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Last Updated: July 27, 2024

Claims for Patent: 7,851,470


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Summary for Patent: 7,851,470
Title:Composition and methods for modulating a kinase cascade
Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase cascade.
Inventor(s): Hangauer, Jr.; David G. (Lancaster, NY), Coughlin; Daniel (Hackettstown, NJ), Gale; Jonathan (West Townsend, MA), Cody; Jeremy A. (Clifton Springs, NY), Patra; Debasis (Manlius, NY)
Assignee: Kinex Pharmaceuticals, LLC (Buffalo, NY)
Application Number:12/005,792
Patent Claims: 1. A composition comprising KX2-391 a salt, solvate, hydrate, or prodrug thereof, having a purity greater than 98.0% as determined by HPLC.

2. The composition of claim 1, wherein the KX2-391 has a purity of 99.0%.

3. The composition of claim 1, wherein the KX2-391 has a purity of 99.5%.

4. The composition of claim 1, wherein the KX2-391 has a purity of 99.6%.

5. The composition of claim 1, wherein the KX2-391 has a purity of 99.7%.

6. The composition of claim 1, wherein the composition contains less than 2% of an impurity selected from ethyl chloride, ethanol, ethyl acetate, heptane, anisole, palladium, and combinations thereof.

7. A composition according to claim 1 further comprising a pharmaceutically acceptable carrier or excipient.

8. A method of treating or preventing a disease or disorder that is modulated by kinase inhibition, comprising administering a pharmaceutical composition comprising a compound according to claim 1 and at least one pharmaceutically acceptable excipient to a subject in need thereof.

9. The method according to claim 8, wherein kinase is selected from a serine kinase, focal adhesion kinase, and a tyrosine kinase.

10. The method according to claim 9, wherein the tyrosine kinase is a Src family protein kinase.

11. The method according to claim 8, wherein the compound is administered orally.

12. The method according to claim 8, wherein the compound is administered topically.

13. The method according to claim 8, wherein the component of the kinase cascade is responsible for the manifestation of a disease or disorder selected from hyperproliferative disorders, hematologic tumor, hematologic malignancy, childhood leukemia, lymphoma, multiple myeloma, Hodgkin's disease, lymphoma of lymphocytic or cutaneous origin, acute or chronic leukemia, lymphoblastic leukemia, acute myelocytic leukemia, chronic myelocytic leukemia, plasma cell neoplasm, lymphoid neoplasm, a cancer associated with AIDS, cancer of the lung, cancer of the breast, cancer of the colon, cancer of the ovary, cancer of the brain, cancer of the liver, cancer of the pancreas, cancer of the prostate, malignant melanoma, non-melanoma skin cancer, osteoporosis, cardiovascular disorders, immune system dysfunction, type II diabetes, obesity, ophthalmic disease, macular edema, chronic neuropathic pain, hearing loss, and transplant rejection.

14. A method of treating a cell proliferation disorder comprising administering a pharmaceutical composition comprising a compound according to claim 1 and at least one pharmaceutically acceptable excipient to a subject in need thereof.

15. A method of treating or preventing a disease or disorder that is modulated by tyrosine kinase inhibition, comprising administering a pharmaceutical composition comprising a compound according to claim 1 and at least one pharmaceutically acceptable excipient to a subject in need thereof.

16. The method of claim 15, wherein the disease or disorder that is modulated by tyrosine kinase inhibition is a cell proliferation disorder selected from cancer wherein said cancer is a solid tumor, a hyperproliferative disorder, and a microbial infection.

17. The method of claim 16, wherein the microbial infection is a bacterial, fungal, parasitic or viral infection.

18. The method of claim 16, wherein said cell proliferation disorder is a hyperproliferative disorder selected from psoriases, diabetic retinopathy and macular degeneration.

19. The method of claim 16, wherein said cell proliferation disorder is cancer wherein said cancer is a solid tumor.

20. The method of claim 19, wherein said cancer is cancer of the lung, breast, colon, ovary, brain, liver, pancreas, or prostate, a malignant melanoma, or a non-melanoma skin cancer.

21. The method of claim 19, wherein said cancer is breast, colon, or lung cancer.

22. The method of claim 19, wherein said cancer is a hematologic tumor, hematologic malignancy, childhood leukemia, lymphoma, multiple myeloma, Hodgkin's disease, lymphoma of lymphocytic or cutaneous origin, acute or chronic leukemia, lymphoblastic leukemia, acute myelocytic leukemia, chronic myelocytic leukemia, plasma cell neoplasm, lymphoid neoplasm or a cancer associated with AIDS.

23. The method of claim 16, wherein said cell proliferation disorder is an epidermic cyst, dermoid cyst, lipoma, adenoma, capillary hemangioma, cutaneous hemangioma, lymphangioma, nevi lesion, teratoma, nephroma, myofibromatosis, osteoplastic tumor, or a dysplastic mass.

24. The method of claim 8 wherein the subject is a human.

25. The composition of claim 1, where the KX2-391 is a dihydrochloride salt.

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