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公开(公告)号：US06576766B1
公开(公告)日：2003-06-10
申请号：US09554230
申请日：2000-08-17
申请人： Manfred Weigele , Regine Bohacek , Virginia A. Jacobsen , Karina Macek , Michael G. Yang , Noriyuki H. Kawahata , Rajeswari Sundaramoorthi , Yihan Wang , Craig S. Takeuchi , George P. Luke , Chester A. Metcalf, III , William C. Shakespeare , Tomi K. Sawyer
发明人： Manfred Weigele , Regine Bohacek , Virginia A. Jacobsen , Karina Macek , Michael G. Yang , Noriyuki H. Kawahata , Rajeswari Sundaramoorthi , Yihan Wang , Craig S. Takeuchi , George P. Luke , Chester A. Metcalf, III , William C. Shakespeare , Tomi K. Sawyer
IPC分类号： C07D30789
CPC分类号： C07D307/92 , A61K38/00 , C07C237/22 , C07C2601/14 , C07F9/12 , C07F9/3834 , C07F9/3869 , C07F9/3873 , C07F9/3882 , C07F9/65527 , C07K5/06191
摘要： This invention concerns compounds for inhibiting intracellular signal transduction, especially intracellular signal transduction mediate by one or more molecular interactions involving a phosphotyrosine-containing protein. This invention also relates to pharmaceutic compositions containing the compounds and prophylactic and therapeutic methods involving pharmaceutical and veterinary administration of the compounds. The compounds are of formula (1) as defined herein.
摘要翻译： 本发明涉及用于抑制细胞内信号转导的化合物，特别是通过涉及含磷酸酪氨酸的蛋白质的一种或多种分子相互作用介导的细胞内信号转导。 本发明还涉及包含化合物的药物组合物和涉及化合物的药物和兽药施用的预防和治疗方法。 化合物是如本文所定义的式（1）。
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公开(公告)号：US07115589B2
公开(公告)日：2006-10-03
申请号：US09740393
申请日：2000-12-18
申请人： Manfred Weigele , Tomi K. Sawyer , Regine Bohacek , William C. Shakespeare , Rajeswari Sundaramoorthi , Yihan Wang , David C. Dalgarno , Chester A. Metcalf, III
发明人： Manfred Weigele , Tomi K. Sawyer , Regine Bohacek , William C. Shakespeare , Rajeswari Sundaramoorthi , Yihan Wang , David C. Dalgarno , Chester A. Metcalf, III
IPC分类号： C07F9/6561 , A61K31/675 , A61P19/10 , A61P19/08 , A61P35/00
CPC分类号： C07D471/04 , A61K47/548 , C07D487/04 , C07F9/4012 , C07F9/405 , C07F9/58 , C07F9/65583 , C07F9/6561 , C07F9/65616
摘要： This invention relates to compounds of the general formula: in which RA, RB, RC and RD are as defined herein, and to their preparation and use. In these compounds, RB is an aliphatic, heteroaliphatic, aryl, or heteroaryl moiety which comprises one or more phosphorus-containing moieties.
摘要翻译： 本发明涉及以下通式的化合物：其中R A，R B，R C和R D D均为 >如本文所定义，以及其制备和使用。 在这些化合物中，R B是包含一个或多个含磷部分的脂族，杂脂族，芳基或杂芳基部分。
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公开(公告)号：US20050065171A1
公开(公告)日：2005-03-24
申请号：US10876116
申请日：2004-06-24
申请人： William Shakespeare , Chester Metcalf , Tomi Sawyer , Yihan Wang , Rajeswari Sundaramoorthi , David Dalgarno , Regine Bohacek , Manfred Weigele
发明人： William Shakespeare , Chester Metcalf , Tomi Sawyer , Yihan Wang , Rajeswari Sundaramoorthi , David Dalgarno , Regine Bohacek , Manfred Weigele
IPC分类号： A61K20060101 , A61K31/522 , A61K31/675 , A61P35/00 , A61P35/02 , C07D473/12 , C07F9/6561 , C12Q1/68
CPC分类号： C07F9/65616
摘要： This invention relates to compounds of the general formula: in which Y, RA, RC and R6 are as defined herein, and to their preparation and use.
