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1. 发明申请

WO2005061483A2 MODULATORS OF PERIPHERAL 5-HT RECEPTORS 审中-公开
标题翻译：外周5-HT受体的调节剂
公开(公告)号：WO2005061483A2
公开(公告)日：2005-07-07
申请号：PCT/NO2004/000399
申请日：2004-12-23
申请人： BIO-MEDISINSK INNOVASJON AS , KLAVENESS, Jo , LEVY, Finn, Olav , BRUDELI, Bjarne
发明人： KLAVENESS, Jo , LEVY, Finn, Olav , BRUDELI, Bjarne
IPC分类号： C07D401/00
CPC分类号： C07D401/12 , A61K31/343 , A61K31/404 , A61K31/415 , A61K31/4184 , A61K31/428 , A61K31/445 , C07D209/14 , C07D211/22 , C07D211/26 , C07D211/58 , C07D405/12
摘要： Novel modulators of 5-HT4 receptors have been developed which have a selectivity for peripheral receptors rather than those of the central nervous systems. Theses include novel derivatives of known modulators as well as entirely novel entities. Surprisingly, the derivatised compounds of the known modulators maintain a high binding affinity to 5-HT4 receptors, despite the presence of an acidic moiety at the end of an optional chain. The entirely novel entities also exhibit good binding affinity to 5-HT4 receptors. All of the compounds of the invention have a common motif which includes a basic nitrogen moiety and an acidic moiety. The compounds of the invention, due at least in part to their high ionisation potential at physiological pH, have the unique properties of selectively for peripheral 5HT4 receptors over those of the CNS, good binding affinity, and selectively of 5HT4 receptors over other serotonin receptors.
摘要翻译：新型的5-HT 4受体调节剂已被开发出来，它们对外周受体而不是中枢神经系统的那些具有选择性。论文包括已知调制器的新颖衍生物以及完全新颖的实体。令人惊讶的是，尽管在任选链末端存在酸性部分，已知调节剂的衍生化合物仍维持对5-HT 4受体的高结合亲和力。全新的实体也表现出对5-HT 4受体的良好结合亲和力。本发明的所有化合物都具有包含碱性氮部分和酸性部分的共同基序。本发明化合物至少部分归因于它们在生理pH下的高电离电位，对于外周5HT4受体选择性优于CNS的独特性质，具有良好的结合亲和性，并且选择性地选择性拮抗其他血清素受体上的5HT4受体。

2. 发明申请

WO2009024591A1 PVII PHAGE DISPLAY 审中-公开
标题翻译： PVII PHAGE显示
公开(公告)号：WO2009024591A1
公开(公告)日：2009-02-26
申请号：PCT/EP2008/060908
申请日：2008-08-20
申请人： Bio-Medisinsk Innovasjon AS , LØSET, Geir Åge
发明人： LØSET, Geir Åge
IPC分类号： C12N15/10 , C12N15/62 , C07K19/00
CPC分类号： C12N15/1037 , C07K14/005 , C07K2319/20 , C12N2795/14122
摘要： The present invention provides an alternative scaffold for peptides displayed on filamentous phages through novel fusion proteins primarily originating from pVII. Libraries of filamentous phages can be created from fusion proteins, and a phage display system comprising a phagemid and a helper phage is a part of the invention.An aspect of the invention is a kit containing a phage display system comprising a phagemid and a helper phage that contains a nucleic acid encoding the fusion protein of the invention.
摘要翻译：本发明提供了通过主要来自pVII的新型融合蛋白在丝状噬菌体上显示的肽的替代支架。丝状噬菌体的文库可以由融合蛋白产生，并且包含噬菌粒和辅助噬菌体的噬菌体展示系统是本发明的一部分。本发明的一个方面是包含噬菌体展示系统的试剂盒，其包含噬菌粒和辅助噬菌体其含有编码本发明的融合蛋白的核酸。

