DERIVATIVES OF 4-(2-AMINO-1-HYDROXIETHYL)PHENOL AS β2-ADRENERGIC RECEPTOR ANTAGONISTS Russian patent published in 2012 - IPC C07D215/22 C07C217/60 A61K31/435 A61K31/137 A61P9/00 A61P11/06 A61P29/00 A61P27/06 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to a compound of formula I where: R¹ represents a group selected from among -CH₂OH, -NH(CO)H while R² represents a hydrogen atom or R¹, together with R², forms group -NH-C(O)-CH=CH- where the nitrogen atom is bonded to the carbon atom in the phenyl ring whereto R¹ is bonded, the carbon atom bonded to the carbon atom in the phenyl ring whereto R² is bonded; R^3a and R^3b are independently selected from the group consisting of hydrogen atoms and C_1-4alkyl groups; X and Y are independently selected from the group consisting of an ordinary bond and an oxygen atom; n, m and q (each) independently have a value selected from among 0, 1, 2 and 3; p has a value selected from among 1, 2 and 3; R⁴ and R⁵ are independently selected from the group consisting of hydrogen atoms, a halogen atoms, C_1-4alcoxy, -CONH₂, -NHCONH₂, -SR⁷, -SO₂R⁷ where R⁷ represents C_3-4cycloalkyl; R⁶ is selected from the group consisting of hydrogen atoms, a halogen atoms, C_1-4 alkyl and C_1-4alcoxy or its pharmaceutically acceptable salt or a stereoisomer thereof. Additionally, the invention relates to a pharmaceutical composition based on the compound with formula I and to a method for β2-adrenergic receptor activity modulation.

EFFECT: produced are new 4-(2-amino-1-hydroxiethyl) phenol derivatives possessing the activity of β2-adrenergic receptor antagonists.

22 cl, 32 ex