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1. 发明申请

WO1997019078A1 PYRIDO[2, 3-D] PYRIMIDINE DERIVATIVES AND MEDICINAL COMPOSITIONS THEREOF 审中-公开
标题翻译：吡咯并[2,3-D]吡啶衍生物及其药物组合物
公开(公告)号：WO1997019078A1
公开(公告)日：1997-05-29
申请号：PCT/JP1996003389
申请日：1996-11-20
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD. , TAKAYAMA, Kazuhisa , HISAMICHI, Hiroyuki , IWATA, Masahiro , KUBOTA, Hideki , AOKI, Motonori
发明人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Compounds represented by general formula (I) or pharmaceutically acceptable salts thereof which have the effect of inhibiting the activity of type IV phosphodiesterases and are usable as drugs, in particular, type IV phosphodiesterase inhibitors or preventives and remedies for diseases in association with the sthenic type IV phosphodiesterase activity, in particular, respiratory diseases such as bronchial asthma. In said formula (I), X represents oxygen or sulfur; R represents lower alkyl, cycloalkyl(lower alkyl) or cycloalkyl; R represents hydrogen, halogeno, lower alkyl, halo(lower alkyl), hydroxy(lower alkyl), mercapto(lower alkyl), (lower alkoxy)(lower alkyl), (lower alkylthio)(lower alkyl), (lower alkanoyloxy)(lower alkyl), (lower alkanoylthio)(lower alkyl), (lower alkanoyl)(lower alkyl), hydroxyimino(lower alkyl), (lower alkoxyimino)(lower alkyl), cycloalkyl, aryl or lower alkanoyl; R represents hydrogen, halogeno or lower alkyl; R represents hydrogen, or lower alkyl; R represents cycloalkyl optionally substituted by the same group as R ; naphthyl optionally substituted by the same group as R ; a 5- or 6-membered monocyclic heterocycle optionally substituted by the same group as R , optionally fused with a benzene ring and having one to four heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur atoms; or a group of formula (a); and R represents halogeno, lower alkyl, halo(lower alkyl), hydroxy, lower alkoxy, cyano or nitro.
摘要翻译：具有抑制IV型磷酸二酯酶活性的通式（I）表示的化合物或其药学上可接受的盐，可用作药物，特别是IV型磷酸二酯酶抑制剂或预防药物以及与该类型相关的疾病的治疗方法 IV磷酸二酯酶活性，特别是呼吸道疾病如支气管哮喘。在所述式（I）中，X表示氧或硫; R 1表示低级烷基，环烷基（低级烷基）或环烷基; R 2表示氢，卤代低级烷基，卤代（低级烷基），羟基（低级烷基），巯基（低级烷基），（低级烷氧基）（低级烷基），（低级烷硫基）（低级烷基），（低级烷酰基）（低级烷基），（低级烷酰基）（低级烷基），羟基亚氨基（低级烷基），（低级烷氧基亚氨基）（低级烷基），环烷基，芳基或低级烷酰基。 R 3表示氢，卤代或低级烷基; R 4表示氢或低级烷基; R 5表示任选被与R 6相同的基团取代的环烷基; 任选被与R 6相同基团取代的萘基; 任选地被与R 6相同的基团取代的5-或6-元单环杂环，任选地与苯环稠合并具有一至四个选自氮，氧和硫原子的杂原子; 或一组式（a）; 和R 6表示卤代，低级烷基，卤代（低级烷基），羟基，低级烷氧基，氰基或硝基。

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