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Generated: August 21, 2017

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Title:Tropane derivatives useful in therapy
Abstract:The present invention provides compounds of the formula: ##STR00001## wherein R.sup.1 is C.sub.3-6 cycloalkyl optionally substituted by one or more fluorine atoms, or C.sub.1-6 alkyl optionally substituted by one or more fluorine atoms, or C.sub.3-6 cycloalkylmethyl optionally ring-substituted by one or more fluorine atoms; and R.sup.2 is phenyl optionally substituted by one or more fluorine atoms, to pharmaceutically acceptable salts and solvates thereof, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such compounds.
Inventor(s): Perros; Manoussos (Sandwich, GB), Price; David Anthony (Sandwich, GB), Stammen; Blanda Luzia Christa (Sandwich, GB), Wood; Anthony (Sandwich, GB)
Assignee: Pfizer, Inc. (New York, NY)
Application Number:12/023,334
Patent Claims: 1. A crystalline, polymorph form A of N-{(1S)-3-[3-(3-Isopropyl-5-methyl-4H-1,2,4-triazol-4-yl)-exo-8-azabicycl- o[3.2.1]oct-8-yl]-1-phenylpropyl}-4,4-difluorocyclohexanecarboxamide.

2. The crystalline, polymorph form A of N-{(1S)-3-[3-(3-Isopropyl-5-methyl-4H-1,2,4-triazol-4-yl)-exo-8-azabicycl- o[3.2.1]oct-8-yl]-1-phenylpropyl}-4-difluorocyclo of claim 1 having a powder X-ray diffraction pattern obtained using a wavelength of 1.54178 .ANG. TABLE-US-00004 Angle 2-Theta 8.4 18.4 20.4 22.0.

3. The crystalline, polymorph form A of N-{(1S)-3-[3-(3-isopropyl-5-methyl-4H-1,2,4-triazol-4-yl)-exo-8-azabicycl- o[3.2.1]oct-8-yl]-1-phenylpropyl}-4,4-difluorocyclo of claim 2 having a powder X-ray diffraction pattern obtained using a wavelength of 1.54178 .ANG. as follows: TABLE-US-00005 Angle 2-Theta 7.9 8.4 18.4 20.4 21.3 22.0 22.7.

4. The crystalline, polymorph form B of N-{(1S)-3-[3-(3-Isopropyl-5-methyl-4H-1,2,4-triazol-4-yl)-exo-8-azabicycl- o[3.2.1]oct-8-yl]-1-phenylpropyl}-4,4-difluorocyclohexanecarboxamide.

5. The crystalline, polymorph form B of N-{(1S)-3-[3-(3-Isopropyl-5-methyl-4H-1,2,4-triazol-4-yl)-exo-8-azabicycl- o[3.2.1]oct-8-yl]-1-phenylpropyl}-4,4-difluorocyclohexanecarboxamide of claim 4 having a powder X-ray diffraction pattern obtained using a wavelength of 1.54178 .ANG. as follows: TABLE-US-00006 Angle 2-Theta 10.0 11.2 12.6 17.4.

6. The crystalline, polymorph form B of N-{(1S)-3-[3-(3-Isopropyl-5-methyl-4H-1,2,4-triazol-4-yl)-exo-8-azabicycl- o[3.2.1]oct-8-yl]-1-phenylpropyl}-4.4-difluorocyclohexanecarboxamide of claim 5 having a powder X-ray diffraction pattern as follows: TABLE-US-00007 Angle 2-Theta 10.0 11.2 12.6 17.1 17.4 19.2.
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