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US 2021/0230171 A1Published application
Selective a2a receptor antagonist
AssigneeInxmed (Nanjing) Co., Ltd.
InventorsZaiqi WANG, Lihu YANG
Life of this patent
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Abstract
The present invention relates to a selective A2A receptor antagonist, and in particular to a selective A2A receptor antagonist of Formula (I), a pharmaceutical composition comprising the antagonist, use of the antagonist in manufacturing a medicament and in treatment of a disease: wherein the groups in Formula (I) are defined as in the specification.
Claims19
A compound of Formula (I), or a stereoisomer or pharmaceutically acceptable salt thereof:
- wherein
- n is 0 or 1,
- m is 1 or 2,
- A is nitrogen or carbon;
- X is each independently —R1COOR2,
- R1 is a direct bond or a C1-4 alkylene,
- R2 is H or a C1-4 alkyl,
- with the proviso that when A is nitrogen, X is not attached to A.
5 more elements
(canceled)
A method for increasing oral bioavailability of compound SCH-58261 and/or prolonging the in vivo half-life of SCH-58261, comprising:
- introducing 1 or 2 substituents X onto the benzene ring of the molecule of SCH-58261, the substituent X being —R1COOR2;
- wherein R1 is a direct bond and R2 is H or a C1-4 alkyl.
10-12. (canceled)
Dependencies are inferred from the claim text.