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Last Updated: December 22, 2024

Claims for Patent: 10,189,837

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Summary for Patent: 10,189,837

Title:	Crystalline (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,- 9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt
Abstract:	Provided herein are (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,- 9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt forms, including crystalline forms, and methods of their preparation. Pharmaceutical compositions comprising a (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,- 9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt are also provided, as are methods of using (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,- 9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt to treat a disease or condition, such as a cancer.
Inventor(s):	Wang; Bing (San Jose, CA), Chu; Daniel (Santa Clara, CA), Liu; Yongbo (Shanghai, CN), Peng; Shichun (Shanghai, CN)
Assignee:	Medivation Technologies LLC (San Francisco, CA)
Application Number:	15/651,735
Patent Claims:	1. A crystalline tosylate salt of (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,- 9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one having an X-ray powder diffraction pattern comprising peaks at 2.theta. angle degrees .+-.0.2 of 7.5, 20.1, and 24.1. 2. The crystalline tosylate salt of claim 1, having an X-ray powder diffraction pattern comprising peaks at 2.theta. angle degrees .+-.0.2 of 7.5, 15.1, 18.1, 20.1, 20.5, 22.6, and 24.1. 3. A crystalline tosylate salt of (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,- 9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one exhibiting a solid state .sup.13C NMR spectrum with peaks at 143.2, 136.0, 131.8, 123.9, 112.2, 105.2, and 100.3 ppm .+-.0.2 ppm. 4. A pharmaceutical composition comprising the crystalline tosylate salt of claim 1 and a pharmaceutically acceptable excipient. 5. A pharmaceutical composition comprising the crystalline tosylate salt of claim 3 and a pharmaceutically acceptable excipient. 6. A pharmaceutical composition comprising the crystalline tosylate salt of claim 2 and a pharmaceutically acceptable excipient.

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