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2. 发明申请

WO0249993A3 HIGH AFFINITY SMALL MOLECULE C5A RECEPTOR MODULATORS 审中-公开
标题翻译：高亲和力小分子C5A受体调节剂
公开(公告)号：WO0249993A3
公开(公告)日：2003-02-20
申请号：PCT/US0026816
申请日：2000-09-29
申请人： NEUROGEN CORP , THURKAUF ANDREW , ZHANG XIAOYAN , HE XIA-SHU , ZHAO HE , PETERSON JOHN , MAYNARD GEORGE , OHLIGER ROBERT
发明人： THURKAUF ANDREW , ZHANG XIAOYAN , HE XIA-SHU , ZHAO HE , PETERSON JOHN , MAYNARD GEORGE , OHLIGER ROBERT
IPC分类号： C12N15/09 , A61K31/165 , A61K31/166 , A61K31/216 , A61K31/36 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/402 , A61K31/415 , A61K31/4155 , A61K31/417 , A61K31/4178 , A61K31/4184 , A61K31/427 , A61K31/437 , A61K31/44 , A61K31/4418 , A61K31/4439 , A61K31/47 , A61K31/4709 , A61K31/472 , A61K31/4965 , A61P1/04 , A61P3/10 , A61P7/00 , A61P7/04 , A61P7/06 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P21/04 , A61P25/00 , A61P25/28 , A61P29/00 , A61P31/04 , A61P37/02 , A61P37/06 , C07C233/73 , C07D207/32 , C07D207/327 , C07D213/38 , C07D215/12 , C07D217/04 , C07D217/06 , C07D217/14 , C07D217/16 , C07D231/12 , C07D233/54 , C07D233/64 , C07D235/18 , C07D235/30 , C07D317/58 , C07D333/24 , C07D333/28 , C07D333/54 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D417/12 , C07D471/04 , C07D521/00 , C12Q1/02 , C07D215/00 , C07D233/02 , C07D235/02 , C07D317/44 , C07D405/00 , C07D419/00 , C07D471/02
CPC分类号： C07D207/327 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/44 , A61K31/47 , C07D217/04 , C07D231/12 , C07D233/56 , C07D233/64 , C07D249/08 , C07D333/24 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D471/04
摘要： The invention includes low molecular weight, non-peptidic, non-peptidommetic, organic molecules that can act as modulators of mammalian complement C5a receptors, preferably ones that act as high affinity C5a receptor ligands and also such ligands that can act as antagonists or inverse agonists of complement C5a receptors. Preferred compounds of the invention possess some or all of the following properties in that they are: 1) multi-aryl in structure; 2) heteroaryl in structure; 3) a pharmaceutically acceptable oral dose can provide a detectable in vivo effect; 4) comprise fewer than four or preferably no amide bonds, and 5) capable of habiting leukocyte chemotaxis at nanomolar or sub-nanomolar concentrations. The invention also includes pharmaceutical composition comprising such compounds and the use of such compounds in treating a variety of inflammatory and immune system disorders.
摘要翻译：本发明包括可以充当哺乳动物补体C5a受体的调节剂的低分子量非肽，非肽，有机分子，优选用作高亲和力C5a受体配体的那些，以及可以作为拮抗剂或反向激动剂的这种配体的补体C5a受体。本发明优选的化合物具有一些或全部以下性质，因为它们是：1）结构上的多芳基; 2）结构中的杂芳基; 3）药学上可接受的口服剂量可以提供可检测的体内效应; 4）包含少于四个或优选不存在酰胺键，以及5）能够以纳摩尔或亚纳摩尔浓度吸收白细胞趋化性。本发明还包括包含这些化合物的药物组合物和这些化合物在治疗各种炎性和免疫系统疾病中的用途。

3. 发明申请

WO2005007087A3 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：WO2005007087A3
公开(公告)日：2006-03-30
申请号：PCT/US2004021191
申请日：2004-06-30
申请人： NEUROGEN CORP , 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： A61K20060101 , C07D401/00 , C07D211/00 , C07D215/00 , C07D217/00 , C07D403/00 , C07D413/00
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
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

