发明名称 CORTICOTROPIN-RELEASING FACTOR ANTAGONISTS
摘要 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 R16/ 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
申请公布号 RU2221799(C2) 申请公布日期 2004.01.20
申请号 RU19970100192 申请日期 1995.06.06
申请人 发明人 CHEN JUKHPING L.
分类号 C07D213/89;A61K31/00;A61K31/435;A61K31/4353;A61K31/437;A61K31/44;A61K31/4418;A61K31/4427;A61K31/443;A61K31/505;A61K31/52;A61K31/522;A61P1/00;A61P1/12;A61P1/14;A61P3/00;A61P3/04;A61P3/08;A61P3/10;A61P5/38;A61P11/00;A61P11/06;A61P17/00;A61P25/00;A61P25/04;A61P25/08;A61P25/16;A61P25/18;A61P25/20;A61P25/24;A61P25/26;A61P25/28;A61P29/00;A61P31/00;A61P31/12;A61P35/00;A61P37/00;A61P37/08;A61P39/00;A61P39/02;C07D213/69;C07D213/71;C07D213/74;C07D213/80;C07D239/26;C07D239/34;C07D239/38;C07D239/42;C07D239/48;C07D239/50;C07D239/52;C07D401/04;C07D401/12;C07D405/12;C07D471/04;C07D473/22;C07D473/28;C07D473/32;C07D473/34;C07D473/40;C07D487/04 主分类号 C07D213/89
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