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2. 发明申请

WO1997025986A1 INTIMAL THICKENING INHIBITORS 审中-公开
标题翻译：最终增稠抑制剂
公开(公告)号：WO1997025986A1
公开(公告)日：1997-07-24
申请号：PCT/JP1997000065
申请日：1997-01-16
申请人： TAIHO PHARMACEUTICAL CO., LTD. , SATO, Atsushi , ASAO, Tetsuji , HAGIWARA, Yuichi , KITADE, Makoto , YAMAZAKI, Yasundo
发明人： TAIHO PHARMACEUTICAL CO., LTD.
IPC分类号： A61K31/40
CPC分类号： C07D401/06 , C07D209/34 , C07D401/14 , C07D471/04
摘要： Intimal thickening inhibitors containing as the active ingredient oxyindole derivatives represented by general formula (1) or salts thereof (wherein R represents hydrogen, phenyl optionally substituted by lower alkyl, lower alkoxy, lower alkylaminoalkoxy, hydroxy, amino, lower alkylamino or halogeno, or pyridyl optionally substituted by lower alkyl, lower alkoxy, lower alkylaminoalkoxy, hydroxy, amino, lower alkylamino, halogeno, lower alkoxycarbonyl or carboxy; R represents optionally substituted phenyl, or pyridyl optionally substituted by lower alkyl, lower alkoxy, lower alkylamino-alkoxy, hydroxy, amino, lower alkylamino, halogeno, lower alkoxycarbonyl or carboxy; R represents hydrogen, optionally substituted lower alkyl, benzyl or benzenesulfonyl, or acyl; R represents hydrogen, lower alkoxy, halogeno, amino, lower alkylamino, carboxy, lower alkoxycarbonyl, optionally substituted phenylcarbamoyl, or trifluoromethyl; X represents CH or N; n represents the number of the substituents ranging from 0 to 4; and the double line composed of dotted and solid lines means that this bond is either a single or a double bond). These drugs show excellent effects of inhibiting intimal thickening and thus useful in preventing, treating and relieving proliferative vascular lesions such as vascular reconstriction after percutaneous transluminal coronary recanalization, arterial sclerosis, peripheral embolism and angiitis.
摘要翻译：含有作为活性成分的由通式（1）表示的氧吲哚衍生物或其盐（其中R 1表示氢，任选被低级烷基，低级烷氧基，低级烷基氨基烷氧基，羟基，氨基，低级烷基氨基或卤素取代的苯基）的内增稠抑制剂或任选被低级烷基，低级烷氧基，低级烷基氨基烷氧基，羟基，氨基，低级烷基氨基，卤代，低级烷氧基羰基或羧基取代的吡啶基; R 2表示任选取代的苯基，或任选被低级烷基，低级烷氧基，低级烷基氨基 - 烷氧基，羟基，氨基，低级烷基氨基，卤代，低级烷氧基羰基或羧基; R 3表示氢，任选取代的低级烷基，苄基或苯磺酰基或酰基; R 4表示氢，低级烷氧基，，低级烷基氨基，羧基，低级烷氧基羰基，任选取代的苯基氨基甲酰基或三氟甲基; X表示CH或N; n表示取代基为0至4; 并且由虚线和实线组成的双线意味着该键是单键或双键）。这些药物显示出优异的抑制内膜增厚的效果，因此可用于预防，治疗和缓解经皮冠状动脉冠状动脉再通，动脉硬化，周围栓塞和血管炎等增殖性血管病变如血管再狭窄。

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