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1. (AU2007212542) Process for preparing an A2A-Adenosine receptor agonist and its polymorphs
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The claims defining the invention are as follows:
1.           A monohydrate of (1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl] 6-aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide, wherein the monohydrate is in a crystalline form.
2.           The monohydrate of claim 1, wherein the crystalline form has a X-ray diffraction pattern as shown in Figure 3.
3.           The monohydrate of claim 1, wherein the crystalline form has a thermogravimetic analysis pattern and a differential scanning calorimetry pattern as shown in Figure 2.
4.           The monohydrate of claim 1, wherein the crystalline form is obtainable by a method comprising crystallizing (1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6 aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide in an aqueous protic solvent or an aqueous polar solvent.
5.           The monohydrate of claim 1, wherein the crystalline form is obtainable by a method comprising crystallizing (1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6 aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide in a solvent selected from a mixture of ethanol and water and a mixture of dimethylsulfoxide and water.
6.           A method for preparing the monohydrate of claim 1, comprising crystallizing (1-{9 [(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminopurin-2-yl}pyrazol-4 yl)-N-methylcarboxamide in an aqueous protic solvent or an aqueous polar solvent.
7.           The method of claim 6, wherein the aqueous protic solvent or the aqueous polar solvent is selected from a mixture of ethanol and water and a mixture of dimethylsulfoxide and water.
8.           The monohydrate of claim 1, wherein the crystalline form has a 'H NMR spectrum as shown in Figure 1.
9.           The monohydrate of claim 1, wherein the crystalline form is free of any impurity represented by the following structure:
10.         The monohydrate of claim 1, wherein the monohydrate exhibits an X-ray powder diffraction pattern having at least one peak at diffraction angle 20 (*) of about 6 as measured by Cu-Kal X-ray powder diffractometry.
11.         The monohydrate of claim 1, wherein the monohydrate exhibits an X-ray powder diffraction pattern having peaks at diffraction angle 20 (0) of about 6, about 9, about 11, about 13, about 14.5, about 16.5, and about 18 as measured by Cu-Kal X-ray powder diffractometry.
12.        A  monohydrate      according    to  claim   1,  substantially     as  herein   described.