Details for Patent: 7,265,119

Title:	Tartrate salts of 5,8,14-triazatetracyclo[10.3.1.0.sup.2,11.0.sup.4.9]-hexadeca-2(11),3,5,7- ,9-pentaene and pharmaceutical compositions thereof
Abstract:	The present invention is directed to the tartrate salts of 5,8,14-triazatetracyclo[10.3.1.0.sup.2,11.0.sup.4,9]-hexadeca-2(11),3,5,7- ,9-pentaene: ##STR00001## and pharmaceutical compositions thereof. The present invention in particular is directed to the L-tartrate salt, and further to the various polymorphs of the L-tartrate salt, including two distinct anhydrous polymorphs (referred to herein as Forms A and B) and a hydrate polymorph (referred to herein as Form C). In addition, the present invention is also directed to the D-tartrate salt of 5,8,14-triazatetracyclo[10.3.1.0.sup.2,11.0.sup.4,9]-hexadeca-2(11),3,5,7- ,9-pentaene and the various polymorphs thereof; as well as the D,L-tartrate salt thereof and its polymorphs, and the meso-tartrate salt thereof and its polymorphs.
Inventor(s):	Bogle; David E. (Jewett City, CT), Williams; Glenn R. (Oaksville, CA), Rose; Peter R. (Ledyard, CT)
Assignee:	Pfizer Inc (New York, NY)
Filing Date:	Feb 28, 2005
Application Number:	11/069,724
Claims:	1. The anhydrous L-tartrate salt of 5,8,14-triazatetracyclo[10.3.1.0.sup.2,11.0.sup.4,9]-hexadeca-2(11),3,5,7- ,9-pentaene, characterized substantially by at least one of the following powder x-ray diffraction pattern peaks expressed in term of 2.theta. as measured with copper radiation chosen from: 6.1, 16.8 and 21.9. 2. A compound according to claim 1 characterized substantially by the following principal powder x-ray diffraction pattern peaks expressed in terms of 2.theta. and d-spacings as measured with copper radiation: TABLE-US-00027 Angle 2.theta. d-value (.ANG.) 6.1 14.5 12.2 7.2 13.0 6.8 14.7 6.0 16.8 5.3 19.4 4.6 21.9 4.1 24.6 3.6. 3. A compound according to claim 1 characterized substantially by solid state .sup.13C NMR resonance peaks at 178.4, 145.1, and 122.9 ppm. 4. The anhydrous L-tartrate salt of 5,8,14-triazatetracyclo[10.3.1.0.sup.2,110..sup.4,9]-hexadeca-2(11 ),3,5,7,9-pentaene, characterized substantially by at least one of the following powder x-ray diffraction pattern peaks expressed in terms of 2.theta. as measured with copper radiation chosen from: 5.9 and 21.8. 5. A compound according to claim 4 characterized substantially by the principal powder x-ray diffraction pattern peaks in terms of 2.theta. and d-spacings measured with copper radiation: TABLE-US-00028 Angle 2.theta. d-value (.ANG.) 5.9 15.0 12.8 6.9 14.4 6.1 15.3 5.8 16.9 5.2 17.2 5.2 21.8 4.1 23.8 3.7 25.1 3.5. 6. A compound according to claim 4 characterized substantially by the solid state .sup.13C NMR principal resonance peaks at: 179.2, 178.0, 144.4, 124.8 and 122.5 ppm. 7. The L-tartrate hydrate salt of 5,8,14-triazatetracyclo[10.3.1 0.sup.2,11 0..sup.4,9]-hexadeca-2(11),3,5,7,9-pentaene, characterized substantially by at least one of the following powder x-ray diffraction pattern peaks expressed in terms of 2.theta. as measured with copper radiation chosen from: 11.8, 16.5, 23.1 and 26.5. 8. A compound according to claim 7 characterized substantially by the principal powder x-ray diffraction pattern peaks in terms of 2.theta. and d-spacings as measured with copper radiation: TABLE-US-00029 Angle 2.theta. d-value (.ANG.) (.+-.0.2) (.+-.0.2) 5.9 15.1 11.8 7.5 16.5 5.4 21.2 4.2 23.1 3.8 23.8 3.7 26.5 3.4. 9. A compound according to claim 7 characterized substantially by solid state .sup.13C NMR principal resonance peaks: 179.0, 176.1, 147.5 and 144.5 ppm. 10. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound according to claim 1. 11. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound according to claim 4. 12. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound according to claim 7. 13. A method of treatment for nicotine dependency, addiction and withdrawal comprising the administration of a compound according to claim 1 to a subject in need thereof. 14. A method of treatment for nicotine dependency, addiction and withdrawal comprising the administration of a compound according to claim 4 to a subject in need thereof. 15. A method of treatment for nicotine dependency, addiction and withdrawal comprising the administration of a compound according to claim 7 to a subject in need thereof.