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1. 发明授权

US06642249B2 Immunomodulating compounds 有权
标题翻译：免疫调节化合物
公开(公告)号：US06642249B2
公开(公告)日：2003-11-04
申请号：US10179731
申请日：2002-06-26
申请人： Per Axel Björk , Tomas Fex , Lars Olof Göran Pettersson , Pous Sørensen , Dorthe Da Graça Thrige
发明人： Per Axel Björk , Tomas Fex , Lars Olof Göran Pettersson , Pous Sørensen , Dorthe Da Graça Thrige
IPC分类号： A61K314745
CPC分类号： C07D471/04 , C07D491/04 , C07D495/04
摘要： The present invention relates to a novel heterocyclic compound, a pharmaceutical composition comprisining said compound, a method and use of said compound for clinical treatment of medical conditions which may benefit from immunomodulation, e.g. rheumatoid arthritis, multiple sclerosis, diabetes, asthma, transplantation, systemic lupus erythematosis and psoriasis. More particularly the present invention relates to novel heterocyclic compounds, which are CD80 antagonists capable of inhibiting the interactions between CD80 and CD28. A method of screening compounds for their ability of inhibiting ligand-induced co-stimulatory receptor internalization pathways in immune competent human cells is described. Said immune competent human cells are incubated at conditions capable of inducing co-stimulatory receptor internalization in the presence of at least one test compound and the suppression of the ligand-induced co-stimulatory receptor internalization determined. There is also described a kit for use in such a method, as well as an immunoregulatory drug capable of blocking down-modulation of a ligand-induced receptor.
摘要翻译：本发明涉及一种新的杂环化合物，包括所述化合物的药物组合物，所述化合物的方法和用途，用于临床治疗可受益于免疫调节的医学病症，例如，类风湿关节炎，多发性硬化症，糖尿病，哮喘，移植，系统性红斑狼疮和牛皮癣。更具体地说，本发明涉及能够抑制CD80和CD28之间相互作用的CD80拮抗剂的新型杂环化合物。描述了筛选化合物在免疫感受态人细胞中抑制配体诱导的共刺激受体内化途径的能力的方法。所述免疫感受态人细胞在能够在至少一种测试化合物存在下诱导共同刺激受体内化的条件下温育并测定配体诱导的共刺激受体内化的抑制。还描述了用于这种方法的试剂盒，以及能够阻断配体诱导受体下调的免疫调节药物。

2. 发明授权

US07674906B2 Tetracyclic immunomodulatory compounds 有权
标题翻译：四环免疫调节化合物
公开(公告)号：US07674906B2
公开(公告)日：2010-03-09
申请号：US10537538
申请日：2003-12-12
申请人： Ian Richard Matthews , Philip Huxley , Filippo Magaraci , Chris James Brennan , Muhammed Kamal Uddin , Lars Olof Göran Pettersson , Dorthe da Graca Thrige
发明人： Ian Richard Matthews , Philip Huxley , Filippo Magaraci , Chris James Brennan , Muhammed Kamal Uddin , Lars Olof Göran Pettersson , Dorthe da Graca Thrige
IPC分类号： C07D471/04 , A61K31/437
CPC分类号： C07D471/04
摘要： The present invention relates to novel heterocyclic compounds, to methods for their preparation, to compositions containing them, and to methods and use for clinical treatment of medical conditions which may benefit from immunomodulation, including rheumatoid arthritis, multiple sclerosis, diabetes, asthma, transplantation, systemic lupus erythematosis and psoriasis. More particularly, the present invention relates to novel heterocyclic compounds, which are CD80 antagonists capable of inhibiting the interactions between CD80 and CD28.
摘要翻译：本发明涉及新的杂环化合物，其制备方法，含有它们的组合物，以及用于临床治疗可能受益于免疫调节的医学病症的方法和用途，所述免疫调节包括类风湿性关节炎，多发性硬化，糖尿病，哮喘，移植，系统性红斑狼疮和牛皮癣。更具体地说，本发明涉及能够抑制CD80和CD28之间相互作用的CD80拮抗剂的新型杂环化合物。

3. 发明授权

US07081456B2 Immunomodulatory compounds 有权
标题翻译：免疫调节化合物
公开(公告)号：US07081456B2
公开(公告)日：2006-07-25
申请号：US10717519
申请日：2003-11-21
申请人： Ian Richard Matthews , Thomas Stephen Coulter , Chiara Ghiron , Chris James Brennan , Muhammed Kamal Uddin , Lars Olof Göran Pettersson , Dorthe da Graca Thrige , Philip Huxley
发明人： Ian Richard Matthews , Thomas Stephen Coulter , Chiara Ghiron , Chris James Brennan , Muhammed Kamal Uddin , Lars Olof Göran Pettersson , Dorthe da Graca Thrige , Philip Huxley
IPC分类号： C07D471/06 , C07D495/06 , A61K31/437 , A61K31/4162 , A61P37/02
CPC分类号： C07D519/00 , C07D471/04 , C07D491/04 , C07D495/04
摘要： The present invention relates to novel heterocyclic compounds, to methods for their preparation, to compositions containing them, and to methods and use for clinical treatment of medical conditions which may benefit from immunomodulation, including rheumatoid arthritis, multiple sclerosis, diabetes, asthma, transplantation, systemic lupus erythematosis and psoriasis. More particularly the present invention relates to novel heterocyclic compounds, which are CD80 antagonists capable of inhibiting the interactions between CD80 and CD28.
摘要翻译：本发明涉及新的杂环化合物，其制备方法，含有它们的组合物，以及用于临床治疗可能受益于免疫调节的医学病症的方法和用途，所述免疫调节包括类风湿性关节炎，多发性硬化，糖尿病，哮喘，移植，系统性红斑狼疮和牛皮癣。更具体地说，本发明涉及能够抑制CD80和CD28之间相互作用的CD80拮抗剂的新型杂环化合物。

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