CAMPOTECIN COMPOUNDS, METHODS OF PREPARATION THEREOF, INTERMEDIATES, AND THERAPEUTIC COMPOSITIONS Russian patent published in 2001 - IPC

FIELD: pharmaceutical chemistry. SUBSTANCE: invention provides novel campotecin compounds with general formulas I or II: (I), (II) in racemic form, in enantiomeric form, or in any combination of these forms, where R₁ denotes lower alkyl, lower haloalkyl, or lower alkoxy-lower alkyl; R₂,R₃,R₄ independently denote hydrogen, halogen, lower haloalkyl, lower alkyl, (CH₂)_mNR₆R₇, (CH₂)_mOR₆, optionally lower alkyl-substituted (CH₂)_n[N=X]; R₂ and R₃ can also form together methylenoxy or ethylenoxy group; R₅ denotes hydrogen, halogen, lower alkyl, lower alkoxy, (CH₂)_mNR₆R₇, or optionally lower alkyl-substituted (CH₂)_n[N=X]; R₆ and R₇ independently denote hydrogen, lower alkyl, aryl-lower alkyl, or halogen-lower alkyl; R₉ lower alkyl or arylalkyl; R₁₆ halogen or OR₂₁; R₁₇ denotes OR₆; R₁₈ and R₁₉ independently denote hydrogen, halogen, lower alkyl, lower alkoxy, or hydroxy; R₂₀ denotes hydrogen or halogen; R₂₁ hydrogen, lower alkyl, or CHO; m is integer from 0 to 6; n = 1 or 2; and [N=X] denotes optionally substituted 4-7-membered heterocyclic group, wherein X is selected from group including O, S,.CH₂, CH, NH, and NR₉; or pharmaceutically acceptable salts thereof. Preparation methods, intermediates, and pharmaceutical compositions are also described. Novel compounds are useful as inhibitors of topoisomerase and as antitumor agents. EFFECT: extended assortment of therapeutic preparations. 25 cl, 2 tbl, 42 ex