Isoxazoline derivatives as antiparasitic agents

597248 Provided is a solid dispersion comprising, in essentially non-crystalline form, a Bcl-2 protein family inhibitor compound of the general formula (I), where R0, X3 and X4 are described in the specification, dispersed in a solid matrix that comprises (a) a water-soluble polymeric carrier and (b...

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Hauptverfasser: Vaillancourt Valerie Ann, Kyne Graham M, Wendt John A, Skalitzky Donald James, Howson William, Sheehan Susan Mary Kult, Chubb Nathan A. L, Menon Sanjay Rajagopal, Curtis Michael Paul
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creator Vaillancourt Valerie Ann
Kyne Graham M
Wendt John A
Skalitzky Donald James
Howson William
Sheehan Susan Mary Kult
Chubb Nathan A. L
Menon Sanjay Rajagopal
Curtis Michael Paul
description 597248 Provided is a solid dispersion comprising, in essentially non-crystalline form, a Bcl-2 protein family inhibitor compound of the general formula (I), where R0, X3 and X4 are described in the specification, dispersed in a solid matrix that comprises (a) a water-soluble polymeric carrier and (b) a surfactant. Inhibition of Bcl-2 family proteins promotes apoptosis. A preferred compound is the Bcl-2 protein family inhibitor ABT-263. Further provided is a process for preparing the solid dispersion comprising dissolving the compound, the polymeric carrier and the surfactant in a suitable solvent, and removing the solvent to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. Also provided is the use of the solid dispersion in the preparation of a medicament for oral administration to a subject with a disease characterized by apoptotic dysfunction and/or overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.
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subjects AGRICULTURE
ANIMAL HUSBANDRY
BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES, AS HERBICIDES
CHEMISTRY
FISHING
FORESTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HUNTING
METALLURGY
ORGANIC CHEMISTRY
PEST REPELLANTS OR ATTRACTANTS
PLANT GROWTH REGULATORS
PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTSTHEREOF
TRAPPING
title Isoxazoline derivatives as antiparasitic agents
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