3. 发明申请

WO2007007072A1 5-HTX MODULATORS 审中-公开
标题翻译： 5-HTX调制器
公开(公告)号：WO2007007072A1
公开(公告)日：2007-01-18
申请号：PCT/GB2006/002542
申请日：2006-07-07
申请人： BIO-MEDISINSK INNOVASJON AS , COCKBAIN, Julian , KLAVENESS, Jo , BRUDELI, Bjame , LEVY, Finn, Olav
发明人： KLAVENESS, Jo , BRUDELI, Bjame , LEVY, Finn, Olav
IPC分类号： C07D401/06 , C07D401/04 , C07D401/12 , C07D211/58 , C07D211/22 , C07D498/04 , C07D405/12 , C07D405/14 , A61K31/517 , A61K31/4468 , A61K31/445 , A61K31/5365 , A61K31/501 , A61P25/00
CPC分类号： C07D211/62 , C07D207/14 , C07D209/42 , C07D209/80 , C07D211/22 , C07D211/26 , C07D211/58 , C07D211/70 , C07D295/26 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07D471/04
摘要： This invention relates to compounds which bind to serotonin receptors inside or outside the central nervous system, in particular compounds which bind to the 5-HT 2 or 5-HT 7 receptors, their preparation and use, compositions containing them, and methods of treatment using them.
摘要翻译：本发明涉及在中枢神经系统内部或外部结合血清素受体的化合物，特别是结合5-HT 2或5-HT 7受体的化合物，其制备和使用，含有它们的组合物和使用它们的治疗方法。

4. 发明申请

WO2005061483A3 MODULATORS OF PERIPHERAL 5-HT RECEPTORS 审中-公开
标题翻译：外周5-HT受体的调节剂
公开(公告)号：WO2005061483A3
公开(公告)日：2005-10-27
申请号：PCT/NO2004000399
申请日：2004-12-23
申请人： BIO MEDISINSK INNOVASJON AS , KLAVENESS JO , LEVY FINN OLAV , BRUDELI BJARNE
发明人： KLAVENESS JO , LEVY FINN OLAV , BRUDELI BJARNE
IPC分类号： A61K31/343 , A61K31/404 , A61K31/415 , A61K31/4184 , A61K31/428 , A61K31/445 , C07D209/14 , C07D211/00 , C07D211/22 , C07D211/26 , C07D211/58 , C07D401/00 , C07D401/12 , C07D405/12 , C07D498/04 , A61P1/00 , A61P9/00 , A61P13/00
CPC分类号： C07D401/12 , A61K31/343 , A61K31/404 , A61K31/415 , A61K31/4184 , A61K31/428 , A61K31/445 , C07D209/14 , C07D211/22 , C07D211/26 , C07D211/58 , C07D405/12
摘要： Novel modulators of 5-HT4 receptors have been developed which have a selectivity for peripheral receptors rather than those of the central nervous systems. Theses include novel derivatives of known modulators as well as entirely novel entities. Surprisingly, the derivatised compounds of the known modulators maintain a high binding affinity to 5-HT4 receptors, despite the presence of an acidic moiety at the end of an optional chain. The entirely novel entities also exhibit good binding affinity to 5-HT4 receptors. All of the compounds of the invention have a common motif which includes a basic nitrogen moiety and an acidic moiety. The compounds of the invention, due at least in part to their high ionisation potential at physiological pH, have the unique properties of selectively for peripheral 5HT4 receptors over those of the CNS, good binding affinity, and selectively of 5HT4 receptors over other serotonin receptors.
摘要翻译：已经开发了具有对外周受体而不是中枢神经系统的选择性的5-HT 4受体的新型调节剂。论文包括已知调制剂的新型衍生物以及完全新颖的实体。令人惊奇的是，尽管已知调节剂的衍生化合物在任选链的末端存在酸性部分，但仍保持与5-HT 4受体的高结合亲和力。完全新颖的实体也表现出对5-HT4受体的良好的结合亲和力。本发明的所有化合物都具有共同的基序，其包括碱性氮部分和酸性部分。本发明的化合物至少部分地由于其在生理pH下的高电离电位具有对于周围5HT4受体的选择性优于CNS的那些的独特性质，良好的结合亲和力以及5HT4受体的选择性超过其他5-羟色胺受体。

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