Abstract:
NEW MATERIAL:The compound of formula I [R1 and R2 are H, halogen, trihalomethyl or nitro; R3 is lower alkyl or group of formula II (B is 7-16C alkylene); A is C or N]. EXAMPLE:2,6-Demethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarbo xylic acid 3-methyl ester 5-[8-(1-imidarzolyl)octyl] ester. USE:A drug having vasodilating, blood flow increasing, thrombocyte coagulation inhibiting, and thromboxane-A2 formation inhibiting activities, and useful as a vasodilator, hypotensor, an antithrombotic agent, an antiarteriosclerotic agent, etc. The coronary blood flow can be increased and keeps the high level for a long period by the administration of the compound. PREPARATION:The compound of formula I can be prepared e.g. by reacting the compound of formula III (Y is active group) with imidazole or its alkali metal salt in an inert solvent at room temperature -80 deg.C for several -24hr while stirring.
Abstract:
NEW MATERIAL:The compound of formula I (R1 is H, lower alkyl, lower alkoxy, etc.; R2 is H or lower alkyl; R3 is nitroxy, trifluoromethyl or F; R4 and R5 are H, lower alkyl, halogen-substituted benzoyl, etc.; A is single bond, O imino, residue of -CONH-, etc.; B is O or residue of -NHCO-; X1 and X2 are aklylene). EXAMPLE:2-Dimethylamino-2'-methoxy-5'-(2-nitroxyethoxy)-acetanilide. USE:Useful as a drug for the circulatory system, e.g. hypotensor, anti-stenocardia, antiarrhythmic agent, etc. PREPARATION:The objective compound of e.g. formula II is produced by using a substituted aniline or a substituted phenol as a starting substance, and reacting e.g. a substituted aniline with a halogeno-aliphatic carboxylic acid or N-protected amino-apliphatic carboxylic acid and its reactive derivative.
Abstract:
NEW MATERIAL:An α-methylcinnamic acid derivative expressed by formula I (R is H or lower alkyl; n is an integer 0W3) or a salt thereof. EXAMPLE: α-Methyl-p-( 2-pyridylmethyloxy )-cinnamic acid. USE: An antilipemic agent, having the ability to reduce the concentrations of cholesterol and triglycerides in blood, and suitably administered in a dose of 200W500mg/day. PROCESS: A pyridine derivative expressed by formula II (X is halogen) is reacted with a p-hydorxy-α-methylcinnamic acid derivative expressed by formula III in a suitable inert solvent in the presence of an alkali under heating and refluxing for 2W3hr to give the compound expressed by formula I. COPYRIGHT: (C)1982,JPO&Japio