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21. 发明申请

US20050113379A1 Heteroaryl fused pyridines, pyrazines and pyrimidines as CRF1 receptor ligands 审中-公开
标题翻译：杂芳基稠合吡啶，吡嗪和嘧啶作为CRF1受体配体
公开(公告)号：US20050113379A1
公开(公告)日：2005-05-26
申请号：US10933834
申请日：2004-09-03
申请人： Ping Ge , Raymond Horvath , Lu Yan Zhang , Yasuchika Yamaguchi , Bernd Kaiser , Xuechun Zhang , Suoming Zhang , He Zhao , Stanly John , Neil Moorcroft , Greg Shutske
发明人： Ping Ge , Raymond Horvath , Lu Yan Zhang , Yasuchika Yamaguchi , Bernd Kaiser , Xuechun Zhang , Suoming Zhang , He Zhao , Stanly John , Neil Moorcroft , Greg Shutske
IPC分类号： A61K31/437 , A61K31/4375 , A61K31/4985 , C07D471/04 , C07D487/04 , C07D519/00 , A61K31/519 , A61K31/522 , C07D473/02 , C07D491/02 , C07D498/02
CPC分类号： C07D471/04 , C07D487/04
摘要： Substituted heteroaryl fused pyridine, pyrazine, and pyrimidine compounds that act as selective modulators of CRF 1 receptors are provided. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.
摘要翻译：提供了作为CRF 1受体的选择性调节剂的取代的杂芳基稠合的吡啶，吡嗪和嘧啶化合物。这些化合物可用于治疗许多中枢神经系统和周围疾病，特别是压力，焦虑，抑郁，心血管疾病和进食障碍。还提供了治疗这种疾病以及包装的药物组合物的方法。本发明的化合物也可用作CRF受体定位的探针，并且作为用于CRF受体结合的测定中的标准物。给出了在受体定位研究中使用化合物的方法。

22. 发明授权

US08703742B2 Boron-containing small molecules 有权
标题翻译：含硼的小分子
公开(公告)号：US08703742B2
公开(公告)日：2014-04-22
申请号：US13227444
申请日：2011-09-07
申请人： Vincent S. Hernandez , Charles Ding , Jacob J. Plattner , Michael Richard Kevin Alley , Fernando Rock , Suoming Zhang , Eric Easom , Xianfeng Li , Ding Zhou
发明人： Vincent S. Hernandez , Charles Ding , Jacob J. Plattner , Michael Richard Kevin Alley , Fernando Rock , Suoming Zhang , Eric Easom , Xianfeng Li , Ding Zhou
IPC分类号： A61K31/69 , A61P31/04 , A61P31/00 , A61P31/06 , C07F5/02 , C12N9/99
CPC分类号： C07F5/025
摘要： This invention relates to, among other items, benzoxaborole compounds and their use for treating bacterial infections.
摘要翻译：本发明涉及苯并恶唑化合物及其用于治疗细菌感染的用途。

23. 发明授权

US08183263B2 Heteroaryl substituted thiazoles 失效
标题翻译：杂芳基取代的噻唑
公开(公告)号：US08183263B2
公开(公告)日：2012-05-22
申请号：US12125554
申请日：2008-05-22
申请人： Xiangzhu Wang , Suoming Zhang , Venkat Gadhachanda , Cuixian Liu , Jesse Quinn , Shouming Lee , Dawei Chen , Milind Deshpande , Avinash Phadke
发明人： Xiangzhu Wang , Suoming Zhang , Venkat Gadhachanda , Cuixian Liu , Jesse Quinn , Shouming Lee , Dawei Chen , Milind Deshpande , Avinash Phadke
IPC分类号： A01N43/40 , A61K31/44 , C07D417/04 , C07D417/14
CPC分类号： C07D417/04
摘要： The invention provides heteroaryl substituted thiazolo compounds of Formula I and II and pharmaceutically acceptable salts thereof. The variables A and R3 to R7 are defined herein. The invention also includes methods for preparing compounds and salts of Formula I and II. The present invention also includes pharmaceutical compositions containing heteroaryl substituted thiazolo compounds and methods for using heteroaryl substituted thiazolo compounds, including methods for using the compounds in the treatment of hepatitis C virus.
摘要翻译：本发明提供式I和II的杂芳基取代的噻唑烷化合物及其药学上可接受的盐。变量A和R3至R7在本文中定义。本发明还包括制备式I和II的化合物和盐的方法。本发明还包括含有杂芳基取代的噻唑烷化合物的药物组合物和使用杂芳基取代的噻唑烷化合物的方法，包括使用该化合物治疗丙型肝炎病毒的方法。

