Compositions and methods for double-targeting virus...

C - Chemistry – Metallurgy – 07 – H

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C07H 19/06 (2006.01) A61K 31/685 (2006.01) A61K 31/7052 (2006.01) A61P 31/12 (2006.01) A61P 35/00 (2006.01) C07F 9/10 (2006.01) C07H 19/16 (2006.01)

Patent

CA 2389544

The invention includes compositions and methods useful for treatment of a virus infection in a mammal by double-targeting the virus (i.e. targeting the virus at more than one stage of the virus life cycle) and thereby inhibiting virus replication. The compositions of the invention include compounds which comprise a phosphocholine moiety covalently conjugated with one or more antiviral agents (e.g. nucleoside analogue, protease inhibitor, etc.) to a lipid backbone. The invention also includes pharmaceutical compositions and kits for use in treatment of a virus infection in mammals. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition of the invention, in an amount effective to treat the infection, to a mammal infected with a virus. Additionally, the invention includes compositions and methods useful for combating a cancer in a mammal and for facilitating delivery of a therapeutic agent to a mammalian cell. The compositions of of the invention include compounds which comprise an alkyl lipid or phospholipid moiety covalently conjugated with an anticancer agent (e.g. a nucleoside analogue). The invention also includes pharmaceutical compositions and kits for combating a cancer and for facilitating delivery of a therapeutic agent to a mammalian cell. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition of the invention, in an amount effective to combat a cancer or to facilitate delivery of a therapeutic agent to a mammalian cell.

La présente invention concerne des compositions et des méthodes utilisées dans le traitement d'une infection virale chez un mammifère consistant à double cibler le virus(c.-à-d. à cibler le virus au cours de plusieurs périodes de son cycle de vie) et par conséquent, à inhiber la réplication du virus. Les compositions de l'invention contiennent des composés qui renferment un fragment de phosphocholine conjugué de façon covalente avec un ou plusieurs agents antiviraux (par exemple, un analogue de nucléoside, un inhibiteur de protéase, etc.) à un squelette de lipide. En outre, cette invention concerne des compositions pharmaceutiques et des kits destinés à être utilisés dans le traitement d'une infection virale chez des mammifères. Les méthodes de cette invention consistent à administrer à un mammifère infecté par un virus, un composé de l'invention, un sel de celui-ci acceptable sur le plan pharmaceutique, ou une composition pharmaceutique de l'invention, selon un dosage efficace pour traiter l'infection. De plus, cette invention concerne des compostions et des méthodes utiles pour combattre le cancer chez un mammifère et pour faciliter l'administration d'un agent thérapeutique à une cellule mammifère. Les compositions de l'invention contiennent des composés qui renferment un lipide alkyle ou un fragment de phospholipide conjugué de manière covalente à un agent anticancéreux (par exemple, un analogue nucléoside). Par ailleurs, cette invention concerne des compositions pharmaceutiques et des kits destinés à combattre le cancer et à faciliter l'administration d'un agent thérapeutique à une cellule mammifère. Les méthodes de cette invention consistent à administrer un composé de l'invention, un sel de celui-ci acceptable sur le plan pharmaceutique, ou une composition pharmaceutique de l'invention, selon un dosage efficace pour combattre le cancer ou pour faciliter l'administration d'un agent thérapeutique à une cellule mammifère.

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