CORTICOTROPIN-RELEASING FACTOR ANTAGONISTS Russian patent published in 2004 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to new compounds of general formulas (I) , (II) and (III) or their pharmaceutically acceptable salts wherein dotted lines mean optional double bonds; A means -CR₇ or nitrogen atom; B means or -C(O)R₂, N-ethyl-2,2,2-trifluoroacetamide; G means oxygen, sulfur atom, NH, NH₃, hydrogen atom, methoxy-, ethoxy-, trifluoromethoxy-group, methyl, ethyl, thiomethoxy-group, NH₂, NHCH₃, N(CH₃)₂ or trifluoromethyl; Y means nitrogen atom; Z means NH, oxygen, sulfur atom, -N-(C₁-C₂-alkyl) or -C(R₁₃R₁₄) wherein R₁₃ and R₁₄ mean independently of one another hydrogen atom, trifluoromethyl or methyl; either one of members R₁₃ and R₁₄ means cyano-group and another means hydrogen atom or methyl; R₁ means C₁-C₆-alkyl that can be optionally substituted with one or two substituents R₈ taken independently of one another among group including hydroxygroup, fluorine, chlorine, bromine, iodine atom, CF₃, C₁-C₄-alkoxy-group, -O-CO-(C₁-C₄-alkyl) wherein -alkyl moieties of above indicated groups R₁ can comprise optionally one carbon-carbon double or triple bond; R₂ means C₁-C₁₂-alkyl, aryl or (C₁-C₄-alkylene)aryl wherein aryl means phenyl, naphthyl; R₃ means methyl, ethyl, fluorine, chlorine, bromine, iodine atom, cyano-, methoxy-group, OCF₃, methylthio-group, methylsulfonyl, CH₂OH or CH₂OCH₃; R₄ means hydrogen atom, C₁-C₄-alkyl, fluorine, chlorine, bromine, iodine atom, C₁-C₄-alkoxy-, trifluoromethoxy-group, -CH₂OCH₃, -CH₂OCH₂CH₃, -CH₂CH₂OCH₃, -CF₃, amino-, nitro-group, -NH-(C₁-C₄-alkyl), -N(CH₃)₂, -NHCOCH₃, -NHCONHCH₃, hydroxy-group, -CO-(C₁-C₄- alkyl), -CHO, COOH, cyano-group or COO-(C₁-C₄-alkyl) wherein C₁-C₄-alkyl can be substituted with one substituent taken among group including hydroxy-, amino-group, NHCOCH₃, -NH-(C₁-C₂-alkyl), -N-(C₁-C₂-alkyl), fluorine, chlorine atom, cyano-, nitro-group; R₅ means phenyl, naphthyl, pyridyl, pyrimidyl wherein each among above indicated groups R₅ is substituted with one-three substituents that are taken independently of one another among fluorine, chlorine atom, C₁-C₆-alkyl or C₁-C₆-alkoxyl or with one substituent taken among group including hydroxy-group, iodine, bromine atom, formyl, cyano-, nitro-group, trifluoromethyl, amino-(C₁-C₆-alkyl)-O-C₁-C₆-alkyl and wherein C₁-C₄-alkyl and C₁-C₄-alkyl moieties of above indicated groups R₅ can be optionally substituted with one hydroxy-group; R₆ means hydrogen atom or C₁-C₆-alkyl; R₇ means hydrogen atom, methyl; R₁₁ means hydrogen atom, hydroxy-group, fluorine atom or methoxy- group; R₁₂ means hydrogen atom or C₁-C₄-alkyl; and R₁₆ and R₁₇ represent independently of one another hydrogen atom, hydroxy-group, methyl, ethyl, methoxy- or ethoxy-group with exception that both members R_16/ and R₁₇ can't mean methoxy- or ethoxy-group simultaneously; either R₁₆ and R₁₇ form in common group oxo (= O); under condition that if G means oxygen, sulfur atom, NH or NCH₃, then it is attached by double bond to five-membered ring of the formula (III) and further under condition that R₆ is absent if nitrogen atom to which it is bound is attached by double bond to adjacent carbon atom in ring. Compounds are antagonists of corticotropin-releasing factor that allows their using as components of pharmaceutical composition. Invention describes method for preparing these compounds. EFFECT: improved preparing method, valuable biological and medicinal properties of compounds. 26 cl, 112 ex