公开(公告)号：US20030220360A1

公开(公告)日：2003-11-27

申请号：US10291429

申请日：2002-11-12

申请人： Nippon Suisan Kaisha, Ltd., a Japan corporation

发明人： Shuji Jinno ,  Takaaki Okita ,  Naomi Ohtsuka ,  Shinya Yamashita ,  Junichiro Hata ,  Jiro Takeo

IPC分类号： C07D337/12 ,  C07D337/16 ,  C07D491/02 ,  C07D498/02 ,  A61K031/4743 ,  A61K031/4741 ,  A61K031/335 ,  A61K031/38

CPC分类号： C07D405/04 ,  A61K31/31 ,  A61K31/335 ,  A61K31/343 ,  A61K31/38 ,  A61K31/381 ,  A61K31/4353 ,  A61K31/4427 ,  C07D313/14 ,  C07D337/14 ,  C07D407/04 ,  C07D409/04 ,  C07D491/04

摘要： Compounds represented by formula (1), 1 wherein X is, for example, CH, CH2, CHR (wherein R is a lower alkyl group or a substituted lower alkyl group) or CRRnull (wherein R and Rnull are the same as the above defined R); Y is, for example, CH, CH2 or CnullO; Z is, for example, O, S, SnullO or SO2; U is C or N; R1 to R4 are each independently, for example, a hydrogen atom, OR, SR (wherein R is the same as defined above), or an aromatic ring, a substituted aromatic ring or a heterocycle; at least one of R5 and R8 is, for example, OH and the remaining of R5 and R8 are each independently, for example, a hydrogen atom or OH, optical isomers thereof, conjugates thereof or pharmaceutically acceptable salts thereof are provided. These compounds are characterized in having a wide range of pharmacological actions such as an excellent relaxing action of tracheal smooth muscles, an inhibition of airway hypersensitivity and an inhibition of infiltration of inflammatory cells into the airway and, in addition, high safety.

摘要翻译： 由式（1）表示的化合物，其中X为例如CH，CH 2，CHR（其中R为低级烷基或取代的低级烷基）或CRR'（其中R和R'与上述相同 定义R）; Y为例如CH，CH 2或C = O; Z是例如O，S，S = O或SO 2; U是C或N; R 1至R 4各自独立地为例如氢原子，OR，SR（其中R与上述定义相同），或芳香环，取代的芳环或杂环; R5和R8中的至少一个是例如OH，并且R5和R8的剩余部分各自独立地为例如氢原子或OH，其光学异构体，其缀合物或其药学上可接受的盐。 这些化合物的特征在于具有广泛的药理作用，例如气管平滑肌的优异的缓解作用，气道超敏反应的抑制和抑制炎症细胞浸润到气道中，另外还具有高安全性。