4. 发明申请

WO0204433A3 MELANIN CONCENTRATING HORMONE RECEPTOR LIGANDS 审中-公开
标题翻译： MELANIN浓缩HORMONE受体配体
公开(公告)号：WO0204433A3
公开(公告)日：2003-09-25
申请号：PCT/US0141289
申请日：2001-07-06
申请人： NEUROGEN CORP , BAKTHAVATCHALAM RAJAGOPAL , HUTCHISON ALAN , THURKAUF ANDREW
发明人： BAKTHAVATCHALAM RAJAGOPAL , HUTCHISON ALAN , THURKAUF ANDREW
IPC分类号： G01N33/53 , A61K31/451 , A61K31/495 , A61P3/04 , A61P3/10 , A61P9/10 , A61P15/00 , A61P15/10 , A61P25/18 , C07D211/14 , C07D295/08 , C07D295/096 , G01N33/566 , A61K31/445 , C07D211/22 , C07D295/06 , C07D295/18
CPC分类号： C07D295/096
摘要： Disclosed are compounds of formula (I), and the pharmaceutically acceptable salts thereof wheren Q, X, Y, Z, and R1 R9, and R12-R19 are defined herein. These compounds are selective modulators of MCH 1 receptors that are, therefore, useful in the treatment of a variety of metabolic, feeding, and sexual disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also disclosed.
摘要翻译：公开了式（I）化合物及其药学上可接受的盐，其中Q，X，Y，Z和R 1 R 9和R 12 -R 19如本文所定义。这些化合物是MCH 1受体的选择性调节剂，因此可用于治疗各种代谢，喂养和性功能障碍。还公开了治疗这种病症以及包装的药物组合物的方法。

5. 发明申请

WO0000489A3 6-(4-ARYLALKYLPIPERAZIN-1-YL)BENZODIOXANE AND 6-(4-ARYLALKYLPIPERAZIN-1-YL)CHROMANE DERIVATIVES: DOPAMINE RECEPTOR SUBTYPE SPECIFIC LIGANDS 审中-公开
标题翻译： 6-（4-芳基烷基哌嗪-1-基）苯并二恶烷和6-（4-芳基烷基哌嗪-1-基）胆烷衍生物：多巴胺受体亚型特异性配体
公开(公告)号：WO0000489A3
公开(公告)日：2000-02-10
申请号：PCT/US9914426
申请日：1999-06-25
申请人： NEUROGEN CORP , TRAN JENNIFER N , THURKAUF ANDREW
发明人： TRAN JENNIFER N , THURKAUF ANDREW
IPC分类号： A61K31/496 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P43/00 , C07D307/79 , C07D311/58 , C07D313/08 , C07D319/18 , C07D321/10 , C07D405/04 , C07D311/04
CPC分类号： C07D319/18 , C07D311/58 , C07D313/08 , C07D321/10
摘要： Disclosed are compounds of formula (I) or the pharmaceutically acceptable acid addition salts thereof, wherein: R1, R2, R3, R4 and R5 are the same or different and represent hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C4 alkylthio, hydroxy, amino, mono- or di(C1-C6)alkylamino, cyano, nitro, trifluoromethyl or trifluoromethoxy; and X is oxygen, a bond, C1-C2 alkylene or methyleneoxy, which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.
摘要翻译：公开了式（I）化合物或其药学上可接受的酸加成盐，其中：R 1，R 2，R 3，R 4和R 5相同或不同，并且表示氢，卤素，C 1 -C 6烷基，C 1 -C 6烷氧基， C 1 -C 4烷硫基，羟基，氨基，一或二（C 1 -C 6）烷基氨基，氰基，硝基，三氟甲基或三氟甲氧基; 和X是氧，键，C1-C2亚烷基或亚甲氧基，这些化合物可用于治疗和/或预防神经心理障碍，包括但不限于精神分裂症，躁狂症，痴呆，抑郁症，焦虑症，强迫行为，物质滥用，帕金森样运动障碍和与使用精神安定剂有关的运动障碍。

6. 发明申请

WO0012500A3 2-ARYL-4-(1-[4-HETEROARYL]PIPERAZIN-1-YL) METHYLIMIDAZOLES: DOPAMINE D4 RECEPTOR SUBTYPE LIGANDS 审中-公开
标题翻译： 2-亚氨基-4-（1- [4-异丙基]哌嗪-1-基）甲基咪唑烷酮：DOPAMINE D4受体亚型配体
公开(公告)号：WO0012500A3
公开(公告)日：2000-07-27
申请号：PCT/US9920176
申请日：1999-09-02
申请人： NEUROGEN CORP , CHEN XI , THURKAUF ANDREW
发明人： CHEN XI , THURKAUF ANDREW
IPC分类号： C07D215/38 , C07D239/84 , C07D241/44 , C07D401/12 , C07D403/12 , A61K31/47
CPC分类号： C07D215/38 , C07D239/84 , C07D241/44 , C07D401/12 , C07D403/12
摘要： Disclosed are compounds of formula: (I) or the pharmaceutically acceptable acid addition salts thereof wherein Ra represents (II) where X, Y and Z are the same or different and represent CH or nitrogen; R1, R2, R3 and R4 independently represent organic or inorganic groups: and R5 is hydrogen, C1-C6 alkyl or halogen, which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behaviour, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.
摘要翻译：公开了式（I）化合物或其药学上可接受的酸加成盐，其中R a表示（II），其中X，Y和Z相同或不同，表示CH或氮; R1，R2，R3和R4独立地表示有机或无机基团：R5是氢，C1-C6烷基或卤素，该化合物可用于治疗和/或预防神经心理障碍，包括但不限于精神分裂症，躁狂症，痴呆，抑郁，焦虑，强迫行为，药物滥用，帕金森氏样运动障碍和与使用精神安定药有关的运动障碍。

