SUBSTITUTED ARYLPIPERIDINYLALKYNYL ADENOSINES AS AR AGONISTS Russian patent published in 2012 - IPC C07H19/16 A61K31/7076 

FIELD: chemistry.

SUBSTANCE: invention refers to A_2A receptor agonists that are represented by the formula (I) compound or its pharmaceutically acceptable salt where R¹ and R² are independently represented by H; each R is independently chosen from the group consisting of H, C₁-C₄alkyl, cyclopropyl, cyclobutyl and (CH₂)_acyclopropyl; X is represented by N; Y is chosen from the group consisting of O, NR¹, -(OCH₂CH₂O)_mCH₂- and -(NR¹CH₂CH₂O)_mCH₂- under the condition that when Y is represented by O or NR¹, then there is at least one substitute in Z; Z is represented by 6-membered aryl where Z is substituted by 0-4 groups independently chosen from the group consisting of F, Cl, Br, I, (C₁-C₄)alkyl, -(CH₂)_aOR³, -(CH₂)_aNR³R³, -NHOH, nitro, -(CH₂)_aCN, -(CH₂)_aCO₂R³, -(CH₂)_aCONR³R³, trifluoromethyl and trifluoromethoxy; R³ is independently chosen from the group consisting of H, (C₁-C₆)alkyl and cycloalkyl; R⁴ is chosen from the group consisting of CH₂OR, C(O)NRR and CO₂R; R⁵ is chosen from the group consisting of CH₂CH₂, CH=CH and C≡C; a is chosen from 0, 1 and 2; m is chosen from 1, 2 and 3; n denotes 1; each p independently denotes 1; and q is chosen from 0 and 1. The invention also refers to the pharmaceutical composition that is agonistic towards adenosine A_2A receptors and contains the above mentioned compound, and the invention refers to application of the above mentioned compound in production of a drug for treatment of the disease connected with A_2A receptors.

EFFECT: application of the compound in production of a drug for treatment of the disease connected with A_2A receptors.

12 cl, 1 tbl, 57 ex