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公开(公告)号:US06489327B1
公开(公告)日:2002-12-03
申请号:US09601317
申请日:2000-10-20
申请人: Thomas Bär , Thomas Martin , Josef Stadlwieser , Wolf-Rüdiger Ulrich , Andreas Dominik , Ulrich Thibaut , Daniela Bundschuh , Rolf Beume , Karl-Josef Goebel , Wolfram Bode , Luis Moroder , Pedro Jose Barbosa Pereira , Andreas Bergner , Robert Huber , Christian Sommerhoff , Norbert Schaschke
发明人: Thomas Bär , Thomas Martin , Josef Stadlwieser , Wolf-Rüdiger Ulrich , Andreas Dominik , Ulrich Thibaut , Daniela Bundschuh , Rolf Beume , Karl-Josef Goebel , Wolfram Bode , Luis Moroder , Pedro Jose Barbosa Pereira , Andreas Bergner , Robert Huber , Christian Sommerhoff , Norbert Schaschke
IPC分类号: A61K31495
CPC分类号: C07D213/81 , C07C279/16 , C07D211/58 , C07D213/82 , C07D295/185 , C07D295/215 , C07D401/14
摘要: The invention relates to novel inhibitors of human tryptase which are used in the pharmaceutical industry for the production of medicaments.
摘要翻译: 本发明涉及用于药物工业用于生产药物的人类类胰蛋白酶的新型抑制剂。
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公开(公告)号:US06613769B1
公开(公告)日:2003-09-02
申请号:US09601318
申请日:2001-01-22
申请人: Wolfram Bode , Luis Moroder , Pedro Jose Barbosa Pereira , Andreas Bergner , Robert Huber , Christian Sommerhoff , Norbert Schaschke , Thomas Bär , Thomas Martin , Josef Stadlwieser , Wolf-Rüdiger Ulrich , Andreas Dominik , Ulrich Thibaut , Daniela Bundschuh , Rolf Beume , Karl-Josef Goebel
发明人: Wolfram Bode , Luis Moroder , Pedro Jose Barbosa Pereira , Andreas Bergner , Robert Huber , Christian Sommerhoff , Norbert Schaschke , Thomas Bär , Thomas Martin , Josef Stadlwieser , Wolf-Rüdiger Ulrich , Andreas Dominik , Ulrich Thibaut , Daniela Bundschuh , Rolf Beume , Karl-Josef Goebel
IPC分类号: A61K31495
CPC分类号: C07D213/81 , C07C237/22 , C07C279/16 , C07D211/58 , C07D213/82 , C07D295/185 , C07D295/215 , C07D401/14
摘要: The invention relates to bifunctional tryptase inhibitors of formula (I) wherein H1 and H2 comprise a Q group and L is a linker of formula and the conformation of the H1, H2 and L groups is such that the groups are separated by a distance of from 20 to 45 Å. Pharmaceutical compositions and crystal forms of the compounds are described in addition to methods for producing and identifying such compounds, as well as the use of such compounds in methods of treating allergic and inflammatory diseases.
摘要翻译: 本发明涉及式(I)的双功能类胰蛋白酶抑制剂,其中H1和H2包含Q基团,L是式的连接体,并且H1,H2和L基团的构象使得基团被隔开距离为20 至45Å。 除了制备和鉴定这些化合物的方法之外,还描述了化合物的药物组合物和晶体形式,以及这些化合物在治疗过敏性和炎性疾病的方法中的用途。
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