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1. 发明申请

WO2006083271A3 SUBSTITUTED ARYL ACYLTHIOUREAS AND RELATED COMPOUNDS; INHIBITORS OF VIRAL REPLICATION 审中-公开
公开(公告)号：WO2006083271A3
公开(公告)日：2006-08-10
申请号：PCT/US2005/017308
申请日：2005-05-17
申请人： ACHILLION PHARMACEUTICALS, INC. , PHADKE, Avinash , CHEN, Dawei , DESHPANDE, Milind , THURKAUF, Andrew , WANG, Xiangzhu , SHEN, Yiping , LIU, Cuixian , QUINN, Jesse , LI, Shouming , OHKANDA, Junko
发明人： PHADKE, Avinash , CHEN, Dawei , DESHPANDE, Milind , THURKAUF, Andrew , WANG, Xiangzhu , SHEN, Yiping , LIU, Cuixian , QUINN, Jesse , LI, Shouming , OHKANDA, Junko
IPC分类号： C07C335/26 , A61K31/17 , A61P31/12 , C07D211/22 , C07D211/46 , C07D211/60 , C07D211/64 , C07D211/78 , C07D213/56 , C07D213/82 , C07D215/54 , C07D231/14 , C07D233/54 , C07D233/90 , C07D237/24
摘要： The invention provides certain acylthiourea derivatives and pharmaceutically acceptable salts thereof. These compounds possess potent antiviral activity. The invention particularly provides compounds that are potent and/or selective inhibitors of hepatitis C virus replication. The invention also provides pharmaceutical compositions containing a compound of the invention and at least one pharmaceutically acceptable excipient and packaged pharmaceutical compositions comprising such a pharmaceutical composition in a container together with instructions for using the composition to treat a viral infection. The invention further comprises a method of inhibiting hepatitis C virus replication by contacting a compound of the invention with a cell that is infected by hepatitis C virus and a method of treating or preventing hepatitis C viral infection by administering an amount of a compound of the invention to a subject in need thereof.

2. 发明申请

WO2004046095A1 SUBSTITUTED ARYL THIOUREAS AND RELEATED COMPOUNDS; INHIBITORS OF VIRAL REPLICATION 审中-公开
标题翻译：取代的芳香化合物和相关化合物; VIRAL REPLICATION的抑制剂
公开(公告)号：WO2004046095A1
公开(公告)日：2004-06-03
申请号：PCT/US2003/036809
申请日：2003-11-18
申请人： ACHILLION PHARMACEUTICALS, INC. , CHEN, Dawei , DESHPANDE, Milind , THURKAUF, Andrew , PHADKE, Avinash , WANG, Xiangzhu , SHEN, Yiping , LIU, Cuixian , QUINN, Jesse , OHKANDA, Junko , LI, Shouming
发明人： CHEN, Dawei , DESHPANDE, Milind , THURKAUF, Andrew , PHADKE, Avinash , WANG, Xiangzhu , SHEN, Yiping , LIU, Cuixian , QUINN, Jesse , OHKANDA, Junko , LI, Shouming
IPC分类号： C07C335/26
CPC分类号： C07D209/48 , C07C335/26 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D207/12 , C07D207/16 , C07D207/34 , C07D207/416 , C07D209/42 , C07D211/14 , C07D211/62 , C07D211/70 , C07D211/86 , C07D213/64 , C07D213/65 , C07D213/81 , C07D215/06 , C07D215/48 , C07D217/04 , C07D231/14 , C07D233/42 , C07D233/90 , C07D239/26 , C07D241/24 , C07D241/44 , C07D249/06 , C07D257/04 , C07D261/18 , C07D263/34 , C07D263/57 , C07D271/08 , C07D271/12 , C07D277/56 , C07D277/66 , C07D277/68 , C07D285/06 , C07D295/135 , C07D295/15 , C07D307/52 , C07D307/68 , C07D307/85 , C07D311/24 , C07D311/66 , C07D317/66 , C07D319/20 , C07D333/20 , C07D333/34 , C07D333/38 , C07D333/70 , C07D405/04 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D487/04 , C07D495/04
摘要： The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A1, A2, R1, R2, V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/ or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These infectious diseases include viral infections, particularly HCV infections. The invention is particularly includes methods of treating human patients suffering from an infectious disease, but also encompasses methods of treating other animals, including livestock and domesticated companion animals, suffering from an infectious disease. Methods of treatment include administering a compound of Formula I as a single active agent or administering a compound of Formula I in combination with on or more other therapeutic agent.
摘要翻译：本发明提供式I的化合物和药学上可接受的盐，其中变量A1，A2，R1，R2，V，W，X，Y和Z在本文中定义。某些本文所述的具有强抗病毒活性的式I化合物。本发明特别提供了作为丙型肝炎病毒复制的有效和/或选择性抑制剂的式I化合物。本发明还提供含有一种或多种式I化合物或这些化合物的盐，溶剂化物或酰化前药以及一种或多种药学上可接受的载体，赋形剂或稀释剂的药物组合物。本发明还包括通过向这些患者施用一定量的有效减少疾病或病症的体征或症状的式I化合物来治疗患有某些感染性疾病的患者的方法。这些传染病包括病毒感染，特别是HCV感染。本发明特别包括治疗患有感染性疾病的人类患者的方法，还包括治疗其它动物（包括患有传染病的家畜和驯养的伴侣动物）的方法。治疗方法包括给予式I化合物作为单一活性剂或将一种式I化合物与一种或多种其它治疗剂组合施用。

