BENZYLAMINE DERIVATIVES AS INHIBITORS OF PLASMA KALLIKREIN Russian patent published in 2017 - IPC C07K5/65 C07C237/22 C07C311/06 A61K38/05 A61P27/02 A61P7/00 

FIELD: chemistry.

SUBSTANCE: present invention relates to compounds of formula (I), compositions containing such compounds; use of such compounds in therapy for treating or preventing diseases or conditions, involving plasma kallikrein activity; and methods of treating patients with using said compounds; where R¹ is selected from H, alkyl, -COalkyl, -COaryl, -COheteroaryl, -(CH₂)_aOH, -(CH₂)_bCOOR¹⁰, -(CH₂)_cCONH₂, -SO₂alkyl, -SO₂aryl, -SO₂(CH₂)_hR¹³, -CO(CH₂)_iR¹⁴, -COcycloalkyl, -COCH=CHR¹⁵, -CO(CH₂)_jNHCO(CH₂)kR¹⁶ and -CONR¹⁷R¹⁸; R² is selected from H and alkyl; R³ is selected from alkyl, -(CH₂)_daryl, -(CH₂)_eheteroaryl, (CH₂)_fcycloalkyl, -CH(cycloalkyl)₂ and -(CH₂)_laryl-O-(CH₂)_m-aryl; R⁴ and R⁶ are independently selected from H and alkyl; R⁵ is selected from H and OH; or R⁴ and R⁵, together with atoms to which they are bonded, can be bonded to form a 5- or 6-member azacycloalkyl structure; R⁷ is selected from H and halogen; R⁸ is selected from H, alkyl, halogen and CF₃; R⁹ represents aryl or heteroaryl; R¹⁰ represents H or alkyl; a, b, c, d, e, f, g, h, i, j, l and m independently represent 1, 2 or 3; k is equal to 0, 1, 2 or 3; *1 and *2 denote chiral centres.

EFFECT: novel compounds.

19 cl, 2 dwg, 15 tbl, 201 ex