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Last Updated: January 29, 2022

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Claims for Patent: 10,189,833


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Summary for Patent: 10,189,833
Title:Solid forms of a compound modulating kinases
Abstract: Solid forms of the compound, [5-(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-ylmethyl)-pyridin-2-yl]-(6-triflu- oromethyl-pyridin-3-ylmethyl)-amine HCl salt (Compound I) and its free base, active on the receptor protein kinases c-Kit and/or c-Fms and/or Flt3, were prepared and characterized: ##STR00001## Also provided are methods of using the solid forms.
Inventor(s): Ibrahim; Prabha N. (Mountain View, CA), Visor; Gary Conard (Castro Valley, CA)
Assignee: Plexxikon Inc. (Berkeley, CA)
Application Number:15/725,197
Patent Claims: 1. A method for treating a subject suffering from a disease or condition mediated by a protein kinase selected from c-fms, c-kit, Flt3 or a combination thereof, or mediated by macrophages or microglia, comprising administering to the subject a therapeutically effective amount of a crystalline form of Compound I: ##STR00005## characterized by an X-ray powder diffractogram comprising peaks (.+-.0.2.degree.) at 7.3, 23.3 and 28.2.degree. 2.theta. as determined on a diffractometer using Cu--K.alpha. radiation.

2. A method for treating a subject suffering from a disease or condition mediated by a protein kinase selected from c-fms, c-kit, Flt3 or a combination thereof, or mediated by macrophages or microglia, comprising administering to the subject a composition comprising a therapeutically effective amount of a crystalline form of Compound I: ##STR00006## characterized by an X-ray powder diffractogram comprising peaks (.+-.0.2.degree.) at 7.3, 23.3 and 28.2.degree. 2.theta. as determined on a diffractometer using Cu--K.alpha. radiation, and a pharmaceutically acceptable excipient.

3. The method of claim 1, wherein the disease or condition is selected from osteoporosis, neurofibromatosis, Alzheimer's disease, epilepsy, traumatic brain injury, tauopathies, non-small cell lung cancer, anterior eye disease, posterior eye disease, lysosomal storage disease, multiple sclerosis, complex regional pain syndrome, neuro-inflammation, neuroinflammatory disorders, HIV, binswager type dementia, dementia with lewy bodie, cerebral palsy, progressive supranuclear palsy, glaucoma, vascular dementias, multi infarct dementia, fronto temporal dementia, pseudo-dementia, bladder cancer, ovarian cancer, acute myeloid leukemia, chronic lymphocytic leukemia, breast cancer, cholangiocarcinoma, colon cancer, endometrial cancer, esophageal cancer, glioma, glioblastoma, hepatocellular carcinoma, Hodgkin lymphoma, leukemia, lung cancer, melanoma, mesothelioma, pancreatic cancer, renal cancer, monocytic leukemia, malignant peripheral nerve sheath tumors (MPNST), plexiform neurofibromas, salivary gland tumors, mucoepidermoid carcinoma of the salivary gland, acinic cell carcinoma of the salivary gland, gastrointestinal stromal tumors (GIST), giant cell tumors (GCT), GCT of bone, pigmented villonodular synovitis (PVNS), tenosynovial giant cell tumor (TGCT), or TCGT of tendon sheath (TGCT-TS).

4. The method of claim 1, further comprising administering to the subject a therapeutically effective amount of another therapeutic agent, wherein the another therapeutic agent is: i) an alkylating agent; ii) an antibiotic; iii) an antimetabolite; iv) an antibody therapy agent; v) a hormone or hormone antagonist; vi) a taxane; vii) a retinoid; viii) an alkaloid; ix) an antiangiogenic agent; x) a topoisomerase inhibitor; xi) a protein kinase inhibitor selected from a PI3K inhibitor, Cdk4 inhibitors; an Akt inhibitor; a Mek inhibitor, a c-Kit mutant inhibitor, or an EGFR inhibitor; xii) a targeted signal transduction inhibitor; xiii) a biological response modifier; xiv) a chemotherapeutic agent; xv) an Hsp90 inhibitor; xvi) a farnesyltransferase inhibitor; xvii) an aromatase inhibitor; xvii) an IDO inhibitor; xix) a histone acetyltransferase (HAT) inhibitor; xx) histone deacetylase (HDAC) inhibitor; xxi) a sirtuin (SIRT) inhibitor; xxii) a BET inhibitor; or xxiii) an antiangiogenic agent.

