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公开(公告)号：US20090069371A1
公开(公告)日：2009-03-12
申请号：US12274887
申请日：2008-11-20
申请人： Mitchell A. deLong , Marcos L. Sznaidman , Robert H. Oakley , Allen E. Eckhardt , Christine Hudson , Jeffrey D. Yingling , Michael Peel , Thomas E. Richardson , Clare Louise Murray , Byappanahally N. Narasinga Rao , Brian H. Heasley , Paresma R. Patel
发明人： Mitchell A. deLong , Marcos L. Sznaidman , Robert H. Oakley , Allen E. Eckhardt , Christine Hudson , Jeffrey D. Yingling , Michael Peel , Thomas E. Richardson , Clare Louise Murray , Byappanahally N. Narasinga Rao , Brian H. Heasley , Paresma R. Patel
IPC分类号： A61K31/47 , C07D217/22 , A61P27/02 , A61P9/00 , A61P1/00 , A61P15/08 , A61P35/00 , A61P19/08 , C12N5/00
CPC分类号： C07D217/02
摘要： Isoquinoline compounds with G are provided that influence, inhibit or reduce the action of a G-protein receptor kinase. Pharmaceutical compositions including therapeutically effective amounts of the isoquinoline compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, osteoporosis and glaucoma are also provided.
摘要翻译： 提供了具有G的异喹啉化合物，其影响，抑制或降低G蛋白受体激酶的作用。 还提供包含治疗有效量的异喹啉化合物和药学上可接受的载体的药物组合物。 还提供了使用化合物和/或组合物影响疾病状态或病症如癌症，骨质疏松症和青光眼的各种方法。
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公开(公告)号：US20100093790A1
公开(公告)日：2010-04-15
申请号：US12639670
申请日：2009-12-16
申请人： Mitchell A. deLong , Marcos L. Sznaidman , Robert H. Oakley , Allen E. Eckhardt , Christine Hudson , Jeffrey D. Yingling , Michael Peel , Thomas E. Richardson , Clare Louise Murray , Byappanahally N. Narasinga Rao , Brian H. Heasley , Paresma R. Patel
发明人： Mitchell A. deLong , Marcos L. Sznaidman , Robert H. Oakley , Allen E. Eckhardt , Christine Hudson , Jeffrey D. Yingling , Michael Peel , Thomas E. Richardson , Clare Louise Murray , Byappanahally N. Narasinga Rao , Brian H. Heasley , Paresma R. Patel
IPC分类号： A61K31/472 , C07D217/02 , C07D401/12 , C12N5/00 , A61K31/4725 , A61P27/02 , A61P19/00 , A61P9/00 , A61P13/12
CPC分类号： C07D217/02
摘要： Isoquinoline compounds with G are provided that influence, inhibit or reduce the action of a G-protein receptor kinase. Pharmaceutical compositions including therapeutically effective amounts of the isoquinoline compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, osteoporosis and glaucoma are also provided.
摘要翻译： 提供了具有G的异喹啉化合物，其影响，抑制或降低G蛋白受体激酶的作用。 还提供包含治疗有效量的异喹啉化合物和药学上可接受的载体的药物组合物。 还提供了使用化合物和/或组合物影响疾病状态或病症如癌症，骨质疏松症和青光眼的各种方法。
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公开(公告)号：US07470787B2
公开(公告)日：2008-12-30
申请号：US11485172
申请日：2006-07-11
申请人： Mitchell A. deLong , Marcos L. Sznaidman , Robert H. Oakley , Allen E. Eckhardt , Christine Hudson , Jeffrey D. Yingling , Michael Peel , Thomas E. Richardson , Claire Louise Murray , Byappanahally N. Narasinga Rao , Brian H. Heasley , Paresma R. Patel
发明人： Mitchell A. deLong , Marcos L. Sznaidman , Robert H. Oakley , Allen E. Eckhardt , Christine Hudson , Jeffrey D. Yingling , Michael Peel , Thomas E. Richardson , Claire Louise Murray , Byappanahally N. Narasinga Rao , Brian H. Heasley , Paresma R. Patel
IPC分类号： C07D217/00 , C07D401/00 , C07D215/00
CPC分类号： C07D217/02
摘要： Isoquinoline compounds with G are provided that influence, inhibit or reduce the action of a G-protein receptor kinase. Pharmaceutical compositions including therapeutically effective amounts of the isoquinoline compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, osteoporosis and glaucoma are also provided.