3. 发明申请

WO2005007601A2 SUBSTITUTED ARYLTHIOUREA DERIVATIVES USEFUL AS INHIBITORS OF VIRAL REPLICATION 审中-公开
标题翻译：用作病毒复制抑制剂的取代的芳香硫脲衍生物
公开(公告)号：WO2005007601A2
公开(公告)日：2005-01-27
申请号：PCT/US2004/022599
申请日：2004-07-08
申请人： ACHILLION PHARMACEUTICALS, INC. , PHADKE, Avinash , QUINN, Jesse , OHKANDA, Junko , THURKAUF, Andrew , SHEN, Yiping , LIU, Cuixian , CHEN, Dawei , LI, Shouming
发明人： PHADKE, Avinash , QUINN, Jesse , OHKANDA, Junko , THURKAUF, Andrew , SHEN, Yiping , LIU, Cuixian , CHEN, Dawei , LI, Shouming
IPC分类号： C07C15/00
CPC分类号： C07D211/64 , C07C335/12 , C07C335/14 , C07C335/16 , C07C335/18 , C07C335/20 , C07C335/22 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/44 , C07D211/14 , C07D211/62 , C07D215/06 , C07D217/04 , C07D295/135 , C07D317/66
摘要： Substituted arylthiourea compounds of Formula I, and the pharmaceutically acceptable salts of such compounds, useful as antiviral agents, are provided herein. Certain substituted arylthioureas disclosed herein are potent and/ or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions containing one or more substituted arylthiourea compounds and one or more pharmaceutically acceptable carriers, excipients, or diluents are provided herein. Such pharmaceutical compositions may contain a substituted arylthiourea as the only active agent or may contain a combination of a substituted arylthiourea derivative and one or more other pharmaceutically active agents. Methods of treating Hepatitis C viral infections in mammals are also provided herein.
摘要翻译：本文提供了式I的取代的芳基硫脲化合物和可用作抗病毒剂的此类化合物的药学上可接受的盐。本文公开的某些取代的芳基硫脲是病毒复制的有效和/或选择性抑制剂，特别是丙型肝炎病毒复制。本文提供了含有一种或多种取代的芳基硫脲化合物和一种或多种药学上可接受的载体，赋形剂或稀释剂的药物组合物。这种药物组合物可以含有取代的芳基硫脲作为唯一的活性剂，或者可以含有取代的芳基硫脲衍生物和一种或多种其它药物活性剂的组合。本文还提供了治疗哺乳动物的丙型肝炎病毒感染的方法。

