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INDOLINE DERIVATIVE AND 5-HT3 RECEPTOR ANTAGONIST CONTAINING THE SAME AS ACTIVE INGREDIENT
INDOLINE DERIVATIVE AND 5-HT3 RECEPTOR ANTAGONIST CONTAINING THE SAME AS ACTIVE INGREDIENT
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机译:包含相同活性成分的吲哚衍生物和5-HT3受体拮抗剂
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摘要
An indoline derivative represented by general formula (I); a physiologically acceptable salt thereof; solvates of these compounds; and a 5-HT3 receptor antagonist containing the same as the active ingredient. In said formula, R1 represents the group (a) ou (b); R2 represents optionally substituted phenyl or heteroaryl; and R3 represents hydrogen, halogen, lower alkyl, hydroxy, lower alkoxy, carbamoyl or lower alkoxycarbonyl. The derivative has a potent antagonism against 5-HT¿3? receptors in the intestinal tract as compared with the known 5-HT3 receptor antagonists and is excellent in the persistence of the activity. Hence it is useful for preventing or treating vomiting or nausea induced by chemotherapy or radiation, irritable bowel syndrom and diarrhea.
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机译:通式(I)表示的二氢吲哚衍生物;其生理上可接受的盐;这些化合物的溶剂化物;和含有5-HT3受体拮抗剂作为有效成分的5-HT3受体拮抗剂。在上述式中,R 1表示基团(a)或ou(b); R 2表示任选取代的苯基或杂芳基; R 3代表氢,卤素,低级烷基,羟基,低级烷氧基,氨基甲酰基或低级烷氧羰基。该衍生物对5-HT?3具有强烈的拮抗作用?与已知的5-HT 3受体拮抗剂相比,其在肠道中的受体是有效的,并且在活性持久性方面是极好的。因此,它对于预防或治疗由化学疗法或放射线引起的呕吐或恶心,肠易激综合征和腹泻是有用的。
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