公开(公告)号：EP1070713B1

公开(公告)日：2006-10-18

申请号：EP99912111.4

申请日：1999-04-06

申请人： TOYAMA CHEMICAL CO., LTD.

发明人： HAYASHI, Kazuya ,  KITO, Tokunori ,  MITSUYAMA, Junichi ,  YAMAKAWA, Tetsumi ,  KURODA, Hiroshi ,  KAWAFUCHI, Hiroyo

IPC分类号： C07D401/04 ,  A61K31/47

CPC分类号： C07D401/04 ,  Y02P20/55

摘要： Novel quinolonecarboxylic acid derivatives represented by general formula (1) which have potent antibacterial effects on gram-positive bacteria, in particular, Propionibacterium acnes, wherein R1 represents hydrogen or a carboxyl-protective group; R2 represents optionally substituted cycloalkyl; R3 represents hydrogen, halogeno, optionally substituted alkyl, alkoxy or alkylthio, optionally protected hydroxy or amino, or nitro; R4 represents optionally substituted alkyl or alkoxy; Z represents halogeno, optionally substituted alkyl, alkenyl, cycloalkyl, alkoxy, alkylthio, amino or pyridin-4-yl or pyridin-3-yl optionally having one or more substituents selected from among optionally substituted hydroxy and amino.

公开(公告)号：EP1076056A1

公开(公告)日：2001-02-14

申请号：EP99918266.0

申请日：1999-04-28

申请人： TOYAMA CHEMICAL CO., LTD.

发明人： CHAKI, Hisaaki ,  AIKAWA, Yukihiko ,  MIYAJIMA, Mikako ,  TAKAKURA, Tadakazu ,  NISHIO, Morihiro ,  KURODA, Hiroshi ,  TANAKA, Keiichi ,  KAJITA, Tetsuya ,  HIRONO, Shuichi ,  SHIOZAWA, Shunichi

IPC分类号： C07D277/60 ,  C07D417/04 ,  C07D417/06 ,  C07D513/10 ,  C07K5/04 ,  A61K31/425 ,  A61K31/44 ,  A61K31/445 ,  A61K38/04

CPC分类号： C07D277/60 ,  A61K38/00 ,  C07D417/04 ,  C07D417/06 ,  C07D417/08 ,  C07D417/12 ,  C07D513/10 ,  C07K5/06139

摘要： The spiro compounds of the present invention represented by the following general formula:
wherein A, R 2 , R 3 , R 4 , R 5 , R 6 and n are as defined in the specification, exhibit an AP-1 activity inhibitory action and, based on the AP-1 inhibitory action, suppresses the expression of a wide variety of genes and are useful as an agent for treating and preventing autoimmune diseases with lessened side reactions.

摘要翻译： 如在定义 worin A，R <2> [R <3>，R <4> - [R <5> - [R <6>和n：由下述通式表示的本发明的螺环化合物 AP-1活性抑制作用的说明书中，表现出和，基于AP-1抑制作用，抑制了各种基因的表达，并且作为用于治疗和减轻与副反应预防自身免疫性疾病的药剂是有用的。

公开(公告)号：EP1070713A1

公开(公告)日：2001-01-24

申请号：EP99912111.4

申请日：1999-04-06

申请人： TOYAMA CHEMICAL CO., LTD.

发明人： HAYASHI, Kazuya ,  KITO, Tokunori ,  MITSUYAMA, Junichi ,  YAMAKAWA, Tetsumi ,  KURODA, Hiroshi ,  KAWAFUCHI, Hiroyo

IPC分类号： C07D401/04 ,  A61K31/47

CPC分类号： C07D401/04 ,  Y02P20/55

摘要： Novel quinolonecarboxylic acid derivatives represented by general formula (1) which have potent antibacterial effects on gram-positive bacteria, in particular, Propionibacterium acnes , wherein R 1 represents hydrogen or a carboxyl-protective group; R 2 represents optionally substituted cycloalkyl; R 3 represents hydrogen, halogeno, optionally substituted alkyl, alkoxy or alkylthio, optionally protected hydroxy or amino, or nitro; R 4 represents optionally substituted alkyl or alkoxy; Z represents halogeno, optionally substituted alkyl, alkenyl, cycloalkyl, alkoxy, alkylthio, amino or pyridin-4-yl or pyridin-3-yl optionally having one or more substituents selected from among optionally substituted hydroxy and amino.

摘要翻译： 对通式（1）表示的新型喹诺酮羧酸衍生物，其对革兰氏阳性细菌，特别是痤疮丙酸杆菌具有强力的抗菌作用，其中R 1表示氢或羧基保护基; R 2表示任选取代的环烷基; R 3表示氢，卤代，任选取代的烷基，烷氧基或烷硫基，任选保护的羟基或氨基或硝基; R 4表示任选取代的烷基或烷氧基; Z表示卤代，任选取代的烷基，烯基，环烷基，烷氧基，烷硫基，氨基或吡啶-4-基或任选具有一个或多个选自任选取代的羟基和氨基的取代基的吡啶-3-基。