Abstract:
A quinoline derivative represented by general formula (1), a medicinally acceptable salt thereof, and a remedy for cardiac diseases containing the same, wherein ring A represents a furan, dihydrofuran or dioxolane ring, R1 represents hydroxy, carboxy, alkoxycarbonyl, etc., R2s may be the same or different from each other and each represents hydrogen, alkyl, etc., R?3 and R4¿ may be the same or different from each other and each represents hydrogen, halogen, alkyl, amino, alkoxy, etc., R?5, R6, R7 and R8¿ may be the same or different from one another and each represents hydrogen or alkyl, m represents an integer of 0 to 3, and symbol ...... means that there may be a double bond formed by R?6 and R8¿. The compound (1) has a positively inotropic effect on myocardia and an antiarrhythmic effect and can dilate blood vessels without extremely increasing the heart rate. Therefore, a remedy for cardiac diseases containing the same as the active ingredient is remarkably useful for treating cardiac insufficiency, arrhythmia, and so forth.
Abstract:
PURPOSE:To produce a substituted phenylpyridine in a short process. CONSTITUTION:A halopyridine is reacted with 4-bromo-3-nitrophenetole in the presence of copper by using tetrakis(triphenylphosphine)palladium or palladium chloride catalyst in DMF or DMSO.
Abstract:
PURPOSE:To obtain a new compound useful as a therapeutic agent for heart diseases, having anti-arrhythmic action, cardiac action and vasodilating action. CONSTITUTION:A compound of formula [A is 0 or single bond; when A is 0, B is single bond or methylene and when S is single bond, B is 0; R and R are H or lower alkyl; R is (substituted) lower alkyl, lower alkanoyloxy, hydroxyl group, etc.; broken line may contain double bond] such as 2- hydroxymethyl-9-methyl-2,3,1,8-tetrahydrofuro[3,2-g]quinolin-7-one. The compound of formula I, for example, is obtained by reacting a compound of formula II (R is lower alkanoyl) with an alkali halide such as sodium iodide.
Abstract:
NEW MATERIAL:A compound of formula I [R1-R6 are each H, halogen, OH, lower alkyl, lower alkoxy, amino, etc.; R7 and R8 are either each lower alkyl or form 1-4C alkylene through mutual linkage; A and A' are each single bond, -O-, -NH-, -NHCO-, SO2NH-, etc., (- is bond to either to Y or Y'); Y and Y' are each lower alkylene or lower alkenylene] or its acid-added salt. EXAMPLE:N,N'-bis-[4-(3,4,5-trimethoxyphenyl)buthyl]homopiperazine dihydrochloride. USE:Medicines. An active ingredient for brain protectives. Having excellent brain protective effect, low toxic, highly safe and giving great efficacy through oral administration, thus useful for the improvement or promotion inhibition of e.g. brain dysfunction involved in cerebral hemorrhage, subarachnoid hemorrhage, etc. PREPARATION:For example, a compound of formula II (X is halogen, methyloxy, etc.) is reacted with a second compound of formula III to obtain the objective compound of the formula I where Y'=Y and A'=A.