5. The method of claim 3, wherein the disease or condition is plexiform neurofibromas.

6. A method for treating a subject suffering from tenosynovial giant cell tumor comprising administering to the subject a therapeutically effective amount of a crystalline form of Compound I: ##STR00007## characterized by an X-ray powder diffractogram comprising peaks (.+-.0.2.degree.) at 7.3, 23.3 and 28.2.degree. 2.theta. as determined on a diffractometer using Cu--K.alpha. radiation or a composition comprising the crystalline form of Compound I and a pharmaceutically acceptable excipient.

7. A method for treating a subject suffering from pigmented villonodular synovitis comprising administering to the subject a therapeutically effective amount of a crystalline form of Compound I: ##STR00008## characterized by an X-ray powder diffractogram comprising peaks (.+-.0.2.degree.) at 7.3, 23.3 and 28.2 .degree.2.theta. as determined on a diffractometer using Cu--K.alpha. radiation or a composition comprising the crystalline form of Compound I and a pharmaceutically acceptable excipient.

8. A method for treating a subject suffering from malignant peripheral nerve sheath tumors comprising administering to the subject a therapeutically effective amount of a crystalline form of Compound I: ##STR00009## characterized by an X-ray powder diffractogram comprising peaks (.+-.0.2.degree.) at 7.3, 23.3 and 28.2.degree. 2.theta. as determined on a diffractometer using Cu--.alpha. a radiation or a composition comprising the crystalline form of Compound I and a pharmaceutically acceptable excipient.

9. The method of claim 8, further comprising administering to the subject a therapeutically effective amount of sirolimus.

10. A method for treating a subject suffering from ovarian cancer comprising administering to the subject a therapeutically effective amount of a crystalline form of Compound I: ##STR00010## characterized by an X-ray powder diffractogram comprising peaks (.+-.0.2.degree.) at 7.3, 23.3 and 28.2.degree. 2.theta. as determined on a diffractometer using Cu--K.alpha. radiation or a composition comprising the crystalline form of Compound I and a pharmaceutically acceptable excipient.

11. The method of claim 10, further comprising administering to the subject a therapeutically effective amount of paclitaxel.

12. A method for treating a subject suffering from prostate cancer comprising administering to the subject a therapeutically effective amount of a crystalline form of Compound I: ##STR00011## characterized by an X-ray powder diffractogram comprising peaks (.+-.0.2.degree.) at 7.3, 23.3 and 28.2.degree. 2.theta. as determined on a diffractometer using Cu--K.alpha. radiation or a composition comprising the crystalline form of Compound I and a pharmaceutically acceptable excipient.

13. A method for treating a subject suffering from pancreatic cancer comprising administering to the subject a therapeutically effective amount of a crystalline form of Compound I: ##STR00012## characterized by an X-ray powder diffractogram comprising peaks (.+-.0.2.degree.) at 7.3, 23.3 and 28.2.degree. 2.theta. as determined on a diffractometer using Cu--K.alpha. radiation or a composition comprising the crystalline form of Compound I and a pharmaceutically acceptable excipient.

14. A method for treating a subject suffering from colorectal carcinoma comprising administering to the subject a therapeutically effective amount of a crystalline form of Compound I: ##STR00013## characterized by an X-ray powder diffractogram comprising peaks (.+-.0.2.degree.) at 7.3, 23.3 and 28.2.degree. 2.theta. as determined on a diffractometer using Cu--K.alpha. radiation or a composition comprising the crystalline form of Compound I and a pharmaceutically acceptable excipient.

