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：

公开(公告)号：US20120196792A1

公开(公告)日：2012-08-02

申请号：US13439551

申请日：2012-04-04

申请人： Yiyin Ku ,  Keith F. McDaniel ,  Hui-Ju Chen ,  Jason P. Shanley ,  Dale J. Kempf ,  David J. Grampovnik ,  Ying Sun ,  Dong Liu ,  Yonghua Gai ,  Yat Sun Or ,  Seble H. Wagaw ,  Ken Engstrom ,  Tim Grieme ,  Ahmad Sheikh ,  Jianzhang Mei

发明人： Yiyin Ku ,  Keith F. McDaniel ,  Hui-Ju Chen ,  Jason P. Shanley ,  Dale J. Kempf ,  David J. Grampovnik ,  Ying Sun ,  Dong Liu ,  Yonghua Gai ,  Yat Sun Or ,  Seble H. Wagaw ,  Ken Engstrom ,  Tim Grieme ,  Ahmad Sheikh ,  Jianzhang Mei

IPC分类号： A61K38/12 ,  A61P31/12 ,  C07K5/12

CPC分类号： C07K1/113 ,  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.

公开(公告)号：US20100144608A1

公开(公告)日：2010-06-10

申请号：US12584716

申请日：2009-09-10

申请人： Yiyin Ku ,  Keith F. McDaniel ,  Hui-Ju Chen ,  Jason P. Shanley ,  Dale J. Kempf ,  David J. Grampovnik ,  Ying Sun ,  Dong Liu ,  Yonghua Gai ,  Yat Sun Or ,  Seble H. Wagaw ,  Ken Engstrom ,  Tim Grieme ,  Ahmad Sheikh ,  Jianzhang Mei

发明人： Yiyin Ku ,  Keith F. McDaniel ,  Hui-Ju Chen ,  Jason P. Shanley ,  Dale J. Kempf ,  David J. Grampovnik ,  Ying Sun ,  Dong Liu ,  Yonghua Gai ,  Yat Sun Or ,  Seble H. Wagaw ,  Ken Engstrom ,  Tim Grieme ,  Ahmad Sheikh ,  Jianzhang Mei

IPC分类号： A61K38/12 ,  C07D487/04 ,  A61P31/12

CPC分类号： C07K1/113 ,  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。

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.

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。

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

IPC分类号： A61K38/12 ,  A61P31/12 ,  C07K5/087

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。

公开(公告)号：US09193740B2

公开(公告)日：2015-11-24

申请号：US12907614

申请日：2010-10-19

申请人： Yonghua Gai ,  Yat Sun Or ,  Guoqiang Wang

发明人： Yonghua Gai ,  Yat Sun Or ,  Guoqiang Wang

IPC分类号： C07D498/22 ,  A61K38/12 ,  A61K38/21 ,  A61P31/14 ,  A61K31/495 ,  A61K45/06

CPC分类号： C07D498/22 ,  A61K31/495 ,  A61K45/06

摘要： The present invention discloses compounds of formula Ia or Ib 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Ia或Ib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。

公开(公告)号：US20110123496A1

公开(公告)日：2011-05-26

申请号：US12907614

申请日：2010-10-19

申请人： Yonghua Gai ,  Yat Sun Or ,  Guoqiang Wang

发明人： Yonghua Gai ,  Yat Sun Or ,  Guoqiang Wang

IPC分类号： A61K38/12 ,  C07K5/087 ,  C07D498/22 ,  A61P31/12 ,  A61P31/14 ,  A61K38/21 ,  A61K39/00 ,  C07K1/00 ,  C12N7/06

CPC分类号： C07D498/22 ,  A61K31/495 ,  A61K45/06

摘要： The present invention discloses compounds of formula Ia or Ib 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Ia或Ib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。

公开(公告)号：US20110033420A1

公开(公告)日：2011-02-10

申请号：US12759132

申请日：2010-04-13

申请人： Yonghua Gai ,  Yat Sun Or ,  Guoqiang Wang

发明人： Yonghua Gai ,  Yat Sun Or ,  Guoqiang Wang

IPC分类号： A61K38/12 ,  C07K5/083 ,  A61P31/14 ,  A61K38/21 ,  A61P35/00 ,  A61P31/04 ,  A61P31/10

CPC分类号： A61K38/21 ,  A61K45/06 ,  C07K5/06034 ,  C07K5/0808 ,  C07K5/0812 ,  A61K2300/00

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. 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：US08936781B2

公开(公告)日：2015-01-20

申请号：US12759132

申请日：2010-04-13

申请人： Yonghua Gai ,  Yat Sun Or ,  Guoqiang Wang

发明人： Yonghua Gai ,  Yat Sun Or ,  Guoqiang Wang

IPC分类号： A61K38/12 ,  C07K5/083 ,  A61P31/14 ,  A61K38/21 ,  A61P35/00 ,  A61P31/04 ,  A61P31/10 ,  C07K5/087 ,  A61K45/06 ,  C07K5/062

CPC分类号： A61K38/21 ,  A61K45/06 ,  C07K5/06034 ,  C07K5/0808 ,  C07K5/0812 ,  A61K2300/00

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. 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。