Claims for Patent: 11,684,620

Summary for Patent: 11,684,620

Title:	Pharmaceutical compositions comprising N-(3,5-dimethoxyphenyl)-N′-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine
Abstract:	The invention relates to pharmaceutical compositions comprising N-(3,5-dimethoxyphenyl)-N′-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine, or a pharmaceutically acceptable salt thereof or a solvate thereof; to processes for the preparation of said compositions and to the use of said compositions for the manufacture of a medicament for the prophylaxis of or the treatment, in particular the treatment, of diseases, e.g. cancer.
Inventor(s):	Diego Fernando Domenico BROGGINI
Assignee:	Cilag AG , Astex Therapeutics Ltd
Application Number:	US17/125,261
Patent Claims:	1. A method of treating cancer comprising administering to a patient in need thereof a pharmaceutical composition comprising N-(3,5-dimethoxyphenyl)-N′-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine, a pharmaceutically acceptable salt thereof or a solvate thereof; a formaldehyde scavenger; and a pharmaceutically acceptable carrier, wherein the formaldehyde scavenger is meglumine base, and wherein the cancer is bladder cancer, urothelial cancer, metastatic urothelial cancer, surgically unresectable urothelial cancer, or non-muscle-invasive bladder cancer. 2. The method according to claim 1, wherein the composition comprises from about 0.1 to about 3% w/w of the formaldehyde scavenger. 3. The method according to claim 2, wherein the composition comprises from about 0.5 to about 1.5% w/w of the formaldehyde scavenger. 4. The method according to claim 1, wherein the composition is a tablet or a capsule. 5. The method according to claim 1, wherein the composition comprises from 0-2% w/w of 6,8-dimethoxy-4-(1-methylethyl)-1-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine, a pharmaceutically acceptable salt thereof or a solvate thereof. 6. The method according to claim 5, wherein the composition comprises from 0-0.05 w/w of 6,8-dimethoxy-4-(1-methylethyl)-1-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine, a pharmaceutically acceptable salt thereof or a solvate thereof. 7. The method according to claim 1, wherein the composition comprises from 2 mg to 6 mg base equivalent of N-(3,5-dimethoxyphenyl)-N′-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine, a pharmaceutically acceptable salt thereof or a solvate thereof. 8. The method according to claim 1, wherein the composition comprises N-(3,5-dimethoxyphenyl)-N′-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine base. 9. The method according to claim 2, wherein the composition comprises 3 mg of N-(3,5-dimethoxyphenyl)-N′-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine base. 10. The method according to claim 2, wherein the composition comprises 4 mg of N-(3,5-dimethoxyphenyl)-N′-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine base. 11. The method according to claim 2, wherein the composition comprises 5 mg of N-(3,5-dimethoxyphenyl)-N′-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine base. 12. The method according to claim 3, wherein the composition comprises 3 mg of N-(3,5-dimethoxyphenyl)-N′-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine base. 13. The method according to claim 3, wherein the composition comprises 4 mg of N-(3,5-dimethoxyphenyl)-N′-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine base. 14. The method according to claim 3, wherein the composition comprises 5 mg of N-(3,5-dimethoxyphenyl)-N′-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine base. 15. The method according to claim 6, wherein the composition comprises 3 mg of N-(3,5-dimethoxyphenyl)-N′-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine base. 16. The method according to claim 6, wherein the composition comprises 4 mg of N-(3,5-dimethoxyphenyl)-N′-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine base. 17. The method according to claim 6, wherein the composition comprises 5 mg of N-(3,5-dimethoxyphenyl)-N′-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine base. 18. The method according to claim 7, wherein the composition comprises N-(3,5-dimethoxyphenyl)-N′-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine base. 19. The method according to claim 8, wherein the composition comprises 3 mg of N-(3,5-dimethoxyphenyl)-N′-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine base. 20. The method according to claim 8, wherein the composition comprises 4 mg of N-(3,5-dimethoxyphenyl)-N′-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine base. 21. The method according to claim 8, wherein the composition comprises 5 mg of N-(3,5-dimethoxyphenyl)-N′-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine base. 22. The method according to claim 1, wherein the cancer is bladder cancer. 23. The method according to claim 1, wherein the cancer is urothelial cancer. 24. The method according to claim 1, wherein the cancer is metastatic urothelial cancer. 25. The method according to claim 1, wherein the cancer is surgically unresectable urothelial cancer. 26. The method according to claim 1, wherein the cancer is non-muscle-invasive bladder cancer. 27. The method according to claim 1, wherein the cancer is a cancer with a FGFR genomic alteration. 