Process for removing bile salts from a patient and alkylated...

Details Process for removing bile salts from a patient and alkylated... Process for removing bile salts from a patient and alkylated...

C - Chemistry, Metallurgy

08

F

C08F 26/02 (2006.01) A61K 31/785 (2006.01) A61P 1/14 (2006.01) C08F 8/02 (2006.01) C08F 8/44 (2006.01)

Patent

CA 2191478

A method for removing bile salts from a patient that includes administering to the patient a therapeutically effective amount of the reaction product of: a) one or more highly cross-linked polymers characterized by a repeat unit selected from the group consisting essentially of: (1), (2), (3): (NR-CH2 - CH2)n, (4): (NR-CH2CH2-NR-CH2CH2-NR-CH2CHOH-CH2)n and salts and copolymers thereof, where n is an integer and each R, independently, is H or a C1-C8 alkyl group; and b) at least one alkylating agent. The reaction product is characterized in that: (i) at least some of the nitrogen atoms in said repeat units are unreacted with said alkylating agent; (ii) less than 10 mol% of the nitrogen atoms in the repeat units that react with the alkylating agent form quaternary ammonium units; and (iii) the reaction product is non-toxic and stable once ingested.

L'invention concerne un procédé pour éliminer les sels biliaires chez un patient, consistant à lui administrer une dose thérapeutiquement efficace du produit de réaction de: a) un ou plusieurs polymères à haute réticulation, caractérisés par une unité répétitive choisie dans le groupe composé essentiellement de (1), (2), (NR-CH¿2?CH¿2?)¿n? (3), (NR-CH¿2?CH¿2?-NR-CH¿2?CH¿2?-NR-CH¿2?CHOH-CH¿2?)¿n? (4) et de leurs sels et copolymères, où n est un entier et chaque R, indépendamment, est H ou bien un groupe alkyle C¿1?-C¿8?; et b) au moins un agent d'alkylation. Ce produit de réaction est caractérisé en ce que: (i) au moins certains des atomes d'azote dans lesdites unités répétitives n'ont pas réagi avec ledit agent d'alkylation; (ii) moins de 10 % en moles des atomes d'azote dans les unités répétitives qui réagissent avec l'agent d'alkylation forment des unités d'ammonium quaternaire; et (iii) une fois ingéré, ce produit de réaction est non toxique et stable.

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