.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Claims for Patent: 8,106,183

« Back to Dashboard

Claims for Patent: 8,106,183

Title:Process for preparing an A.sub.2A-adenosine receptor agonist and its polymorphs
Abstract: Disclosed is a synthesis suitable for large scale manufacture of an A.sub.2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.
Inventor(s): Zablocki; Jeff (Mountain View, CA), Elzein; Elfaith (Fremont, CA)
Assignee: Gilead Sciences, Inc. (Foster City, CA)
Application Number:12/765,623
Patent Claims: 1. A monohydrate of (1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminop- urin-2-yl}pyrazol-4-yl)-N-methylcarboxamide, which 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 FIG. 3.

3. The monohydrate of claim 1, wherein the crystalline form has a thermogravimetric analysis pattern and a differential scanning calorimetry pattern as shown in FIG. 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-aminop- urin-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-aminop- urin-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-aminop- urin-2-yl}pyrazol-4-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 .sup.1H NMR spectrum as shown in FIG. 1.

9. The monohydrate of claim 1, wherein the crystalline form is free of any impurity represented by the following structure: ##STR00024##
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

How are People Using DrugPatentWatch?

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc