NEW CC-1065 ANALOGS AND THEIR CONJUGATES Russian patent published in 2017 - IPC C07D403/06 C07D417/06 A61K31/427 A61K31/403 A61K31/4192 A61P35/00 

FIELD: pharmacology.

SUBSTANCE: invention relates to a compound of formula

or a pharmaceutically acceptable salt thereof, wherein DB is a DNA-binding group and is DB6 group

;

R¹ is chlorine; R², R²', R³, R³', R⁴, R⁴', R¹² and R¹⁹are H; X² is selected from C(R¹⁴)(R¹⁴'), where R¹⁴' has the same value as defined for R⁷' and is independently selected, and R¹⁴' and R⁷' are absent, which gives a double bond between the atoms carrying R⁷' and R¹⁴'; R⁵, R⁶ and R⁷ are independently selected from H, R, where R^e are selected from C₁Alkyl, and R⁵'+R⁶', are absent, which gives a double bond between the atoms carrying R⁵ and R⁶, and/or R⁶ and R⁷, and/or R⁷ and R¹⁴ respectively; X¹ is selected from O; X³ is selected from S, N, and NR¹⁵; X⁴ is selected from N and CR¹⁶; X⁵ is selected from O; X^6* is selected from CR¹¹; X⁷ is selected from CR⁸, N; X⁸ is selected from CR⁹, N; X^9* is selected from CR¹⁰; X^10* is selected from CR²⁰; X^11* is selected from C; X^7* and X^8* have the same values as those defined for X⁷ and X⁸ respectively, and are chosen independently; X³⁴ is selected from C; annular atom B in X^11* in DB⁶ is connected to the ring atom of ring A, so that ring A and ring B in DB⁶ are directly connected through a direct link; fig. implies that the said bond can be a or a non-cumulated direct bond, optionally delocalized, double bond; R^8, R⁹, R¹⁰, R¹¹, R¹⁵, R¹⁶, R²⁰ are each independently selected from H, N(R^h)C(O)Rⁱ, where R^h, Rⁱ are independently selected from H and optionally substituted C6 aryl, one optional substituent in Rⁱ is -OH or -NH₂; a is 0 and b is 1. The invention relates to a pharmaceutical composition for tumour treatment or prevention for a mammal, comprising a therapeutically effective amount of formula (I) compound and a pharmaceutically acceptable carrier.

EFFECT: DNA-alkylating agent SS-1065 analogues.

6 cl, 13 dwg, 1 tbl, 23 ex