N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate anhydrate and monohydrate
View Patent ↗The present invention relates to the anhydrous and hydrate forms of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate. The invention also relates to pharmaceutical compositions containing N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate and to methods of treating hyperproliferative disorders, such as cancer, by administering N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate.
1. A hydrate form of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate.
2. A pharmaceutical composition comprising from about 0.001 to about 100 mg per kg body weight per day of N-(ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate or of a hydate form of N-(ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate, and a pharmaceutically acceptable carrier.
3. The pharmaceutical composition of claim 2 , comprising from about 1 to about 35 mg/kg/day of the compound.
4. A pharmaceutical composition comprising from about 0.05 to about 7 g/day of N-(ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate or of a hydate form of N-(ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate, and a pharmaceutically acceptable carrier.
5. The pharmaceutical composition of claim 4 , comprising from about 0.2 to about 2.5 g/day of the compound.
6. The pharmaceutical composition of claim 5 , in the form of a tablet, capsule, pill, powder, sustained release formulations, solution, parenteral injection as a sterile solution, suspension or emulsion, or suppository.
7. The pharmaceutical composition of claim 6 , in the form of a parenteral injection.
8. The pharmaceutical composition of claim 6 , in the form of a tablet.
9. A method of treating a mammal suffering from a hyperproliferative disorder which comprises administering to said mammal an amount of the pharmaceutical composition of claim 2 therapeutically effective to inhibit the epidermal growth factor receptor (“EGFR”) in the mammal, so as to thereby treat the mammal, wherein the hyperproliferative disorder is lung cancer, breast cancer, ovarian cancer, prostate cancer, or colorectal cancer.
10. The method of claim 9 further comprising administering to said mammal a therapeutically effective amount of a compound selected from the group consisting of alkylating agents, anti-metabolites, intercalating antibiotics, growth factor inhibitors, cell-cycle inhibitor, enzymes, topoisomerase, inhibitors, anti-hormones, and anti-androgens.
11. The method of claim 10 wherein the cell-cycle inhibitor is a mitotic inhibitor.
12. The pharmaceutical composition of claim 2 , comprising from about 0.001 to about 100 mg/kg/day of N-(ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate and a pharmaceutically acceptable carrier.
13. The pharmaceutical composition of claim 2 , comprising from about 0.001 to about 100 mg/kg/day of a hydrate form of N-(ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate and a pharmaceutically acceptable carrier.