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公开(公告)号：EP1445249A4
公开(公告)日：2006-03-08
申请号：EP02781763
申请日：2002-11-13
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。 -
2.发明公开NOVEL SPIRO COMPOUNDS OR SALTS THEREOF AND PREVENTIVES/REMEDIES FOR AUTOIMMUNE DISEASES AND AP-1 INHIBITORS CONTAINING THE SAME 审中-公开螺环化合物或其盐和自身免疫预防或治疗剂和含有AP-1抑制剂
公开(公告)号：EP1076056A4
公开(公告)日：2002-08-14
申请号：EP99918266
申请日：1999-04-28
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： A61K38/00 , C07D277/60 , C07D417/04 , C07D417/06 , C07D417/08 , C07D417/12 , C07D513/10 , C07K5/078 , A61K31/425 , A61K38/04 , C07K5/04
CPC分类号： C07D277/60 , A61K38/00 , C07D417/04 , C07D417/06 , C07D417/08 , C07D417/12 , C07D513/10 , C07K5/06139
摘要： Spiro compounds represented by general formula (I), wherein A, R?2, R3, R4, R5, R6¿ and n are each as defined in the specification; which exert an AP-1 activity inhibitory effect. Owing to this effect, these compounds are useful as remedies/preventives for autoimmune diseases which inhibit the expression of various genes and show little side effect.
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公开(公告)号：EP1127869A4
公开(公告)日：2007-05-02
申请号：EP99954398
申请日：1999-11-05
发明人： CHAKI HISAAKI , TAKAKURA TADAKAZU , TSUCHIDA KEIICHI , YOKOTANI JUNICHI , KOTSUBO HIRONORI , AIKAWA YUKIHIKO , HIRONO SHUICHI , SHIOZAWA SHUNICHI
IPC分类号： C07D277/60 , A01N63/00 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/4184 , A61K31/4402 , A61K31/4418 , A61K31/4427 , A61K31/495 , A61K38/00 , A61K45/00 , A61P19/02 , A61P37/02 , A61P37/06 , A61P43/00 , C07C59/64 , C07C59/84 , C07C59/90 , C07C65/24 , C07C65/34 , C07C65/36 , C07C65/38 , C07C65/40 , C07C69/618 , C07C69/738 , C07C69/767 , C07C69/78 , C07C69/94 , C07C229/34 , C07C233/01 , C07C233/47 , C07C235/16 , C07C235/20 , C07C235/84 , C07C251/32 , C07C251/40 , C07C251/48 , C07C251/60 , C07C255/49 , C07C275/24 , C07C311/06 , C07C311/51 , C07D207/04 , C07D207/08 , C07D207/32 , C07D207/333 , C07D209/18 , C07D209/30 , C07D209/40 , C07D209/42 , C07D213/50 , C07D235/26 , C07D241/08 , C07D401/10 , C07D401/14 , C07K7/06 , C07K7/64 , C07C69/73 , C07C205/49
CPC分类号： C07D207/333 , A61K38/00 , C07C59/64 , C07C59/84 , C07C65/24 , C07C65/34 , C07C65/36 , C07C65/38 , C07C65/40 , C07C69/738 , C07C69/94 , C07C229/34 , C07C233/01 , C07C233/47 , C07C235/20 , C07C235/84 , C07C251/32 , C07C251/48 , C07C251/60 , C07C255/49 , C07C275/24 , C07C311/06 , C07C311/51 , C07D207/08 , C07D209/42 , C07D235/26 , C07D277/60 , C07K7/06 , C07K7/64 , Y02P20/55
摘要： Compounds represented by formula (I) wherein N1 represents an atom to which a donor hydrogen atom in a hydrogen bond donor group is bonded or a hydrogen bond acceptor atom in a hydrogen bond acceptor group; N3 represents a hydrogen bond acceptor atom in a hydrogen bond acceptor group; and N2, N4 and N5 represent each an arbitrary carbon atom constituting a hydrophobic group; having an atom corresponding to N3 and atoms corresponding to at least two atoms selected from N1, N2, N4 and N5 among the five atoms constituting a pharmacophore specified by the interatomic distances among N1, N2, N3, N4 and N5; and, in the optimized stereochemical structure thereof, the interatomic distances between the atom corresponding to N3 and atoms corresponding to at least two atoms selected from N1, N2, N4 and N5 fall within the scope of the pharmacophore interatomic distance, or salts thereof. Because of having an effect of inhibiting the activity of a transcription factor AP-1, these compounds are useful as preventives/remedies for diseases in which the excessive expression of AP-1 participates and as AP-1 inhibitors.
