CONDENSED AZEPINE DERIVATIVES AS ANTIDIUTETIC AGENTS Russian patent published in 2006 - IPC C07D223/16 C07D243/12 C07D281/10 C07D401/06 C07D403/12 C07D471/04 C07D487/04 C07D495/04 C07D498/04 A61K31/55 A61P13/00 

FIELD: biochemistry, medicine, in particular new bioactive compounds having peptide hormone vasopressin agonistic activity.

SUBSTANCE: disclosed are compounds of general formula 1 or 2 or tautomers, or pharmaceutically acceptable salts thereof, wherein W represents N or C-R⁴; R¹-R⁴ are independently H, F, Cl, Br, alkyl, O-alkyl, NH₂, NH-alkyl, N(alkyl)₂, NO₂ or R² and R³ together may form -CH=CH-CH=CH-; G¹ represents bicyclic or tricyclic condensed azepine derivatives selected from general formulae 3-8 wherein A¹, A⁴, A⁷, and A¹⁰ are independently CH₃, O, and NR⁵; A², A³, A⁹, A¹¹, A¹², A¹⁴, and A¹⁵ are independently CH and N; or A⁵ represents covalent bond and A⁶ represents S; or A⁵ represents N=CN and A⁶ represents covalent bond; A⁸ and A¹² are independently NH, N-CH₃ and S; A¹⁶ and A¹⁷ both represent CH₂ or one of A¹⁶ and A¹⁷ represents CH₂ and the other represents CH(OH), CF₂, O, SO_a, and NR⁵; R⁵ represents H, alkyl, CO-alkyl, and (CH₂)_bR⁶; R⁶ represents phenyl, pyridyl, OH, CO₂H; a = 0-2; b = 1-4; Y represents CH or N; Z represents CH=CH or S; and G² represents group selected from groups of formulae 9-11 wherein Ar represents phenyl, pyridyl, naphthyl, and mono- or polysubstituted phenyl, pyridyl, wherein substituents are selected from F, Cl, Br, alkyl, NO₂; D represents covalent bond or NH; E¹ and E² both are H, OMe, F, or one of E¹ and E² represents OH, O-alkyl, OBn, OPh, OAc, F, Cl, Br, N₂, NH₂, NHBn or NHAc and the other represents H; or E¹ and E² together form =O, -O(CH₂)_gO- or -S(CN₂)_gS-; F¹ and F² both represent H or together form =O or =R; L represents OH, O-alkyl, NH₂, NH-alkyl, and NR⁹R¹⁰; R⁷ represents COR⁸; R⁸ represents OH, O-alkyl, NH₂, NH-alkyl, N(alkyl)₂, pyrolidinyl, and piperidinyl; R⁹ and R¹⁰ both are alkyl or together form -(CH₂)_h-; V represents O, N-CN or S; c = 0 or 1; d = 0 or 1, e = 0 or 1; f = 0-4; g = 2 or 3; h = 3-5, with the proviso, that both d and e are not 0. Also disclosed are pharmaceutical composition having agonistic activity in relate to V₂ receptor, method for treatment one or more diseases (e.g., enuresis, nycturia, diabetes insipidus, hemorrhage disorders, urinary incontinence.

EFFECT: new compounds with value biological characteristics.

41 cl, 19 tbl, 193 ex