anhydride. The resulting compounds are obtained in their acid form or as sodium or potassium salts. Nuevos amidoderivados de ácidos biliares funcionalizados en la posición 3 del anillo A y procedimientos para su obtención y aplicaciones. Los nuevos compuestos resultan de la conjugación de los 3{be}-aminoderivados de ácidos biliares naturales (ácidos cólico, desoxicólico, ursodesoxicólico, chenodesoxicólico y litocólico) con cloruros derivados de los ácidos que se mencionan a continuación, así como c