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21. 发明授权

US07842813B2 Processes for the preparation of O-[5-(4-amino-thiazol-2-yl)-pyridin-2-ylmethyl]-hydroxylamine 有权
标题翻译：制备O- [5-（4-氨基 - 噻唑-2-基） - 吡啶-2-基甲基] - 羟胺的方法
公开(公告)号：US07842813B2
公开(公告)日：2010-11-30
申请号：US12437636
申请日：2009-05-08
申请人： Datong Tang , Yinglin Han , Yanhe Huang , Ly Tam Phan , Yat Sun Or , Zhe Wang
发明人： Datong Tang , Yinglin Han , Yanhe Huang , Ly Tam Phan , Yat Sun Or , Zhe Wang
IPC分类号： C07D417/04
CPC分类号： C07D417/04
摘要： The present invention relates generally to novel methods for the synthesis of O-[5-(4-amino-thiazol-2-yl)-pyridin-2-ylmethyl]-hydroxylamine which is an essential reagent in the synthesis of one of the bridged erythromycin derivatives and their respective pharmaceutically acceptable salts in PCT Application WO 03/097659 A1. In particular, the present invention relates to processes and intermediates for the preparation of a compound of formula (Ia):
摘要翻译：本发明一般涉及合成O- [5-（4-氨基 - 噻唑-2-基） - 吡啶-2-基甲基] - 羟胺的新方法，其是合成桥接的红霉素衍生物及其各自的药学上可接受的盐在PCT申请WO 03/097659 A1中。特别地，本发明涉及制备式（Ia）化合物的方法和中间体：

22. 发明授权

US07718769B2 Tri-peptide hepatitis C serine protease inhibitors 有权
标题翻译：三肽丙型肝炎丝氨酸蛋白酶抑制剂
公开(公告)号：US07718769B2
公开(公告)日：2010-05-18
申请号：US11602586
申请日：2006-11-20
申请人： Zhenwei Miao , Ying Sun , Suanne Nakajima , Datong Tang , Zhe Wang , Yat Sun Or
发明人： Zhenwei Miao , Ying Sun , Suanne Nakajima , Datong Tang , Zhe Wang , Yat Sun 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。

23. 发明授权

US07718612B2 Pyridazinonyl macrocyclic hepatitis C serine protease inhibitors 有权
标题翻译：哒嗪基大环丙型肝炎丝氨酸蛋白酶抑制剂
公开(公告)号：US07718612B2
公开(公告)日：2010-05-18
申请号：US11832893
申请日：2007-08-02
申请人： Joel D. Moore , Datong Tang , Yat Sun Or , Zhe Wang
发明人： Joel D. Moore , Datong Tang , Yat Sun Or , Zhe Wang
IPC分类号： A61K38/12 , C07K5/12
CPC分类号： C07K5/0802 , A61K38/21 , A61K45/06 , A61K2300/00
摘要： The present invention relates to 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 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）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。

24. 发明申请

US20100070509A1 System And Method For High-Dimensional Similarity Search 审中-公开
标题翻译：高维相似性搜索的系统与方法
公开(公告)号：US20100070509A1
公开(公告)日：2010-03-18
申请号：US12542640
申请日：2009-08-17
申请人： Kai Li , Moses Charikar , Qin Lv , William Josephson , Zhe Wang
发明人： Kai Li , Moses Charikar , Qin Lv , William Josephson , Zhe Wang
IPC分类号： G06F17/30
CPC分类号： G06F16/2264 , G06F16/41 , G06K9/6277
摘要： A computer-implemented method for searching a plurality of stored objects. Data objects are placed in a hash table, an ordered sequence of locations (probing sequence) in the hash table from a query object is generated and data objects in the hash table locations in the generated ordered sequence are examined to find objects whose relationships with the query object satisfy a certain predetermined function defined on pairs of objects.
摘要翻译：一种用于搜索多个存储对象的计算机实现的方法。数据对象被放置在哈希表中，生成来自查询对象的散列表中的位置（探测序列）的有序序列，并且检查生成的有序序列中的哈希表位置中的数据对象，以查找与查询对象满足在对对象上定义的某个预定函数。

