HETEROCYCLIC CONDENSED COMPOUNDS USEFUL AS ANTIDIURETIC AGENTS Russian patent published in 2009 - IPC C07D403/12 C07D487/04 C07D403/14 C07D413/12 C07D405/12 C07D519/00 C07D498/04 C07D417/12 C07D495/04 C07D413/04 C07D409/14 C07D409/12 A61K31/55 A61K31/5513 A61P7/12 

FIELD: chemistry.

SUBSTANCE: invention is related to the compound of general formula 1 or its tautomer or pharmaceutically acceptable salt, where W selected from N and CR⁴; X is selected from CH(R⁸), O, S, N(R⁸), C(=O), C(=O)O, C(=O)N(R⁸), OC(=O), N(R⁸)C(=O), C(R⁸)-CH and C(=R⁸); G¹ - bicyclic or tricyclic condensed derivative of azepin, selected from general formulas 2-9 , or derivative of aniline of common formula 10 , where A¹, A⁴, A⁷ and A¹⁰ are independently selected from CH₂, C=O, O and NR¹⁰; A², A³, A⁹, A¹¹, A¹³, A¹⁴, A¹⁵, A¹⁹ and A²⁰ are independently selected from CH and N; or A⁵ stands for covalent connection, and A⁶ represents S; or A⁵ stands for N=CH, and A⁶ represents covalent connection; A⁸ , A¹² , A¹⁸ and A²¹ are independently selected from CH=CH, NH, NCH₃ and S; A¹⁶ and A¹⁷ both represent CH₂, or one from A¹⁶ and A¹⁷ represents CH₂, and the one another is selected from C=O, CH(OH), CF₂, O, SO_c and NR¹⁰; Y is selected from CH=CH or S; R¹ and R² are independently selected from H, F, Cl, Br, alkyl, CF₃ and group O-alkyl; R³ is selected from H and alkyl; R⁴-R⁷ are independently selected from H, F, Cl, Br, alkyl, CF₃, OH and group O-alkyl; R⁸ is selected from H, (CH₂)_bR⁹ and (C=O)(CH₂)_bR⁹; R⁹ is selected from H, alkyl, possibly substituted aryl, possibly substituted heteroaryl, OH, groups O-alkyl, OC(=O)alkyl, NH₂, NHalkyl, N(alkyl)₂, CHO, CO₂H, CO₂alkyl, CONH₂, CONHalkyl, CON(alkyl)₂ and CN; R¹⁰ is selected from H, alkyl, group COalkyl and (CH₂)_dOH; R¹¹ is selected from alkyl, (CH₂)_dAr, (CH₂)_dOH, (CH₂)_dNH₂, group (CH₂)_aCOOalkyl, (CH₂)_dCOOH and (CH₂)_dOAr; R¹² and R¹³ are independently selected from H, alkyl, F, CI, Br, CH(OCH₃)₂, CHF₂, CF₃, groups COOalkyl, CONHalkyl, (CH₂)_dNHCH₂Ar, CON(alkyl)₂, CHO, COOH, (CH₂)_dOH, (CH₂)_dNH₂, N(alkyl)₂, CONH(CH₂)_dAr and Ar; Ar is selected from possibly substituted heterocycles or possibly substituted phenyl; a is selected from 1, 2 and 3; b is selected from 1, 2, 3 and 4; c is selected from 0, 1 and 2; and d is selected from 0, 1, 2 and 3. Besides, the invention is related to pharmaceutical compound and to method for activation of vasopressin receptors of type 2.

EFFECT: compounds according to invention represent agonists of receptor of vasopressin V₂, which stipulates for their application (another object of invention) for preparation of medicine for treatment of condition selected from polyuria, including polyuria, which is due to central diabetes insipidus, nocturnal enuresis of nocturnal polyurea, for control of enuresis, to postpone bladder emptying and for treatment of disorders related to bleeds.

21 cl, 228 ex