HETEROARYL[4,3-c]PYRIMIDINE-5-AMINE DERIVATIVE, ITS PREPARATION METHOD AND ITS MEDICAL APPLICATIONS Russian patent published in 2022 - IPC C07D487/04 A61P25/00 A61K31/519 

Abstract RU 2764655 C2

FIELD: medicine.

SUBSTANCE: present invention relates to the field of medicine, namely to a compound of the formula (I)

or its pharmaceutically acceptable salt, where G is N or CR4; ring A is phenyl or furyl; each R1 is identical or distinct and each is independently selected from a group consisting of hydrogen, halogen and C1-6alkyl; R2 is selected from a group consisting of cyano, 6-10-element aryl and 5-10-element heteroaryl having from 1 to 2 heteroatoms N, where each of 6-10-element aryl and 5-10-element heteroaryl is independently optionally substituted with one or more substituents selected from a group consisting of halogen, C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, oxo, 3-6-element cycloalkyl and Rb; R3 is selected from a group consisting of hydrogen, halogen and C1-6alkyl; R4 is hydrogen or C1-6alkyl; Rb is 6-element heterocyclylC1-6alkyl, where 1-2 heterocyclyl atoms are heteroatoms selected from a group consisting of N and O, while 6-element heterocyclyl of 6-element heterocyclylC1-6alkyl is optionally substituted with one or more C1-6alkyl; and n is 1, 2, 3 or 4. An intermediate compound of the formula (IV), a method for obtaining a compound of the formula (II), a pharmaceutical composition, and the use of a compound of the formula (I) to obtain a drug are also proposed.

EFFECT: obtaining new derivatives of heteroaryl[4,2-c]pyrimidine-5-amines, which are applicable as antagonists of the A2a receptor.

15 cl, 3 tbl, 61 ex

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RU 2 764 655 C2

Authors

Lu, Byao

Van, Shenlan

Shen, Syaodun

Khe, Fen

Tao, Vejkan

Dates

2022-01-19Published

2018-03-15Filed