24. 发明授权

US08088806B2 Thiazole compounds and methods of use 失效
标题翻译：噻唑化合物和使用方法
公开(公告)号：US08088806B2
公开(公告)日：2012-01-03
申请号：US11431155
申请日：2006-05-09
申请人： Suoming Zhang , Avinash Phadke , Cuixian Liu , Xiangzhu Wang , Jesse Quinn , Dawei Chen , Venkat Gadhachanda , Shouming Li , Milind Deshpande
发明人： Suoming Zhang , Avinash Phadke , Cuixian Liu , Xiangzhu Wang , Jesse Quinn , Dawei Chen , Venkat Gadhachanda , Shouming Li , Milind Deshpande
IPC分类号： A61K31/426 , A61K31/44
CPC分类号： C07D487/04 , C07D277/38 , C07D277/42 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D513/04
摘要： The present invention provides compounds, salts and hydrates of Formula I, wherein the variables Ar1, R2, R3, R4, r, q, and t are defined herein. Certain compounds of Formula I described herein possess potent antiviral activity. The invention also provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. Certain compounds described herein inhibit assembly of the HCV replication complex. The invention also provides pharmaceutical compositions containing one or more compounds 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. 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，盐和水合物，其中变量Ar1，R2，R3，R4，r，q和t在本文中定义。某些本文所述的式I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I化合物。本文所述的某些化合物抑制HCV复制复合物的组装。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降低疾病体征或症状的式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。

25. 发明授权

US08007767B2 Amino methyl imidazoles and related compounds as C5a receptor modulators 失效
标题翻译：氨基甲基咪唑和相关化合物作为C5a受体调节剂
公开(公告)号：US08007767B2
公开(公告)日：2011-08-30
申请号：US11615054
申请日：2006-12-22
申请人： Andrew Thurkauf , He Zhao , Suoming Zhang , Yang Gao
发明人： Andrew Thurkauf , He Zhao , Suoming Zhang , Yang Gao
IPC分类号： A61K51/00
CPC分类号： C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14
摘要： Amino methyl imidazoles of Formula I are provided: wherein R, R1, R2, R3, R4, R5, and R6 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。

26. 发明申请

US20100292219A1 TERTIARY AMINE SUBSTITUTED PEPTIDES USEFUL AS INHIBITORS OF HCV REPLICATION 失效
标题翻译：作为丙型肝炎病毒复制的抑制剂的有用的胺替代物
公开(公告)号：US20100292219A1
公开(公告)日：2010-11-18
申请号：US12597380
申请日：2008-02-26
申请人： Atul Agarwal , Xiangzhu Wang , Dawei Chen , Suoming Zhang , Avinash Phadke
发明人： Atul Agarwal , Xiangzhu Wang , Dawei Chen , Suoming Zhang , Avinash Phadke
IPC分类号： A61K31/403 , C07D401/06 , C07D403/06 , C07D417/06 , A61K31/454 , A61K31/55 , A61K31/541 , A61K31/496 , A61P31/14
CPC分类号： C07K5/06078 , A61K38/00 , C07K5/06026 , C07K5/06034 , C07K5/0806 , C07K5/0808 , C07K5/0812
摘要： The present invention provides tertiary amine substituted peptides of Formula (I) useful as inhibitors of HCV replication. The variables R and R1-R12 in Formula I are described herein. The invention also includes methods for preparing such compounds. The present invention further includes pharmaceutical compositions containing tertiary amine substituted peptides and methods for using such compounds, including methods for using the compounds to treat hepatitis C infection.
摘要翻译：本发明提供可用作HCV复制抑制剂的式（I）的叔胺取代肽。本文描述了式I中的变量R和R 1 -R 12。本发明还包括制备这些化合物的方法。本发明还包括含有叔胺取代肽的药物组合物和使用这些化合物的方法，包括使用该化合物治疗丙型肝炎感染的方法。

27. 发明申请

US20090304605A1 Substituted Aminothiazole Prodrugs of Compounds with Anti-HCV Activity 失效
标题翻译：具有抗HCV活性的化合物的取代的氨基噻唑前体药物
公开(公告)号：US20090304605A1
公开(公告)日：2009-12-10
申请号：US12479213
申请日：2009-06-05
申请人： Cuixan Liu , Avinash Phadke , Xiangzhu Wang , Suoming Zhang
发明人： Cuixan Liu , Avinash Phadke , Xiangzhu Wang , Suoming Zhang
IPC分类号： A61K9/12 , C07D417/04 , A61K31/4439 , A61K31/675 , C07F9/58 , A61P31/12
CPC分类号： C07D417/04 , C07D417/14
摘要： The invention provides amino-substituted aminothiazole compounds of Formula I and Formula II where A is a group of the formula: and the variables X, Y, R, and R1 to R7 are described herein. These compounds are prodrugs of compounds useful as inhibitors of viral replication. Compositions containing such compounds, and methods of treating viral infections with these compounds, as well as to processes and intermediates useful for preparing such compounds are also provided by the invention.
摘要翻译：本发明提供式I和式II的氨基取代的氨基噻唑化合物，其中A是下式的基团：变量X，Y，R 1和R 1至R 7在本文中描述。这些化合物是可用作病毒复制抑制剂的化合物的前药。含有这些化合物的组合物，以及用这些化合物治疗病毒感染的方法，以及可用于制备这些化合物的方法和中间体也由本发明提供。

