公开(公告)号：US07728148B2

公开(公告)日：2010-06-01

申请号：US11758901

申请日：2007-06-06

申请人： Ying Sun ,  Yat Sun Or ,  Zhe Wang

发明人： Ying Sun ,  Yat Sun Or ,  Zhe Wang

IPC分类号： C07D207/00 ,  C07D295/00

CPC分类号： C07D207/12 ,  A61K38/00 ,  C07D207/16 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D471/04 ,  C07K5/0812

摘要： The present invention discloses compounds of formula I 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 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。

公开(公告)号：US20080125444A1

公开(公告)日：2008-05-29

申请号：US11758901

申请日：2007-06-06

申请人： Ying Sun ,  Yat Sun Or ,  Zhe Wang

发明人： Ying Sun ,  Yat Sun Or ,  Zhe Wang

IPC分类号： A61K31/497 ,  A61K31/4015 ,  A61K31/4025 ,  C07D207/12 ,  C07D403/12 ,  C12N7/06 ,  C07D405/12 ,  C07D401/14 ,  A61P31/12 ,  A61K31/4375

CPC分类号： C07D207/12 ,  A61K38/00 ,  C07D207/16 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D471/04 ,  C07K5/0812

摘要： The present invention discloses compounds of formula I 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 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。

公开(公告)号：US07125845B2

公开(公告)日：2006-10-24

申请号：US10613206

申请日：2003-07-03

申请人： Frank X. H. Wu ,  Suanne Nakajima ,  Zhi-Hui Lu ,  Ying Sun ,  Zhenwei Miao ,  Yat Sun Or ,  Zhe Wang

发明人： Frank X. H. Wu ,  Suanne Nakajima ,  Zhi-Hui Lu ,  Ying Sun ,  Zhenwei Miao ,  Yat Sun Or ,  Zhe Wang

IPC分类号： A61K38/00

CPC分类号： C07K5/06139 ,  A61K38/00 ,  C07K5/06165

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。

公开(公告)号：US08283309B2

公开(公告)日：2012-10-09

申请号：US12338612

申请日：2008-12-18

申请人： Dong Liu ,  Yat Sun Or ,  Zhe Wang

发明人： Dong Liu ,  Yat Sun Or ,  Zhe Wang

IPC分类号： A61K38/00

CPC分类号： C07D273/00

摘要： The present invention discloses compounds of formula I, 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. More specifically, the invention relates to oxime compounds containing a carbocyclic P2 unit, and the oxime is tethered to one of the carboxylic acid on P2. 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： 本发明公开了式I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。 更具体地，本发明涉及含有碳环P2单元的肟化合物，并且肟与P2上的一种羧酸结合。 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。

公开(公告)号：US20090180985A1

公开(公告)日：2009-07-16

申请号：US12338612

申请日：2008-12-18

申请人： DONG LIU ,  Yat Sun Or ,  Zhe Wang

发明人： DONG LIU ,  Yat Sun Or ,  Zhe Wang

IPC分类号： A61K38/21 ,  C07D498/00 ,  A61K31/33 ,  A61P31/12 ,  A61K38/46

CPC分类号： C07D273/00

摘要： The present invention discloses compounds of formula I, 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. More specifically, the invention relates to oxime compounds containing a carbocyclic P2 unit, and the oxime is tethered to one of the carboxylic acid on P2. 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： 本发明公开了式I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。 更具体地，本发明涉及含有碳环P2单元的肟化合物，并且肟与P2上的一种羧酸结合。 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。

公开(公告)号：US08426360B2

公开(公告)日：2013-04-23

申请号：US12269941

申请日：2008-11-13

申请人： Dong Liu ,  Yat Sun Or ,  Zhe Wang

发明人： Dong Liu ,  Yat Sun Or ,  Zhe Wang

IPC分类号： A61K38/00

CPC分类号： C07D471/04 ,  C07D225/04 ,  C07D245/04 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12

摘要： The present invention discloses compounds of formula I, 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. More specifically, the invention relates to oxime compounds containing a carbocyclic P2 unit. 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： 本发明公开了式I，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。 更具体地，本发明涉及含有碳环P2单元的肟化合物。 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。

公开(公告)号：US20090149491A1

公开(公告)日：2009-06-11

申请号：US12269941

申请日：2008-11-13

申请人： Dong Liu ,  Yat Sun Or ,  Zhe Wang

发明人： Dong Liu ,  Yat Sun Or ,  Zhe Wang

IPC分类号： A61K31/4709 ,  C07D245/02 ,  C07D215/00 ,  C07D471/12 ,  A61K31/4375

CPC分类号： C07D471/04 ,  C07D225/04 ,  C07D245/04 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12

摘要： The present invention discloses compounds of formula I, 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. More specifically, the invention relates to oxime compounds containing a carbocyclic P2 unit. 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： 本发明公开了式I，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。 更具体地，本发明涉及含有碳环P2单元的肟化合物。 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。

公开(公告)号：US20050187169A1

公开(公告)日：2005-08-25

申请号：US11029640

申请日：2005-01-05

申请人： Nha Vo ,  Guoqiang Wang ,  Guoyou Xu ,  Ying Hou ,  Ying Sun ,  Ly Phan ,  Zhe Wang ,  Yat Or

发明人： Nha Vo ,  Guoqiang Wang ,  Guoyou Xu ,  Ying Hou ,  Ying Sun ,  Ly Phan ,  Zhe Wang ,  Yat Or

IPC分类号： A61K31/70 ,  A61K31/7048 ,  C07H17/08

CPC分类号： C07H17/08

摘要： The present invention discloses compounds of formulaes I, II, III, or IV, or a racemate, enantiomer, regioisomer, salt, ester or prodrug 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，II，III或IV的化合物或其外消旋体，对映异构体，区域异构体，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。

公开(公告)号：US20050261200A1

公开(公告)日：2005-11-24

申请号：US10849107

申请日：2004-05-19

申请人： Zhenwei Miao ,  Ying Sun ,  Suanne Nakajima ,  Datong Tang ,  Zhe Wang ,  Yat Or

发明人： Zhenwei Miao ,  Ying Sun ,  Suanne Nakajima ,  Datong Tang ,  Zhe Wang ,  Yat Or

IPC分类号： A61K38/00 ,  A61K38/05 ,  C07K5/06 ,  C07K5/083

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。

公开(公告)号：US07273851B2

公开(公告)日：2007-09-25

申请号：US10849107

申请日：2004-05-19

申请人： Zhenwei Miao ,  Ying Sun ,  Suanne Nakajima ,  Datong Tang ,  Zhe Wang ,  Yat S. Or

发明人： Zhenwei Miao ,  Ying Sun ,  Suanne Nakajima ,  Datong Tang ,  Zhe Wang ,  Yat S. Or

IPC分类号： A61K38/00

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。