公开(公告)号：EP2260869A2

公开(公告)日：2010-12-15

申请号：EP10182147.8

申请日：2007-04-19

申请人： Takeda Pharmaceutical Company Limited

发明人： Iizawa, Yuji ,  Kawamoto, Tomohiro ,  Ii, Masayuki

IPC分类号： A61K45/00 ,  A61K31/216 ,  A61K31/41 ,  A61K31/4192 ,  A61K31/428 ,  A61K45/06 ,  A61P9/00 ,  A61P25/00 ,  A61P29/00 ,  A61P31/00 ,  A61P37/00

CPC分类号： C07D249/06 ,  A61K31/216 ,  A61K31/41 ,  A61K31/4192 ,  A61K31/428 ,  A61K45/06 ,  C07D249/08 ,  C07D257/04 ,  C07D275/06 ,  A61K2300/00

摘要： An agent for suppressing the production of various cytokines (IL-8 and the like) and inflammatory mediators, an agent for suppressing the expression of COX-II and the like, or an inhibitor of various phosphorylation enzymes (ATF2 and the like), which contains a TLR signaling inhibitory substance, preferably a compound represented by the formula (I) or the formula (II)


wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.

摘要翻译： 用于抑制各种细胞因子（IL-8等）和炎性介质的产生的药剂，抑制COX-II等的表达的试剂或各种磷酸化酶（ATF2等）的抑制剂，其中 含有TLR信号传导抑制物质，优选式（I）或式（II）表示的化合物，其中每个符号如说明书中所定义，或其盐或其前药。

公开(公告)号：EP2260869A3

公开(公告)日：2011-03-23

申请号：EP10182147.8

申请日：2007-04-19

申请人： Takeda Pharmaceutical Company Limited

发明人： Iizawa, Yuji ,  Kawamoto, Tomohiro ,  Ii, Masayuki

IPC分类号： A61K45/00 ,  A61K31/216 ,  A61K31/41 ,  A61K31/4192 ,  A61K31/428 ,  A61K45/06 ,  A61P9/00 ,  A61P25/00 ,  A61P29/00 ,  A61P31/00 ,  A61P37/00

CPC分类号： C07D249/06 ,  A61K31/216 ,  A61K31/41 ,  A61K31/4192 ,  A61K31/428 ,  A61K45/06 ,  C07D249/08 ,  C07D257/04 ,  C07D275/06 ,  A61K2300/00

摘要： An agent for suppressing the production of various cytokines (IL-8 and the like) and inflammatory mediators, an agent for suppressing the expression of COX-II and the like, or an inhibitor of various phosphorylation enzymes (ATF2 and the like), which contains a TLR signaling inhibitory substance, preferably a compound represented by the formula (I) or the formula (II)


wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.

公开(公告)号：EP1524263A1

公开(公告)日：2005-04-20

申请号：EP05000768.1

申请日：1999-03-08

申请人： Takeda Pharmaceutical Company Limited

发明人： Ichimori, Yuzo ,  Ii, Masayuki ,  Itoh, Katsumi ,  Kitazaki, Tomoyuki ,  Yamada, Junji

IPC分类号： C07C311/14 ,  C07C303/38 ,  C07D275/06 ,  A61K31/235 ,  A61K31/425 ,  C07D249/08 ,  C07D257/04 ,  C07D249/06

CPC分类号： C07D249/08 ,  C07C311/14 ,  C07C2601/10 ,  C07C2601/16 ,  C07C2601/18 ,  C07D249/06 ,  C07D257/04 ,  C07D275/06

摘要： The present invention provides a prodrug of a compound represented by the formula:
wherein R represents an aliphatic hydrocarbon group optionally having substituents, an aromatic hydrocarbon group optionally having substituents, a heterocyclic group optionally having substituents, a group represented by the formula: OR 1 (wherein R 1 represents a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents) or a group represented by the formula:
wherein R 1b represents a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents, R 1c is, same with or different from R 1b , a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents, R 0 represents a hydrogen atom or an aliphatic hydrocarbon group, or R and R 0 represents a bond with each other, Ar represents an aromatic hydrocarbon group optionally having substituents,
and n is an integer of 1 to 4, or a salt thereof, which is a agent for preventing or treating diseases such as cardiac disease, autoimmune disease, septick shock, etc..

摘要翻译： 本发明提供由下式表示的化合物的前药：其中R表示任选具有取代基的脂族烃基，任选具有取代基的芳族烃基，任选具有取代基的杂环基，由下式表示的基团：其中， R 1表示氢原子或任选具有取代基的脂族烃基）或由下式表示的基团：其中R 1b表示氢原子或任选具有取代基的脂族烃基，R 1c与R 1b相同或不同，为氢原子 或任选具有取代基的脂族烃基，R 0表示氢原子或脂族烃基，或R和R 0彼此键合，Ar表示任选具有取代基的芳族烃基，并且n是1至4的整数 或其盐，其是用于预防或治疗诸如心脏病的药剂 疾病，自身免疫性疾病，septick休克等。