.

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: 7,183,264

« Back to Dashboard

Claims for Patent: 7,183,264

Title:N-pyrazole A2A receptor agonists
Abstract:2-adenosine N-pyrazole compounds having the following formula: ##STR00001## and methods for using the compounds as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heart are disclosed.
Inventor(s): Zablocki; Jeff (Mountain View, CA), Elzein; Elfatih O. (Fremont, CA), Palle; Venkata P. (Gurgaon, IN), Belardinelli; Luiz (Palo Alto, CA)
Assignee: CV Therapeutics, Inc. (Palo Alto, CA)
Application Number:10/652,378
Patent Claims: 1. A method for stimulating coronary vasodilatation in a mammal by administering to the mammal a therapeutically effective amount of a compound of Formula I ##STR00021## namely (1-{9-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminop- urin-2-yl}pyrazol-4-yl)-N-methylcarboxamide.

2. The method of claim 1 wherein the mammal is a human.

3. A pharmaceutical composition comprising the compound of Formula I ##STR00022## namely (1-{9-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminop- urin-2-yl}pyrazol-4-yl)-N-methylcarboxamide, and one or more pharmaceutical excipients.

4. The pharmaceutical composition of claim 3 wherein the pharmaceutical composition is in the form of a solution.

5. A method of producing coronary vasodilation without peripheral vasodilation comprising administering a compound of Formula I ##STR00023## namely (1-{9-[(2R,3R,4S ,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminopurin-2-yl}pyrazo- l-4-yl)-N-methylcarboxamide, to a human.

6. The method of claim 5 wherein the compound of Formula I is administered by iv bolus.

7. The method of claim 6 wherein the compound of Formula I is administered in from about 10 to about 30 seconds.

8. A method of myocardial perfusion imaging of a human, comprising administering a radionuclide and a compound of Formula I. ##STR00024## namely (1-{9-[(2R,3R,4S ,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminopurin-2-yl}pyrazo- l-4-yl)-N-methylcarboxamide, to the human wherein the myocardium is examined for areas of insufficient blood flow following administration of the radionuclide and the compound of Formula I.

9. The pharmaceutical composition of claim 3 wherein the pharmaceutical composition is formulated for injection.

10. The method of claim 1, wherein the amount of the compound of Formula I is sufficient to stress the heart and induce a coronary steal situation.

11. The method of claim 1, wherein the amount of the compound of Formula I administered is sufficient for imaging heart or coronary activity in the mammal.

12. The method of claim 1 wherein the compound of Formula I is administered by iv bolus.

13. The method of claim 12 wherein the compound of Formula I is administered in from about 10 to about 30 seconds.

14. The method of claim 5, wherein the amount of the compound of Formula I is sufficient to stress the heart and induce a coronary steal situation.

15. The method of claim 5, wherein the amount of the compound of Formula I administered is sufficient for imaging heart or coronary activity in the mammal.

16. The method of claim 5 wherein the therapeutically effective amount ranges from about 0.01 to about 100 mg/kg weight of the mammal.

17. The method of claim 8, wherein the amount of the compound of Formula I is sufficient to stress the heart and induce a coronary steal situation.

18. The method of claim 8, wherein the amount of the compound of Formula I administered is sufficient for imaging heart or coronary activity in the mammal.

19. The method of claim 8 wherein the compound of Formula I is administered by iv bolus.

20. The method of claim 19 wherein the compound of Formula I is administered in from about 10 to about 30 seconds.

21. The method of claim 8 wherein the therapeutically effective amount ranges from about 0.01 to about 100 mg/kg weight of the mammal.

22. The method of claim 1 wherein the therapeutically effective amount ranges from about 0.01 to about 100 mg/kg weight of the mammal.
« Back to Dashboard

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

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