公开(公告)号：EP1025857A1

公开(公告)日：2000-08-09

申请号：EP98943089.7

申请日：1998-09-22

申请人： Eisai Co., Ltd.

发明人： YAMAUCHI, Toshihiko ,  ISHIBASHI, Akira ,  TOKUHARA, Naoki ,  NAGAI, Mitsuo

IPC分类号： A61K45/00 ,  A61K31/44 ,  A61K31/505 ,  A61K31/495 ,  A61K31/53 ,  A61K31/535 ,  A61K31/47 ,  A61K31/41 ,  A61K31/475 ,  A61K31/55 ,  A61K31/40 ,  A61K31/34 ,  A61K31/38 ,  A61K31/35 ,  A61K31/395 ,  A61K31/19 ,  A61K31/195

CPC分类号： A61K31/695 ,  A61K31/00 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/4155 ,  A61K31/498 ,  A61K31/55

摘要： Therapeutic or preventive agents for system lupus erythematosus, glomerulonephritis, lupus nephritis, idiopathic thrombocytopenic purpura or autoimmune anemia, which can be substituted for conventional steroid preparations or immunosuppressive agents. The active ingredients of the therapeutic or preventive agents are agonists for retinoic acid receptors, particularly retinoic receptor, subtype α (i.e., RAR α), and examples of the agonists include (1) carboxylic acid derivatives bearing fused rings as represented by general formula (I) wherein rings L and M are fused with each other, and are each independently an optionally substituted aromatic hydrocarbon ring or an optimally substituted heterocycle; rings A and B are each independently an optionally substituted aromatic hydrocarbon ring or a heterocycle; and D is optionally protected carboxyl, and (2) 4-{[(3,5-bistrimethylsilylphenyl)carbonyl]amino}benzoic acid and 4{2-[5-(3-methoxymethyl-5,6,7,8-tetrahydro-5,5,8,8,-tetramethylnaphthalen-2-yl)-pyrrolyl]}benzoic acid.

摘要翻译： 用于系统性红斑狼疮，肾小球性肾炎，狼疮性肾炎，特发性血小板减少性紫癜或自身免疫性贫血的治疗或预防剂，其可替代常规类固醇制剂或免疫抑制剂。 治疗或预防剂的活性成分是视黄酸受体的激动剂，特别是视黄酸受体，亚型α（即RARα），激动剂的实例包括（1）带有稠合环的羧酸衍生物，如通式（ I）其中环L和M彼此稠合，并且各自独立地为任选取代的芳族烃环或最佳取代的杂环; 环A和B各自独立地为任选取代的芳族烃环或杂环; 和D是任选保护的羧基，和（2）4-Δ（3,5-双三甲基甲硅烷基苯基）羰基氨基苯甲酸和4,2-⑤-（3-甲氧基甲基-5,6,7,8-四氢-5,5,8,8 ，四甲基萘-2-基） - 吡咯基ü苯甲酸。

公开(公告)号：EP0930075A1

公开(公告)日：1999-07-21

申请号：EP97943141.8

申请日：1997-10-02

申请人： Eisai Co., Ltd.

发明人： YAMAUCHI, Toshihiko ,  ISHIBASHI, Akira ,  TOKUHARA, Naoki ,  NAGAI, Mitsuo

IPC分类号： A61K45/00 ,  A61K31/00

CPC分类号： A61K31/498 ,  A61K31/192 ,  A61K31/203 ,  A61K31/4025

摘要： The present invention provides remedies for graft-versus-host disease (GVHD) and graft rejection reactions in organ transplantation which comprise retinoic acid receptor (RAR) agonists as an active ingredient. Main examples thereof include 9-(4-methoxy-2,3,6-trimethylphenyl)-7,8-dimethylnona-2,4,6,8-tetraen-1-oic acid, 4-[(E)-2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethylnaphthalen-2-yl)propenyl]benzoic acid, 4-{2-[5-(4,7-dimethylbenzofuran-2-yl)pyrroyl]}benzoic acid, 4-{2-[5-(5-chloro-7-ethylbenzofuran-2-yl)pyrrolyl]}benzoic acid and 4-{2-[5-(4,7-dimethylbenzothiophen-2-yl)pyrrolyl]}benzoic acid.

摘要翻译： 本发明提供了一种移植物抗宿主病（GVHD）和在器官移植排斥反应，其包含视黄酸受体（RAR）激动剂作为活性成分的补救措施。 其主要的例子包括9-（4-甲氧基-2,3,6-三甲基苯基）-7,8- dimethylnona -2,4,6,8-四烯-1- -oic酸，4-A（E）-2- （5,6,7,8-四氢-5,5,8,8-四甲基吡啶-2-基）丙烯ylÜbenzoic酸，4- AE2 A5-（-4,7-二甲基吡啶-2-基）pyrroylÜübenzoic酸，4- -A2-A5-（5-氯-7-乙基苯并呋喃-2-基）pyrrolylÜübenzoic酸和4- AE2 A5-（4,7- dimethylbenzothiophene -2-基）pyrrolylÜübenzoic酸。