Aminopyrimidine five-membered heterocyclic compound, and intermediate, preparation method, pharmaceutical composition and application thereof
AssigneeGuangzhou Maxinovel Pharmaceuticals Co., Ltd.
InventorsYuguang WANG, Nong ZHANG, Tianzhi WU
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Abstract
Disclosed in the present invention is an aminopyrimidine five-membered heterocyclic compound, and an intermediate, preparation method, pharmaceutical composition and application thereof. The aminopyrimidine five-membered heterocyclic compound provided by the present invention has a significant antagonistic effect on adenosine A2A receptors, and may be used as an antagonist for adenosine A2A receptors to effectively relieve or treat immune tolerance, diseases of the central nervous system, inflammatory diseases and like related diseases, while the preparation method is simple.
Claims21
An aminopyrimidine five-membered heterocyclic compound represented by formula I-1, a pharmaceutically acceptable salt, a tautomer, an enantiomer or a diastereomer or a prodrug thereof:
- wherein, “” represents for a single bond or a double bond;
- when“” is a single bond, Z is N or CR5;
- R5 is H, D or C1-C20 alkyl;
- when“” is double bond, Z is C;
- X is O, CO or NR3;
- Y is CO, CH2 or NR4;
- each of R1 and R2 is independently selected from substituted or unsubstituted C1-C20 alkyl, substituted or unsubstituted C6-C30 aryl or substituted or unsubstituted C2-C30 heteroaryl;
- the C2-C30 heteroaryl in the substituted or unsubstituted C2-C30 heteroaryl refers to a C2-C30 heteroaryl that comprising 1-4 heteroatoms which is selected from the group consisting of N, O or S;
- the substituent in the substituted C1-C20 alkyl group, the substituted C6-C30 aryl or the substituted C2-C30 heteroaryl is selected from one or more of the group consisting of one or more halogens, C1-C120 alkyl, halogenated C1-C20 alkyl, oxo, hydroxyl, amino,
- cyano, C1-C20 alkoxyl, halogenated C1-C20 alkoxyl and C1-C20 alkylthio;
- when the number of the substituent is more than one, the substituents are the same or different;
- wherein, each of Ra and Rb is independently H or C1-C20 alkyl;
- Rc is C1-C20 alkyl;
- R3 is H, C1-C20 alkyl or C3-C30 cycloalkyl;
- R4 is H, C1-C20 alkyl or C3-C30 cycloalkyl;
- m is 0, 1, 2 or 3;
- n is 0, 1, 2 or 3.
(canceled)
Dependencies are inferred from the claim text.