25. 发明授权

US07635683B2 Quinoxalinyl tripeptide hepatitis C virus inhibitors 有权
标题翻译：喹喔啉三肽丙型肝炎病毒抑制剂
公开(公告)号：US07635683B2
公开(公告)日：2009-12-22
申请号：US11499917
申请日：2006-08-04
申请人： Yonghua Gai , Deqiang Niu , Yat Sun Or , Zhe Wang
发明人： Yonghua Gai , Deqiang Niu , Yat Sun Or , Zhe Wang
IPC分类号： A61K38/06
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。

26. 发明申请

US20090274657A1 DIFLUOROMETHYL-CONTAINING MACROCYCLIC COMPOUNDS AS HEPATITIS C VIRUS INHIBITORS 有权
标题翻译：含有大分子化合物作为丙型肝炎病毒抑制剂
公开(公告)号：US20090274657A1
公开(公告)日：2009-11-05
申请号：US12433191
申请日：2009-04-30
申请人： Yonghua Gai , Dong Liu , Joel D. Moore , Yat Sun Or , Zhe Wang
发明人： Yonghua Gai , Dong Liu , Joel D. Moore , Yat Sun Or , Zhe Wang
IPC分类号： A61K38/21 , C07D241/36 , A61K31/4985 , A61K31/70 , A61P31/12
CPC分类号： C07D513/22 , C07D498/22 , C07D515/22
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。

27. 发明申请

US20090180985A1 BRIDGED CARBOCYCLIC OXIME HEPATITIS C VIRUS SERINE PROTEASE INHIBITORS 有权
标题翻译： BRIDGED CARBOCYCLIC OXIME HEPATITIS C病毒丝氨酸蛋白酶抑制剂
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。

28. 发明申请

US20090180983A1 BICYCLIC, C5-SUBSTITUTED PROLINE DERIVATIVES AS INHIBITORS OF THE HEPATITIS C VIRUS NS3 PROTEASE 有权
标题翻译：作为乙型肝炎病毒NS3蛋白酶的抑制剂的双相，C5取代的丙泊酚衍生物
公开(公告)号：US20090180983A1
公开(公告)日：2009-07-16
申请号：US12324048
申请日：2008-11-26
申请人： Joel D. Moore , Yat Sun Or , Zhe Wang
发明人： Joel D. Moore , Yat Sun Or , Zhe Wang
IPC分类号： A61K38/21 , C07D225/04 , A61K31/407 , A61K31/517 , A61K31/47 , A61K31/7052 , A61P31/12
CPC分类号： C07K5/0812 , A61K38/00 , C07K5/06165
摘要： The present invention relates to 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 a compound 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。

29. 发明申请

US20090123423A1 HYDROXYAMIC ANALOGS AS HEPATITIS C VIRUS SERINE PROTEASE INHIBITOR 审中-公开
标题翻译：羟脯氨酸类似物作为丙型肝炎病毒丝氨酸蛋白酶抑制剂
公开(公告)号：US20090123423A1
公开(公告)日：2009-05-14
申请号：US12108962
申请日：2008-04-24
申请人： Yonghua Gai , Yat Sun Or , Zhe Wang
发明人： Yonghua Gai , Yat Sun Or , Zhe Wang
IPC分类号： A61K31/498 , C07D409/14 , A61P31/12 , A61K31/4035 , A61K31/7056 , A61K38/21 , A61K31/4709 , C07D403/12 , C07D417/14
CPC分类号： C07D409/14 , A61K38/212 , A61K38/215 , C07D403/12 , C07D403/14 , C07D417/12 , C07D417/14 , A61K2300/00
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。

30. 发明申请

US20090047248A1 TRIAZOLYL MACROCYCLIC HEPATITIS C SERINE PROTEASE INHIBITORS 失效
标题翻译：三唑基大环内酯类抗坏血酸C蛋白酶抑制剂
公开(公告)号：US20090047248A1
公开(公告)日：2009-02-19
申请号：US11835657
申请日：2007-08-08
申请人： Ying Sun , Deqiang Niu , Yat Sun Or , Zhe Wang
发明人： Ying Sun , Deqiang Niu , Yat Sun Or , Zhe Wang
IPC分类号： A61K31/4192 , A61K31/427 , A61K31/4439 , A61K31/4709 , A61K31/506 , A61K31/5377 , A61K31/7056 , A61K38/21 , A61P31/00 , C07D487/04
CPC分类号： C07D487/04 , A61K31/4192 , A61K31/427 , A61K31/4439 , A61K31/4709 , A61K31/506 , A61K31/5377 , A61K31/7056 , A61K38/21 , C07D471/04 , 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 to the subject 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。

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