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公开(公告)号：US07368467B2
公开(公告)日：2008-05-06
申请号：US11075629
申请日：2005-03-07
IPC分类号： A61K31/4184 , C07D233/54 , C07D235/04 , C07D403/12
CPC分类号： C07D233/84 , A61K31/4164 , A61K31/4178 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D417/12 , C07D417/14
摘要： The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of ion channel function, and treatment of disease and disease symptoms, particularly those mediated by certain calcium channel subtype targets.
摘要翻译： 本发明涉及化合物，包含该化合物的组合物，以及使用该化合物和化合物组合物的方法。 本文所述的化合物，组合物和方法可用于治疗性调节离子通道功能，以及治疗疾病和疾病症状，特别是由某些钙通道亚型靶标介导的那些症状。
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公开(公告)号：US20100267697A1
公开(公告)日：2010-10-21
申请号：US12518342
申请日：2007-12-11
申请人： Vincent P. Galullo , Robert Zelle , Danielle Soenen , Christopher Todd Baker , Paul Will , Hormoz Mazdiyasni , Jinsong Guo , Andrew Fensome , Jeffrey Curtis Kern , William Jay Moore , Edward George Melenski , Justin Kaplan
发明人： Vincent P. Galullo , Robert Zelle , Danielle Soenen , Christopher Todd Baker , Paul Will , Hormoz Mazdiyasni , Jinsong Guo , Andrew Fensome , Jeffrey Curtis Kern , William Jay Moore , Edward George Melenski , Justin Kaplan
IPC分类号： A61K31/5513 , A61K31/55 , A61K31/54 , A61K31/535 , A61K31/5355 , A61K31/4995 , A61K31/501 , A61K31/497 , A61K31/506 , A61K31/44 , A61K31/4725 , A61K31/426 , A61K31/4709 , A61K31/4458 , A61K31/4453 , A61K31/4402 , A61K31/445 , A61K31/166 , C07D403/04 , C07D401/04 , C07D413/04 , C07D417/04 , C07D413/12 , C07D403/12 , C07D241/36 , C07D497/10 , C07D217/00 , C07D215/00 , C07D401/12 , C07D211/98 , C07D213/04 , C07D405/12 , C07D213/73 , C07D277/593 , C07C233/42
CPC分类号： C07D213/72 , C07D277/42
摘要： The present teachings provide compounds of Formula (I) and pharmaceutically acceptable salts, hydrates, and esters thereof, wherein Ar, R1, R2, R3, p, and X are defined herein. The present teachings also provide processes for producing said compounds and their pharmaceutically acceptable salts, hydrates and esters, and methods of treating a pathological condition or disorder, or alleviating a symptom thereof, using said compounds including their pharmaceutically acceptable salts, hydrates and esters. The compounds can be useful in modulating ion channel activity including treating a variety of conditions associated with the abnormal modulation of one or more voltage-gated calcium channels.
摘要翻译： 本发明提供式（I）化合物及其药学上可接受的盐，水合物和酯，其中Ar，R 1，R 2，R 3，p和X如本文所定义。 本教导还提供使用所述化合物，包括其药学上可接受的盐，水合物和酯来制备所述化合物及其药学上可接受的盐，水合物和酯的方法，以及治疗病理状况或病症或减轻其症状的方法。 该化合物可用于调节离子通道活性，包括治疗与一个或多个电压门控钙通道的异常调节相关的多种病症。
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公开(公告)号：US20070281937A1
公开(公告)日：2007-12-06
申请号：US10592451
申请日：2005-03-07
申请人： Robert Zelle , Vincent Galullo , Christopher Baker , Paul Will , William Frazee , Hormoz Mazdiyasni , Jinsong Guo
发明人： Robert Zelle , Vincent Galullo , Christopher Baker , Paul Will , William Frazee , Hormoz Mazdiyasni , Jinsong Guo
IPC分类号： A61K31/4184 , A61K31/4164 , A61K31/4196 , A61K31/4245 , A61K31/428 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/5377 , A61P9/12 , A61P9/10 , A61P9/00 , A61P25/00 , A61P13/00 , A61K31/497 , A61K31/47 , A61K31/444 , A61K31/433 , A61K31/426 , A61K31/42 , A61K31/4178
CPC分类号： C07D403/12 , C07D233/84 , C07D249/12 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12
摘要： The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of ion channel function, and treatment of disease and disease symptoms, particularly those mediated by certain calcium channel subtype targets.
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公开(公告)号：US20080090891A1
公开(公告)日：2008-04-17
申请号：US11954894
申请日：2007-12-12
申请人： Robert Zelle , Vincent Galullo , Hormoz Mazdiyasni
发明人： Robert Zelle , Vincent Galullo , Hormoz Mazdiyasni
IPC分类号： A61K31/4178 , A61K31/4164 , A61P9/00
CPC分类号： C07D233/84 , A61K31/4164 , A61K31/4178 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D417/12 , C07D417/14
摘要： The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of ion channel function, and treatment of disease and disease symptoms, particularly those mediated by certain calcium channel subtype targets.