7. 发明申请

WO2006083271A2 SUBSTITUTED ARYL ACYLTHIOUREAS AND RELATED COMPOUNDS; INHIBITORS OF VIRAL REPLICATION 审中-公开
标题翻译：取代的芳基乙二醇和相关化合物; VIRAL REPLICATION的抑制剂
公开(公告)号：WO2006083271A2
公开(公告)日：2006-08-10
申请号：PCT/US2005017308
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 , C07D249/06 , A61K31/17 , A61K31/277 , A61K31/341 , A61K31/343 , A61K31/351 , A61K31/352 , A61K31/381 , A61K31/415 , A61K31/4155 , A61K31/4164 , A61K31/4192 , A61K31/42 , A61K31/421 , A61K31/423 , A61K31/4245 , A61K31/426 , A61K31/428 , A61K31/429 , A61K31/433 , A61K31/4355 , A61K31/437 , A61K31/4375 , A61K31/4406 , A61K31/4412 , A61K31/443 , A61K31/445 , A61K31/455 , A61K31/47 , A61K31/4725 , A61K31/496 , A61K31/498 , A61K31/50 , A61K31/505 , A61K31/506 , A61K31/519 , A61K31/53 , A61K31/5375 , A61K31/5377 , A61P31/12 , C07C335/18 , C07C335/20 , C07D211/20 , C07D211/22 , C07D211/46 , C07D211/60 , C07D211/64 , C07D211/78 , C07D213/56 , C07D213/75 , C07D213/82 , C07D213/84 , C07D213/85 , C07D215/54 , C07D231/14 , C07D233/54 , C07D233/60 , C07D233/90 , C07D237/24 , C07D239/28 , C07D241/24 , C07D241/42 , C07D241/44 , C07D253/06 , C07D253/07 , C07D261/18 , C07D263/34 , C07D263/58 , C07D265/30 , C07D271/12 , C07D277/20 , C07D277/56 , C07D277/68 , C07D285/06 , C07D295/10 , C07D295/14 , C07D295/15 , C07D307/68 , C07D307/84 , C07D307/85 , C07D309/38 , C07D311/04 , C07D311/58 , C07D333/38 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D417/14 , C07D419/12 , C07D471/04 , C07D487/04 , C07D491/04 , C07D491/048 , C07D495/04 , C07D513/04
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 compounds and pharmaceutically acceptable salts of Formula (I) wherein the variables A 1 , A 2 , R 1 , R 2 , 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A 1，A 2，R 1，R 2， 2，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。治疗方法包括施用式（I）化合物作为单一活性剂或与一种或多种其它治疗剂组合施用式（I）化合物。

8. 发明申请

WO2005067900A3 AZABENZOFURAN SUBSTITUTED THIOUREAS AS INHIBITORS OF VIRAL REPLICATION 审中-公开
标题翻译：作为病毒复制的抑制剂的AZABENZOFURAN替代THI
公开(公告)号：WO2005067900A3
公开(公告)日：2005-09-29
申请号：PCT/US2005000339
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 , A61K31/4355 , A61K31/4741 , A61K38/21 , C07D471/04 , C07D491/02 , C07D491/04 , A61P31/14
CPC分类号： A61K31/00 , A61K31/4355 , C07D491/04
摘要： The present invention provides compounds of Formula: (1), wherein the variables Ar, A1, A2, A3, A4, R5, R6, R7, 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。

9. 发明申请

WO2005007601A3 SUBSTITUTED ARYLTHIOUREA DERIVATIVES USEFUL AS INHIBITORS OF VIRAL REPLICATION 审中-公开
标题翻译：作为病毒复制的抑制剂有用的替代芳香酶衍生物
公开(公告)号：WO2005007601A3
公开(公告)日：2005-06-23
申请号：PCT/US2004022599
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： A61K31/17 , A61K31/44 , C07C15/00 , C07C335/14 , C07C335/16 , C07D213/54
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这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有效和/或选择性的病毒复制抑制剂，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。这样的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中丙型肝炎病毒感染的方法。

10. 发明申请

WO2005095345A3 HETEROARYL GUANIDINES AS INHIBITORS OF VIRAL REPLICATION 审中-公开
标题翻译：作为病毒复制抑制剂的异氟烷类药物
公开(公告)号：WO2005095345A3
公开(公告)日：2005-12-01
申请号：PCT/US2005009710
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： A61K31/44 , A61K31/505 , A61K31/517 , C07C279/18 , C07D213/75 , C07D213/82 , C07D239/54 , C07D239/545 , C07D239/84 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D417/12 , A61P31/14
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, Al, R2, R3, R4, R5 and R6 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。

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