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Generated: September 23, 2017

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Title: N-pyrazole A2A adenosine receptor agonists
Abstract:2-adenosine N-pyrazole compositions having the following formula: ##STR1## 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): Zablocki; Jeff A. (Mountain View, CA), Elzein; Elfatih O. (Freemont, CA), Palle; Venkata P. (Mountain View, CA)
Assignee: CV Therapeutics, Inc. (Palo Alto, CA)
Application Number:09/338,185
Patent Claims: 1. A compound having the formula: ##STR15##

wherein

R.sup.1 is --CH.sub.2 OH;

R.sup.2 and R.sup.4 are each hydrogen;

R.sup.3 is selected from the group consisting of CO.sub.2 R.sup.20, --CONR.sup.7 R.sup.8 and aryl wherein the aryl substituent is optionally substituted with from 1 to 2 substituents independently selected from the group consisting of halo, C.sub.1-6 alkyl, CF.sub.3 and OR.sup.20 ;

R.sup.7 is selected from the group consisting of hydrogen, C.sub.1-8 alkyl and aryl, wherein the alkyl and aryl substituents are optionally substituted with one substituent selected from the group consisting of halo, aryl, CF.sub.3, CN, and OR.sup.20 and wherein each optional aryl substituent is optionally substituted with at least one substituent selected from the group consisting of halo, alkyl, CF.sub.3 CN, and OR.sup.20 ;

R.sup.8 is selected from the group consisting of hydrogen and C.sub.1-8 alkyl; and

R.sup.20 is selected from the group consisting of hydrogen and C.sub.1-8 alkyl.

2. The compound of claim 1 wherein R.sup.3 is selected from the group consisting of CO.sub.2 R.sup.20, --CONR.sup.7 R.sup.8, and aryl that is optionally substituted with from 1 to 2 substituents independently selected from the group consisting of halo, C.sub.1-3 alkyl, CF.sub.3 and OR.sup.20 ;

R.sup.7 is selected from the group consisting of hydrogen, and C.sub.1-8 alkyl that is optionally substituted with one substituent selected from the group consisting of halo, CF.sub.3, CN and OR.sup.20 ;

R.sup.8 is selected from the group consisting of hydrogen and C.sub.1-3 alkyl; and

R.sup.20 is selected from the group consisting of hydrogen and C.sub.1-4 alkyl.

3. The compound of claim 1 wherein R.sup.3 is selected from the group consisting of CO.sub.2 R.sup.20, --CONR.sup.7 R.sup.8, and aryl that is optionally substituted with one substituent selected from the group consisting of halo, C.sub.1-3 alkyl, and OR.sup.20 ;

R.sup.7 is selected from the group consisting of hydrogen, and C.sub.1-3 alkyl that is optionally substituted with one substituent selected from the group consisting of halo, CF.sub.3, CN and OR.sup.20 ;

R.sup.8 is hydrogen; and

R.sup.20 is selected from the group consisting of hydrogen and C.sub.1-4 alkyl.

4. The compound of claim 1 wherein R.sup.3 is selected from the group consisting of CO.sub.2 R.sup.20, --CONR.sup.7 R.sup.8, and aryl that is optionally substituted with one substituent selected from the group consisting of halo, C.sub.1-3 alkyl and OR.sup.20 ;

R.sup.7 is selected from the group consisting of hydrogen, and C.sub.1-3 alkyl;

R.sup.8 is hydrogen; and

R.sup.20 is selected from the group consisting of hydrogen and C.sub.1-4 alkyl.

5. The compound of claim 4 wherein R.sup.7 is a methyl.

6. The compound of claim 4 wherein R.sup.3 is --CO.sub.2 Et.

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: ##STR16##

wherein

R.sup.1 is --CH.sub.20 OH;

R.sup.2 and R.sup.4 are each hydrogen;

R.sup.3 is --CONR.sup.7 R.sup.8 ;

R.sup.7 is methyl; and

R.sup.8 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.
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