COMPOUNDS OF FORMULA (I) AND FORMULA (A), PHARMACEUTICAL COMPOSITION, MEDICINAL PRODUCT, USE AND METHOD OF OBTAINING COMPOUNDS OF FORMULA (I) Russian patent published in 2024 - IPC C07D497/14 A61K31/519 A61P35/00 

Abstract RU 2822758 C2

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a compound of formula (Ia) or a pharmaceutically acceptable salt thereof, where R1 represents a 5-membered heteroaryl; preferably R1 is furyl; X1 and X2 are each independently C or N; R1' is absent when X1 is N; or, when X1 is C, R1' is H, halogen, alkyl, heterocyclyl, alkoxy, heterocyclyloxy, aminocarbonyl, hydroxycarbonyl, heterocyclylcarbonyl, alkylsulfoxide, alkylsulfonyl, aminosulfonyl, heterocyclylsulfonyl or alkylsulfonimidoyl; wherein the said substituents are optionally substituted with one to four substituents selected from oxo, halogen, hydroxy, alkyl, heterocyclylalkyl, hydroxyalkyl, dihydroxyalkyl, hydroxyalkylaminoalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, (heterocyclyl)(alkyl)aminoalkyl, heterocyclyl, heteroaryl, alkylheteroaryl, amino, dialkylamino, aminoalkylcarbonylamino, aminocarbonylalkylamino, (aminocarbonylalkyl)(alkyl)amino, hydroxycarbonyl, aminocarbonyl, aminoalkylaminocarbonyl, alkylaminoalkylaminocarbonyl, dialkylaminoalkylaminocarbonyl, heterocyclylalkylaminocarbonyl, (alkylaminoalkyl)(alkyl) aminocarbonyl, heterocyclylcarbonyl, alkyl sulfoxide, alkyl sulfoxide alkyl and alkyl sulfonyl; R2' is H, alkyl, heterocyclyl, alkoxy, heterocyclyloxy, aminocarbonyl, heterocyclylcarbonyl or alkyl sulfoxide; wherein said substituents are optionally substituted with one or two substituents selected from oxo, halogen, hydroxy, cyano, alkyl, heterocyclylalkyl, dihydroxyalkyl, dialkylaminoalkyl, heterocyclyl, heteroaryl, alkylheteroaryl, hydroxycarbonyl, alkyloxycarbonyl, aminocarbonyl, alkylaminoalkylaminocarbonyl, dialkylaminoalkylaminocar bonyl, heterocyclylalkylaminocarbonyl, alkylsulfoxide, alkylsulfoxidealkyl and alkylsulfonyl; or R1' and R2' form, together with the atoms to which they are attached, a 5-membered heterocyclyl ring; substituted oxo; R3' is absent when X2 is N; or, when X2 represents C, R3' represents H or halogen, preferably H or F; R4' represents H or halogen, preferably H or F; and R5' is H; and where the alkyl group, as such or part of another substituent, contains from 1 to 4 carbon atoms; the heterocyclyl group, as such or part of another substituent, contains from 4 to 6 ring atoms and includes 1 or 2 heteroatoms selected from N, O and/or S; and the heteroaryl group, as such or part of another substituent, contains 5 ring atoms and includes from 1 to 4 heteroatoms selected from N and/or O. The invention also relates to a pharmaceutical composition and drug inhibiting the A2A type adenosine receptor based on the above compounds, method of their preparation and intermediate compounds for their preparation.

EFFECT: obtaining new compounds and a pharmaceutical composition based on them which can be used in medicine in the treatment and prevention of cancer.

20 cl, 4 dwg, 10 tbl, 132 ex

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RU 2 822 758 C2

Authors

Krosinyani, Stefano

Gomes, Bruno

Khautkhejs, Erika

Dates

2024-07-12Published

2018-03-30Filed