15. The method according to claim 13, further comprising administering a therapeutically effective amount of durvalumab.

16. The method according to claim 14, further comprising administering a therapeutically effective amount of durvalumab.

17. A method for treating a subject suffering from neurofibromatosis comprising administering to the subject a therapeutically effective amount of a crystalline form of Compound I: ##STR00014## characterized by an X-ray powder diffractogram comprising peaks (.+-.0.2.degree.) at 7.3, 23.3 and 28.2.degree. 2.theta. as determined on a diffractometer using Cu--K.alpha. radiation or a composition comprising the crystalline form of Compound I and a pharmaceutically acceptable excipient.

18. A method for treating a subject suffering from gastrointestinal stromal tumors comprising administering to the subject a therapeutically effective amount of a crystalline form of Compound I: ##STR00015## characterized by an X-ray powder diffractogram comprising peaks (.+-.0.2.degree.) at 7.3, 23.3 and 28.2.degree. 2.theta. as determined on a diffractometer using Cu--K.alpha. radiation or a composition comprising the crystalline form of Compound I and a pharmaceutically acceptable excipient.

19. The method according to claim 18, further comprising administering a c-Kit mutant protein kinase inhibitor.

20. The method according to claim 19, wherein the c-Kit mutant protein kinase inhibitor is (2-phenyl-1H-pyrrolo[2,3-b]pyridin-5-yl)-(3-pyridyl)methanol, (2-phenyl-1H-pyrrolo[2,3-b]pyridin-5-yl)-(3-pyridyl)methanone, N-(3-carbamoylphenyl)-2 -phenyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide, 2-phenyl-N-(1H-pyrazol-3-yl)-1H-pyrrolo[2,3-b]pyridine-5-carboxamide, 2-phenyl-N-(1H-pyrazol-3-yl)-1H-pyrrolo[2,3-b]pyridine-5-carboxamide, ethyl 3-[(2-phenyl-1H-pyrrolo[2,3-b]pyridin-5-yl)carbamoylamino]propanoat- e, 3,4-dimethyl-N-(2-phenyl-1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazole-5-c- arboxamide, 4-methyl-3-phenyl-N-(2-phenyl-1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazole-- 5-carboxamide, 3-cyclopropyl-N-(2-phenyl-1H-pyrrolo[2,3-b]pyridin-5-yl)-1H- pyrazole-5-carboxamide, 5-fluoro-N-(2-phenyl-1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-indazole-3-carboxa- mide, N-(2-phenyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrimidine-4-carboxamide, 3-fluoro-N-(2-phenyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyridine-2-carboxamide- , 3,5-dimethyl-N-(2-phenyl-1H-pyrrolo[2,3-b]pyridin-5-yl)isoxazole-4-carbo- xamide, N-(2-phenyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyridazine-3-carboxamide- , N-(2-phenyl-1H-pyrrolo[2,3-b]pyridin-5-yl)-2H-triazole-4-carboxamide, 3-methyl-N-(2-phenyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyridine-2-carboxamide- , 4,5-dimethyl-N-(2-phenyl-1H-pyrrolo[2,3-b]pyridin-5-yl)isoxazole-3-carbo- xamide or N-(2-phenyl-1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazole-4-sulfona- mide.

21. A method for treating a subject suffering from Alzheimer's disease comprising administering to the subject a therapeutically effective amount of a crystalline form of Compound I: ##STR00016## characterized by an X-ray powder diffractogram comprising peaks (.+-.0.2.degree.) at 7.3, 23.3 and 28.2.degree. 2.theta. as determined on a diffractometer using Cu--K.alpha. radiation or a composition comprising the crystalline form of Compound I and a pharmaceutically acceptable excipient.

22. A method for treating a subject suffering from bone osteolysis and/or bone pain comprising administering to the subject a therapeutically effective amount of a crystalline form of Compound I: ##STR00017## characterized by an X-ray powder diffractogram comprising peaks (.+-.0.2.degree.) at 7.3, 23.3 and 28.2.degree. 2.theta. as determined on a diffractometer using Cu--K.alpha. radiation or a composition comprising the crystalline form of Compound I and a pharmaceutically acceptable excipient.

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