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1. 发明申请

WO1996020194A1 NOVEL QUINUCLIDINE DERIVATIVES AND MEDICINAL COMPOSITION THEREOF 审中-公开
标题翻译：新型喹啉衍生物及其药物组合物
公开(公告)号：WO1996020194A1
公开(公告)日：1996-07-04
申请号：PCT/JP1995002713
申请日：1995-12-27
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD. , TAKEUCHI, Makoto , NAITO, Ryo , HAYAKAWA, Masahiko , OKAMOTO, Yoshinori , YONETOKU, Yasuhiro , IKEDA, Ken , ISOMURA, Yasuo
发明人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D453/02
CPC分类号： C07D221/12 , C07D453/02 , C09K19/3444
摘要： A quinuclidine derivative represented by general formula (I), a salt, N-oxide or quaternary ammonium salt thereof, and a medicinal composition containing the same, wherein the ring A represents optionally substituted aryl, cycloalkyl, cycloalkenyl, heteroaryl containing 1 to 4 heteroatoms selected from among oxygen, nitrogen and sulfur, or 5- to 7-membered saturated heterocycle; X represents a single bond or methylene; R represents halogeno, hydroxy, lower alkoxy, carboxy, lower alkoxycarbonyl, lower acyl, mercapto, lower alkylthio, sulfonyl, lower alkylsulfonyl, sulfinyl, lower alkylsulfinyl, sulfonamido, lower alkanesulfonamido, carbamoyl, thio-carbamoyl, mono- or di(lower alkyl)carbamoyl, nitro, cyano, amino, mono- or di(lower alkyl)amino, methylenedioxy, ethylenedioxy or lower alkyl optionally substituted by halogeno, hydroxy, lower alkoxy, amino or mono- or di(lower alkyl)amino; 1 is 0 or 1; m is an integer of 1 to 3; and n is an integer of 1 or 2. The compound has an antagonistic effect on muscarine M3 receptors and is useful as a preventive or remedy for urologic diseases, respiratory diseases or digestive diseases.
摘要翻译：由通式（I）表示的奎宁环衍生物，其盐，N-氧化物或季铵盐及含有该奎宁环衍生物的药物组合物，其中环A表示任选取代的芳基，环烷基，环烯基，含有1至4个杂原子的杂芳基选自氧，氮和硫，或5-至7-元饱和杂环; X表示单键或亚甲基; R代表卤代，羟基，低级烷氧基，羧基，低级烷氧基羰基，低级酰基，巯基，低级烷硫基，磺酰基，低级烷基磺酰基，亚磺酰基，低级烷基亚磺酰基，亚磺酰氨基，低级烷烃磺酰胺基，氨基甲酰基，硫代氨基甲酰基，氨基，硝基，氰基，氨基，一或二（低级烷基）氨基，亚甲二氧基，亚乙二氧基或任选被卤代，羟基，低级烷氧基，氨基或一或二（低级烷基）氨基取代的低级烷基; 1为0或1; m为1〜3的整数。并且n是1或2的整数。该化合物对毒蕈碱M3受体具有拮抗作用，并且可用作泌尿系统疾病，呼吸系统疾病或消化系统疾病的预防或治疗。

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