摘要翻译： 本发明涉及以下通式的化合物：其中Y，R A，R C和R 6如本文所定义，以及其制备和用途。
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公开(公告)号：US20050096298A1
公开(公告)日：2005-05-05
申请号：US10994962
申请日：2004-11-22
申请人： Chester Metcalf , Manfred Weigele , Tomi Sawyer , Regine Bohacek , William Shakespeare , Rajeswari Sundaramoorthi , Yihan Wang , David Dalgarno
发明人： Chester Metcalf , Manfred Weigele , Tomi Sawyer , Regine Bohacek , William Shakespeare , Rajeswari Sundaramoorthi , Yihan Wang , David Dalgarno
IPC分类号： A61K47/48 , C07D471/04 , C07D487/04 , C07F9/40 , C07F9/58 , C07F9/6558 , C07F9/6561 , A61K31/675
CPC分类号： C07D471/04 , A61K47/54 , A61K47/548 , C07D487/04 , C07F9/4012 , C07F9/405 , C07F9/58 , C07F9/65583 , C07F9/6561 , C07F9/65616
摘要： Novel purines and uses of these compounds for the treatment of bone related disorders and cancer is disclosed.
摘要翻译： 公开了这些化合物用于治疗骨相关疾病和癌症的新型嘌呤和用途。
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公开(公告)号：US06420384B2
公开(公告)日：2002-07-16
申请号：US09740619
申请日：2000-12-18
IPC分类号： C07D40101
CPC分类号： C07D471/04 , A61K47/54 , A61K47/548 , C07D487/04 , C07F9/4012 , C07F9/405 , C07F9/58 , C07F9/65583 , C07F9/6561 , C07F9/65616
摘要： Compounds and methods of treating or preventing bone disorders including osteoporosis, rheumatoid arthritis, and metastatic bone disease are provided. The inventive compounds comprise a bone targeting moiety and a payload. The payload portion of these inventive compounds inhibit the proton pump of osteoclasts, thereby, reducing bone resorption. Compounds of the present invention include compounds of the following formula:
摘要翻译： 提供了治疗或预防包括骨质疏松症，类风湿性关节炎和转移性骨病在内的骨疾病的化合物和方法。 本发明化合物包括骨靶向部分和有效载荷。 这些本发明化合物的有效载荷部分抑制破骨细胞的质子泵，从而减少骨吸收。 本发明的化合物包括下式的化合物：
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公开(公告)号：US09486455B2
公开(公告)日：2016-11-08
申请号：US13040859
申请日：2011-03-04
申请人： Jayhong A. Chong , Christopher Fanger , Glenn R. Larsen , Magdalene M. Moran , Howard Ng , Amy Ripka , Dennis John Underwood , Manfred Weigele , Xiaoguang Zhen
发明人： Jayhong A. Chong , Christopher Fanger , Glenn R. Larsen , Magdalene M. Moran , Howard Ng , Amy Ripka , Dennis John Underwood , Manfred Weigele , Xiaoguang Zhen
IPC分类号： A01N43/58 , A01N43/60 , A61K31/517 , A61K31/519
CPC分类号： A61K31/519 , A61K31/517
摘要： The present application relates to compounds and methods for treating pain and other conditions related to TRPV3.
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7.发明授权Compounds, compositions and methods for the treatment of beta-amyloid diseases and synucleinopathies 有权用于治疗β-淀粉样蛋白病和突触核蛋白病的化合物，组合物和方法公开(公告)号：US08829198B2
公开(公告)日：2014-09-09
申请号：US12244968
申请日：2008-10-03
申请人： Luke A. Esposito , F. Michael Hudson , Thomas Lake , Joel Cummings , Manfred Weigele , Alan D. Snow , Lesley Larsen
发明人： Luke A. Esposito , F. Michael Hudson , Thomas Lake , Joel Cummings , Manfred Weigele , Alan D. Snow , Lesley Larsen
IPC分类号： A61K31/4196 , A61K31/4164 , A61K31/18 , A61K31/05 , C07D249/08 , C07D233/54 , C07C311/29 , C07C39/10
CPC分类号： C07C311/29 , A61K31/05 , A61K31/18 , A61K31/4164 , A61K31/4196 , C07C37/16 , C07C39/10 , C07C39/17 , C07C2603/74 , C07D231/12 , C07D233/54 , C07D233/64 , C07D249/08
摘要： Dihydroxyaryl compounds and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of β-amyloid diseases, such as observed in Alzheimer's disease, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.
