DERIVATIVES OF 4-MERCAPTOPYRROLIDINE AS INHIBITORS OF FARNESYLTRANSFERASE Russian patent published in 2002 - IPC

FIELD: organic chemistry, biochemistry. SUBSTANCE: invention relates to derivatives of 4-mercaptopyrrolidines of formula of the following classes (i), (ii) and (iii) presented by the following formula: class (i) (formula III) where X¹ means H, C_1-6-alkoxy-C_1-6-alkyl, C_1-6-alkoxy-C_1-6-alkylcarbonyl; A means phenyl, naphthyl; X² means H, phenyl, phenyl-C_1-6-alkyl; X³ means H, C_1-6-alkyl; X⁴ means C_1-6-alkylsulfanyl, carbamoyl; class (ii) (formula IV) where X⁵ means +C(O)-C_1-4-alkyl-Ph, -C(O)-C_1-6- -alkyl, -C(O)-C_1-4-alkylpyridyl and Ph and pyridyl are substituted optionally with C_1-4-alkyl, C_1-4-alkoxy-group, C_1-4-alkoxy-C_1-4-alkyl; A means naphthyl; R³ is taken among group including H, OH, NO₂;-(CH₂)_nCOOR⁸ where n = 0-3 and R⁸ means H, C_1-4-alkyl, C_2-4/ -alkenyl, -CON-R⁹R¹⁰ where R⁹ and R¹⁰ mean independently H, C_1-4-alkyl, C_2-4-alkenyl, -CON-(R¹¹)OR¹² where R¹¹ and R¹² mean independently H, C_1-4-alkyl and C_2-4-alkenyl, group of the formula II: -CONR¹³-CHR¹⁴-COOR¹⁷ where R¹³ means H or C_1-4-alkyl; R¹⁷ means H or C_1-6-alkyl; R¹⁴ means carbamoyl-C_1-4-alkyl; p = 0-3 being values R³ can be similar or different; class (iii) (formula V) where X⁶ means any value determined above for X⁵ in (ii); X⁷ means Ph optionally substituted with substitute (substitutes) taken among group including C_1-4-alkoxy-group; A means Ph or naphthyl; R³ and p mean values determined above; or its N-oxide, solvate, ester, pharmaceutically acceptable salt. EFFECT: valuable biochemical properties of compounds. 6 cl, 47 sch