IMMUNOMODULATORY AZALIDES BASED ON UREA Russian patent published in 2024 - IPC C07H17/08 A61K31/7048 A61K31/351 A61P11/00 A61P29/00 A61P37/02 

Abstract RU 2811591 C1

FIELD: chemistry and pharmaceuticals.

SUBSTANCE: immunomodulatory compounds of formula (1), its stereoisomers and its pharmaceutically acceptable salts and a method for treating or preventing an inflammatory response using them. In the general formula (1), W represents H or formula (A), where X represents -Ra, -RcNR5R6, -RcOR7, -RcSR7, -RcN3, -RcCN or -RcX'; X' is F, Cl, I or Br; R represents H; each of Ra, Rb, R0 and R1 independently represents H or C1-C6 alkyl; or R1 represents benzyl, optionally substituted with methoxy; or R1 represents -CH2Het, where Het represents a 5-6 membered heteroaryl ring containing at least one heteroatom selected from N, S and O; and wherein the heteroaryl ring is optionally substituted with at least one R9 substituent; each of R2 and R3 independently represents H, C1-C6 alkyl, RcNRaRb, C0-C3 alkyl, С3-C6 cycloalkyl, C0-C3 alkylaryl, C0-C3 alkyl heterocycle, where the heterocycle is a 5-6 membered saturated heterocyclic ring; or C0-C3 alkylheteroaryl, where heteroaryl represents a 5-6 membered heteroaryl ring; wherein each of the heterocyclic ring and the heteroaryl ring contains at least one heteroatom selected from N and O; and wherein each of the cycloalkyl, aryl, heterocyclic and heteroaryl rings is optionally substituted with at least one R9 substituent; or R2 and R3 together with the nitrogen atom to which they are attached form ring A, a 4-8 membered heterocyclic ring optionally containing at least one additional heteroatom selected from N, O and S; each ring is optionally substituted with at least one R10 substituent; and wherein each ring is optionally fused with Y. The remaining meanings of the radicals are indicated in the claims.

EFFECT: immunomodulary compounds are proposed.

14 cl, 10 dwg, 11 tbl

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RU 2 811 591 C1

Authors

Cox Mark R.

Stuk Timothy L.

Maddux Todd M.

Ewin Richard Andrew

Johnson Paul D.

Respondek Tomasz

Kyne Graham M.

Vairagoundar, Rajendran

Dates

2024-01-15Published

2021-03-11Filed