4. 发明申请

WO2005067900A2 AZABENZOFURAN SUBSTITUTED THIOUREAS; INHIBITORS OF VIRAL REPLICATION 审中-公开
标题翻译： AZABENZOFURAN取代硫酸盐; VIRAL REPLICATION的抑制剂
公开(公告)号：WO2005067900A2
公开(公告)日：2005-07-28
申请号：PCT/US2005/000339
申请日：2005-01-05
申请人： ACHILLION PHARMACEUTICALS, INC. , THURKAUF, Andrew , CHEN, Dawei , PHADKE, Avinash , LI, Shouming , DESHPANDE, Milind
发明人： THURKAUF, Andrew , CHEN, Dawei , PHADKE, Avinash , LI, Shouming , DESHPANDE, Milind
IPC分类号： A61K31/00
CPC分类号： A61K31/00 , A61K31/4355 , C07D491/04
摘要： The present invention provides compounds of Formula: (1), wherein the variables Ar, A 1 , A 2 , A 3 , A 4 , R 5 , R 6 , R 7 , V, W, X, and Y are defined herein. Certain compounds of Formula (1) described herein possess potent antiviral activity. The invention also provides compounds of Formula (1) that are potent and/ or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compounds of Formula (1), or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula (1) effective to reduce signs or symptoms of the disease. These infectious diseases include viral infections, particularly HCV infections. The invention is particularly includes methods of treating human patients suffering from an infectious disease, but also encompasses methods of treating other animals, including livestock and domesticated companion animals, suffering from an infectious disease. Methods of treatment include administering a compound of Formula (1) as a single active agent or administering a compound of Formula (1) in combination with on or more other therapeutic agent.
摘要翻译：本发明提供式（1）的化合物，其中变量Ar，A1，A2，A3，A4，R5，R6，R7，V，W，X和Y在本文中定义。某些本文所述的式（1）化合物具有有效的抗病毒活性。本发明还提供了作为丙型肝炎病毒复制的有效和/或选择性抑制剂的式（1）化合物。本发明还提供了含有一种或多种式（1）化合物或这些化合物的盐，溶剂化物或酰化前药以及一种或多种药学上可接受的载体，赋形剂或稀释剂的药物组合物。本发明还包括通过向这些患者施用一定量的有效减少疾病体征或症状的式（1）化合物来治疗患有某些感染性疾病的患者的方法。这些传染病包括病毒感染，特别是HCV感染。本发明特别包括治疗患有感染性疾病的人类患者的方法，还包括治疗其它动物（包括患有传染病的家畜和驯养的伴侣动物）的方法。治疗方法包括施用作为单一活性剂的式（1）化合物或将式（1）的化合物与一种或多种其它治疗剂组合施用。

5. 发明申请

WO2005095345A2 HETEROARYL GUANIDINES ; INHIBITORS OF VIRAL REPLICATION 审中-公开
标题翻译：国际货币基金组织 VIRAL REPLICATION的抑制剂
公开(公告)号：WO2005095345A2
公开(公告)日：2005-10-13
申请号：PCT/US2005/009710
申请日：2005-03-23
申请人： ACHILLION PHARMACEUTICALS, INC. , CHEN, Xi , LIU, Ciuxan , THURKAUF, Andrew , LOUISE-MAY, Shirley
发明人： CHEN, Xi , LIU, Ciuxan , THURKAUF, Andrew , LOUISE-MAY, Shirley
IPC分类号： C07D213/75
CPC分类号： C07C279/18 , C07D213/75 , C07D213/82 , C07D239/42 , C07D239/47 , C07D239/545 , C07D239/84 , C07D401/12 , C07D403/12 , C07D405/12 , C07D417/12
摘要： Compounds of Formula (1), and pharmaceutically acceptable forms thereof, are provided wherein the variables X, Y, Z, A l , R 2 , R 3 , R 4 , R 5 and R 6 are defined herein. Certain compounds of Formula 1 described herein which possess potent antiviral activity. Certain compounds of Formula (1) that are potent and/ or selective inhibitors of Hepatitis C virus replication. Pharmaceutical compositions containing one or more compounds of Formula (1), or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents are also provided. Methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula (1) effective to reduce signs or symptoms of the disease or disorder are disclosed. These infectious diseases include viral infections, particularly HCV infections. Methods of treating human patients suffering from an infectious disease, but also encompasses methods of treating other animals, including livestock and domesticated companion animals, suffering from an infectious disease. Methods of treatment include administering a compound of Formula (1) as a single active agent or administering a compound of Formula (1) in combination with on or more other therapeutic agent.
摘要翻译：提供式（1）的化合物及其药学上可接受的形式，其中变量X，Y，Z，Al，R 2，R 3，R 4，R 5和R 6在本文中定义。某些本文所述的具有强抗病毒活性的式1的化合物。某些式（1）化合物是丙型肝炎病毒复制的有效和/或选择性抑制剂。还提供了含有一种或多种式（1）化合物或这些化合物的盐，溶剂化物或酰化前药以及一种或多种药学上可接受的载体，赋形剂或稀释剂的药物组合物。公开了通过向这些患者施用一定量的有效减少疾病或病症的体征或症状的式（1）化合物来治疗患有某些感染性疾病的患者的方法。这些传染病包括病毒感染，特别是HCV感染。治疗患有感染性疾病的人类患者的方法，还包括治疗其他动物，包括患有传染病的家畜和驯养的伴侣动物的方法。治疗方法包括施用作为单一活性剂的式（1）化合物或将式（1）的化合物与一种或多种其它治疗剂组合施用。

