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1. 发明授权

US06803375B1 Non-peptide inhibition of T-lymphocyte activation and therapies related thereto 失效
标题翻译：非肽抑制T淋巴细胞活化和与之相关的疗法
公开(公告)号：US06803375B1
公开(公告)日：2004-10-12
申请号：US09479391
申请日：2000-01-06
申请人： K. George Chandy , Heike Wulff
发明人： K. George Chandy , Heike Wulff
IPC分类号： A01K43495
CPC分类号： A61K31/415 , A61K31/065 , A61K31/16 , A61K31/277 , A61K31/40 , A61K31/41 , A61K31/425
摘要： Compounds, preparations and methods for immunosuppressive treatment of autoimmune disorders, graft rejection and/or graft/host disease. Therapeutically effective amounts of certain substituted triarylmethane compounds, such as 1-[(2-chlorophenyl)diphenylmethyl]-1H-pyrazole, are administered to mammalian patients to selectively inhibit the calcium-activated K+ channel (IKCa1) in lymphocytes, monocytes, macrophages, platelets or endothelial cells without concomitant inhibition of P450-dependent enzyme systems, resulting in reduction of antigen-, cytokine-, or mitogen-induced calcium entry through store operated calcium channels in these cells, suppression of cytokine production by these cells, and inhibition of activation of these cells. Such inhibition of the Ca++ activated K+ channel (IKCa1) prevents the pre-Ca++ stage of cell activation and thus causes immunosuppression and an anti-inflammatory response.
摘要翻译：用于免疫抑制治疗自身免疫疾病，移植物排斥和/或移植物/宿主疾病的化合物，制剂和方法。向哺乳动物患者施用治疗有效量的某些取代的三芳基甲烷化合物，例如1 - [（2-氯苯基）二苯基甲基] -1H-吡唑，以选择性抑制淋巴细胞，单核细胞中钙激活的K +通道（IKCa1），巨噬细胞，血小板或内皮细胞，而不伴随着P450依赖性酶系统的抑制，导致通过这些细胞中存储的钙通道降低抗原，细胞因子或丝裂原诱导的钙进入，抑制这些细胞的细胞因子产生，并抑制这些细胞的活化。 Ca ++活化的K +通道（IKCa1）的这种抑制可预防细胞活化前的Ca ++阶段，从而引起免疫抑制和抗炎反应。

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