ARYLCYCLOHEXYL ESTERS OF DIHYDROTETRAAZABENZOAZULENES FOR USE AS VASOPRESSIN V1A RECEPTOR ANTAGONISTS Russian patent published in 2014 - IPC C07D487/04 A61K31/5517 A61P5/24 

FIELD: chemistry.

SUBSTANCE: described are novel arylcyclohexyl esters of 5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulene derivatives of formula I where R¹ is phenyl, optionally substituted with cyano, C_1-7-alkyl, halogen-C_1-7-alkyl, C_1-7-alkoxy or halogen; naphthyl, pyrazinyl or pyridazinyl; pyridinyl, optionally substituted with halogen or C_1-7-alkyl, pyrimidinyl, optionally substituted with C_1-7-alkyl, R² is H, C_1-8-alkyl, optionally substituted with OH or halogen, -(CH₂)_q-R^a, where R^a is a 6-member heteroaryl containing one N as a heteroatom, -C(O)-C_1-8-alkyl, -C(O)(CH₂)_qNRⁱRⁱⁱ, -C(O)O-C_1-8-alkyl, -S(O)₂-C_1-8alkyl, -S(O)₂NRⁱRⁱⁱ, where Rⁱ and Rⁱⁱ are identical and denote C_1-8-alkyl; q =1, R³ is Cl or F, pharmaceutically acceptable salts thereof and a pharmaceutical composition containing said compounds.

EFFECT: present compounds are V1a receptor antagonists and can be used in medicine.

21 cl, 111 ex, 10 tbl