摘要翻译： 提供了具有G的异喹啉化合物，其影响，抑制或降低G蛋白受体激酶的作用。 还提供包含治疗有效量的异喹啉化合物和药学上可接受的载体的药物组合物。 还提供了使用化合物和/或组合物影响疾病状态或病症如癌症，骨质疏松症和青光眼的各种方法。
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公开(公告)号：US08637532B2
公开(公告)日：2014-01-28
申请号：US13148903
申请日：2010-02-04
申请人： Amanda E. Sutton , Ruoxi Lan , Thomas E. Richardson , David Perrey , Harold George Vandeveer , Bayard R. Huck , Srinivasa R. Karra , Xiaoling Chen , Yufang Xiao , Lesley Liu-Bujalski , Andreas Goutopoulos , Frank Stieber , Brian L. Hodous , Hui Qiu , Reinaldo Jones , Brian H. Heasley
发明人： Amanda E. Sutton , Ruoxi Lan , Thomas E. Richardson , David Perrey , Harold George Vandeveer , Bayard R. Huck , Srinivasa R. Karra , Xiaoling Chen , Yufang Xiao , Lesley Liu-Bujalski , Andreas Goutopoulos , Frank Stieber , Brian L. Hodous , Hui Qiu , Reinaldo Jones , Brian H. Heasley
IPC分类号： A01N43/54 , A61K31/517 , C07D239/72 , C07D401/00
CPC分类号： C07D215/04 , A61K31/47 , C07D239/94 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04
摘要： The invention provides novel substituted amino azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
摘要翻译： 本发明提供根据式（I）的新型取代的氨基氮杂环甲酰胺化合物，其用于治疗过度增殖性疾病如癌症的制备和用途。
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公开(公告)号：US20120046269A1
公开(公告)日：2012-02-23
申请号：US13148903
申请日：2010-02-04
申请人： Amanda E. Sutton , Ruoxi Lan , Thomas E. Richardson , David Perrey , Harold George Vandeveer , Bayard R. Huck , Srinivasa R. Karra , Xiaoling Chen , Lesley Liu-Bujalski , Andreas Goutopoulos , Frank Steiber , Brian L. Hodous , Hui Qiu , Reinaldo C. Jones , Brian H. Heasley
发明人： Amanda E. Sutton , Ruoxi Lan , Thomas E. Richardson , David Perrey , Harold George Vandeveer , Bayard R. Huck , Srinivasa R. Karra , Xiaoling Chen , Lesley Liu-Bujalski , Andreas Goutopoulos , Frank Steiber , Brian L. Hodous , Hui Qiu , Reinaldo C. Jones , Brian H. Heasley
IPC分类号： A61K31/517 , C07D401/12 , A61K31/4709 , C07D405/12 , C07D409/12 , C07D403/12 , C07D401/04 , C07D413/12 , A61K31/5377 , C07D413/04 , C07D401/14 , C07D417/12 , C07D413/14 , C07D409/10 , C07D471/04 , A61P35/00 , A61P29/00 , A61P1/18 , A61P13/12 , A61P17/00 , A61P9/00 , A61P17/06 , A61P3/10 , A61P27/02 , C07D239/94
CPC分类号： C07D215/04 , A61K31/47 , C07D239/94 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04
摘要： The invention provides novel substituted amino azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
摘要翻译： 本发明提供根据式（I）的新型取代的氨基氮杂环甲酰胺化合物，其用于治疗过度增殖性疾病如癌症的制备和用途。
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公开(公告)号：US09181226B2
公开(公告)日：2015-11-10
申请号：US13551072
申请日：2012-07-17
申请人： Henry Yu , Jiezhen Li , Thomas E. Richardson , Pandi Bharathi , Brian H. Heasley , Andreas Goutopoulos
发明人： Henry Yu , Jiezhen Li , Thomas E. Richardson , Pandi Bharathi , Brian H. Heasley , Andreas Goutopoulos
IPC分类号： A61K31/496 , C07D405/12 , C07D403/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D403/14 , C07D409/10 , C07D409/12 , C07D409/14 , C07D417/14 , C07D413/12
CPC分类号： C07D417/12 , A61K31/454 , A61K31/496 , A61K31/498 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/551 , C07D233/64 , C07D263/34 , C07D307/68 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/10 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14
摘要： Novel benzamide derivatives of formula (I) wherein W1, W2, R1 to R7, R8, X and Y have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.
