CYTOSKELETALLY ACTIVE RHO-KINASE INHIBITING COMPOUNDS, COMPOSITIONS AND USE THEREOF Russian patent published in 2012 - IPC C07D401/12 C07D403/12 C07D413/14 A61K31/4709 A61K31/416 A61K31/4523 A61K31/5377 A61P27/02 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula II , where Q is (CR₄R₅)_n3; n₁ equals 1 or 2; n₂ equals 1 or 2; n₃ equals 1; R₂ is R₂-1 or R₂-2 , Ar is phenyl or a heteroaryl ring consisting of 8-10 carbon atoms and 1-2 heteroatoms selected from O or S; X denotes 1-2 substitutes located on Ar, each independently selected from a group consisting of OR₈, NR₈R₉, SR₈, SO₂R₈, SO₂NR₈R₉, NR₈SO₂R₉, CONR₈R₉, NR₈C(=O)R₉, NR₈C(=O)OR₉ and CN; R₃-R₅ denote H; R₈ is H, alkyl, cyclopropyl, phenyl or pyridinyl; optionally substituted with one or more halogens or heteroatom-containing substitutes selected from a group consisting of OR₁₁, NR₁₁R₁₂, CO₂R₁₁, CONR₁₁R₁₂, NR_nC(=O)Ri₂; R₉ is H or alkyl; R₁₁-R₁₂ independently denote H, alkyl, pyridinyl or morpholinyl.

EFFECT: compounds are inhibitors of rho-associated protein kinase which can be used in medicine to prevent or treat diseases or conditions associated with cytoskeleton readjustment, specifically treat high intraocular pressure such as primary open angle glaucoma.

10 cl, 3 tbl, 226 ex