摘要翻译： 二羟基芳基化合物和药学上可接受的酯，它们的合成，含有它们的药物组合物，以及它们在治疗淀粉样蛋白疾病（例如在阿尔茨海默病中观察到的）和突触核蛋白病（例如帕金森病中观察到的）和药物制造中的用途 用于治疗。
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公开(公告)号：US20110151559A1
公开(公告)日：2011-06-23
申请号：US13040859
申请日：2011-03-04
申请人： Jayhong A. Chong , Christopher Fanger , Glenn R. Larsen , Magdalene M. Moran , Howard Ng , Amy Ripka , Dennis John Underwood , Manfred Weigele , Xiaoguang Zhen
发明人： Jayhong A. Chong , Christopher Fanger , Glenn R. Larsen , Magdalene M. Moran , Howard Ng , Amy Ripka , Dennis John Underwood , Manfred Weigele , Xiaoguang Zhen
IPC分类号： C12N5/00
CPC分类号： A61K31/519 , A61K31/517
摘要： The present application relates to compounds and methods for treating pain and other conditions related to TRPV3.
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公开(公告)号：US07803790B2
公开(公告)日：2010-09-28
申请号：US11431942
申请日：2006-05-09
申请人： Jayhong A. Chong , Christopher Fanger , Glenn R. Larsen , William C. Lumma, Jr. , Anu Mahadevan , Peter Meltzer , Magdalene M. Moran , Amy Ripka , Dennis John Underwood , Manfred Weigele , Xiaoguang Zhen
发明人： Jayhong A. Chong , Christopher Fanger , Glenn R. Larsen , William C. Lumma, Jr. , Anu Mahadevan , Peter Meltzer , Magdalene M. Moran , Amy Ripka , Dennis John Underwood , Manfred Weigele , Xiaoguang Zhen
IPC分类号： A61K31/33 , A61K31/425 , C07D277/60
CPC分类号： A61K31/4709 , A61K9/0014 , A61K9/0053 , A61K31/427 , A61K31/47 , A61K31/498 , A61K31/506 , A61K31/538 , A61K31/55 , C07D215/54 , C07D409/04 , C07D495/04
摘要： The present application relates to compounds and methods for treating pain and other conditions related to TRPV3.
摘要翻译： 本申请涉及用于治疗与TRPV3相关的疼痛和其它病症的化合物和方法。
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公开(公告)号：US5147871A
公开(公告)日：1992-09-15
申请号：US803757
申请日：1991-12-05
IPC分类号： A61K47/48 , C07D501/34
CPC分类号： B82Y5/00 , A61K47/48115 , A61K47/4813 , A61K47/48761
摘要： There are presented anti-bacterial cephalosporins having broad antimicrobial activity of the formula ##STR1## wherein R.sub.1 is an antibiotically active quinolonyl; R.sub.2 is selected from the group consisting of hydrogen, lower alkoxy, amino, lower alkylthio and amido; R.sub.3 is selected from the group consisting of hydrogen, and acyl group, and m is 0, 1 or 2 and the readily hydrolysable esters or salts of these compounds and hydrates of the compounds of formula I or of their esters or salts.
摘要翻译： 提出了具有广泛的抗菌活性的抗菌头孢菌素，其具有下式其中R 1是抗生物活性喹啉酮; R2选自氢，低级烷氧基，氨基，低级烷硫基和酰氨基; R3选自氢和酰基，m为0,1或2，这些化合物的易水解的酯或盐和式I化合物的水合物或其酯或盐。
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