摘要翻译： 其中W 1，W 2，R 1至R 7，R 8，X和Y具有根据权利要求的含义的式（I）的新型苯甲酰胺衍生物是FSH受体的正变构调节剂，并且可以用于治疗 的生育障碍。
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公开(公告)号：US20140107156A1
公开(公告)日：2014-04-17
申请号：US14105974
申请日：2013-12-13
申请人： Amanda E. Sutton , Thomas E. Richardson , Bayard R. Huck , Srinivasa R. Karra , Xiaoling Chen , Yufang Xiao , Andreas Goutopoulos , Ruoxi Lan , David Perrey , Harold George Vandeveer , Lesley Liu-Bujalski , Frank Steiber , Hui Qiu , Reinaldo C. Jones , Brian H. Heasley
发明人： Amanda E. Sutton , Thomas E. Richardson , Bayard R. Huck , Srinivasa R. Karra , Xiaoling Chen , Yufang Xiao , Andreas Goutopoulos , Ruoxi Lan , David Perrey , Harold George Vandeveer , Lesley Liu-Bujalski , Frank Steiber , Hui Qiu , Reinaldo C. Jones , Brian H. Heasley
IPC分类号： C07D215/04 , A61K31/47
CPC分类号： C07D215/04 , A61K31/47 , C07D239/94 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04
摘要： The invention provides novel substituted amino azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
摘要翻译： 本发明提供根据式（I）的新型取代的氨基氮杂环甲酰胺化合物，其用于治疗过度增殖性疾病如癌症的制备和用途。
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公开(公告)号：US20100113439A1
公开(公告)日：2010-05-06
申请号：US12461318
申请日：2009-08-07
申请人： Mark L. Greenlee , Robert Wilkening , James Apgar , Donald Sperbeck , Kenneth J. Wildonger , Dongfang Meng , Dann L. Parker, JR. , Gregory J. Pacofsky , Brian H. Heasley , Ahmed Mamai , Kingsley Nelson
发明人： Mark L. Greenlee , Robert Wilkening , James Apgar , Donald Sperbeck , Kenneth J. Wildonger , Dongfang Meng , Dann L. Parker, JR. , Gregory J. Pacofsky , Brian H. Heasley , Ahmed Mamai , Kingsley Nelson
IPC分类号： A61K31/5377 , C07D405/04 , C07D405/14 , C07D413/14 , A61P31/10 , C07D417/14 , A61K31/501 , A61K31/497 , A61K31/506 , A61K31/454 , A61K31/427 , A61K31/4192 , A61K31/4196
CPC分类号： A61K31/343 , A01N43/653 , A61K31/21 , A61K31/41 , C07D493/08 , C07D519/00
摘要： Novel derivatives of enfumafungin are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-β-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.
摘要翻译： 本文公开了enfumafungin的新型衍生物及其药学上可接受的盐，水合物和前药。 还公开了包含这种化合物的组合物，制备这些化合物的方法和使用这些化合物作为抗真菌剂和/或（1,3） - ＆bgr-D-葡聚糖合酶抑制剂的方法。 所公开的化合物，其药学上可接受的盐，水合物和前药，以及包含这些化合物，盐，水合物和前药的组合物可用于治疗和/或预防真菌感染和相关疾病和病症。
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公开(公告)号：US08188085B2
公开(公告)日：2012-05-29
申请号：US12461318
申请日：2009-08-07
申请人： Mark L. Greenlee , Robert Wilkening , James Apgar , Donald Sperbeck , Kenneth J. Wildonger , Dongfang Meng , Dann L. Parker, Jr. , Gregory J. Pacofsky , Brian H. Heasley , Ahmed Mamai , Kingsley Nelson
发明人： Mark L. Greenlee , Robert Wilkening , James Apgar , Donald Sperbeck , Kenneth J. Wildonger , Dongfang Meng , Dann L. Parker, Jr. , Gregory J. Pacofsky , Brian H. Heasley , Ahmed Mamai , Kingsley Nelson
IPC分类号： A61K31/41 , A61K31/445 , A61K31/501 , C07D231/02 , C07D249/08 , C07D401/00 , C07D401/02 , C07D405/02 , C07D405/14
CPC分类号： A61K31/343 , A01N43/653 , A61K31/21 , A61K31/41 , C07D493/08 , C07D519/00
摘要： Novel derivatives of enfumafungin are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-β-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.
摘要翻译： 本文公开了enfumafungin的新型衍生物及其药学上可接受的盐，水合物和前药。 还公开了包含这种化合物的组合物，制备这些化合物的方法和使用这些化合物作为抗真菌剂和/或（1,3） - ＆bgr-D-葡聚糖合酶抑制剂的方法。 所公开的化合物，其药学上可接受的盐，水合物和前药，以及包含这些化合物，盐，水合物和前药的组合物可用于治疗和/或预防真菌感染和相关疾病和病症。
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公开(公告)号：US07820703B2
公开(公告)日：2010-10-26
申请号：US11579658
申请日：2005-05-06
CPC分类号： C07F9/65515 , C07F9/091 , C07F9/094 , C07F9/3891 , C07F9/404 , C07F9/5728 , C07F9/58 , C07F9/6506
摘要： The present invention is directed to compositions comprising lysophosphatidic acid analogs and methods of using such analogs as agonist or antagonists of LPA receptor activity. In addition the invention is directed to LPA receptor agonists that vary in the degree of selectivity at individual LPA receptors (i.e. LPA1, LPA2 and LPA3). More particularly the present invention is directed to LPA analogs wherein the glycerol is replaced with ethanolamine and a variety of substitutions have been linked at the second carbon atom.
摘要翻译： 本发明涉及包含溶血磷脂酸类似物的组合物和使用此类类似物作为LPA受体活性的激动剂或拮抗剂的方法。 此外，本发明涉及LPA受体激动剂，其在各个LPA受体（即LPA1，LPA2和LPA3）上的选择度变化。 更具体地说，本发明涉及LPA类似物，其中甘油被乙醇胺替代，并且多种取代已经在第二个碳原子连接。
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