公开(公告)号：EP1445249A1

公开(公告)日：2004-08-11

申请号：EP02781763.4

申请日：2002-11-13

申请人： TOYAMA CHEMICAL CO., LTD. ,  Hirono, Shuichi ,  Shiozawa, Shunichi

发明人： CHAKI, Hisaaki ,  KOTSUBO, Hironori ,  TANAKA, Tadashi ,  AIKAWA, Yukihiko ,  HIRONO, Shuichi ,  SHIOZAWA, Shunichi

IPC分类号： C07C59/90 ,  C07C69/734 ,  C07C69/76 ,  C07C205/34 ,  C07C219/32 ,  C07C255/54 ,  C07C255/37 ,  C07C271/64 ,  C07C235/42 ,  C07C311/29 ,  C07C311/51 ,  C07C311/53 ,  C07C317/22 ,  C07C323/19 ,  A61K31/192

CPC分类号： C07C235/42 ,  A61K31/192 ,  C07C59/90 ,  C07C65/34 ,  C07C65/40 ,  C07C69/738 ,  C07C69/76 ,  C07C69/88 ,  C07C69/94 ,  C07C205/34 ,  C07C217/76 ,  C07C255/54 ,  C07C259/10 ,  C07C271/64 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/10 ,  C07C2601/14 ,  C07C2601/18

摘要： A benzophenone derivative represented by the following formula:
wherein

R 1 represents, for example, an optionally substituted heterocyclic group, or a substituted phenyl group; Z represents, for example, an alkylene group; R 2 represents, for example, a carboxyl group optionally protected with alkyl;
R 3 represents, for example, an optionally protected hydroxyl group; R 4 represents, for example, an optionally substituted cycloalkyloxy group; and R 5 represents, for example, a hydrogen atom,
   or a salt thereof has anti-arthritic activity, inhibits bone destruction caused by arthritis, and provides high safety and excellent pharmacokinetics and thus is useful as therapeutic agent for arthritis. These compounds have inhibitory effect on AP-1 activity and are useful as preventive or therapeutic agent for diseases in which excessive expression of AP-1 is involved.

公开(公告)号：EP1445249A4

公开(公告)日：2006-03-08

申请号：EP02781763

申请日：2002-11-13

申请人： TOYAMA CHEMICAL CO LTD ,  HIRONO SHUICHI ,  SHIOZAWA SHUNICHI

发明人： CHAKI HISAAKI ,  KOTSUBO HIRONORI ,  TANAKA TADASHI ,  AIKAWA YUKIHIKO ,  HIRONO SHUICHI ,  SHIOZAWA SHUNICHI

IPC分类号： C07C59/90 ,  A61K31/192 ,  A61P29/00 ,  C07C65/34 ,  C07C65/40 ,  C07C69/734 ,  C07C69/738 ,  C07C69/76 ,  C07C69/88 ,  C07C69/94 ,  C07C205/34 ,  C07C217/76 ,  C07C219/32 ,  C07C235/42 ,  C07C255/37 ,  C07C255/54 ,  C07C259/10 ,  C07C271/64 ,  C07C311/29 ,  C07C311/51 ,  C07D239/96 ,  C07D261/20 ,  C07D333/38 ,  C07D333/56 ,  C07D409/12

CPC分类号： C07C235/42 ,  A61K31/192 ,  C07C59/90 ,  C07C65/34 ,  C07C65/40 ,  C07C69/738 ,  C07C69/76 ,  C07C69/88 ,  C07C69/94 ,  C07C205/34 ,  C07C217/76 ,  C07C255/54 ,  C07C259/10 ,  C07C271/64 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/10 ,  C07C2601/14 ,  C07C2601/18

摘要： Because of having an anti-arthritic effect, inhibiting bone fracture induced by arthritis and having a high safety, benzophenone derivatives represented by the following general formula or salts thereof are useful as remedies for arthritis with favorable dynamics in vivo: wherein R1 represents an optionally substituted heterocycle, substituted phenyl, etc. Z represents alkylene, etc. R2 represents optionally alkyl-blocked carboxyl, etc. R3 represents an optionally blocked hydroxy, etc. R4 represents an optionally substituted cycloalkyloxy, etc. and R5 represents hydrogen, etc. Moreover, these compounds have an AP-1 activity inhibitory effect, which makes them useful as preventives and remedies for diseases in which the overexpression of AP-1 participates.

摘要翻译： 由下式表示的二苯甲酮衍生物：其中R 1表示例如可以具有取代基的杂环基或取代苯基的 Z表示例如亚烷基; R 2表示例如任选被烷基保护的羧基; R 3表示例如任选保护的羟基; R 4表示例如任选取代的环烷氧基; R 5表示例如氢原子或其盐具有抗关节炎活性，抑制由关节炎引起的骨破坏，提供高安全性和优异的药代动力学，因此可用作关节炎的治疗剂。 这些化合物对AP-1活性具有抑制作用，可用作涉及AP-1过度表达的疾病的预防或治疗剂。