Methods of treating syndrome x with aliphatic polyamines

Details Methods of treating syndrome x with aliphatic polyamines Methods of treating syndrome x with aliphatic polyamines

A - Human Necessities

61

K

A61K 31/785 (2006.01) A61K 31/015 (2006.01) A61K 31/355 (2006.01) A61K 31/375 (2006.01) A61K 31/4415 (2006.01) A61K 31/616 (2006.01) A61K 31/714 (2006.01) A61K 45/00 (2006.01) A61K 45/06 (2006.01) A61P 3/00 (2006.01) A61P 39/00 (2006.01)

Patent

CA 2444028

The invention relates to a method for treating Syndrome X, or inhibiting the onset of symptoms of Syndrome X in a patient, and includes administering a therapeutically effective amount of a salt of at least one alkylated and cross- linked polymer, or a copolymer thereof, the polymer salt formed as a product of the reaction of one or more polymers, or salts and copolymers thereof, having a repeat unit that is essentially (1) or (2); where n is a positive integer and each R, independently, is H or C1-C8 alkyl group; at least one aliphatic alkylating agent; and a cross-linking agent. Long term administration of the cross-linked polyamine salts of the invention increases HDL levels and decreases LDL levels in patients. The invention also provides for administration of the polymer salt colesevelam, in combination with an HMG- CoA reductase inhibitor; the combined administration is effective in further lowering serum total-cholesterol and LDL-cholesterol levels beyond that achieved by either agent alone.

L'invention concerne une méthode pour traiter le syndrome X ou pour inhiber l'apparition de symptômes du syndrome X chez un patient, consistant à administrer une dose thérapeutiquement efficace d'un sel d'au moins un polymère alkylé ou réticulé, ou bien un copolymère de celui-ci, le sel polymère étant le produit de réaction d'un ou de plusieurs polymères, ou de leurs sels et copolymères, ayant une unité de répétition, sensiblement de formule (1) ou (2), où n est un nombre entier positif et chaque R signifie indépendamment H ou un groupe alkyle C¿1?-C¿8?, et d'au moins un agent d'alkylation aliphatique ainsi que d'un agent de réticulation. Une administration de longue durée des sels de polyamine réticulés selon l'invention augmente les niveaux HDL et diminuent les niveaux LDL chez les patients. La présente invention porte également sur l'administration du sel polymère colesevelam, associé à un inhibiteur de réductase HMG-CoA. Cette administration combinée est efficace pour diminuer davantage les niveaux de cholestérol total du sérum et de cholestérol LDL, au-delà des niveaux atteints par chaque agent isolé.

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