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1. 发明申请

WO2008021956A3 ACYLAMINOHETEROARYL HEPATITIS C VIRUS PROTEASE INHIBITORS 审中-公开
公开(公告)号：WO2008021956A3
公开(公告)日：2008-11-13
申请号：PCT/US2007075580
申请日：2007-08-09
申请人： ENANTA PHARM INC , NIU DEQIANG , MOORE JOEL , LIU DONG , GAI YONGHUA , CHEN ZHIGANG , OR YAT SUN , WANG ZHE
发明人： NIU DEQIANG , MOORE JOEL , LIU DONG , GAI YONGHUA , CHEN ZHIGANG , OR YAT SUN , WANG ZHE
IPC分类号： A61K38/12
CPC分类号： C07D487/04 , C07D403/14 , C07D409/14 , C07D417/14
摘要： The present invention discloses compounds of formulae (I) and (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 to the subject a pharmaceutical composition comprising a compound of the present invention.
摘要翻译：本发明公开了式（I）和（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。本发明还涉及通过向受试者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。

2. 发明申请

WO2008002924A2 QUINOXALINYL MACROCYCLIC HEPATITIS C VIRUS SERINE PROTEASE INHIBITORS 审中-公开
标题翻译：喹喔啉大环内酯类抗生素C病毒丝氨酸蛋白酶抑制剂
公开(公告)号：WO2008002924A2
公开(公告)日：2008-01-03
申请号：PCT/US2007072140
申请日：2007-06-26
申请人： ENANTA PHARM INC , OR YAT SUN , MOORE JOEL D , LIU DONG , SUN YING , GAI YONGHUA , TANG DATONG , NIU DEQIANG , XU GUOYOU , WANG ZHE
发明人： OR YAT SUN , MOORE JOEL D , LIU DONG , SUN YING , GAI YONGHUA , TANG DATONG , NIU DEQIANG , XU GUOYOU , WANG ZHE
IPC分类号： A61K31/498 , A61K38/21 , 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蛋白酶活性的化合物，包括式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。

3. 发明申请

WO2009053828A3 P3 HYDROXYAMINO MACROCYCLIC HEPATITIS C SERINE PROTEASE INHIBITORS 审中-公开
标题翻译： P3羟氨基大环内酯类C丝氨酸蛋白酶抑制剂
公开(公告)号：WO2009053828A3
公开(公告)日：2009-12-30
申请号：PCT/IB2008002839
申请日：2008-10-23
申请人： ENANTA PHARM INC , NIU DEQIANG , LIU DONG , GAI YONGHUA , OR YAT SUN , WANG ZHE
发明人： NIU DEQIANG , LIU DONG , GAI YONGHUA , OR YAT SUN , WANG ZHE
IPC分类号： A61K38/00 , C12P13/24
CPC分类号： C07D471/04 , A61K45/06 , C07K5/0804
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，本发明化合物干扰丙型肝炎病毒的生命周期，并且也可用作抗病毒剂。本发明进一步涉及包含前述化合物的药物组合物，用于给予患有HCV感染的受试者。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HCV感染的方法。

4. 发明申请

WO2010030359A8 MACROCYCLIC HEPATITIS C SERINE PROTEASE INHIBITORS 审中-公开
标题翻译：大肠杆菌C型丝氨酸蛋白酶抑制剂
公开(公告)号：WO2010030359A8
公开(公告)日：2011-05-12
申请号：PCT/US2009005082
申请日：2009-09-10
申请人： ENANTA PHARM INC , ABBOTT LAB , KU YIYIN , MCDANIEL KEITH F , CHEN HUI-JU , SHANLEY JASON P , KEMPF DALE J , GRAMPOVNIK DAVID J , SUN YING , LIU DONG , GAI YONGHUA , OR YAT SUN , WAGAW SABLE H , ENGSTROM KEN , GRIEME TIM , SHEIKH AHMAD , MEI JIANZHANG
发明人： KU YIYIN , MCDANIEL KEITH F , CHEN HUI-JU , SHANLEY JASON P , KEMPF DALE J , GRAMPOVNIK DAVID J , SUN YING , LIU DONG , GAI YONGHUA , OR YAT SUN , WAGAW SABLE H , ENGSTROM KEN , GRIEME TIM , SHEIKH AHMAD , MEI JIANZHANG
IPC分类号： A61K38/00 , A61K38/12
CPC分类号： C07K1/113 , C07D487/04
摘要： The present invention relates to novel macrocyclic compounds and methods of use thereof. 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及其使用方法。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。

5. 发明申请

WO2008019289A3 TETRAZOLYL MACROCYCLIC HEPATITIS C SERINE PROTEASE INHIBITORS 审中-公开
标题翻译：四氢大环内酯类抗生素C丝氨酸蛋白酶抑制剂
公开(公告)号：WO2008019289A3
公开(公告)日：2008-07-03
申请号：PCT/US2007075066
申请日：2007-08-02
申请人： ENANTA PHARM INC , SUN YING , LIU DONG , OR YAT SUN , WANG ZHE
发明人： SUN YING , LIU DONG , OR YAT SUN , WANG ZHE
IPC分类号： A61K38/12 , C07K7/64
CPC分类号： C07K5/0804 , A61K31/13 , A61K31/41 , A61K31/7056 , A61K38/212 , A61K38/215 , A61K45/06 , C07D487/04 , A61K2300/00
摘要： The present invention relates to compounds of Formula (I), (II), (III) or (IV), 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：本发明涉及抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒（HCV）的活性的式（I），（II），（III）或（IV）的化合物或其药学上可接受的盐，酯或前药）NS3-NS4A蛋白酶。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。

