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31. 发明授权

US09254292B2 Fused tetracycle derivatives and methods of use thereof for the treatment of viral diseases 有权
标题翻译：熔融四环衍生物及其用于治疗病毒性疾病的方法
公开(公告)号：US09254292B2
公开(公告)日：2016-02-09
申请号：US13876931
申请日：2011-09-28
申请人： Craig A. Coburn , Brian J. Lavey , Michael P. Dwyer , Joseph A. Kozlowski , Stuart B. Rosenblum
发明人： Craig A. Coburn , Brian J. Lavey , Michael P. Dwyer , Joseph A. Kozlowski , Stuart B. Rosenblum
IPC分类号： A61K31/553 , C07D403/14 , C07D405/14 , C07D493/04 , C07D498/04 , A61K31/4178 , A61K31/5517 , A61K45/06 , C07D487/04
CPC分类号： A61K31/553 , A61K31/4178 , A61K31/5517 , A61K45/06 , C07D403/14 , C07D405/14 , C07D487/04 , C07D493/04 , C07D498/04 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/395
摘要： The present invention relates to novel Fused Tetracycle Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, A′, B, G, R1, U, V, W, W′, X, X′, Y and Y′ are as defined herein. The present invention also relates to compositions comprising at least one Fused Tetracycle Derivative, and methods of using the Fused Tetracycle Derivatives for treating or preventing HCV infection in a patient.
摘要翻译：本发明涉及式（I）的新型熔融四环衍生物及其药学上可接受的盐，其中A，A'，B，G，R 1，U，V，W，W'，X，X'，Y和Y '如本文所定义。本发明还涉及包含至少一种熔融四环衍生物的组合物，以及使用熔融四环衍生物治疗或预防患者HCV感染的方法。

32. 发明申请

US20150057246A1 SILYL-CONTAINING HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES 审中-公开
标题翻译：含有SILYL的杂环化合物及其用于治疗病毒性疾病的方法
公开(公告)号：US20150057246A1
公开(公告)日：2015-02-26
申请号：US14345130
申请日：2012-09-11
申请人： Michael P. Dwyer , Kartik M. Keertikar , Qingbei Zeng , Robert D. Mazzola, JR. , John P. Caldwell , Haiqun Tang , Anilkumar Gopinadhan Nair , Bandarpalle B. Shankar , Stuart B. Rosenblum , Joseph A. Kozlowski
发明人： Michael P. Dwyer , Kartik M. Keertikar , Qingbei Zeng , Robert D. Mazzola, JR. , John P. Caldwell , Haiqun Tang , Anilkumar Gopinadhan Nair , Bandarpalle B. Shankar , Stuart B. Rosenblum , Joseph A. Kozlowski
IPC分类号： C07F7/08 , A61K45/06 , A61K31/695
CPC分类号： C07F7/0816 , A61K31/695 , A61K45/06 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/395
摘要： The present invention relates to novel Silyl-Containing Heterocyclic Compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, B, C, D and R2 are as defined herein. The present invention also relates to compositions comprising at least one Silyl-Containing Heterocyclic Compound, and methods of using the Silyl-Containing Heterocyclic Compounds for treating or preventing HCV infection in a patient.
摘要翻译：本发明涉及式（I）的新的含甲硅烷基的杂环化合物：（I）及其药学上可接受的盐，其中A，B，C，D和R2如本文所定义。本发明还涉及包含至少一种含甲硅烷基的杂环化合物的组合物，以及使用含有甲硅烷基的杂环化合物治疗或预防患者HCV感染的方法。

33. 发明授权

US08901139B2 Tricyclic indole derivatives and methods of use thereof 有权
标题翻译：三环吲哚衍生物及其使用方法
公开(公告)号：US08901139B2
公开(公告)日：2014-12-02
申请号：US12997654
申请日：2009-06-10
申请人： Srikanth Venkatraman , Anilkumar Gopinadhan Nair , Kevin X. Chen , Francisco Velazquez , Qingbei Zeng , Duan Liu , Yueheng Jiang , Joseph A. Kozlowski , F. George Njoroge , Stuart B. Rosenblum , Stephen J. Gavalas , Patrick A. Pinto , Oleg B. Selyutin , Bancha Vibulbhan
发明人： Srikanth Venkatraman , Anilkumar Gopinadhan Nair , Kevin X. Chen , Francisco Velazquez , Qingbei Zeng , Duan Liu , Yueheng Jiang , Joseph A. Kozlowski , F. George Njoroge , Stuart B. Rosenblum , Stephen J. Gavalas , Patrick A. Pinto , Oleg B. Selyutin , Bancha Vibulbhan
IPC分类号： C07D491/04 , C07D519/00 , C07D491/048 , A61K31/517 , A61P31/12 , C07D401/14
CPC分类号： C07D491/048 , C07D491/04 , C07D519/00
摘要： The present invention relates to Tricyclic Indole Derivatives, compositions comprising at least one Tricyclic Indole Derivatives, and methods of using the Tricyclic Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
摘要翻译：本发明涉及三环吲哚衍生物，包含至少一种三环吲哚衍生物的组合物，以及使用三环吲哚衍生物治疗或预防患者病毒感染或病毒相关病症的方法。

