DEAZAPURINES AND USE THEREOF Russian patent published in 2010 - IPC C07D471/04 A61K31/437 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to novel deazapurines of formula (I): and pharmaceutically acceptable salts thereof, where n = 0; R₁ is H, -NH₂, -NHCH₃, -NH-Ac, -OH, F, -OCH₃, -CN, -NH(C=O)OC₂H₅; R₂ is H, -NR_AR_B, -OR_A, C_1-20alkyl, C_1-20halogenalkyl, C_6-10aryl, where R_A and R_B each independently represents H, C_1-20alkyl, where C_6-10aryl can be independently unsubstituted or substituted with one or more substitutes selected from a group consisting of C_1-20alkyl, C_1-20alkoxy and C_1-20thioalkyl; each R₃ independently represents H, halogen, CN, C_1-20alkyl, C_1-20alkoxy, C_1-20thioalkyl, a -G-R_C group, where G is absent or represents CH₂-, -(CH₂)₂-, -CH=CH-CH₂-, -CH-CH-, -OC-, -O- or (C=O) and where R_C is H, -NR_F-R_G , -OR_F, -SR_F, -S(=O)R_F, -S(=O)₂R_F, C_1-20alkyl, C_1-20alkenyl, C_1-20alkynyl, C_3-10cycloalkyl, C_3-10cycloalkenyl, tert-butyl dimethyl silyloxy, heterocycle, C_6-10aryl, C_5-14heteroaryl with one N atom as a heteroatom, where R_F and R_G each independently represents H, C_1-20alkyl, C_1-20alkenyl, C_1-20alkynyl, C_3-10cycloalkyl, C_3-10cycloalkenyl, C_6-10aryl, 6-member heterocycle with one O atom as a heteroatom, where R_F and R_G together form a 3-, 4-, 5-, 6-, 7- or 8-member cycloalkyl, cycloalkenyl, where the said heterocycle relates to a non-aromatic 5-, 6-, 7-member ring or bi- or tri-cyclic group containing condensed 6-member rings with 1-2 heteroatoms independently selected from O, S, N; where each of the said alkyl, alkenyl, cycloalkyl, cycloalkenyl, heterocycle, heteroaryl can be independently unsubstituted or substituted with one or more substitutes selected from a group consisting of O, halogen, OH, -CN, C_1-20halogenalkyl, -CH₂CF₃, C_1-20alkyl, C_1-20alkoxy, C_3-6cycloalkyl, C_6-10aryl, 5- or 6-member heterocycle with one or two N atoms as heteroatoms, NHR_h, NR_hR_i, N-OR_h, OR_h, C(=O)R_h, S(=O)R_h, S(=O)₂R_h, =CR₄R₅, =NR₄, where R_h and R_j present C_1-20alkyl, C_6-10aryl, and each of R₄, R₅ independently represents H, OH, OR_x or C_1-6alkyl, where R_x is C_1-6alkyl, where the said aryl can be independently further unsubstituted or substituted with one or more substitutes selected from a group consisting of halogen, C_1-20alkyl or C_1-20alkoxy.

EFFECT: compounds can inhibit cytokine induced expression of adhesion molecules with endothelial cells, which enables their use in pharmaceutical compositions.

54 cl