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US 2010/0160442 A1Published application
Formulations for cancer treatment
OwnerValeria S. OSSOVSKAYA, Barry M. Sherman +5inventors
InventorsValeria S. OSSOVSKAYA, Barry M. Sherman, Kathy Powell, Stephen Nava, Helen N. Han, Lingyun Li, Richard J. Bastin
Life of this patent
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Abstract
The present invention provides compositions of matter, kits, and methods for use in treating cancer and viral conditions. In particular the invention provides for pharmaceutical compositions containing nitrobenzamide compounds that have enhanced solubility in aqueous solutions.
Claims40
A pharmaceutical composition comprising a compound of formula (Ia)
- wherein R1, R2, R3, R4, and R5 are, independently selected from the group consisting of hydrogen, hydroxy, amino, nitro, iodo, bromo, fluoro, chloro, (C1-C6) alkyl, (C1-C6) alkoxy, (C3-C7) cycloalkyl, and phenyl, wherein at least two of the five R1, R2, R3, R4, and R5 substituents are always hydrogen, at least one of the five substituents are always nitro, and at least one substituent positioned adjacent to a nitro is always iodo, and pharmaceutically acceptable salts, solvates, isomers, tautomers, metabolites, analogs, or prodrugs thereof, and
- at least one pharmaceutically acceptable solubilizer.
A pharmaceutical composition comprising a compound of formula (Ia)
- wherein R1, R2, R3, R4, and R5 are, independently selected from the group consisting of hydrogen, hydroxy, amino, nitro, iodo, bromo, fluoro, chloro, (C1-C6) alkyl, (C1-C6) alkoxy, (C3-C7) cycloalkyl, and phenyl, wherein at least two of the five R1, R2, R3, R4, and R5 substituents are always hydrogen, at least one of the five substituents are always nitro, and at least one substituent positioned adjacent to a nitro is always iodo, and pharmaceutically acceptable salts, solvates, isomers, tautomers, metabolites, analogs, or prodrugs thereof, and
- a surfactant.
A pharmaceutical composition comprising a compound of formula (Ia)
- wherein R1, R2, R3, R4, and R5 are, independently selected from the group consisting of hydrogen, hydroxy, amino, nitro, iodo, bromo, fluoro, chloro, (C1-C6) alkyl, (C1-C6) alkoxy, (C3-C7) cycloalkyl, and phenyl, wherein at least two of the five R1, R2, R3, R4, and R5 substituents are always hydrogen, at least one of the five substituents are always nitro, and at least one substituent positioned adjacent to a nitro is always iodo, and pharmaceutically acceptable salts, solvates, isomers, tautomers, metabolites, analogs, or prodrugs thereof, and
- a cyclodextrin.
A pharmaceutical composition comprising a compound of formula (Ia)
- wherein R1, R2, R3, R4, and R5 are, independently selected from the group consisting of hydrogen, hydroxy, amino, nitro, iodo, bromo, fluoro, chloro, (C1-C6) alkyl, (C1-C6) alkoxy, (C3-C7) cycloalkyl, and phenyl, wherein at least two of the five R1, R2, R3, R4, and R5 substituents are always hydrogen, at least one of the five substituents are always nitro, and at least one substituent positioned adjacent to a nitro is always iodo, and pharmaceutically acceptable salts, solvates, isomers, tautomers, metabolites, analogs, or prodrugs thereof, and
- a co-solvent.
A method for treating a condition selected from cancer, and a viral condition, comprising treating a subject suspected of having said condition with a pharmaceutical composition comprising a compound of formula (Ia)
- wherein R1, R2, R3, R4, and R5 are, independently selected from the group consisting of hydrogen, hydroxy, amino, nitro, iodo, bromo, fluoro, chloro, (C1-C6) alkyl, (C1-C6) alkoxy, (C3-C7) cycloalkyl, and phenyl, wherein at least two of the five R1, R2, R3, R4, and R5 substituents are always hydrogen, at least one of the five substituents are always nitro, and at least one substituent positioned adjacent to a nitro is always iodo, and pharmaceutically acceptable salts, solvates, isomers, tautomers, metabolites, analogs, or prodrugs thereof, and
- one or more of the group consisting of:
- a cyclodextrin, a surfactant, and a co-solvent.
A kit comprising a compound of formula (Ia)
- wherein R1, R2, R3, R4, and R5 are, independently selected from the group consisting of hydrogen, hydroxy, amino, nitro, iodo, bromo, fluoro, chloro, (C1-C6) alkyl, (C1-C6) alkoxy, (C3-C7) cycloalkyl, and phenyl, wherein at least two of the five R1, R2, R3, R4, and R5 substituents are always hydrogen, at least one of the five substituents are always nitro, and at least one substituent positioned adjacent to a nitro is always iodo, and pharmaceutically acceptable salts, solvates, isomers, tautomers, metabolites, analogs, or prodrugs thereof, and
- a cyclodextrin, a surfactant, a co-solvent, or mixtures thereof.
An aqueous solution comprising a compound of formula (Ia)
- wherein R1, R2, R3, R4, and R5 are, independently selected from the group consisting of hydrogen, hydroxy, amino, nitro, iodo, bromo, fluoro, chloro, (C1-C6) alkyl, (C1-C6) alkoxy, (C3-C7) cycloalkyl, and phenyl, wherein at least two of the five R1, R2, R3, R4, and R5 substituents are always hydrogen, at least one of the five substituents are always nitro, and at least one substituent positioned adjacent to a nitro is always iodo, and pharmaceutically acceptable salts, solvates, isomers, tautomers, metabolites, analogs, or prodrugs thereof, and
- a cyclodextrin, a surfactant, a co-solvent, or mixtures thereof.
A unit dosage comprising a compound of formula (Ia)
- wherein R1, R2, R3, R4, and R5 are, independently selected from the group consisting of hydrogen, hydroxy, amino, nitro, iodo, bromo, fluoro, chloro, (C1-C6) alkyl, (C1-C6) alkoxy, (C3-C7) cycloalkyl, and phenyl, wherein at least two of the five R1, R2, R3, R4, and R5 substituents are always hydrogen, at least one of the five substituents are always nitro, and at least one substituent positioned adjacent to a nitro is always iodo, and pharmaceutically acceptable salts, solvates, isomers, tautomers, metabolites, analogs, or prodrugs thereof, and
- at least one pharmaceutically acceptable solubilizer.
The unit dosage of 35, wherein the surfactant is selected from the group of:
- Polysorbate 80, Polysorbate 20, Cremophor EL, Cremophor RH40, Poloxamer 118, and Solutol HS-15.
A parenteral pharmaceutical composition comprising a compound of formula (Ia)
- wherein R1, R2, R3, R4, and R5 are, independently selected from the group consisting of hydrogen, hydroxy, amino, nitro, iodo, bromo, fluoro, chloro, (C1-C6) alkyl, (C1-C6) alkoxy, (C3-C7) cycloalkyl, and phenyl, wherein at least two of the five R1, R2, R3, R4, and R5 substituents are always hydrogen, at least one of the five substituents are always nitro, and at least one substituent positioned adjacent to a nitro is always iodo, and pharmaceutically acceptable salts, solvates, isomers, tautomers, metabolites, analogs, or prodrugs thereof;
- a cyclodextrin;
- and
- water.
1 more element
Dependencies are inferred from the claim text.