ARYLALANINE DERIVATIVES AS AGONISTS OF β ADRENERGIC RECEPTOR Russian patent published in 2009 - IPC C07D215/227 C07D401/12 C07D295/92 C07C215/60 C07C233/43 A61K31/4704 A61K31/4709 A61K31/5377 A61K31/496 A61K31/167 A61P11/00 A61P11/06 

FIELD: pharmacology.

SUBSTANCE: invention concerns novel compounds of formula (I): , where each of R¹, R², R³ and R⁴ is independently selected out of hydrogen, hydroxy, and -NHCHO, or R¹ and R² together are selected out of -NHC(=O)CH=CH- and -CH=CHC(=O)NH-; R¹ can also be -CH₂OH; one of R⁵ and R⁶ is -[X-C_1-6alkylenyl]_n-NR¹⁰R¹¹ or C_1-6alkylenyl-NR¹²R¹³, and the other of R⁵ and R⁶ is selected out of hydrogen, C_1-4alkoxy and C_1-4alkyl, where C_1-4alkylis optionally substituted by halogen, where each X is -O-; each of R¹⁰, R¹¹, R¹² and R¹³ is independently hydrogen or C_1-4alkyl; or R¹⁰ and R¹¹ together with nitrogen atom linking them, or R¹⁰ together with nitrogen atom linking it and carbon atom from neighbour C_1-6alkylenyl form heterocyclic or heteroaryl ring with 5 to 7 atoms in ring and optionally with additional heteroatom selected out of oxygen and nitrogen, where nitrogen atom is optionally substituted by -S(O)₂-C_1-4alkyl; and n is 1 or 2; and each of R⁷, R⁸ and R⁹ is independently hydrogen; and pharmaceutically acceptable salt or solvate or stereoisomer of claimed compounds. Also invention claims application and pharmaceutical composition based on the compounds and having agonistic effect on β₂ adrenergetic receptor.

EFFECT: obtaining novel compounds for application in therapy of asthma or chronic obstructive lung disease.

25 cl, 1 tbl, 6 dwg, 17 ex