Pharmaceutical formulations, processes for preparation, and methods of use
AssigneeSunesis Pharmaceuticals, Inc.
InventorGene Curtis JAMIESON
Life of this patent
Estimating the term…
Abstract
The invention relates to pharmaceutical compositions, comprising a solid dispersion extrudate comprising any of certain active compounds that modulate cellular survival pathways implicating certain protein kinases, as described, for the treatment of cancer, and processes for the preparation of such compositions. The invention also relates to methods of administering such pharmaceutical compositions to patients for the treatment of cancer.
Claims27
A pharmaceutical composition comprising a solid dispersion extrudate comprising:
- a polymer carrier,
- a solubilizer/plasticizer,
- a bioavailability enhancer, and
- an active compound selected from:
- 3-[4-(3-Amino-1H-pyrazolo[3,4-b]pyrazin-5-yl)-benzylamino]-6-cyano-pyrazine-2-carboxylic acid [1-(3,4-difluoro-phenyl)-ethyl]-amide,
- 6-Cyano-3-[4-(3-methylamino-1H-pyrazolo[3,4-b]pyridin-5-yl)-benzylamino]-pyrazine-2-carboxylic acid [1-(3,4-difluoro-phenyl)-ethyl]-amide, and
- 3-[4-(3-Amino-1H-pyrazolo[3,4-b]pyridin-5-yl)-benzylamino]-6-cyano-pyrazine-2-carboxylic acid [1-(3,4-difluoro-phenyl)-ethyl]-amide,
- or a pharmaceutically acceptable salt thereof.
-5. (canceled)
-8. (canceled)
-11. (canceled)
-17. (canceled)
-21. (canceled)
An orally administrable preparation of an active compound comprising:
- a solid dispersion extrudate comprising:
- an active compound,
- a polymer carrier,
- a solubilizer/plasticizer, and
- a bioavailability enhancer;
- and
- one or more pharmaceutically acceptable excipients;
- wherein the active compound is selected from:
- 3-[4-(3-Amino-1H-pyrazolo[3,4-b]pyrazin-5-yl)-benzylamino]-6-cyano-pyrazine-2-carboxylic acid [1-(3,4-difluoro-phenyl)-ethyl]-amide,
- 6-Cyano-3-[4-(3-methylamino-1H-pyrazolo[3,4-b]pyridin-5-yl)-benzylamino]-pyrazine-2-carboxylic acid [1-(3,4-difluoro-phenyl)-ethyl]-amide, and
- 3-[4-(3-Amino-1H-pyrazolo[3,4-b]pyridin-5-yl)-benzylamino]-6-cyano-pyrazine-2-carb oxylic acid [1-(3,4-difluoro-phenyl)-ethyl]-amide,
- or a pharmaceutically acceptable salt thereof.
-28. (canceled)
A process for preparing a pharmaceutical composition,
- which comprises the steps of:
- (i) hot melt extruding a mixture of:
- a polymer carrier,
- a solubilizer/plasticizer,
- a bioavailability enhancer, and
- an active compound selected from:
- 3-[4-(3-Amino-1H-pyrazolo[3,4-b]pyrazin-5-yl)-benzylamino]-6-cyano-pyrazine-2-carboxylic acid [1-(3,4-difluoro-phenyl)-ethyl]-amide,
- 6-Cyano-3-[4-(3-methylamino-1H-pyrazolo[3,4-b]pyridin-5-yl)-benzylamino]-pyrazine-2-carboxylic acid [1-(3,4-difluoro-phenyl)-ethyl]-amide, and
- 3-[4-(3-Amino-1H-pyrazolo[3,4-b]pyridin-5-yl)-benzylamino]-6-cyano-pyrazine-2-carboxylic acid [1-(3,4-difluoro-phenyl)-ethyl]-amide,
- or a pharmaceutically acceptable salt thereof,
- to form a solid dispersion extrudate;
- and
- (ii) blending the resulting solid dispersion extrudate with one or more pharmaceutically acceptable excipients.
-44. (canceled)
Dependencies are inferred from the claim text.