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4.发明公开
公开(公告)号：EP2258361A4
公开(公告)日：2012-01-04
申请号：EP09724165
申请日：2009-03-25
发明人： AIKAWA YUKIHIKO , SHIOZAWA SHUNICHI
IPC分类号： A61K31/12 , A61K31/194 , A61K31/423 , A61K31/5377 , A61K39/395 , A61K45/00 , A61K45/06 , A61P1/00 , A61P1/16 , A61P13/12 , A61P19/02 , A61P29/00 , A61P37/02 , A61P37/06 , A61P43/00 , C07D261/20
CPC分类号： A61K31/12 , A61K31/194 , A61K31/423 , A61K31/5377 , A61K39/3955 , A61K45/06 , C07D261/20 , C07K16/241 , A61K2300/00
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5.发明公开
公开(公告)号：EP2266557A4
公开(公告)日：2011-09-21
申请号：EP09735250
申请日：2009-04-20
发明人： AIKAWA YUKIHIKO , SHIOZAWA SHUNICHI
IPC分类号： A61K31/194 , A61K31/42 , A61K31/423 , A61K31/519 , A61K31/5377 , A61K31/573 , A61K45/06 , A61P29/00 , A61P37/06 , A61P43/00
CPC分类号： A61K45/06 , A61K31/194 , A61K31/42 , A61K31/423 , A61K31/519 , A61K31/5377 , A61K31/573 , A61K2300/00
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6.发明公开IMMUNOMODULATOR, CELL ADHESION INHIBITOR, AND AGENT FOR TREATING AND PREVENTING AUTOIMMUNE DISEASES 失效免疫调节剂，细胞粘连抑制剂和手段用于治疗和自身免疫疾病的预防
公开(公告)号：EP0695547A4
公开(公告)日：1997-05-28
申请号：EP94912070
申请日：1994-04-07
发明人： TANAKA KEIICHI , MAKINO SHINJI , OSHIO ICHIRO , SHIMOTORI TOMOYA , AIKAWA YUKIHIKO , INABA TAKIHIRO , YOSHIDA CHOSAKU , TAKANO SHUNTARO , TANIGUCHI YOICHI
IPC分类号： C07D311/22 , C07D311/24 , C07D311/26 , A61K31/35 , A61K31/38 , A61K31/40 , A61K31/41 , A61K31/44 , A61K31/445 , C07D311/44 , C07D311/54 , C07D311/56
CPC分类号： C07D311/26 , C07D311/22 , C07D311/24
摘要： A 4H-1-benzopyran-4-one derivative of general formula Ä1Ü, or a salt thereof exerts excellent effects of immunomodulation and cell adhesion inhibition, and is further expected to have the effect of relieving autoimmune diseases at a level comparable to that of steroids. Thus the compound of general formula Ä1Ü is useful in the treatment and prevention of autoimmune diseases fundamentally caused by immunopathy or abnormally accelerated cell adhesion, for example, chronic rheumatoid arthritis, systemic lupus erythematosus, sclerema, mixed connective tissue disease, polyarteritis nodosa, polymyositis/dermatomyositis, Sjögren's syndrome, Behcet's disease, multiple sclerosis, autoimmune diabetes, Hashimoto's disease, psoriasis, primary myxedema, pernicious anemia, serious adynamia, ulcerative colitis, chronic active hepatitis, autoimmune hemolytic anemia and idiopathic thrombocytopenic purpura.
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