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公开(公告)号：US20060122128A1
公开(公告)日：2006-06-08
申请号：US11008581
申请日：2004-12-07
申请人： Yat Or , Datong Tang , Yonghua Gai , Ying Sun , Guoyou Xu , Zhe Wang
发明人： Yat Or , Datong Tang , Yonghua Gai , Ying Sun , Guoyou Xu , Zhe Wang
IPC分类号： A61K31/7048 , C07H17/08
CPC分类号： C07H17/08
摘要： The present invention discloses compounds of formula (I) or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.
摘要翻译： 本发明公开了具有抗菌性质的式（I）化合物或其药学上可接受的盐，酯或前药。 本发明还涉及包含上述化合物的药物组合物，用于给予需要抗生素治疗的受试者。 本发明还涉及通过施用包含本发明化合物的药物组合物来治疗受试者的细菌感染的方法。 本发明还包括制备本发明化合物的方法。
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公开(公告)号：US20060148731A1
公开(公告)日：2006-07-06
申请号：US11302529
申请日：2005-12-13
申请人： Datong Tang , Yonghua Gai , Ying Sun , Zhigang Chen , Yat Or , Zhe Wang
发明人： Datong Tang , Yonghua Gai , Ying Sun , Zhigang Chen , Yat Or , Zhe Wang
IPC分类号： A61K31/7052 , C07H17/08
CPC分类号： C07H17/08
摘要： The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.
摘要翻译： 本发明公开了式I化合物或其药学上可接受的盐，酯或前药：其表现出抗菌性质。 本发明还涉及包含上述化合物的药物组合物，用于给予需要抗生素治疗的受试者。 本发明还涉及通过施用包含本发明化合物的药物组合物来治疗受试者的细菌感染的方法。 本发明还包括制备本发明化合物的方法。
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公开(公告)号：US20060142214A1
公开(公告)日：2006-06-29
申请号：US11295736
申请日：2005-12-06
申请人： Yat Or , Datong Tang , Ying Sun , Yonghua Gai , Guoyou Xu , Zhe Wang
发明人： Yat Or , Datong Tang , Ying Sun , Yonghua Gai , Guoyou Xu , Zhe Wang
IPC分类号： C07H17/08 , A61K31/7052
CPC分类号： C07H17/08
摘要： The present invention discloses compounds of formula (I) or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.
摘要翻译： 本发明公开了具有抗菌性质的式（I）化合物或其药学上可接受的盐，酯或前药。 本发明还涉及包含上述化合物的药物组合物，用于给予需要抗生素治疗的受试者。 本发明还涉及通过施用包含本发明化合物的药物组合物来治疗受试者的细菌感染的方法。 本发明还包括制备本发明化合物的方法。
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公开(公告)号：US20060142215A1
公开(公告)日：2006-06-29
申请号：US11302525
申请日：2005-12-13
申请人： Datong Tang , Yonghua Gai , Ying Sun , Yat Or , Zhe Wang
发明人： Datong Tang , Yonghua Gai , Ying Sun , Yat Or , Zhe Wang
IPC分类号： A61K31/7052 , C07H17/08
CPC分类号： C07H17/08
摘要： The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.
摘要翻译： 本发明公开了式I化合物或其药学上可接受的盐，酯或前药：其表现出抗菌性质。 本发明还涉及包含上述化合物的药物组合物，用于给予需要抗生素治疗的受试者。 本发明还涉及通过施用包含本发明化合物的药物组合物来治疗受试者的细菌感染的方法。 本发明还包括制备本发明化合物的方法。
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55.发明授权Alpha-and beta-substituted trifluoromethyl ketones as phospholipase inhibitors 有权α-和β-取代的三氟甲基酮作为磷脂酶抑制剂公开(公告)号：US06414179B1
公开(公告)日：2002-07-02
申请号：US09816574
申请日：2001-03-23
申请人： Jacques Banville , Anne Marinier , Yonghua Gai , Serge Plamondon , Stephan Roy , Neelakantan Balasubramanian
发明人： Jacques Banville , Anne Marinier , Yonghua Gai , Serge Plamondon , Stephan Roy , Neelakantan Balasubramanian
IPC分类号： C07C26100
CPC分类号： C07D303/48 , A61K31/192 , A61K31/216 , A61K31/277 , A61K31/695 , C07C217/22 , C07C317/18 , C07C323/12 , C07C323/52
摘要： Inhibitors of the cytosolic phospholipase A2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases. The inhibitors of the present invention have the general formula where X, Z, R1, R2, R3, R4, Ra and Rb are as defined in the specification.
