NEW GLP-1 RECEPTOR MODULATORS Russian patent published in 2017 - IPC C07D211/22 C07D233/54 C07D233/60 C07D239/26 C07D239/34 C07D241/08 C07D255/02 C07D263/32 C07D271/06 C07D277/24 C07D285/12 C07D401/04 C07D403/04 C07D409/12 C07D413/04 C07D417/12 C07D495/04 C07D271/107 C07D403/12 C07D413/14 C07D413/10 C07D413/12 C07D243/08 A61K31/505 A61K31/506 A61K31/433 A61K31/4245 A61K31/4709 A61K31/551 A61K38/26 A61K31/454 A61K31/4545 A61P3/10 A61P3/04 

FIELD: pharmacology.

SUBSTANCE: compounds can be used in combination to reduce glucose with exenatide. In the formula IR

or IS

,

A is a heteroaryl selected from imidazole, oxadiazole, thiadiazole, thiazole, oxazole, pyridine, pyrimidine, pyridazine, triazine; B is a heterocyclyl selected from isoxazole, oxazole, pyrimidine, pyrazole, thiazole, thiophenyl, thiadiazole, azepine, optionally fused to another nitrogen-containing 6-membered heterocyclic ring; C is an aryl selected from phenyl and naphthyl, benzyl; Y₁ and Y₂ are absent; Z is -C(O)-; each R₁ is independently H or C_1-4 alkyl; R₂ is -O-R₈, -N(R₁)-SO₂-R₈, -NR₄₁R₄₂, -N(R₁)-(CR_aR_b)_m-COOH, -N(R₁)-(CR_aR_b)_m-CO-N(R₁)-heterocyclyl, -N(R₁)-(CR_aR_b)_m-CO-N(R₁)(R₇) or -N(R₁)-heterocyclyl, wherein R₂ is not -OH or -NH₂, and heterocyclyl is a 5-6 membered heterocyclyl containing 1 to 3 heteroatoms selected from N and S; each R₃ and R₄ is independently halogen, C₁-C₄alkyl, C₁-C₄alkyl substituted with R₃₁, C₁-C₄alkoxy, halogenC₁-C₄alkyl, perhalogenC₁-C₄alkyl, halogenC₁-C₄alkoxy, -OH, -NR₁R₈, -C(O)R₈, -C(O)NR₁R₈, -S(O)₂R₈, -OS(O)₂R₈, -(CR_aR_b)_mNR₁R₈, -(CR_aR_b)_mO(CR_aR_b)_mR₈; or any two R₃ or R₄ groups on the same carbon atom, taken together, form oxo, values of R₃₁, R₄₀, R₄₁, R₄₂ are indicated in the claims; W₁ is absent; each R_a and R_b have values indicated in the claims; R₅ is R₇, -(CH₂)_m-L₂-(CH₂)_m-R₇ or -(-L₃-(CR_aR_b)_r-)_s-L₃-R₇; R₇, R₈ have values indicated in the claims; L2 is independently, from the near to the far end of the structure of the formula I-R or I-S, absent or -O-; each L3 is independently absent, -O- or -N(R₁)-, each m is independently 0, 1, 2, 3, 4, 5 or 6; each n is independently 0, or 1, or 2; P is 0, 1, 2, or 3; Q is 0, 1, 2, or 3.

EFFECT: compounds have activity for glucagon-like peptide 1 and can be used to treat diseases for which modulation or potentiation of GLP-1R is prescribed, particularly for the treatment of diabetes.

8 cl, 2 tbl, 381 ex