Claims for Patent: 6,403,567

Summary for Patent: 6,403,567

Title:	N-pyrazole A2A adenosine receptor agonists
Abstract:	2-adenosine N-pyrazole compositions having the following formula: and methods for using the compositions as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heart.
Inventor(s):	Jeff A. Zablocki, Elfatih O. Elzein, Venkata P. Palle
Assignee:	TPG-AXON LEX SUB-TRUST, Gilead Sciences Inc
Application Number:	US09/338,185
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 6,403,567
Patent Claims:	1. A compound having the formula: wherein R1 is —CH2OH; R2 and R4 are each hydrogen; R3 is selected from the group consisting of CO2R20, —CONR7R8 and aryl wherein the aryl substituent is optionally substituted with from 1 to 2 substituents independently selected from the group consisting of halo, C1-6 alkyl, CF3 and OR20; R7 is selected from the group consisting of hydrogen, C1-8 alkyl and aryl, wherein the alkyl and aryl substituents are optionally substituted with one substituent selected from the group consisting of halo, aryl, CF3, CN, and OR20 and wherein each optional aryl substituent is optionally substituted with at least one substituent selected from the group consisting of halo, alkyl, CF3 CN, and OR20; R8 is selected from the group consisting of hydrogen and C1-8 alkyl; and R20 is selected from the group consisting of hydrogen and C1-8 alkyl. 2. The compound of claim 1 wherein R3 is selected from the group consisting of CO2R20, —CONR7R8, and aryl that is optionally substituted with from 1 to 2 substituents independently selected from the group consisting of halo, C1-3 alkyl, CF3 and OR20; R7 is selected from the group consisting of hydrogen, and C1-8 alkyl that is optionally substituted with one substituent selected from the group consisting of halo, CF3, CN and OR20; R8 is selected from the group consisting of hydrogen and C1-3 alkyl; and R20 is selected from the group consisting of hydrogen and C1-4 alkyl. 3. The compound of claim 1 wherein R3 is selected from the group consisting of CO2R20, —CONR7R8, and aryl that is optionally substituted with one substituent selected from the group consisting of halo, C1-3 alkyl, and OR20; R7 is selected from the group consisting of hydrogen, and C1-3 alkyl that is optionally substituted with one substituent selected from the group consisting of halo, CF3, CN and OR20; R8 is hydrogen; and R20 is selected from the group consisting of hydrogen and C1-4 alkyl. 4. The compound of claim 1 wherein R3 is selected from the group consisting of CO2R20, —CONR7R8, and aryl that is optionally substituted with one substituent selected from the group consisting of halo, C1-3 alkyl and OR20; R7 is selected from the group consisting of hydrogen, and C1-3 alkyl; R8 is hydrogen; and R20 is selected from the group consisting of hydrogen and C1-4 alkyl. 5. The compound of claim 4 wherein R7 is a methyl. 6. The compound of claim 4 wherein R3 is —CO2Et. 7. The compound of claim 1 selected from the group consisting of 2-(4-methylaminocarbonylpyrazol-1-yl)adenosine; 2-(4-ethoxycarbonylpyrazol-1-yl)adenosine; 2-[4-(4-chlorophenyl)pyrazol-1-yl)]adenosine; 2-[4-(4-methoxyphenyl)pyrazol-1-yl)]adenosine; 2-[4-(4-methylphenyl)pyrazol-1-yl)]adenosine; and 2-(4-carboxypyrazol-1-yl)adenosine. 8. A compound having the following formula: wherein R1 is —CH20OH; R2 and R4 are each hydrogen; R3 is —CONR7R8; R7 is methyl; and R8 is hydrogen. 9. A pharmaceutical composition comprising a compound of claim 1 and one or more pharmaceutically acceptable excipients. 10. The pharmaceutical composition of claim 9 wherein the pharmaceutical composition is in the form of a solution. 11. A method for stimulating coronary vasodilation in a mammal by administering to the mammal a therapeutically effective amount of a compound of claim 1 that is sufficient to stress the heart and induce a coronary steal situation for the purposes of imaging the heart. 12. The method of claim 11 wherein the therapeutically effective amount ranges from about 0.01 to about 100 mg/kg weight of the mammal. 13. The method of claim 11 wherein the mammal is a human.