BORON-CONTAINING DIACYLHYDRASINES Russian patent published in 2017 - IPC C07F5/02 C07F5/04 A01N55/08 A61K31/69 A61P35/00 

FIELD: pharmacology.

SUBSTANCE: invention relates to a compound that has formula I , or its pharmaceutically acceptable salts, which can be used to modulate the expression of exogenous gene. In formula I, R¹ and R² each is independently selected from the group consisting of hydrogen, C_1-4 alkyl and C_1-4 haloalkyl; R³ is selected from the group consisting of hydrogen, C_1-4 alkyl, C_1-4 haloalkyl and C_6-14 aryl; R⁴ is selected from the group consisting of R⁴-1 , R⁴-2 and R⁴-5 X¹ is selected from the group consisting of -O- and -N(R^8a)-; Y¹ is -(CR^9aR^9b)_m-; Z¹ is selected from the group consisting of -O- and -N(R^8b)-, or Z¹ absent; R^6a is selected from the group consisting of hydroxy, C_1-4 alkyl and C_1-4 alkoxy; or R^6a forms an amino acid adduct; R^7a and R^7b each is independently selected from the group consisting of hydrogen, halogen and C_1-4 alkyl; R^8a and R^8b each is independently selected from the group consisting of hydrogen and C_1-4 alkyl; R^9a and R^9b each is independently selected from the group consisting of hydrogen and C_1-4 alkyl; m is 1, 2, 3 or 4; X² is -O-; Y² is -(CR^9cR^9d)_n-; Z² absent; R^6b is selected from the group consisting of hydroxy, C_1-4 alkyl and C_1-4 alkoxy; or R^6b forms an amino acid adduct; R^7c and R^7d each is independently selected from the group consisting of hydrogen, halogen and C_1-4 alkyl; R^9c and R^9d each is independently selected from the group consisting of hydrogen and C_1-4 alkyl; n is 1, 2, 3 or 4; R^10a is selected from the group consisting of hydrogen and -(CR^11aR^11b)_o-B(R^12a) (R^12b); R^10b, R^10c and R^10d each is independently selected from the group consisting of hydrogen, halogen, hydroxy, C_1-4 alkyl, C_1-4 haloalkyl, C_1-4 alkoxy C_1-4 alkyl, C_1-4 haloalkoxy, C_1-4 hydroxyalkyl and C_1-4 alkoxy; R^11a and R^11b each is independently selected from the group consisting of hydrogen and C_1-4 alkyl; R^12a and R^12b are selected from the group consisting of hydroxy and C_1-4 alkoxy; or R^12a and R^12b together form a joint -O(CR^13aR^13b)_pO-; or -B (R^12a) (R^12b) forms a fluoride adduct; R^13a and R^13b each is independently selected from the group consisting of hydrogen and C_1-4 alkyl; o is 0, 1, 2, 3, 4, or 5; p is 2, 3 or 4; R⁵ is selected from the group consisting of R⁵-3 , R⁵-4 and R⁵-5 ; R^10e is selected from the group consisting of hydrogen and -(CR^11cR^11d)_s-B(R^12c)(R^12d); R^10f, R^10g and R^10h are independently selected from the group consisting of hydrogen, halogen, C_1-4 alkyl, C_1-4 haloalkyl, C_1-4 hydroxyalkyl and C_1-4 alkoxy; R^11c and R^11d each is independently selected from the group consisting of hydrogen and C_1-4 alkyl; R^12c and R^12d are selected from the group consisting of hydroxy and C_1-4 alkoxy; or R^12c and R^12d together form a joint -O(CR^13cR^13d)_tO-; or -B(R^12c)(R^12d) forms a fluoride adduct; R^13c and R^13d each is independently selected from the group consisting of hydrogen and C_1-4 alkyl; s is 0, 1, 2, 3, 4, or 5; t is 2, 3 or 4; R^14a and R^14b each is independently selected from the group consisting of hydrogen, halogen, C_1-4 alkyl, C_1-4 haloalkyl, C_1-4 hydroxyalkyl, C_1-4 alkoxy and -COR¹⁶; R^15a and R^15b each is independently selected from the group consisting of hydrogen, halogen, C_1-4 alkyl, C_1-4 haloalkyl, C_1-4 hydroxyalkyl and C_1-4 alkoxy; R¹⁶ is C_1-4 alkyl. The invention also relates to a pharmaceutical composition, a method for cancer treatment, a method for reduction or prevention of insects spread, and a kit for control of the expression of an exogenous gene using these compounds.

EFFECT: increased efficiency.

24 cl, 3 dwg, 3 tbl, 20 ex