SPIRO-5,6-DIHYDRO-4H-2,3,5,10B-TETRA-AZA-BENZO[E]AZULENES Russian patent published in 2014 - IPC C07D487/10 C07D495/10 C07D491/107 A61K31/438 A61K31/5517 A61P9/00 A61P25/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to spiro-5,6-dihydro-4H-2,3,5,10b-tetra-aza-benzo[e]azulene derivatives of formula I, where X-Y represents C(R^aR^b)-O, where each of R^a and R^b independently represents H or C_1-4-alkyl, C(R^cR^d)-S(O)_p, where each of R^c and R^d independently represents H, C(O)O, CH₂OCH₂, CH₂CH₂O, Z represents CH or N; R¹ represents halogeno, R² represents H, C_1-6-alkyl, non-substituted or having as substituents one OH, -(CH₂)_q-R^e, where R^e represents pyridyl, -C(O)-C_1-6-alkyl, -C(O)(CH₂)_qNRⁱRⁱⁱ, -C(O)O-C_1-6-alkyl, -S(O)₂NRⁱRⁱⁱ, each of Rⁱ and Rⁱⁱ independently represents C_1-6-alkyl, R³ represents Cl or F, n has value 1 or 2, m has value 0, 1, p has value 0 or 2, q has value 1, or to their pharmaceutically acceptable salts. Invention also relates to pharmaceutical composition, possessing antagonistic activity with respect to receptors V1a, on the basis of said compounds.

EFFECT: obtained are novel compounds and pharmaceutical composition on their basis, which can be applied in medicine as drugs of peripheral and central action in case of the following states: dysmenorrhea, male or female sexual disfunction, hypertension, chronic heart failure, inadequate secretion of vasopressin, liver cirrhosis, nephritic syndrome, anxiety, depressive disorders, obsessive-compulsive disorder, autism spectrum disorders, schizophrenia and aggressive behaviour.

20 cl, 10 tbl, 37 ex