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51. 发明授权

US06720322B2 Butyne diol derivatives 失效
标题翻译：丁炔二醇衍生物
公开(公告)号：US06720322B2
公开(公告)日：2004-04-13
申请号：US10168752
申请日：2002-06-24
申请人： Martin Bolli , Christoph Boss , Martine Clozel , Walter Fischli
发明人： Martin Bolli , Christoph Boss , Martine Clozel , Walter Fischli
IPC分类号： A61K315377
CPC分类号： C07D239/47 , C07D239/52 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/14
摘要： The present invention relates to novel butyne diol derivatives of the general formula I and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more compounds of the general formula I and especially their use as endothelin receptor antagonists.
摘要翻译：本发明涉及通式Ⅰ的新型丁炔二醇衍生物及其在制备药物组合物中作为活性成分的用途。本发明还涉及包括制备化合物的方法，含有一种或多种通式I化合物的药物组合物，特别是其作为内皮素受体拮抗剂的用途的相关方面。

52. 发明授权

US5270313A Sulfonamides and uses 失效
标题翻译：磺酰胺和用途
公开(公告)号：US5270313A
公开(公告)日：1993-12-14
申请号：US869274
申请日：1992-04-15
申请人： Kaspar Burri , Martine Clozel , Walter Fischli , Georges Hirth , Bernd M. Loffler , Henri Ramuz
发明人： Kaspar Burri , Martine Clozel , Walter Fischli , Georges Hirth , Bernd M. Loffler , Henri Ramuz
IPC分类号： A61K31/505 , A61K31/495 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , C07D239/42 , C07D239/46 , C07D239/47 , C07D239/48 , C07D239/69 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/12
CPC分类号： C07D401/12 , C07D239/69 , C07D405/12 , C07D409/12 , C07D413/10
摘要： Sulfonamides of formula I, in which the symbols R.sup.1 -R.sup.6, X, Y and n have the significance given in the description and which are in part novel compounds, and salts thereof, which can be used as active ingredients for the manufacture of medicaments for the treatment of circulatory disorders, especially hypertension, ischemia, vasospasms and angina pectoris, are described.
摘要翻译：式I的磺酰胺，其中符号R1-R6，X，Y和n具有在说明书中给出的并且部分新化合物的含义及其盐，其可以用作制备药物的活性成分描述了循环系统疾病，特别是高血压，局部缺血，血管痉挛和心绞痛的治疗。

53. 发明授权

US06596719B1 6 alkoxy-4-pyrimidinyl bis-sulfonamides 失效
标题翻译： 6烷氧基-4-嘧啶基双磺酰胺
公开(公告)号：US06596719B1
公开(公告)日：2003-07-22
申请号：US10031555
申请日：2001-08-16
申请人： Martin Bolli , Christoph Boss , Martine Clozel , Walter Fischli
发明人： Martin Bolli , Christoph Boss , Martine Clozel , Walter Fischli
IPC分类号： C07D23947
CPC分类号： C07D239/69 , C07D401/12
摘要： The present invention relates to novel bis-sulfonamides represented, for example, by formula I below and a pure diastereomer, a mixture of diastereomers, a diastereomeric racemate, a mixture of diastereomeric racemates and meso-forms and a pharmaceutically acceptable salt thereof, wherein R1 represents aryl; aryl-lower alkyl; aryl-lower alkenyl; heteroaryl; or heteroaryl-lower alkyl; and R2 represents lower alkyl; trifluoromethyl; lower alkoxy-lower alkyl; lower alkenyl; lower alkynyl; aryl; aryl-lower alkyl; aryl-lower alkenyl; heterocyclyl; heterocyclyl-lower alkyl; heteroaryl; heteroaryl-lower alkyl; cycloalkyl; or cycloalkyl-lower alkyl. The present invention also relates to a process for manufacturing those compounds, pharmaceutical compositions containing one or more of those compounds as endothelin antagonists, and a method of treating a subject having a disorder involving endothelin with the compounds of the invention.
摘要翻译：本发明涉及例如由下式I表示的新型双磺酰胺和纯非对映异构体，非对映异构体的混合物，非对映体外消旋体，非对映体外消旋体和内消旋体的混合物及其药学上可接受的盐，其中R 1 表示芳基; 芳基 - 低级烷基; 芳基 - 低级烯基; 杂芳基; 或杂芳基 - 低级烷基; 并且R 2表示低级烷基; 三氟甲基低级烷氧基 - 低级烷基; 低级链烯基低级炔基芳基; 芳基 - 低级烷基; 芳基 - 低级烯基; 杂环基杂环基 - 低级烷基; 杂芳基; 杂芳基 - 低级烷基; 环烷基或环烷基 - 低级烷基。本发明还涉及制备这些化合物的方法，含有作为内皮素拮抗剂的那些化合物中的一种或多种的药物组合物，以及本发明化合物治疗患有内皮素疾病的受试者的方法。

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