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    • 3. 发明授权
    • Benzene compound and pharmaceutical use thereof
    • 苯化合物及其药物用途
    • US06187821B1
    • 2001-02-13
    • US09309818
    • 1999-05-12
    • Tetsuro FujitaKunitomo AdachiToshiyuki KoharaMasatoshi KiuchiKenji ChibaKoji TeshimaTadashi Mishina
    • Tetsuro FujitaKunitomo AdachiToshiyuki KoharaMasatoshi KiuchiKenji ChibaKoji TeshimaTadashi Mishina
    • A61K31135
    • C07C215/56C07C215/28C07C215/30C07C217/64C07C217/72C07C219/22C07C225/16C07C233/18C07C233/31C07C233/36C07C233/73C07C271/16C07C271/18C07C2601/02
    • A benzene compound of the formula: wherein each symbol is as defined in the specification; an optically active isomer or salt thereof, a medicinal composition containing the same, and an immunosuppressant containing the same as the active ingredient. The compound, optically active isomer or salt has an excellent immunosuppressive effect and is useful as an inhibitor for the rejection reaction occurring in organ or bone marrow transplantation, and as a preventive or remedy for articular rheumatism, atopic eczema (dermatitis), Behcet's disease, uveal disease, systemic lupus erythematosus, Sjögren's syndrome, multiple sclerosis, myasthenia gravis, type I diabetes, endocrine ophthalmopathy, primary biliary, cirrhosis, Crohn's disease, glomerulonephritis, sarcoidosis, psoriasis, pemphigus, aplastic anemia, idiopathic thrombocytopenic purpura, allergy, polyarteritis nodosa, progressive systemic sclerosis, mixed connective-tissue disease, aortitis syndrome, polymyositis, dermatomyositis, Wegener's granuloma, ulcerative colitis, active chronic hepatitis, autoimmune hemolytic anemia, Evans' syndrome, bronchial asthma and pollinosis. It is useful also as an antifungal agent and hair growth stimulant.
    • 一种下式的苯化合物:其中每个符号如说明书中所定义;光学活性异构体或其盐,含有该化合物的药用组合物和含有该有效成分的免疫抑制剂。化合物,旋光异构体或 盐具有优异的免疫抑制作用,可用作器官或骨髓移植中发生的排斥反应的抑制剂,并且作为关节风湿病,特应性湿疹(皮炎),贝切特氏病,葡萄膜疾病,系统性红斑狼疮, Sjögren综合征,多发性硬化症,重症肌无力,I型糖尿病,内分泌眼病,原发性胆汁性肝硬化,克罗恩病,肾小球性肾炎,结节病,牛皮癣,天疱疮,再生障碍性贫血,特发性血小板减少性紫癜,变态反应,结节性多动脉炎,进行性系统性硬化症 组织病,主动脉炎综合征,多发性肌炎,皮肌炎,威基 r肉芽肿,溃疡性结肠炎,活动性慢性肝炎,自身免疫性溶血性贫血,伊文思综合征,支气管哮喘和花粉症。 它也可用作抗真菌剂和毛发生长兴奋剂。
    • 7. 发明授权
    • Compositions and methods of using compositions with accelerated lymphocyte homing immunosuppressive properties
    • 使用具有加速淋巴细胞归巢免疫抑制性质的组合物的组合物和方法
    • US06667025B2
    • 2003-12-23
    • US09334213
    • 1999-06-15
    • Kenji ChibaKunitomo Adachi
    • Kenji ChibaKunitomo Adachi
    • A61K4900
    • A61K31/135Y10S514/885
    • The methods and compositions of the invention and the compounds used in the invention involve a novel immunosuppression mechanism, accelerated lymphocyte homing immunosuppression (ALH-immunosuppression). For example, the compound FTY720 specifically directs lymphocytes to the peripheral lymph nodes, mesenteric lymph nodes, and Peyer's patches. By reversibly sequestering lymphocytes in these tissues, the compounds can inhibit an immune response in a mammal. Understanding these mechanisms provides a novel immunosuppression therapy that can synergistically interact with other immunosuppressive compounds. Screening methods for identifying similar ALH-immunosuppression compounds are also described. The invention allows better treatments and therapies wherever an immunosuppression regimen is desired.