摘要翻译： 本发明涉及化合物，包含该化合物的组合物，以及使用该化合物和化合物组合物的方法。 本文所述的化合物，组合物和方法可用于治疗性调节离子通道功能，以及治疗疾病和疾病症状，特别是由某些钙通道亚型靶标介导的那些症状。
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公开(公告)号：US20050203159A1
公开(公告)日：2005-09-15
申请号：US11075629
申请日：2005-03-07
申请人： Robert Zelle , Vincent Galullo , Hormoz Mazdiyasni
发明人： Robert Zelle , Vincent Galullo , Hormoz Mazdiyasni
IPC分类号： A61K31/4166 , A61K31/4178 , C07D233/84 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D417/12 , C07D417/14
CPC分类号： C07D233/84 , A61K31/4164 , A61K31/4178 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D417/12 , C07D417/14
摘要： The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of ion channel function, and treatment of disease and disease symptoms, particularly those mediated by certain calcium channel subtype targets.
摘要翻译： 本发明涉及化合物，包含该化合物的组合物，以及使用该化合物和化合物组合物的方法。 本文所述的化合物，组合物和方法可用于治疗性调节离子通道功能，以及治疗疾病和疾病症状，特别是由某些钙通道亚型靶标介导的那些症状。
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公开(公告)号：US07547717B2
公开(公告)日：2009-06-16
申请号：US10592269
申请日：2005-03-07
申请人： Robert Zelle , Vincent P. Galullo
发明人： Robert Zelle , Vincent P. Galullo
IPC分类号： A61K31/4164 , C07D233/30
CPC分类号： C07D233/42 , C07D233/84 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D413/12 , C07D417/06 , C07D417/12
摘要： The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of ion channel function, and treatment of disease and disease symptoms, particularly those mediated by certain calcium channel subtype targets.
摘要翻译： 本发明涉及化合物，包含该化合物的组合物，以及使用该化合物和化合物组合物的方法。 本文所述的化合物，组合物和方法可用于治疗性调节离子通道功能，以及治疗疾病和疾病症状，特别是由某些钙通道亚型靶标介导的那些症状。
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公开(公告)号：US20080293722A1
公开(公告)日：2008-11-27
申请号：US10592893
申请日：2005-03-15
IPC分类号： A61K31/155 , A61P9/00 , A61P11/00 , A61P25/00 , C07C257/14 , C07D295/14 , C07D307/22 , A61K31/495 , C07D211/26 , C07D213/58 , A61K31/5375 , A61K31/4453 , A61K31/341 , A61K31/44
CPC分类号： C07D213/38 , C07C257/14 , C07D213/53 , C07D233/24
摘要： The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of ion channel function, and treatment of disease and disease symptoms, particularly those mediated by certain calcium channel subtype targets.
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公开(公告)号：US20080139560A1
公开(公告)日：2008-06-12
申请号：US10592208
申请日：2005-03-07
申请人： Robert Zelle , Vincent P. Galullo
发明人： Robert Zelle , Vincent P. Galullo
IPC分类号： A61K31/4196 , C07D249/12 , C07D413/06 , A61K31/4439 , A61P3/00 , A61P9/00 , A61K31/5377 , C07D401/06
CPC分类号： C07D249/12 , C07D401/06 , C07D403/06 , C07D417/06
摘要： The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of ion channel function, and treatment of disease and disease symptoms, particularly those mediated by certain calcium channel subtype targets.
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公开(公告)号：US20070208070A1
公开(公告)日：2007-09-06
申请号：US10592269
申请日：2005-03-07
申请人： Robert Zelle , Vincent Galullo
发明人： Robert Zelle , Vincent Galullo
IPC分类号： A61K31/4166 , A61K31/4178 , C07D403/02 , C07D233/42
CPC分类号： C07D233/42 , C07D233/84 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D413/12 , C07D417/06 , C07D417/12
摘要： The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of ion channel function, and treatment of disease and disease symptoms, particularly those mediated by certain calcium channel subtype targets.
摘要翻译： 本发明涉及化合物，包含该化合物的组合物，以及使用该化合物和化合物组合物的方法。 本文所述的化合物，组合物和方法可用于治疗性调节离子通道功能，以及治疗疾病和疾病症状，特别是由某些钙通道亚型靶标介导的那些症状。
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公开(公告)号：US20100029716A1
公开(公告)日：2010-02-04
申请号：US12296927
申请日：2007-04-10
申请人： Roger Tung , Robert Zelle
发明人： Roger Tung , Robert Zelle
IPC分类号： A61K31/47 , C07D215/00 , G01N31/00 , C12Q1/00
CPC分类号： C07D215/42 , Y10T436/10
摘要： The present invention relates to a novel derivative of Compound 1 selectively substituted with fluorine and/or deuterium and optionally further substituted with deuterium and 13C elsewhere in the molecule. The compounds of this invention are cholesterol esterase transfer protein inhibitors and possess unique biopharmaceutical and pharmacokinetic properties compared to Compound 1. They may also be used to accurately determine the concentration of Compound 1 in biological fluids and tissues and to determine metabolic patterns of Compound 1 and its isotopologues. The invention further provides compositions comprising these compounds and methods of treating diseases and conditions that are responsive to inhibition of cholesterol esterase transfer protein, alone and in combination with additional agents.
摘要翻译： 本发明涉及化合物1的新型衍生物，其选择性地被氟和/或氘取代并且任选进一步被分子中的氘和13C取代。 本发明的化合物是胆固醇酯酶转移蛋白抑制剂，与化合物1相比具有独特的生物药物和药代动力学特性。它们还可用于准确测定化合物1在生物流体和组织中的浓度，并确定化合物1和 其同位素学。 本发明进一步提供了包含这些化合物的组合物以及治疗单独和与其它试剂组合对胆固醇酯酶转移蛋白的抑制有反应的疾病和病症的方法。
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