摘要翻译： 提供了细胞溶质磷脂酶A2酶的抑制剂，其可用于控制多种炎性疾病。 本发明的抑制剂具有通式，X，Z，R 1，R 2，R 3，R 4，R a和R b如本说明书中所定义。
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公开(公告)号：US06255496B1
公开(公告)日：2001-07-03
申请号：US09300111
申请日：1999-04-27
IPC分类号： C07D20708
CPC分类号： C07D207/08 , C07C17/269 , C07C25/18 , C07C45/515 , C07C45/673 , C07C45/74 , C07C49/245 , C07C49/248 , C07C49/255 , C07C69/63 , C07C69/712 , C07C69/738 , C07C217/22 , C07C229/12 , C07C233/18 , C07C235/20 , C07C311/04 , C07C317/18 , C07C323/12 , C07D207/12 , C07D207/16 , C07D211/14 , C07D211/46 , C07D215/14 , C07D231/12 , C07D271/06 , C07D277/04 , C07D311/20 , C07D313/08 , C07D317/34 , C07F7/1804 , C07F9/113 , C07F9/2458
摘要： Selective inhibitors of the cPLA2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases. The inhibitors of the present invention have the general formula
摘要翻译： 提供cPLA2酶的选择性抑制剂，其可用于控制多种炎性疾病。 本发明的抑制剂具有通式
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57.发明授权公开(公告)号：US08513253B2
公开(公告)日：2013-08-20
申请号：US12840612
申请日：2010-07-21
申请人： Michael F. Parker , Katharine E. McElhone , Robert A. Mate , Joanne J. Bronson , Yonghua Gai , Carl P. Bergstrom , Lawrence R. Marcin , John E. Macor
发明人： Michael F. Parker , Katharine E. McElhone , Robert A. Mate , Joanne J. Bronson , Yonghua Gai , Carl P. Bergstrom , Lawrence R. Marcin , John E. Macor
IPC分类号： A01N43/58 , A61K31/495 , C07D403/00
CPC分类号： C07D207/325 , C07C311/19 , C07C317/32 , C07C323/49 , C07C323/60 , C07C2601/02 , C07C2601/14 , C07D211/28 , C07D211/60 , C07D213/42 , C07D213/74 , C07D215/06 , C07D217/04 , C07D231/12 , C07D233/56 , C07D235/14 , C07D249/08 , C07D257/04 , C07D261/08 , C07D271/06 , C07D271/10 , C07D277/28 , C07D285/01 , C07D295/13 , C07D295/135 , C07D307/68 , C07D333/20
摘要： There is provided a series of novel α-(N-sulfonamido)acetamide compounds of the Formula (I) wherein R, R1, R2 and R3 are defined herein, which are inhibitors of β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by anti-amyloid activity.
摘要翻译： 提供了一系列式（I）的新型α-（N-亚磺酰氨基）乙酰胺化合物，其中R，R 1，R 2和R 3在本文中定义，其是β-淀粉样蛋白肽（β-AP）产生的抑制剂，并且是 可用于治疗阿尔茨海默病和其他受抗淀粉样蛋白活性影响的病症。
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公开(公告)号：US20050203035A1
公开(公告)日：2005-09-15
申请号：US11057476
申请日：2005-02-14
申请人： Datong Tang , Guoyou Xu , Yonghua Gai , Zhe Wang , Yat Or , Hui-Yin Li
发明人： Datong Tang , Guoyou Xu , Yonghua Gai , Zhe Wang , Yat Or , Hui-Yin Li
IPC分类号： A61K31/40 , A61K31/7052 , C07H17/08
CPC分类号： C07H17/08
摘要： The present invention includes EP-13420 polymorphic crystalline forms: Form I, Form II, Form Ia, and monohydrate and amorphous EP-13420 which posses distinct physical properties. In another embodiment of the present invention, there are provided methods of producing the various polymorphic forms in pure form or in combination with one another. The present invention also provides pharmaceutical compositions and formulations comprising the polymorphic and amorphous forms and methods of treating bacterial infections by administering the pharmaceutical compositions to a subject in need of such treatment.
摘要翻译： 本发明包括具有不同物理性质的EP-13420多晶型形式：I型，II型，Ia型和一水合物和无定型EP-13420。 在本发明的另一个实施方案中，提供了以纯形式或彼此组合生产各种多晶形式的方法。 本发明还提供药物组合物和制剂，其包含多形态和无定形形式以及通过将药物组合物施用于需要这种治疗的受试者来治疗细菌感染的方法。
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59.发明授权Alpha-substituted thio, -oxo trifluoromethylketones as phospholipase inhibitors 有权α-取代的硫代氧基三氟甲基酮作为磷脂酶抑制剂公开(公告)号：US06492550B2
公开(公告)日：2002-12-10
申请号：US09779411
申请日：2001-02-08
IPC分类号： C07C59147
CPC分类号： A61K31/216 , A61K31/255 , A61K31/662
摘要： Inhibitors of the cytosolic phospholypase A2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases. The inhibitors of the present invention have the general formula where X, Z, X1, R1, R2, Ra and Rb are as defined in the specification.
摘要翻译： 提供胞质磷酸酯酶A2酶的抑制剂，其可用于控制各种炎性疾病。 本发明的抑制剂具有通式，X，Z，X 1，R 1，R 2，R a和R b如本说明书中所定义。
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公开(公告)号：US06350892B1
公开(公告)日：2002-02-26
申请号：US09507782
申请日：2000-02-18
IPC分类号： C07F704
CPC分类号： C07D207/08 , C07C17/269 , C07C25/18 , C07C45/515 , C07C45/673 , C07C45/74 , C07C49/245 , C07C49/248 , C07C49/255 , C07C69/63 , C07C69/712 , C07C69/738 , C07C217/22 , C07C229/12 , C07C233/18 , C07C235/20 , C07C311/04 , C07C317/18 , C07C323/12 , C07D207/12 , C07D207/16 , C07D211/14 , C07D211/46 , C07D215/14 , C07D231/12 , C07D271/06 , C07D277/04 , C07D311/20 , C07D313/08 , C07D317/34 , C07F7/1804 , C07F9/113 , C07F9/2458
摘要： Selective inhibitors of the cPLA2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases. The inhibitors of the present invention have the general formula where (R′), p, D, Y, Z, Ra, Rb and A are as defined in the specification.
摘要翻译： 提供cPLA2酶的选择性抑制剂，其可用于控制多种炎性疾病。 本发明的抑制剂具有通式（R'），p，D，Y，Z，Ra，Rb和A如说明书中所定义。
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