28. 发明申请

US20060199823A1 Heteroaryl fused pyridines, pyrazines and pyrimidines as CRF1 receptor ligands 审中-公开
标题翻译：杂芳基稠合吡啶，吡嗪和嘧啶作为CRF1受体配体
公开(公告)号：US20060199823A1
公开(公告)日：2006-09-07
申请号：US11389646
申请日：2006-03-24
申请人： Ping Ge , Raymond Horvath , Lu Zhang , Yasuchika Yamaguchi , Bernd Kaiser , Xuechun Zhang , Suoming Zhang , He Zhao
发明人： Ping Ge , Raymond Horvath , Lu Zhang , Yasuchika Yamaguchi , Bernd Kaiser , Xuechun Zhang , Suoming Zhang , He Zhao
IPC分类号： A61K31/498 , C07D487/02
CPC分类号： C07D471/04 , C07D487/04
摘要： Substituted heteroaryl fused pyridine, pyrazine, and pyrimidine compounds that act as selective modulators of CRF 1 receptors are provided. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.
摘要翻译：提供了作为CRF 1受体的选择性调节剂的取代的杂芳基稠合的吡啶，吡嗪和嘧啶化合物。这些化合物可用于治疗许多中枢神经系统和周围疾病，特别是压力，焦虑，抑郁，心血管疾病和进食障碍。还提供了治疗这种疾病以及包装的药物组合物的方法。本发明的化合物也可用作CRF受体定位的探针，并且作为用于CRF受体结合的测定中的标准物。给出了在受体定位研究中使用化合物的方法。

29. 发明授权

US06355620B1 C-2 modified erythromycin derivatives 有权
标题翻译： C-2修饰红霉素衍生物
公开(公告)号：US06355620B1
公开(公告)日：2002-03-12
申请号：US09312517
申请日：1999-05-14
申请人： Zhenkun Ma , Yat Sun Or , Ly Tam Phan , Suoming Zhang , Richard F. Clark
发明人： Zhenkun Ma , Yat Sun Or , Ly Tam Phan , Suoming Zhang , Richard F. Clark
IPC分类号： A61K3170
CPC分类号： C07H17/08
摘要： A compound having the formula selected from the group consisting of a compound of formula I a compound of formula II a compound of formula III as well as and pharmaceutically acceptable salts, esters, solvates, metabolites, and prodrugs thereof, are useful in treating bacterial infections. Also provided are pharmaceutically acceptible compositions, methods of treating bacterial infections, and processes for the preparation of the compounds.
摘要翻译：具有下式的化合物选自式Ia化合物式IIa化合物式III化合物及其药学上可接受的盐，酯，溶剂合物，代谢物和前药，可用于治疗细菌感染。还提供了药学上可接受的组合物，治疗细菌感染的方法和化合物的制备方法。

30. 发明授权

US08785378B2 Macrocyclic peptides as inhibitors of viral replication 有权
标题翻译：大环肽作为病毒复制的抑制剂
公开(公告)号：US08785378B2
公开(公告)日：2014-07-22
申请号：US12955413
申请日：2010-11-29
申请人： Avinash Phadke , Xiangzhu Wang , Suoming Zhang , Atul Agarwal
发明人： Avinash Phadke , Xiangzhu Wang , Suoming Zhang , Atul Agarwal
IPC分类号： A61K38/00
CPC分类号： A61K38/05 , A61K38/00 , A61K38/12 , A61K45/06 , C07K5/02 , C07K5/06078 , C07K5/06139 , C07K5/06165 , C07K5/06191 , C07K5/0808 , C07K5/12
摘要： The invention provides 4-amino-4-oxobutanoyl peptide compounds of Formula I and the pharmaceutically salts and hydrates thereof. The variables R1-R9, R16, R18, R19, n, M, n, M, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. Certain 4-amino-4-oxobutanoyl peptide compounds disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptide compounds and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain 4-amino-4-oxobutanoyl peptide compound as the only active agent or may contain a combination of 4-amino-4-oxobutanoyl peptide containing peptides compound and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections, in mammals.
摘要翻译：本发明提供了式I的4-氨基-4-氧代丁酰基肽化合物及其药学上可接受的盐和水合物。变量R1-R9，R16，R18，R19，n，M，n，M和Z在本文中定义。某些式I化合物可用作抗病毒剂。本文公开的某些4-氨基-4-氧代丁酰基肽化合物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。本发明还提供含有一种或多种4-氨基-4-氧代丁酰基肽化合物和一种或多种药学上可接受的载体的药物组合物。这样的药物组合物可以含有4-氨基-4-氧代丁酰基肽化合物作为唯一的活性剂，或者可以含有含有4-氨基-4-氧代丁酰基肽的肽化合物和一种或多种其它药物活性剂的组合。本发明还提供了用于治疗哺乳动物中的病毒感染（包括丙型肝炎感染）的方法。

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