RESIQUIMOD DERIVATIVES Russian patent published in 2023 - IPC C07D471/04 A61K31/4738 A61K31/4745 A61P31/00 A61P35/00 

Abstract RU 2808163 C2

FIELD: pharmaceutics.

SUBSTANCE: novel deuterated resiquimod derivatives characterized by structural formula I, or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are each independently selected from -CH3 and -CD3; Y1a, Y1b, Y2a, Y2b, Y3a, Y3b, Y4a, Y4b, Y4c and Y4d are each independently selected from hydrogen and deuterium; wherein each position designated as containing deuterium has at least 50.1% inclusion of deuterium at that position; and at least R1 or both R2 and R3 are CD3. The present invention also relates to a pharmaceutical composition containing an effective amount of the claimed compound of formula (I), and the use of compounds of Formula (I) for the treatment of a disease, the treatment of which is favored by agonism of Toll-like receptor 7 or Toll-like receptor 8, and the specified disease is selected from cancer, autoimmune disease and infectious disease.

EFFECT: agonism of TLR7/TLR8 and the manifestation of beneficial effects, such as improved pharmacokinetic properties provided by the compound of Formula I.

34 cl, 10 dwg, 2 tbl, 7 ex

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RU 2 808 163 C2

Authors

Yan, Likhu

Dates

2023-11-24Published

2018-05-18Filed