    • 本发明的方法和组合物和本发明中使用的化合物涉及新的免疫抑制机制,加速淋巴细胞归巢免疫抑制(ALH-免疫抑制)。 例如,化合物FTY720特异性地将淋巴细胞引导到外周淋巴结,肠系膜淋巴结和派耶氏斑块。 通过在这些组织中可逆地螯合淋巴细胞,化合物可以抑制哺乳动物的免疫应答。 了解这些机制提供了可以与其他免疫抑制化合物协同相互作用的新型免疫抑制治疗。 还描述了鉴定类似的ALH-免疫抑制化合物的筛选方法。 本发明允许在需要免疫抑制方案的地方进行更好的治疗和治疗。
    • 8. 发明授权
    • Benzene compound and pharmaceutical use thereof
    • 苯化合物及其药物用途
    • US06372800B1
    • 2002-04-16
    • US09691099
    • 2000-10-19
    • Tetsuro FujitaKunitomo AdachiToshiyuki KoharaMasatoshi KiuchiKenji ChibaKoji TeshimaTadashi Mishina
    • Tetsuro FujitaKunitomo AdachiToshiyuki KoharaMasatoshi KiuchiKenji ChibaKoji TeshimaTadashi Mishina
    • A61K3135
    • C07C215/56C07C215/28C07C215/30C07C217/64C07C217/72C07C219/22C07C225/16C07C233/18C07C233/31C07C233/36C07C233/73C07C271/16C07C271/18C07C2601/02
    • A benzene compound of the formula wherein each symbol is as defined in the specification; an optically active isomer or salt thereof, a medicinal composition containing the same, and an immunosuppressant containing the same as the active ingredient. The compound, optically active isomer or salt has an excellent immunosuppressive effect and is useful as an inhibitor for the rejection reaction occurring in organ or bone marrow transplantation, and as a preventive or remedy for articular rheumatism, atopic eczema (dermatitis), Behcet's disease, uveal disease, systemic lupus erythematosus, Sjögren's syndrome, multiple sclerosis, myasthenia gravis, type I diabetes, endocrine ophthalmopathy, primary biliary, cirrhosis, Crohn's disease, glomerulonephritis, sarcoidosis, psoriasis, pemphigus, aplastic anemia, idiopathic thrombocytopenic purpura, allergy, polyarteritis nodosa, progressive systemic sclerosis, mixed connective-tissue disease, aortitis syndrome, polymyositis, dermatomyositis, Wegener's granuloma, ulcerative colitis, active chronic hepatitis, autoimmune hemolytic anemia, Evans' syndrome, bronchial asthma and pollinosis. It is useful also as an antifingal agent and hair growth stimulant.
    • 每个符号的苯甲醛的苯化合物如说明书中所定义; 其光学活性异构体或其盐,含有它们的药用组合物和含有该活性成分的免疫抑制剂。该化合物,旋光异构体或盐具有优异的免疫抑制作用,可用作抑制反应发生的抑制剂 在器官或骨髓移植中,作为关节风湿病,特应性湿疹(皮炎),贝切特氏病,葡萄膜疾病,系统性红斑狼疮,Sjögren综合征,多发性硬化症,重症肌无力,I型糖尿病,内分泌眼病,原发性 胆汁,肝硬化,克罗恩病,肾小球肾炎,结节病,牛皮癣,天疱疮,再生障碍性贫血,特发性血小板减少性紫癜,变态反应,结节性多动脉炎,进行性系统性硬化症,混合性结缔组织病,主动脉炎综合征,多发性肌炎,皮肌炎,韦格纳肉芽肿,溃疡性结肠炎, 活动性慢性肝炎,自身免疫性溶血性贫血, 伊文思综合征,支气管哮喘和花粉症。 它也可用作抗衰老剂和毛发生长兴奋剂。