DERIVATIVES OF BENZIMIDAZOLE AND PHARMACEUTICAL COMPOSITIONS COMPRISING PRODRUG OF PROTON PUMP INHIBITOR Russian patent published in 2004 - IPC

FIELD: organic chemistry, pharmacy.

SUBSTANCE: invention relates to inhibitors of proton pump. Invention describes derivatives of benzimidazole of the formula: Het₁-X-S(O)-Het₂ wherein Het₁ has structure:

X has structure:

Het₂ has structure:

R₁, R₂, R₃ are taken independently among hydrogen atom, alkyl comprising 1-10 carbon atoms, fluoro-substituted alkyl comprising 1-10 carbon atoms, alkoxy-group with 1-10 carbon atoms and fluoro-substituted alkoxy-group with 1-10 carbon atoms; R₆-R₉ are taken among hydrogen atom, alkyl with 1-10 carbon atoms, halogen-substituted alkyl with 1-10 carbon atoms, alkoxy-group with 1-10 carbon atoms and halogen-substituted alkoxy-group with 1-10 carbon atoms; R₁₀ means hydrogen atom, alkyl with 1-10 carbon atoms; R₁₅ has formula:

wherein R₁₇ means alkyl with 1-10 carbon atoms, halogen-substituted alkyl with 1-10 carbon atoms, alkoxy-group with 1-10 carbon atoms, halogen-substituted alkoxy-group with 1-10 carbon atoms, alkylthio-group with 1-10 carbon atoms, halogen-substituted alkylthio-group with 1-10 carbon atoms, alkoxycarbonyl with 1-10 carbon atoms, halogen-substituted alkoxycarbonyl with 1-10 carbon atoms, F, Cl, Br, J, NO₂, CN, OCO-alkyl, NH₂, alkylamino- and dialkylamino-group wherein indicated alkyl groups comprise 1-10 carbon atoms, carbamoyl, N-substituted carbamoyl, alkylcarbonyl with 1-10 carbon atoms. (Alkoxycarbonyl)-alkoxy-groups in each of indicated alkoxy-groups comprise 1-10 carbon atoms, (alkoxycarbonyl)-alkyl groups in each of indicated alkoxy-group or alkyl group comprise 1-10 carbon atoms, (carbamoyl)-alkoxy-group with 1-10 carbon atoms, (N-alkylcarbamoyl)-alkoxy-group with 1-10 carbon atoms, (N,N-dialkylcarbamoyl)-alkoxy-group with 1-10 carbon atoms, (N-substituted or unsubstituted carbamoyl)poly(alkoxy)-group with 1-10 carbon atoms, (N-substituted or unsubstituted carbamoyl)-alkyl with 1-10 carbon atoms, [N-(heteroaryl)carbamoyl]-alkyl with 1-10 carbon atoms, [N-(heteroaryl)carbamoyl]-alkoxy-group with 1-10 carbon atoms, [N-(substituted aryl)carbamoyl]alkoxy-group with 1-10 carbon atoms being poly(alkoxy)-group in each indicated alkoxy-groups comprises 1-10 carbon atoms, cyclic polyalkoxy-group, guanidinyl-group, ureido-group, dialkylamino-poly(alkoxy)-group, [N-(carbamoylalkyl)carbamoyl]-alkoxy-group, [N-(carbamoylalkyl)carbamoyl]-alkyl, [N-[[N-(heteroaryl)carbamoyl]alkyl)carbamoyl]-alkoxy-group, [N-[[N-(substituted heteroaryl)carbamoyl]alkyl]carbamoyl]-alkoxy-group, (sulfonato)-alkyl, (sulfonato)-alkoxy-group, N-[(sulfonato)alkyl]-amido-group, (substituted)maleimido-group, (substituted)succinimido-group, [(trialkyl)ammonium]alkoxy-group; R₂₁ means (aryl)alkyl, (heteroaryl)alkyl, phenyl, naphthyl or heteroaryl comprising 1-3 heteroatoms taken independently among N, O and S wherein indicated phenyl, naphthyl or heteroaryl groups are substituted or unsubstituted 1-5 groups R₁₇; or pharmaceutically acceptable salts of indicated compounds. Invention describes also pharmaceutical compositions based on derivatives of benzimidazole. Invention provides preparing new compounds eliciting valuable biological properties.

EFFECT: valuable properties of compounds.

16 cl, 4 tbl, 67 ex