NOVEL CC-1065 ANALOGUES AND THEIR CONJUGATES Russian patent published in 2015 - IPC C07D403/06 C07D471/04 C07D495/04 A61K31/403 A61P35/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to formula compound or its pharmaceutically acceptable salt, where DB represents DNA-binding group and represents group DB1, R¹ represents halogen; R², R^2', R³, R^3', R⁴, R^4', R¹² and R¹⁹ represent H, X² represents C(R¹⁴)(R^14') and where R^14' and R^7' are absent, which results in double bond between atoms, carrying R^7' and R^14'; R⁵, R⁶ and R⁷ are independently selected from H and R^e, where R^e is selected from C_1-3alkyl; R^5'+R^6' are absent, which results in double bond between atoms, carrying R^5'′ and R^6'; X¹ represents O; X³ is selected from N and NR¹⁵; X⁴ represents CR¹⁶; X⁵ represents O; X⁶ is selected from CR¹¹, CR¹¹(R^11') and N; X⁷ is selected from CR⁸, CR⁸(R^8'), NR⁸ and N; X⁸ is selected from CR⁹, CR⁹(R^9′), NR⁹ and N; X⁹ is selected from CR¹⁰, CR¹⁰(R^10′) and N; X¹¹ represents C; X¹² is selected from C and N; X³⁴ represents C; supposes that said bond can be optionally delocalised, double bond; R⁸ represents H and N(R^h)C(O)Rⁱ; R⁸, R⁹, R^9', R¹⁰, R^10', R¹¹, R^11', R¹⁵, R^16' represent H, R^h represents H; Rⁱ is selected from C₆-C₉aryl and indole, substituted with one or several substituents, selected from OH, NH₂, (CH₂CH₂O)_2-4H and O(CH₂CH₂O)_2-4CH₃; a and b are independently selected from 0 and 1; on condition that ring B in DB1 represents heterocycle. Invention also relates to pharmaceutical composition for treatment or prevention of tumour in mammals, containing therapeutically efficient quantity of formula (I) compound. Formula (I) compound, conjugated with antibody, represents conjugate for treatment or prevention of tumour.

EFFECT: analogues of DNA-alkylating CC-1065 preparation and their analogues.

7 cl, 14 dwg, 1 tbl, 23 ex