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公开(公告)号：US07419962B2
公开(公告)日：2008-09-02
申请号：US11295736
申请日：2005-12-06
申请人： Yat Sun Or , Datong Tang , Ying Sun , Yonghua Gai , Guoyou Xu , Zhe Wang
发明人： Yat Sun Or , Datong Tang , Ying Sun , Yonghua Gai , Guoyou Xu , 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：US07229972B2
公开(公告)日：2007-06-12
申请号：US11008581
申请日：2004-12-07
申请人： Yat Sun Or , Datong Tang , Yonghua Gai , Ying Sun , Guoyou Xu , Zhe Wang
发明人： Yat Sun Or , Datong Tang , Yonghua Gai , Ying Sun , Guoyou Xu , 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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13.发明授权公开(公告)号：US08809264B2
公开(公告)日：2014-08-19
申请号：US11768723
申请日：2007-06-26
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
IPC分类号： A61K38/00 , C07D245/04 , A61K38/21 , C07D403/12
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：US20090180981A1
公开(公告)日：2009-07-16
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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15.发明申请公开(公告)号：US20090005387A1
公开(公告)日：2009-01-01
申请号：US12016599
申请日：2008-01-18
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
IPC分类号： A61K31/495 , A61K31/497 , A61P31/00
CPC分类号： A61K31/497 , A61K31/495 , A61K38/13 , A61K38/212 , A61K38/215 , C07D245/04 , C07D403/12 , C07D487/04 , 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：US20070060510A1
公开(公告)日：2007-03-15
申请号：US11489011
申请日：2006-07-18
申请人： Suanne Nakajima , Zhenwei Miao , Ying Sun , Datong Tang , Guoyou Xu , Brian Porter , Yat Or , Zhe Wang
发明人： Suanne Nakajima , Zhenwei Miao , Ying Sun , Datong Tang , Guoyou Xu , Brian Porter , Yat Or , Zhe Wang
IPC分类号： A61K38/12 , A61K31/497 , C07K5/12 , C07D487/14
CPC分类号： C07K5/0802 , A61K38/212 , A61K38/215 , C07D487/04 , C07K5/0804 , A61K2300/00
摘要： The present invention relates to compounds of Formula I or II, 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或II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：US20050153877A1
公开(公告)日：2005-07-14
申请号：US10774047
申请日：2004-02-06
申请人： Zhenwei Miao , Ying Sun , Suanne Nakajima , Datong Tang , Frank Wu , Guoyou Xu , Yat Or , Zhe Wang
发明人： Zhenwei Miao , Ying Sun , Suanne Nakajima , Datong Tang , Frank Wu , Guoyou Xu , Yat Or , Zhe Wang
CPC分类号： C07D487/04 , A61K38/12 , C07K5/0806 , E05F15/73 , E05F2015/763
摘要： The present invention relates to compounds of Formula I, II or Ill, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: wherein W is a substituted or unsubstituted heterocyclic ring system. The compounds 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： 本发明涉及式I，II或III的化合物或其药学上可接受的盐，酯或前药：其中W是取代或未取代的杂环体系。 该化合物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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![Processes for the preparation of 0-(2-aminobenzo[d]oxazol-5-yl)methyl hydroxylamine for the synthesis of 6,11-bicyclic erythromycin derivative EDP-182](/abs-image/US/2009/07/21/US07563877B2/abs.jpg.150x150.jpg)
18.发明授权Processes for the preparation of 0-(2-aminobenzo[d]oxazol-5-yl)methyl hydroxylamine for the synthesis of 6,11-bicyclic erythromycin derivative EDP-182 有权用于合成6,11-双环红霉素衍生物EDP-182的O-（2-氨基苯并[d]恶唑-5-基）甲基羟胺的制备方法公开(公告)号：US07563877B2
公开(公告)日：2009-07-21
申请号：US11657393
申请日：2007-01-23
申请人： Guoyou Xu , Yonghua Gai , Guoqlang Wang , Yat Sun Or , Zhe Wang
发明人： Guoyou Xu , Yonghua Gai , Guoqlang Wang , Yat Sun Or , Zhe Wang
IPC分类号： C07H17/08 , C07D263/58 , C07D263/60 , C07D413/00 , C07D498/00
CPC分类号： C07H17/08
摘要： The present invention relates to processes and intermediates for the preparation of 6-11 bicyclic erythromycin derivative known as EDP-182 (IX-a). In particular, the present invention relates to processes and intermediates for the preparation of O-(2-aminobenzo[d]oxazol-5-yl)methyl hydroxylamine:
摘要翻译： 本发明涉及制备称为EDP-182（IX-a）的6-11双环红霉素衍生物的方法和中间体。 特别地，本发明涉及制备O-（2-氨基苯并[d]恶唑-5-基）甲基羟胺的方法和中间体：
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![Processes for the preparation of 0-(2-aminobenzo[d]oxazol-5-yl)methyl hydroxylamine for the synthesis of 6,11-bicyclic erythromycin derivative EDP-182](/abs-image/US/2007/09/06/US20070207972A1/abs.jpg.150x150.jpg)
19.发明申请Processes for the preparation of 0-(2-aminobenzo[d]oxazol-5-yl)methyl hydroxylamine for the synthesis of 6,11-bicyclic erythromycin derivative EDP-182 有权用于合成6,11-双环红霉素衍生物EDP-182的O-（2-氨基苯并[d]恶唑-5-基）甲基羟胺的制备方法公开(公告)号：US20070207972A1
公开(公告)日：2007-09-06
申请号：US11657393
申请日：2007-01-23
申请人： Guoyou Xu , Yonghua Gai , Guoqlang Wang , Yat Sun Or , Zhe Wang
发明人： Guoyou Xu , Yonghua Gai , Guoqlang Wang , Yat Sun Or , Zhe Wang
IPC分类号： A61K31/7052 , C07H17/08
CPC分类号： C07H17/08
摘要： The present invention relates to processes and intermediates for the preparation of 6-11 bicyclic erythromycin derivative known as EDP-182 (IX-a). In particular, the present invention relates to processes and intermediates for the preparation of O-(2-aminobenzo[d]oxazol-5-yl)methyl hydroxylamine:
摘要翻译： 本发明涉及制备称为EDP-182（IX-a）的6-11双环红霉素衍生物的方法和中间体。 特别地，本发明涉及制备O-（2-氨基苯并[d]恶唑-5-基）甲基羟胺的方法和中间体：
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公开(公告)号：US08236807B2
公开(公告)日：2012-08-07
申请号：US12505725
申请日：2009-07-20
申请人： Suanne Nakajima , Zhenwei Miao , Ying Sun , Datong Tang , Guoyou Xu , Brian Porter , Yat Sun Or , Zhe Wang
发明人： Suanne Nakajima , Zhenwei Miao , Ying Sun , Datong Tang , Guoyou Xu , Brian Porter , Yat Sun Or , Zhe Wang
IPC分类号： C07D401/12 , C07D409/14 , A61K31/38 , A61K31/395 , A61P31/12
CPC分类号： C07K5/0802 , A61K38/212 , A61K38/215 , C07D487/04 , C07K5/0804 , A61K2300/00
摘要： The present invention relates to compounds of Formula I or II, 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或II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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