| 摘要 |
PROBLEM TO BE SOLVED: To obtain a new compound capable of treating gastrointestinal injuries, irritable intestinal symptoms, diarrhea, urge incontinence, and pains and useful as aδ-opioid agonist. SOLUTION: A compound of formula I [A is N or C-X (X is H or a 1-4C alkyl); G is C-Y (Y is H or a 1-4C alkyl); B and L are each a (substituted) 1-6C hydrocarbyl; D is H, a 1-10C hydrocarbyl or the like; E is hydroxy, a 1-4C alkoxy or the like; F is the combination of phenyl with a heterocyclic group], for example, a compound of formula II. The compound of formula I is obtained by reacting a compound of formula III (Lg is Cl, Br or the like) with a compound of formula IV in the presence of a base such as potassium carbonate in an organic solvent (for example, dry toluene) at room temperature to the refluxing temperature of the reaction solution. The compound of formula I is compounded with a binder, a lubricant, a suspending agent, etc., and subsequently administered preferably at a dose of 0.1-20 mg/kg. The compound of formula I may intravenously be injected at a dose of 0.001-10 mg/kg/hr.
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