6. 发明申请

WO2008021733A2 TETRAZOLYL ACYCLIC HEPATITIS C SERINE PROTEASE INHIBITORS 审中-公开
标题翻译：四氯乙烯ACYCLIC HEPATITIS C丝氨酸蛋白酶抑制剂
公开(公告)号：WO2008021733A2
公开(公告)日：2008-02-21
申请号：PCT/US2007075015
申请日：2007-08-02
申请人： ENANTA PHARM INC , SUN YING , LIU DONG , OR YAT SUN , WANG ZHE
发明人： SUN YING , LIU DONG , OR YAT SUN , WANG ZHE
IPC分类号： A61K38/06
CPC分类号： C07K5/0808 , A61K38/21 , A61K2300/00
摘要： The present invention relates to compounds of Formula (I), (II), (III) or (IV), or pharmaceutically acceptable salts, esters or prodrugs thereof: which can 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），（II），（III）或（IV）的化合物或其药学上可接受的盐，酯或前药：可抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒）NS3-NS4A蛋白酶。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。

7. 发明申请

WO2010030359A3 MACROCYCLIC HEPATITIS C SERINE PROTEASE INHIBITORS 审中-公开
标题翻译：大肠杆菌C型丝氨酸蛋白酶抑制剂
公开(公告)号：WO2010030359A3
公开(公告)日：2010-05-27
申请号：PCT/US2009005082
申请日：2009-09-10
申请人： ENANTA PHARJMACEUTICALS INC , ABBOTT LAB , KU YIYIN , MCDANIEL KEITH F , CHEN HUI-JU , SHANLEY JASON P , KEMPF DALE J , GRAMPOVNIK DAVID J , SUN YING , LIU DONG , GAI YONGHUA , OR YAT SUN , WAGAW SABLE H , ENGSTROM KEN , GRIEME TIM , SHEIKH AHMAD , MEI JIANZHANG
发明人： KU YIYIN , MCDANIEL KEITH F , CHEN HUI-JU , SHANLEY JASON P , KEMPF DALE J , GRAMPOVNIK DAVID J , SUN YING , LIU DONG , GAI YONGHUA , OR YAT SUN , WAGAW SABLE H , ENGSTROM KEN , GRIEME TIM , SHEIKH AHMAD , MEI JIANZHANG
IPC分类号： A61K38/00 , A61K38/12
CPC分类号： C07K1/113 , C07D487/04
摘要： The present invention relates to novel macrocyclic compounds and methods of use thereof. 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及其使用方法。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。

8. 发明申请

WO2009085978A1 BRIDGED CARBOCYCLIC OXIME HEPATITIS C VIRUS SERINE PROTEASE INHIBITORS 审中-公开
标题翻译：桥环碳氧酶丙型肝炎病毒丝氨酸蛋白酶抑制剂
公开(公告)号：WO2009085978A1
公开(公告)日：2009-07-09
申请号：PCT/US2008087470
申请日：2008-12-18
申请人： ENANTA PHARCEUTICALS INC , LIU DONG , OR YAT SUN , WANG ZHE
发明人： LIU DONG , OR YAT SUN , WANG ZHE
IPC分类号： A01N33/24 , A61K31/15
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，本发明化合物干扰丙型肝炎病毒的生命周期，并且也可用作抗病毒剂。更具体地说，本发明涉及含有碳环P2单元的肟化合物，肟与P2上的一个羧酸连接。本发明进一步涉及包含前述化合物的药物组合物，用于给予患有HCV感染的受试者。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HCV感染的方法。

9. 发明公开

EP2066326A4 QUINOXALINYL MACROCYCLIC HEPATITIS C VIRUS SERINE PROTEASE INHIBITORS 审中-公开
标题翻译：甲基胆碱酯酶蛋白酶抑制剂乙型肝炎病毒
公开(公告)号：EP2066326A4
公开(公告)日：2010-09-29
申请号：EP07784548
申请日：2007-06-26
申请人： ENANTA PHARM INC
发明人： OR YAT SUN , MOORE JOEL D , LIU DONG , SUN YING , GAI YONGHUA , TANG DATONG , NIU DEQIANG , XU GUOYOU , WANG ZHE
IPC分类号： A61K31/4965 , A61P31/12 , C07D245/04 , C07D403/12
CPC分类号： C07D245/04 , A61K38/212 , A61K38/215 , C07D403/12 , A61K2300/00

10. 发明公开

EP2219454A4 MACROCYCLIC TETRAZOLYL HEPATITIS C SERINE PROTEASE INHIBITORS 审中-公开
标题翻译：抑制剂的大环四唑基丙型肝炎丝氨酸蛋白酶
公开(公告)号：EP2219454A4
公开(公告)日：2012-05-30
申请号：EP08850897
申请日：2008-11-14
申请人： ENANTA PHARM INC
发明人： SUN YING , LIU DONG , OR YAT SUN , WANG ZHE
IPC分类号： C07K5/08 , A61K38/06 , A61P31/14
CPC分类号： C07K5/0808 , A61K38/212 , A61K38/215 , C07K5/0812 , A61K2300/00

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