28. The method according to claim 1, wherein the cancer is a cancer with a FGFR translocation. 29. The method according to claim 28, wherein the translocation is a FGFR3-TACC3 translocation. 30. The method according to claim 1, wherein the cancer is a cancer with a FGFR mutation. 31. The method according to claim 30, wherein the mutation is FGFR3 R248C. 32. The method according to claim 30, wherein the mutation is FGFR3 S249C. 33. The method according to claim 2, wherein the cancer is bladder cancer. 34. The method according to claim 2, wherein the cancer is urothelial cancer. 35. The method according to claim 2, wherein the cancer is metastatic urothelial cancer. 36. The method according to claim 2, wherein the cancer is surgically unresectable urothelial cancer. 37. The method according to claim 2, wherein the cancer is non-muscle-invasive bladder cancer. 38. The method according to claim 2, wherein the cancer is a cancer with a FGFR genomic alteration. 39. The method according to claim 2, wherein the cancer is a cancer with a FGFR translocation. 40. The method according to claim 39, wherein the translocation is a FGFR3-TACC3 translocation. 41. The method according to claim 2, wherein the cancer is a cancer with a FGFR mutation. 42. The method according to claim 41, wherein the mutation is FGFR3 R248C. 43. The method according to claim 41, wherein the mutation is FGFR3 S249C. 44. The method according to claim 3, wherein the cancer is bladder cancer. 45. The method according to claim 3, wherein the cancer is urothelial cancer. 46. The method according to claim 3, wherein the cancer is metastatic urothelial cancer. 47. The method according to claim 3, wherein the cancer is surgically unresectable urothelial cancer. 48. The method according to claim 3, wherein the cancer is non-muscle-invasive bladder cancer. 49. The method according to claim 3, wherein the cancer is a cancer with a FGFR genomic alteration. 50. The method according to claim 3, wherein the cancer is a cancer with a FGFR translocation. 51. The method according to claim 50, wherein the translocation is a FGFR3-TACC3 translocation. 52. The method according to claim 3, wherein the cancer is a cancer with a FGFR mutation. 53. The method according to claim 52, wherein the mutation is FGFR3 R248C. 54. The method according to claim 52, wherein the mutation is FGFR3 S249C. 55. The method according to claim 6, wherein the cancer is bladder cancer. 56. The method according to claim 6, wherein the cancer is urothelial cancer. 57. The method according to claim 6, wherein the cancer is metastatic urothelial cancer. 58. The method according to claim 6, wherein the cancer is surgically unresectable urothelial cancer. 59. The method according to claim 6, wherein the cancer is non-muscle-invasive bladder cancer. 60. The method according to claim 6, wherein the cancer is a cancer with a FGFR genomic alteration. 61. The method according to claim 6, wherein the cancer is a cancer with a FGFR translocation. 62. The method according to claim 61, wherein the translocation is a FGFR3-TACC3 translocation. 63. The method according to claim 6, wherein the cancer is a cancer with a FGFR mutation. 64. The method according to claim 63, wherein the mutation is FGFR3 R248C. 65. The method according to claim 63, wherein the mutation is FGFR3 S249C. 66. The method according to claim 9, wherein the cancer is bladder cancer. 67. The method according to claim 10, wherein the cancer is bladder cancer. 68. The method according to claim 11, wherein the cancer is bladder cancer. 69. The method according to claim 9, wherein the cancer is urothelial cancer. 70. The method according to claim 10, wherein the cancer is urothelial cancer. 71. The method according to claim 11, wherein the cancer is urothelial cancer. 72. The method according to claim 9, wherein the cancer is metastatic urothelial cancer. 73. The method according to claim 10, wherein the cancer is metastatic urothelial cancer. 74. The method according to claim 11, wherein the cancer is metastatic urothelial cancer. 75. The method according to claim 9, wherein the cancer is surgically unresectable urothelial cancer. 76. The method according to claim 10, wherein the cancer is surgically unresectable urothelial cancer. 77. The method according to claim 11, wherein the cancer is surgically unresectable urothelial cancer. 78. The method according to claim 9, wherein the cancer is non-muscle-invasive bladder cancer. 79. The method according to claim 10, wherein the cancer is non-muscle-invasive bladder cancer. 80. The method according to claim 11, wherein the cancer is non-muscle-invasive bladder cancer. 81. The method according to claim 26, wherein the cancer is a cancer with a FGFR genomic alteration. 82. The method according to claim 26, wherein the cancer is a cancer with a FGFR translocation. 83. The method according to claim 82, wherein the translocation is a FGFR3-TACC3 translocation. 84. The method according to claim 26, wherein the cancer is a cancer with a FGFR mutation. 85. The method according to claim 84, wherein the mutation is FGFR3 R248C. 86. The method according to claim 84, wherein the mutation is FGFR3 S249C. 87. The method according to claim 26, wherein the composition comprises N-(3,5-dimethoxyphenyl)-N′-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine base.