6. 发明申请

WO2003082826A1 SUBSTITUTED BIARYL AMIDES AS C5A RECEPTOR MODULATORS 审中-公开
标题翻译：作为C5A受体调节剂的取代的二元胺
公开(公告)号：WO2003082826A1
公开(公告)日：2003-10-09
申请号：PCT/US2003/009045
申请日：2003-03-25
申请人： NEUROGEN CORPORATION , GAO, Yang , HUTCHISON, Alan , PETERSON, John , PRINGLE, Wallace , THURKAUF, Andrew , YOON, Taeyoung , ZHAO, He
发明人： GAO, Yang , HUTCHISON, Alan , PETERSON, John , PRINGLE, Wallace , THURKAUF, Andrew , YOON, Taeyoung , ZHAO, He
IPC分类号： C07D215/00
CPC分类号： C07D249/08 , C07C233/65 , C07C235/62 , C07C2602/08 , C07D207/327 , C07D209/08 , C07D231/12 , C07D231/56 , C07D233/56 , C07D235/06 , C07D317/58 , C07D333/24
摘要： Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
摘要翻译：提供式I的取代的联芳酰胺。这些化合物是可用于在体内或体外调节C5a受体活性的配体，并且特别可用于治疗与人类，驯养的伴侣动物和家畜中的病理性C5a受体激活相关的病症。还提供了用于治疗这些病症的药物组合物和方法，以及使用这些配体进行受体定位研究的方法。

