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公开(公告)号：US20120101031A1
公开(公告)日：2012-04-26
申请号：US13154721
申请日：2011-06-07
申请人： Hui-Ju Chen , Keith F. McDaniel , Brian E. Green , Jason P. Shanley , Albert W. Kruger , Jorge Gandarilla , Dennie S. Welch , Russell D. Cink , Steven C. Cullen , Yonghua Gai , Guoqiang Wang , Yat Sun Or
发明人： Hui-Ju Chen , Keith F. McDaniel , Brian E. Green , Jason P. Shanley , Albert W. Kruger , Jorge Gandarilla , Dennie S. Welch , Russell D. Cink , Steven C. Cullen , Yonghua Gai , Guoqiang Wang , Yat Sun Or
CPC分类号： C07K5/081 , C07D487/04
摘要： The present invention relates to novel macrocyclic compounds and methods of treating a hepatitis C infection in a subject in need of such therapy with said macrocyclic compounds. The present invention further relates to pharmaceutical compositions comprising the compounds of the present invention, or pharmaceutically acceptable salts, esters, or prodrugs thereof, in combination with a pharmaceutically acceptable carrier or excipient.
摘要翻译： 本发明涉及新的大环化合物和在需要用所述大环化合物进行这种治疗的受试者中治疗丙型肝炎感染的方法。 本发明还涉及包含本发明化合物或其药学上可接受的盐，酯或前药与药学上可接受的载体或赋形剂组合的药物组合物。
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公开(公告)号：US07517859B2
公开(公告)日：2009-04-14
申请号：US11416739
申请日：2006-05-03
申请人： Yonghua Gai , Datong Tang , Ying Sun , Zhigang Chen , Yat Sun Or , Zhe Wang
发明人： Yonghua Gai , Datong Tang , Ying Sun , Zhigang Chen , Yat Sun Or , Zhe Wang
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：US20080248105A1
公开(公告)日：2008-10-09
申请号：US12105482
申请日：2008-04-18
申请人： Datong Tang , Guoyou Xu , Yonghua Gai , Zhe Wang , Yat Sun Or , Hui-Yin Li
发明人： Datong Tang , Guoyou Xu , Yonghua Gai , Zhe Wang , Yat Sun Or , Hui-Yin Li
IPC分类号： A61K9/48 , C07H17/08 , A61K9/12 , A61P29/00 , A61K31/7052
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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公开(公告)号：US07384921B2
公开(公告)日：2008-06-10
申请号：US11057476
申请日：2005-02-14
申请人： Datong Tang , Guoyou Xu , Yonghua Gai , Zhe Wang , Yat Sun Or , Hui-Yin Li
发明人： Datong Tang , Guoyou Xu , Yonghua Gai , Zhe Wang , Yat Sun Or , Hui-Yin Li
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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公开(公告)号：US20080032936A1
公开(公告)日：2008-02-07
申请号：US11499917
申请日：2006-08-04
申请人： Yonghua Gai , Deqiang Niu , Yat Sun Or , Zhe Wang
发明人： Yonghua Gai , Deqiang Niu , Yat Sun Or , Zhe Wang
CPC分类号： C07K5/0808 , A61K38/00
摘要： The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
摘要翻译： 本发明涉及抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒（HCV）NS3-NS4A蛋白酶活性的式I化合物或其药学上可接受的盐，酯或前药。 因此，本发明的化合物干扰丙型肝炎病毒的生命周期，也可用作抗病毒剂。 本发明还涉及药物组合物，其包含用于给患有HCV感染的受试者施用的上述化合物。 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HCV感染的方法。
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公开(公告)号：US20080008681A1
公开(公告)日：2008-01-10
申请号：US11768712
申请日：2007-06-26
申请人： Deqiang Niu , Dong Liu , Joel Moore , Guoyou Xu , Ying Sun , Yonghua Gai , Datong Tang , Yat Sun Or , Zhe Wang
发明人： Deqiang Niu , Dong Liu , Joel Moore , Guoyou Xu , Ying Sun , Yonghua Gai , Datong Tang , Yat Sun Or , Zhe Wang
IPC分类号： A61K38/21 , A61K31/498 , A61P31/12 , C07D245/04
CPC分类号： C07D245/04 , A61K38/212 , A61K38/215 , C07D403/12 , A61K2300/00
摘要： The present invention relates to compounds, including compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
摘要翻译： 本发明涉及包括式I化合物或其药学上可接受的盐，酯或前药的化合物，其抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒（HCV）NS3-NS4A蛋白酶的活性。 因此，本发明的化合物干扰丙型肝炎病毒的生命周期，也可用作抗病毒剂。 本发明还涉及药物组合物，其包含用于给患有HCV感染的受试者施用的上述化合物。 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HCV感染的方法。
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公开(公告)号：US20060252713A1
公开(公告)日：2006-11-09
申请号：US11416739
申请日：2006-05-03
申请人： Yonghua Gai , Datong Tang , Ying Sun , Zhigang Chen , Yat Or , Zhe Wang
发明人： Yonghua Gai , Datong Tang , Ying Sun , Zhigang Chen , Yat Or , 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.
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8.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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公开(公告)号：US08962551B2
公开(公告)日：2015-02-24
申请号：US12327538
申请日：2008-12-03
申请人： Deqiang Niu , Dong Liu , Joel D. Moore , Guoyou Xu , Ying Sun , Yonghua Gai , Datong Tang , Yat Sun Or , Zhe Wang
发明人： Deqiang Niu , Dong Liu , Joel D. Moore , Guoyou Xu , Ying Sun , Yonghua Gai , Datong Tang , Yat Sun Or , Zhe Wang
CPC分类号： C07D487/04 , A61K38/212 , A61K38/215 , C07K5/06165 , C07K5/0812 , A61K2300/00
摘要： The present invention relates to compounds of Formula I or II, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising a compound of the present invention.
摘要翻译： 本发明涉及式I或II的化合物或其药学上可接受的盐，酯或前药：其抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒（HCV）NS3-NS4A蛋白酶的活性。 因此，本发明的化合物干扰丙型肝炎病毒的生命周期，也可用作抗病毒剂。 本发明还涉及药物组合物，其包含用于给患有HCV感染的受试者施用的上述化合物。 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HCV感染的方法。
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