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US 2010/0249084 A1Published application
Substituted pyrimidines as adenosine receptor antagonists
OwnerYoungsheng Chen, Manisha Moorjani +3inventors
InventorsYoungsheng Chen, Manisha Moorjani, Deborah Slee, John Tellew, Xiaohu Zhang
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Abstract
Compounds of formula (I): wherein R1, R2 and R3 are as defined herein, including pharmaceutically acceptable salt, ester, solvate or stereoisomer thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof.
Claims20
A compound of formula (I)
- or a pharmaceutically acceptable salt, ester, solvate or stereoisomer thereof, wherein:
- R1 is a heterocycle optionally substituted by one or more members selected from the group of lower alkyl, lower alkoxy, halogen and cyano;
- R2 is phenyl or pyridyl, wherein the phenyl or pyridyl ring is substituted by 1 to 4 R4 groups;
- or
- R2 is isoquinoline, dihydroisoquinoline or tetrahydroisoquinoline ring, wherein the isoquinoline, dihydroisoquinoline or tetrahydroisoquinoline ring is optionally substituted by R5;
- R3 is H, R7, COR7, CONR7R8, or COOR7;
- R4 is at each occurrence selected from the group of halogen, —(X)m—(O), —(Y)p—R5, or —(X)m—(O)n—(Y)p—NR5R6;
- each of R5 and R6 is independently hydrogen, lower alkyl, lower C2-6 alkoxy, lower C2-6 alkoxyalkyl, lower C2-6 hydroxyalkyl, cyano, C(O)—C1-C6alkyl or C(O)O—C1-C6alkyl;
- or
- R5 and R6 together with the nitrogen to which they are attached form a heterocyclic ring optionally substituted by one or more members selected from the group of halogen, hydroxyl, lower alkyl, lower alkoxy, lower alkoxyalkyl, lower hydroxyalkyl, cyano, and —C(O)—C1-C6alkyl;
- R7 is lower alkyl optionally substituted by one or more members selected from the group of lower alkyl, lower alkoxy, hydroxyl, halogen, amino, alkylamino and dialkylamino;
- R8 is selected from the group of lower alkyl, lower alkoxy, alkoxyalkyl, —C(O)—C1-C6alkyl or lower alkenyl, wherein the lower alkyl, lower alkoxy, alkoxyalkyl, —C(O)—C1-C6alkyl, and lower alkenyl groups are optionally substituted by one or more lower alkyl, halogen, lower alkoxy, hydroxyl, or cyano;
- or
- R7 and R8 together with the nitrogen to which they are attached form a heterocyclic ring optionally substituted by one or more members selected from the group of halogen, hydroxyl, lower alkyl, lower alkoxy, lower alkoxyalkyl, lower hydroxyalkyl and cyano;
- each of X and Y is independently lower alkyl, cycloalkyl or saturated heterocyclyl;
- m is at each occurrence 0 or 1;
- n is at each occurrence 0 or 1;
- and
- p is at each occurrence 0 or 1.
16 more elements
Dependencies are inferred from the claim text.