7. 发明授权

EP1747196B1 SUBSTITUTED ARYL ACYLTHIOUREAS AND RELATED COMPOUNDS; INHIBITORS OF VIRAL REPLICATION 有权
标题翻译：取代的芳基acylthioureas及相关化合物病毒复制抑制剂
公开(公告)号：EP1747196B1
公开(公告)日：2010-02-10
申请号：EP05856726.4
申请日：2005-05-17
申请人： Achillion Pharmaceuticals, Inc.
发明人： PHADKE, Avinash , CHEN, Dawei , DESHPANDE, Milind , THURKAUF, Andrew , WANG, Xiangzhu , SHEN, Yiping , CUIXIAN, Liu , JESSE, Quinn , LI, Shouming , OHKANDA, Junko
IPC分类号： C07C335/26 , A61K31/17 , A61P31/12 , C07D211/22 , C07D211/46 , C07D211/64 , C07D211/78 , C07D213/16 , C07D213/82 , C07D215/54 , C07D231/14 , C07D233/54 , C07D233/90 , C07D237/24
CPC分类号： C07D295/15 , C07C335/26 , C07D211/22 , C07D211/46 , C07D211/60 , C07D211/64 , C07D211/78 , C07D213/56 , C07D213/82 , C07D215/54 , C07D231/14 , C07D233/54 , C07D233/64 , C07D233/90 , C07D237/24 , C07D239/28 , C07D241/24 , C07D241/44 , C07D249/06 , C07D253/07 , C07D261/18 , C07D263/34 , C07D263/58 , C07D265/30 , C07D271/12 , C07D277/56 , C07D277/68 , C07D285/06 , C07D307/68 , C07D307/84 , C07D307/85 , C07D309/38 , C07D311/58 , C07D333/38 , C07D401/04 , C07D401/12 , C07D405/04 , C07D409/04 , C07D409/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D417/14 , C07D419/12 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04 , C07D513/04
摘要： The invention provides certain acylthiourea derivatives and pharmaceutically acceptable salts thereof. These compounds possess potent antiviral activity. The invention particularly provides compounds that are potent and/or selective inhibitors of hepatitis C virus replication. The invention also provides pharmaceutical compositions containing a compound of the invention and at least one pharmaceutically acceptable excipient and packaged pharmaceutical compositions comprising such a pharmaceutical composition in a container together with instructions for using the composition to treat a viral infection. The invention further comprises a method of inhibiting hepatitis C virus replication by contacting a compound of the invention with a cell that is infected by hepatitis C virus and a method of treating or preventing hepatitis C viral infection by administering an amount of a compound of the invention to a subject in need thereof.

8. 发明申请

WO2004018460A1 AMINO METHYL IMIDAZOLES AS C5A RECEPTOR MODULATORS 审中-公开
标题翻译：氨基甲基咪唑作为C5A受体调节剂
公开(公告)号：WO2004018460A1
公开(公告)日：2004-03-04
申请号：PCT/US2003/026432
申请日：2003-08-21
申请人： NEUROGEN CORPORATION , THURKAUF, Andrew , ZHAO, He , ZHANG, Suoming , GAO, Yang
发明人： THURKAUF, Andrew , ZHAO, He , ZHANG, Suoming , GAO, Yang
IPC分类号： C07D405/12
CPC分类号： C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14
摘要： Amino methyl imidazoles of Formula (I) are provided: wherein R, R l , R 2 , R 3 , R 4 , R 5 , and R 6 are defined herein.Such compounds are ligands of C5a receptors. Preferred compounds of Formula (I) bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. This invention also relates to pharmaceutical compositions comprising such compounds. It further relates to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. Additionally, this invention provides labeled amino methyl imidazoles compounds, which are useful as probes for the localization of C5a receptors.
摘要翻译：提供式（I）的氨基甲基咪唑：其中R，R 1，R 2，R 3，R 4，R 5和R 6在本文中定义。这些化合物是C5a受体的配体。优选的式（I）化合物以高亲和力结合C5a受体，并在C5a受体上呈现中性拮抗剂或反向激动剂活性。本发明还涉及包含这些化合物的药物组合物。它还涉及这些化合物在治疗各种炎性，心血管和免疫系统疾病中的用途。此外，本发明提供标记的氨基甲基咪唑化合物，其可用作C5a受体定位的探针。

9. 发明申请

WO2005007087A2 SUBSTITUTED (HETEROCYCLOALKYL)METHYL AZOLE DERIVATIVES AS C5A RECEPTOR MODULATORS 审中-公开
标题翻译：作为C5A受体调节剂的取代（杂环烷基）甲基偶氮衍生物
公开(公告)号：WO2005007087A2
公开(公告)日：2005-01-27
申请号：PCT/US2004/021191
申请日：2004-06-30
申请人： NEUROGEN CORPORATION , ZHANG, Suoming , HE, Zhao , GAO, Yang , THURKAUF, Andrew , MAYNARD, George , BERTRAND, Chenard , OHLIGER, Robert , PETERSON, John, M.
发明人： ZHANG, Suoming , HE, Zhao , GAO, Yang , THURKAUF, Andrew , MAYNARD, George , BERTRAND, Chenard , OHLIGER, Robert , PETERSON, John, M.
IPC分类号： A61K
CPC分类号： C07D405/14 , C07D233/68 , C07D401/06 , C07D401/14 , C07D403/06 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/14
摘要： (Heterocycloalkyl)methyl azole derivatives of Formula (I) are provided: Formula I wherein A is oxygen, sulfur, or NR; J and K and each L are independently oxygen, sulfur, NH, or CH 2 ; and the remaining variables are defined herein. Such compounds are modulators of C5a receptors, and preferably bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. Also provided herein are pharmaceutical compositions comprising such compounds, as well as methods for using such compounds in treating a variety of inflammatory and immune system disorders.
摘要翻译：（I）的（杂环烷基）甲基唑衍生物：式I其中A是氧，硫或NR; J和K各自独立地为氧，硫，NH或CH 2; 并且其余的变量在本文中定义。这些化合物是C5a受体的调节剂，优选以高亲和力结合C5a受体，并在C5a受体上显示中性拮抗剂或反向激动剂活性。本文还提供了包含这些化合物的药物组合物，以及使用这些化合物治疗各种炎性和免疫系统疾病的方法。

