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1. 发明申请

WO2004091502A3 1,2,4-OXADIAZOLE BENZOIC ACID COMPOUNDS 审中-公开
公开(公告)号：WO2004091502A3
公开(公告)日：2004-10-28
申请号：PCT/US2004/011106
申请日：2004-04-09
申请人： PTC THERAPEUTICS, INC. , KARP, Gary, Mitchell , HWANG, Seongwoo , CHEN, Guangming , ALMSTEAD, Neil, Gregory
发明人： KARP, Gary, Mitchell , HWANG, Seongwoo , CHEN, Guangming , ALMSTEAD, Neil, Gregory
IPC分类号： C07D271/06
摘要： Novel 1,2,4-oxadiazole benzoic acid compounds, methods of using and pharmaceutical compositions comprising an 1,2,4-oxadiazole benzoic acid derivative are disclosed. The methods include methods of treating or preventing a disease ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay, or ameliorating one or more symptoms associated therewith.

2. 发明申请

WO2004010106A2 METHODS FOR IDENTIFYING SMALL MOLEDULES THAT MODULATE PREMATURE TRANSLATION TERMINATION AND NONSENSE MEDIATED mRNA DECAY 审中-公开
标题翻译：鉴定调节早期翻译终止和非感染介导的mRNA衰变的小模型的方法
公开(公告)号：WO2004010106A2
公开(公告)日：2004-01-29
申请号：PCT/US2003/023075
申请日：2003-07-24
申请人： PTC THERAPEUTICS, INC. , WELCH, Ellen, M. , ALMSTEAD, Neil, Gregory , RANDO, Robert, F. , PELLEGRINI, Mathew, C.
发明人： WELCH, Ellen, M. , ALMSTEAD, Neil, Gregory , RANDO, Robert, F. , PELLEGRINI, Mathew, C.
IPC分类号： G01N
CPC分类号： B82Y30/00 , G01N33/5308 , G01N2500/04
摘要： The present invention relates to a method for screening and identifying compounds that modulate premature translation termination and/or nonsense-mediated messenger ribonucleic acid ("mRNA") by interacting with a preselected target ribonucleic acid ("RNA"). In particular, the present invention relates to identifying compounds that bind to regions of the 28S ribosomal RNA ("rRNA") and analogs thereof. Direct, noncompetitive binding assays are advantageously used to screen libraries of compounds for those that selectively bind to a preselected target RNA. Binding of target RNA molecules to a particular compound is detected using any physical method that measures the altered physical property of the target RNA bound to a compound. The structure of the compound attached to the labeled RNA is also determined. The methods used will depend, in part, on the nature of the library screened. The methods of the present invention provide a simple, sensitive assay for high-throughput screening of libraries of compounds to identify pharmaceutical leads.
摘要翻译：本发明涉及用于筛选和鉴定通过与预先选择的靶核糖核酸（“mRNA”）相互作用来调节过早翻译终止和/或无义介导的信使核糖核酸（“mRNA”）的化合物 ; RNA＆QUOT）。具体而言，本发明涉及鉴定与28S核糖体RNA（“rRNA”）及其类似物的区域结合的化合物。直接非竞争性结合测定法有利地用于筛选选择性结合预先选择的靶RNA的化合物文库。使用任何物理方法检测靶RNA分子与特定化合物的结合，所述物理方法测量与化合物结合的靶RNA的改变的物理性质。与标记的RNA连接的化合物的结构也被确定。所用的方法部分取决于筛选的图书馆的性质。本发明的方法提供了用于高通量筛选化合物文库以鉴定药物导致的简单，灵敏的测定。

3. 发明授权

EP1618098B1 1,2,4-OXADIAZOLE BENZOIC ACID COMPOUNDS AND THEIR USE FOR NONSENSE SUPPRESSION AND THE TREATMENT OF DISEASE 有权
标题翻译： 1,2,4-OXADIAZOLBENZOESÄUREVERBINDUNGEN和它们在义抑制和治疗疾病的
公开(公告)号：EP1618098B1
公开(公告)日：2014-11-19
申请号：EP04759404.9
申请日：2004-04-09
申请人： PTC Therapeutics, Inc.
发明人： KARP, Gary, Mitchell , HWANG, Seongwoo , CHEN, Guangming , ALMSTEAD, Neil, Gregory , MOON, Young-Choon
IPC分类号： C07D271/06 , A61P35/00 , A61K31/4245
CPC分类号： A61K31/4245 , A61K9/0053 , A61K9/12 , A61K9/48 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/5377 , A61K31/655 , A61K45/06 , A61P27/02 , C07D271/06 , C07D271/12 , C07D285/14 , C07D413/02 , C07D413/04 , C07D413/10
摘要： The present invention relates to a compound 3-[5-(2-Fluoro-phenyl)-[1,2,4]oxadiazol-3-yl]-benzoic acid, having the structure: or a pharmaceutically acceptable salt thereof. The present invention also relates to a pharmaceutical composition and a single unit dosage thereof, as well as the said compound for use in a method of treating, preventing or ameliorating diseases as defined herein.

4. 发明公开

EP1543157A2 METHODS FOR IDENTIFYING SMALL MOLEDULES THAT MODULATE PREMATURE TRANSLATION TERMINATION AND NONSENSE MEDIATED mRNA DECAY 审中-公开
标题翻译：于鉴定小方法，早期的翻译和无义介导的mRNA拆卸控制调节分子
公开(公告)号：EP1543157A2
公开(公告)日：2005-06-22
申请号：EP03765998.4
申请日：2003-07-24
申请人： PTC Therapeutics, Inc.
发明人： WELCH, Ellen, M. , ALMSTEAD, Neil, Gregory , RANDO, Robert, F. , PELLEGRINI, Mathew, C.
IPC分类号： C12Q1/68
CPC分类号： B82Y30/00 , G01N33/5308 , G01N2500/04
摘要： The present invention relates to a method for screening and identifying compounds that modulate premature translation termination and/or nonsense-mediated messenger ribonucleic acid ('mRNA') by interacting with a preselected target ribonucleic acid ('RNA'). In particular, the present invention relates to identifying compounds that bind to regions of the 28S ribosomal RNA ('rRNA') and analogs thereof. Direct, noncompetitive binding assays are advantageously used to screen libraries of compounds for those that selectively bind to a preselected target RNA. Binding of target RNA molecules to a particular compound is detected using any physical method that measures the altered physical property of the target RNA bound to a compound. The structure of the compound attached to the labeled RNA is also determined. The methods used will depend, in part, on the nature of the library screened. The methods of the present invention provide a simple, sensitive assay for high-throughput screening of libraries of compounds to identify pharmaceutical leads.

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