TRIAZOLO-PYRIMIDINE COMPOUNDS AND THEIR USE Russian patent published in 2023 - IPC C07D487/04 C07D519/00 A61K31/505 A61K31/519 A61P11/06 A61P25/00 A61P25/08 A61P25/24 A61P25/28 A61P35/00 A61P35/02 A61P35/04 

Abstract RU 2802866 C2

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to novel triazolo-pyrimidine compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein X is selected from amino; ring A is selected from:

Z is selected from halogen, amino, N-(C1-12alkyl)amino, N,N-(C1-12alkyl)2amino, 3-12 membered saturated or unsaturated carbocyclyl, or 3-12 membered saturated or unsaturated a heterocyclyl having 1, 2 or 3 heteroatoms selected from N, O or S, which may optionally be mono- or independently polysubstituted with R2; Y represents -WV, where W represents -NH-, C1-12alkylene, V represents a 5-6 membered saturated or unsaturated carbocyclyl or a 5-6 membered saturated or unsaturated heterocyclyl having 1 or 2 heteroatoms, selected from N, O or S, which may optionally be mono- or independently polysubstituted with R3; each R1 is independently selected from halogen, cyano, amino, C1-12alkyl, C1-12haloalkyl, C1-12alkoxy, C1-12haloalkoxy, C1-12alkyl-OH, N-(C1- 12alkyl)amino, N,N-(C1-12alkyl)2amino, 3-10 membered saturated or unsaturated carbocyclyl or 3-10 membered saturated heterocyclyl having 1 heteroatom selected from O and S, where the sulfur atom possibly can be oxidized to form S-oxides; each R 2 is independently selected from halogen, amino, C1-12alkyl, C1-12haloalkyl, C1-12alkoxy, C1-12haloalkoxy, N-(C1-12alkyl)amino, N,N-(C1-12alkyl)2amino; each R3 is independently selected from halo, cyano, amino, C1-12alkyl, C1-12haloalkyl, C1-12haloalkoxy, N-(C1-12alkyl)amino, N,N-(C1-12alkyl)2 amino; m is 0, 1, 2, 3, or 4. Also the invention relates to pharmaceutical compositions containing one or more of these compounds as an active ingredient, to the use of these compounds in the treatment of diseases associated with adenosine receptors (AR), such as cancer, such as NSCLC (non-small cell lung cancer), RCC (renal cell carcinoma), prostate cancer and breast cancer, to a method for inhibiting an adenosine receptor, to a combination of one or more of these compounds and an immunotherapeutic or chemotherapeutic agent.

Formula (I)

EFFECT: production of new triazolo-pyrimidine compounds that specifically act on adenosine receptors, in particular A1 and A2, specifically A2a.

34 cl, 4 tbl, 128 ex

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RU 2 802 866 C2

Authors

Tszen Tsinbej

Tsi Chankhe

Tsuj Khunchun

Yan Chzhenfan

Chzhan Syaolin

Dates

2023-09-05Published

2019-09-12Filed