10. 发明申请

WO2003082829A1 NEW ARYL IMIDAZOLES AND RELATED COMPOUNDS AS C5A RECEPTOR MODULATORS 审中-公开
标题翻译：作为C5A受体调节剂的新ARYL咪唑和相关化合物
公开(公告)号：WO2003082829A1
公开(公告)日：2003-10-09
申请号：PCT/US2003/009938
申请日：2003-03-28
申请人： NEUROGEN CORPORATION , LUKE, George, P. , MAYNARD, George , MITCHELL, Scott , THURKAUF, Andrew , XIE, Linghong , ZHANG, LuYan , ZHANG, Suoming , ZHAO, He , CHENARD, Bertrand, L. , GAO, Yang , HAN, Bingsong , HE, Xiao, Shu
发明人： LUKE, George, P. , MAYNARD, George , MITCHELL, Scott , THURKAUF, Andrew , XIE, Linghong , ZHANG, LuYan , ZHANG, Suoming , ZHAO, He , CHENARD, Bertrand, L. , GAO, Yang , HAN, Bingsong , HE, Xiao, Shu
IPC分类号： C07D233/54
CPC分类号： C07D233/64 , A61K31/4164 , C07D233/68 , C07D235/02 , C07D235/30 , C07D237/12 , C07D401/04 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The invention provides Aryl substituted imidazoles, pyrazoles, pyridizines and related compounds of the Formula (I) where the ring system represented by Formula (A) is a 5 membered heteroaryl ring system, in which x is 0, A is chosen from carbon and heteroatoms nitrogen, oxygen, and sulfur, and E and G are independently carbon or nitrogen, provided that the 5 membered heteroaryl ring system does not contain more than 3 heteroatoms or more than 1 oxygen or sulfur atom, or a 6 membered heteroaryl ring system, in which x is 1, A, B, E, and G are independently chosen from carbon and nitrogen, provided that the 6 membered heteroaryl ring system does not contain more than 3 nitrogen atoms. The remaining variables, Ar 1 , Ar 2 , R, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , y and z are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of the invention act bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. This invention also relates to pharmaceutical compositions comprising such compounds. It further relates to the use of such compounds in treating a variety of inflammatory and immune system disorders.
摘要翻译：本发明提供了式（I）的芳基取代的咪唑，吡唑，吡啶和相关化合物，其中由式（A）表示的环系是5元杂芳基环系，其中x是0，A选自碳和杂原子氮，氧和硫，并且E和G独立地为碳或氮，条件是5元杂芳基环系不包含多于3个杂原子或多于1个氧或硫原子或6元杂芳基环系，其中x为1，A，B，E和G独立地选自碳和氮，条件是6元杂芳基环系不含3个以上的氮原子。剩余的变量Ar1，Ar2，R，R1，R2，R3，R4，R5，R6，y和z在本文中定义。这些化合物是C5a受体的配体。本发明优选的化合物作用以高亲和力结合C5a受体，在C5a受体上表现出中性拮抗剂或反向激动剂活性。本发明还涉及包含这些化合物的药物组合物。它还涉及这些化合物在治疗各种炎性和免疫系统疾病中的应用。

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