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1. 发明授权

US08361958B2 Oximyl HCV serine protease inhibitors 有权
标题翻译： Oximyl HCV丝氨酸蛋白酶抑制剂
公开(公告)号：US08361958B2
公开(公告)日：2013-01-29
申请号：US12328433
申请日：2008-12-04
申请人： Yonghua Gai , Yat Sun Or , Zhe Wang
发明人： Yonghua Gai , Yat Sun Or , Zhe Wang
IPC分类号： A61K38/00
CPC分类号： A61K38/21 , C07D207/12 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
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。

2. 发明授权

US08324155B2 Quinoxaline-containing compounds as hepatitis C virus inhibitors 有权
标题翻译：含喹喔啉的化合物作为丙型肝炎病毒抑制剂
公开(公告)号：US08324155B2
公开(公告)日：2012-12-04
申请号：US12271144
申请日：2008-11-14
申请人： Yonghua Gai , Yat Sun Or , Zhe Wang
发明人： Yonghua Gai , Yat Sun Or , Zhe Wang
IPC分类号： A61K38/00 , A61K31/33 , A61K38/06 , A61K38/05 , A61K31/495 , A61K31/50 , C07D513/00
CPC分类号： C07K5/1027 , C07D498/18 , C07D498/22 , C07K5/0827 , C07K5/1021
摘要： The present invention discloses compounds of formula 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 a pharmaceutical composition comprising the compounds 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. 发明授权

US08101567B2 Heteroaryl-containing tripeptide HCV serine protease inhibitors 有权
标题翻译：含杂芳基的三肽HCV丝氨酸蛋白酶抑制剂
公开(公告)号：US08101567B2
公开(公告)日：2012-01-24
申请号：US12357805
申请日：2009-01-22
申请人： Yonghua Gai , Yat Sun Or , Zhe Wang
发明人： Yonghua Gai , Yat Sun Or , Zhe Wang
IPC分类号： A61K38/00
CPC分类号： A61K31/4965 , A61K38/21 , C07K5/06034 , C07K5/0808 , C07K5/1016 , C07K14/811 , Y02A50/463 , 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。

4. 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。

5. 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。

6. 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。

7. 发明申请

US20090041721A1 ARYLALKOXYL HEPATITIS C VIRUS PROTEASE INHIBITORS 失效
公开(公告)号：US20090041721A1
公开(公告)日：2009-02-12
申请号：US11836288
申请日：2007-08-09
申请人： Deqiang Niu , Yonghua Gai , Yat Sun Or , Zhe Wang
发明人： Deqiang Niu , Yonghua Gai , Yat Sun Or , Zhe Wang
IPC分类号： A61K31/40 , A61K31/4025 , A61K31/407 , A61K31/4709 , A61K31/7056 , A61K38/21 , A61P31/12 , C07D207/16 , C07D401/02 , C07D405/12 , C07D409/12 , C07D487/04
CPC分类号： C07D487/04 , A61K38/21 , A61K38/212 , C07D207/16 , C07D401/12 , C07D405/12 , C07D409/12 , C07K5/0804 , C07K5/0808 , A61K2300/00
摘要： The present invention discloses 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：本发明公开了式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。

8. 发明授权

US07517859B2 Spirocyclic bicyclolides 有权
标题翻译：螺环双环
公开(公告)号：US07517859B2
公开(公告)日：2009-04-14
申请号：US11416739
申请日：2006-05-03
申请人： Yonghua Gai , Datong Tang , Ying Sun , Zhigang Chen , Yat Sun Or , Zhe Wang
发明人： Yonghua Gai , Datong Tang , Ying Sun , Zhigang Chen , Yat Sun Or , Zhe Wang
IPC分类号： A61K31/70 , 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。

9. 发明申请

US20080248105A1 POLYMORPHIC FORMS OF 6-11 BICYCLIC KETOLIDE DERIVATIVES 审中-公开
标题翻译： 6-11双相胶体衍生物的多晶型
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。

10. 发明授权

US07384921B2 Polymorphic forms of 6-11 bicyclic ketolide derivatives 有权
标题翻译： 6-11双环酮内酯衍生物的多形态
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。

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