Claims
- 1. A crystal form of (R)-2-(2-(4-oxazol-4-yl-phenoxy)-ethylamino)-1-pyridin-3-yl-ethanol), p-toluenesulfonate salt.
- 2. The crystal form of claim 1 wherein said crystal form has high-intensity X-ray diffraction peaks at diffraction angles (2 theta) of about 6.0 and 18.1, and X-ray powder diffraction d-spacings (Å) of about 14.7 and 4.9, respectively.
- 3. The crystal form of claim 1 having the following characteristic high-intensity diffraction peaks at diffraction angles (2 theta) and X-ray powder diffraction d-spacing (Å):
- 4. The crystal form of claim 1 wherein said crystal form has an onset melting temperature of about 160° C.
- 5. A crystal form of (R)-2-(2-(4-oxazol-4-yl-phenoxy)-ethylamino)-1-pyridin-3-yl-ethanol), p-toluenesulfonate salt, monohydrate.
- 6. The crystal form of claim 5 wherein said crystal form has high-intensity X-ray diffraction peaks at diffraction angles (2 theta) of about 5.7 and 17.2, and X-ray powder diffraction d-spacings (Å) of about 15.6 and 5.1.
- 7. The crystal form of claim 5 wherein said crystal form has the following characteristic high-intensity diffraction peaks at diffraction angles (2 theta), and X-ray powder diffraction d-spacing (Å):
- 8. A process for preparing crystalline (R)-2-(2-(4-oxazol-4-yl-phenoxy)-ethylamino)-1-pyridin-3-yl-ethanol), p-toluenesulfonate salt comprising the steps of:
(a) preparing a solution of (R)-2-(2-(4-oxazol-4-yl-phenoxy)-ethylamino)-1-pyridin-3-yl-ethanol in a reaction-inert solvent; and (b) treating said solution from step (a) with p-toluenesulfonic acid monohydrate to obtain a final stoichiometric ratio of (R)-2-(2-(4-oxazol-4-yl-phenoxy)-ethylamino)-1-pyridin-3-yl-ethanol to p-toluenesulfonic acid monohydrate of about 1:1.
- 9. A process for preparing crystalline (R)-2-(2-(4-oxazol-4-yl-phenoxy)-ethylamino)-1-pyridin-3-yl-ethanol), p-toluenesulfonate salt, monohydrate comprising the step of contacting (R)-2-(2-(4-oxazol-4-yl-phenoxy)-ethylamino)-1-pyridin-3-yl-ethanol), p-toluenesulfonate salt with water, optionally in the presence of a reaction-inert solvent.
- 10. The process of claim 9 wherein said reaction-inert solvent is tetrahydrofuran.
- 11. The process according to claim 10 wherein said water and said reaction-inert solvent are present in a ratio of from about 0.4:10 to about 7.5:10.
- 12. The process of claim 10 wherein said water and said reaction-inert solvent are present in a ratio of about 1:10.
- 13. A pharmaceutical composition comprising
(i) a therapeutically effective amount of a crystal form of (R)-2-(2-(4-oxazol-4-yl-phenoxy)-ethylamino)-1-pyridin-3-yl-ethanol), p-toluenesulfonate salt, or a crystal form of (R)-2-(2-(4-oxazol-4-yl-phenoxy)-ethylamino)-1-pyridin-3-yl-ethanol), p-toluenesulfonate salt, monohydrate; and (ii) a pharmaceutically acceptable carrier, vehicle, or diluent.
- 14. A method of treating a β3-adrenergic receptor-mediated disease, condition, or disorder comprising the step of administering to a mammal in need of such treatment a therapeutically effective amount of a crystal form of (R)-2-(2-(4-oxazol-4-yl-phenoxy)-ethylamino)-1-pyridin-3-yl-ethanol), p-toluenesulfonate salt; a crystal form of (R)-2-(2-(4-oxazol-4-yl-phenoxy)-ethylamino)-1-pyridin-3-yl-ethanol), p-toluenesulfonate salt, monohydrate; or a pharmaceutical composition comprising said a crystal form of (R)-2-(2-(4-oxazol-4-yl-phenoxy)-ethylamino)-1-pyridin-3-yl-ethanol), p-toluenesulfonate salt, or said crystal form of (R)-2-(2-(4-oxazol-4-yl-phenoxy)-ethylamino)-1-pyridin-3-yl-ethanol), p-toluenesulfonate salt, monohydrate.
- 15. A method of increasing lean meat content of an edible animal comprising the step of administering to said edible animal a lean meat increasing amount of a crystal form of (R)-2-(2-(4-oxazol-4-yl-phenoxy)-ethylamino)-1-pyridin-3-yl-ethanol), p-toluenesulfonate salt; a crystal form of (R)-2-(2-(4-oxazol-4-yl-phenoxy)-ethylamino)-1-pyridin-3-yl-ethanol), p-toluenesulfonate salt, monohydrate; or a pharmaceutical composition comprising said crystal form of (R)-2-(2-(4-oxazol-4-yl-phenoxy)-ethylamino)-1-pyridin-3-yl-ethanol), p-toluenesulfonate salt, or said crystal form of (R)-2-(2-(4-oxazol-4-yl-phenoxy)-ethylamino)-1-pyridin-3-yl-ethanol), p-toluenesulfonate salt, monohydrate.
Parent Case Info
[0001] This application claims the benefit of U.S. Provisional Application No. 60/360,252 filed on Feb. 27, 2002 and incorporated herein by reference in its entirety.
Provisional Applications (1)
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Number |
Date |
Country |
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60360252 |
Feb 2002 |
US |