| 摘要 |
Imidazo[1,2-a]pyridine derivatives and their salts are new. Imidazopyridine derivatives of formula (I) are new: [Image] R1>H, 1-6C alkyl, 1-6C alkenyl, CH2OH, halogen or thiocyano; R2>1-6C alkyl, hydroxyalkyl, 1-6C alkoxy 1-6C alkyl, hydroxy 1-6C alkoxy 1-6C alkyl, 1-6C alkylthio 1-6C alkyl, cyano 1-6C alkyl, halogenated 1-6C alkyl, or aminocarbonyl 1-6C alkyl; R3>H, 1-6C alkoxy, 1-6C alkyl, halogen, hydroxy 1-6C alkyl, hydroxy 1-6C alkoxy, 1-6C alkoxy 1-6C alkyl, 1-6C alkoxy 1-6C alkoxy, 1-6C alkoxycarbonyl, 1-6C alkanoyl, halogenated 1-6C alkyl, NO2, CN, 1-6C sulfonyl, 1-6C sulfinyl, 1-6C alkylthio, 1-6C alkylaminosulfonyl, (1-6C alkyl)2 aminosulfonyl, aminosulfonyl, 1-6C alkylsulfonylamino, (1-6C alkylsulfonyl)2 amino, trifluoromethylsulfonylamino, 1-6C alkylcarbonylamino, 1-6C alkoxycarbonylamino or 1-6C aminocarbonylamino optionally substituted by 1 or 2 1-6C alkyl; R4>H, 1-6C alkyl, halogenated 1-6C alkyl, 1-6C alkoxy or halogen; Ar : R5>, R6> and/or R7> substituted phenyl, thienyl, furanyl, naphthyl or pyridyl; X : a group of formulae (i)-(vi); or R5>H, 1-6C alkyl, 1-6C alkoxy, OH, hydroxy 1-6 alkyl, hydroxy 1-6C alkoxy, halogenated 1-6C alkyl, halogenated 1-6C alkoxy, 1-6C alkoxy 1-6C alkyl, halogen, hydroxy 1-6C alkoxy 1-6C alkyl, CN, 1-6C alkoxycarbonyl, 1-6C alkoxycarbonyloxy, 1-6C alkylsulfonyloxy, trifluoromethylsulfonyloxy, 1-6C acyloxy 1-6C alkyl, 1-6C alkylsulfonyl 1-6C alkyl, 1-6C alkylsulfinyl 1-6C alkyl, 1-6C alkylthio 1-6C alkyl, 1-6C alkoxycarbonylamino 1-6C alkyl, aryl, amino 1-6C alkyl, NHC=OR1>2>, H or 1-4C alkyl substituted oxazolidin-2-one, H or 1-4C alkyl substituted pyrrolidin-2-one or 1-6C alkyl sulfonyl amino; R6>H, 1-6C alkyl, halogen, hydroxy 1-6C alkyl, halogenated 1-6C alkyl, halogenated 1-6C alkoxy, 1-6C alkoxy 1-6C alkyl or CN; R7>H, 1-6C alkyl, 1-6C alkoxy, halogen, NO2, halogenated 1-6C alkyl, halogenated 1-6C alkoxy, aryloxy or CN; R8>H or 1-6C alkyl; R1>2>1-6C alkoxy, 1-6C alkoxy 2-4C alkoxy, NH2, hydroxy 2-4C alkoxy, 1-6C alkyl carbonyloxy 2-4C alkoxy, halogenated 2-4C alkoxy, halogenated 1-4C alkyl, hydroxy 1-4C alkyl, 1-6C alkyl carbonyloxy 1-4C alkyl, aryl, aryl 1-4C alkyl, 1-4C sulfanyl 2-4C alkoxy, 1-4C sulfinyl 2-4C alkoxy, 1-4C sulfonyl 2-4C alkoxy; R5> and R6>are in the ortho positions relative to X; R7>is in the meta or para position relative to X; and R5>+R8>hydroxy- or alkoxy- substituted 5-6 membered ring provided that one of R3> and R4> is not H or halogen; provided that at least one of R5>, R6> and R7> is not H; provided that when R5> = NHC=OR1>2>, H or 1-4C alkyl substituted , H or 1-4C alkyl substituted or 1-6C alkyl sulfonyl amino then one of R3> and R4> is not H; provided that when R1> = H then R7> is not H; provided that when R2> = CH2OH or CH2CN then one of R5> and R6> is not H. [Image] ACTIVITY : None given. MECHANISM OF ACTION : Gastric acid secretion inhibitor. |
