Claims for Patent: 8,754,072

Summary for Patent: 8,754,072

Title:	Salts and polymorphs of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6h-azepino[- 5,4,3-cd]indol-6-one
Abstract:	The present invention relates to novel polymorphic forms of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[- 5,4,3-cd]indol-6-one, and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer.
Inventor(s):	Basford; Patricia Ann (Sandwich, GB), Campeta; Anthony Michael (Ledyard, CT), Gillmore; Adam (Sandwich, GB), Jones; Matthew Cameron (Sandwich, GB), Kougoulos; Eleftherios (Morrisville, NC), Luthra; Suman (Groton, CT), Walton; Robert (Sandwich, GB)
Assignee:	Pfizer Inc. (New York, NY)
Application Number:	13/522,549
Patent Claims:	1. A crystalline camsylate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[- 5,4,3-cd]indol-6-one. 2. The salt of claim 1, wherein the salt is a crystalline anhydrous salt. 3. The salt of claim 1, wherein the camsylate is S-camsylate. 4. The salt of claim 1, wherein the camsylate is R-camsylate. 5. The salt of claim 1, wherein the salt has a powder X-ray diffraction pattern comprising one or more or two or more or three peaks at diffraction angles (2.theta.) selected from the group consisting of 12.2.+-.0.2, 14.8.+-.0.2 and 22.4.+-.0.2, wherein said powder X-ray diffraction pattern is obtained using copper K-alpha.sub.1 X-rays at a wavelength of 1.5406 .ANG.ngstroms. 6. The salt of claim 1, wherein the salt has a solid state NMR spectrum comprising one or more .sup.13C chemical shifts selected from the group consisting of 213.4.+-.0.2, 171.8.+-.0.2, and 17.3.+-.0.2 ppm. 7. The salt of claim 1, wherein the salt has a solid state NMR spectrum comprising one or more .sup.19F chemical shifts selected from the group consisting of -118.9.+-.0.2 and -119.7 ppm.+-.0.2. 8. The salt of claim 1, wherein the salt has a powder X-ray diffraction pattern comprising one or more or two or more or three peaks at diffraction angles (2.theta.) selected from the group consisting of 12.2.+-.0.2, 14.8.+-.0.2 and 22.4.+-.0.2 obtained using copper K-alpha.sub.1 X-rays at a wavelength of 1.5406 .ANG.Angstroms; a solid state NMR spectrum comprising one or more or two or more or three .sup.13C chemical shifts selected from the group consisting of 213.4.+-.0.2, 171.8.+-.0.2, and 17.3.+-.0.2 ppm; and a solid state NMR spectrum comprising one or more or two .sup.19F chemical shifts selected from the group consisting of -118.9.+-.0.2 and -119.7 ppm.+-.0.2. 9. The salt of claim 1, wherein the salt is a substantially pure polymorph of S-camsylate polymorph Form A. 10. The salt of claim 1, wherein the salt is a substantially pure polymorph of S-camsylate polymorph Form B or a substantially pure polymorph of S-camsylate polymorph Form C. 11. A crystalline maleate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[- 5,4,3-cd]indol-6-one. 12. The salt of claim 11, wherein the salt is a crystalline anhydrous salt. 13. The salt of claim 11, wherein the salt has a powder X-ray diffraction pattern comprising peaks at diffraction angles (2.theta.) 6.0.+-.0.2, 20.3.+-.0.2, and 21.7.+-.0.2, wherein said powder X-ray diffraction pattern is obtained using copper K-alpha.sub.1 X-rays at a wavelength of 1.5406 .ANG.ngstroms. 14. The salt of claim 11, wherein the salt is a substantially pure polymorph of maleate polymorph Form A. 15. The salt of claim 11, wherein the salt has a powder X-ray diffraction pattern comprising peaks at diffraction angles (2.theta.) of 7.5.+-.0.2, 11.3.+-.0.2, and 24.3.+-.0.2, wherein said powder X-ray diffraction pattern is obtained using copper K-alpha.sub.1 X-rays at a wavelength of 1.5406 .ANG.ngstroms. 16. The salt of claim 11, wherein the salt has a solid state NMR spectrum comprising one or more .sup.13C chemical shifts selected from the group consisting of 171.3.+-.0.2, 112.4.+-.0.2, and 43.8.+-.0.2 ppm. 17. The salt of claim 11, wherein the salt has a solid state NMR spectrum comprising a .sup.19F chemical shift at -123.1 ppm.+-.0.2. 18. The salt of claim 11, wherein the salt has a powder X-ray diffraction pattern comprising: one or more or two or more or three peaks at diffraction angles (2.theta.) selected from the group consisting of 7.5.+-.0.2, 11.3.+-.0.2, and 24.3.+-.0.2 obtained using copper K-alpha.sub.1 X-rays at a wavelength of 1.5406 .ANG.ngstroms; a solid state NMR spectrum comprising one or more or two or more or three .sup.13C chemical shifts selected from the group consisting of 171.3.+-.0.2, 112.4.+-.0.2, and 43.8.+-.0.2 ppm; and a solid state NMR spectrum comprising a .sup.19F chemical shift at -123.1.+-.0.2 ppm. 19. The salt of claim 11, wherein the salt is a substantially pure polymorph of maleate polymorph Form B. 20. A pharmaceutical composition comprising the salt of claim 1 and a pharmaceutically acceptable carrier. 21. A pharmaceutical composition comprising the salt of claim 11 and a pharmaceutically acceptable carrier.