公开(公告)号：US20060058248A1

公开(公告)日：2006-03-16

申请号：US11257680

申请日：2005-10-25

申请人： Guoyou Xu ,  Datong Tang ,  Yonghua Gai ,  Heejin Kim ,  Guoqiang Wang ,  Ly Phan ,  Yat Or ,  Zhe Wang

发明人： Guoyou Xu ,  Datong Tang ,  Yonghua Gai ,  Heejin Kim ,  Guoqiang Wang ,  Ly Phan ,  Yat Or ,  Zhe Wang

IPC分类号： C07H17/08 ,  A61K31/7052 ,  C07D403/04

CPC分类号： C07D401/04

摘要： The present invention relates to processes and intermediates for the preparation of 6-11 bicyclic erythromycin derivatives. In particular, the present invention relates to processes and intermediates for the preparation of a compound of formula (IX-c):

摘要翻译： 本发明涉及制备6-11双环红霉素衍生物的方法和中间体。 特别地，本发明涉及制备式（Ⅸ-c）化合物的方法和中间体：

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。

公开(公告)号：US20070299078A1

公开(公告)日：2007-12-27

申请号：US11768723

申请日：2007-06-26

申请人： Deqiang Niu ,  Dong Liu ,  Joel Moore ,  Guoyou Xu ,  Ying Sun ,  Yonghua Gai ,  Datong Tang ,  Yat Or ,  Zhe Wang

发明人： Deqiang Niu ,  Dong Liu ,  Joel Moore ,  Guoyou Xu ,  Ying Sun ,  Yonghua Gai ,  Datong Tang ,  Yat Or ,  Zhe Wang

IPC分类号： A61K31/498 ,  A61K31/4985 ,  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。

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。

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。

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。

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。

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

IPC分类号： A61K31/70 ,  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。

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。

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

IPC分类号： A61K38/00 ,  A01N37/18 ,  C07D487/04 ,  A61K38/21 ,  C07K5/078 ,  C07K5/087

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。