34. 发明申请

US20140199264A1 TETRACYCLIC XANTHENE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES 有权
标题翻译：四环素衍生物及其用于治疗病毒性疾病的方法
公开(公告)号：US20140199264A1
公开(公告)日：2014-07-17
申请号：US14005430
申请日：2012-03-16
申请人： Craig A. Coburn , Stuart B. Rosenblum , Joseph A. Kozlowski , Richard Soll , Hao Wu , Bin Hu , Bin Zhong , Dahai Wang , Changmao Shen , Fei Sun
发明人： Craig A. Coburn , Stuart B. Rosenblum , Joseph A. Kozlowski , Richard Soll , Hao Wu , Bin Hu , Bin Zhong , Dahai Wang , Changmao Shen , Fei Sun
IPC分类号： A61K31/5383 , A61K45/06 , A61K31/4178 , C07D498/06 , C07D493/06
CPC分类号： A61K31/5383 , A61K31/4178 , A61K45/06 , C07D491/06 , C07D493/06 , C07D498/06
摘要： The present invention relates to novel Tetracyclic Xanthene Derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, Y1, Y2, Z, Ra, Rb, R1a, R1b and R2 are as defined herein. The present invention also relates to compositions comprising at least one Tetracyclic Xanthene Derivative, and methods of using the Tetracyclic Xanthene Derivatives for treating or preventing HCV infection in a patient.
摘要翻译：本发明涉及式（I）的新型四环Xanthene衍生物及其药学上可接受的盐，其中A，Y1，Y2，Z，Ra，Rb，R1a，R1b和R2如本文所定义。本发明还涉及包含至少一种四环Xanthene衍生物的组合物，以及使用四环Xanthene衍生物治疗或预防患者HCV感染的方法。

35. 发明授权

US08268803B2 5, 6-ring annulated indole derivatives and use thereof 有权
标题翻译： 5，6环环状吲哚衍生物及其用途
公开(公告)号：US08268803B2
公开(公告)日：2012-09-18
申请号：US12519975
申请日：2007-12-17
申请人： Frank Bennett , Srikanth Venkatraman , F. George Njoroge , Kevin X. Chen , Neng-Yang Shih , Stuart B. Rosenblum , Joseph A. Kozlowski
发明人： Frank Bennett , Srikanth Venkatraman , F. George Njoroge , Kevin X. Chen , Neng-Yang Shih , Stuart B. Rosenblum , Joseph A. Kozlowski
IPC分类号： A61K31/437 , C07D209/04 , C07D243/36
CPC分类号： C07D513/04 , C07D401/04 , C07D471/04 , C07D491/04
摘要： The present invention relates to 5,6-ring annulated indole derivatives of the formula (I), compositions comprising at least one 5,6-ring annulated indole derivatives, and methods of using the 5,6-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
摘要翻译：本发明涉及式（I）的5,6环环状吲哚衍生物，包含至少一种5,6环环状吲哚衍生物的组合物，以及使用5,6环环状吲哚衍生物用于治疗或预防患者的病毒感染或病毒相关疾病。

36. 发明申请

US20120157466A1 HETEROCYCLIC COMPOUNDS WITH CXCR3 ANTAGONIST ACTIVITY 审中-公开
标题翻译：具有CXCR3拮抗剂活性的杂环化合物
公开(公告)号：US20120157466A1
公开(公告)日：2012-06-21
申请号：US12519970
申请日：2007-12-20
申请人： Qingbei Zeng , Stuart B. Rosenblum , Joseph A. Kozlowski , Neng-Yang Shih , Brian F. McGuinness , Douglas W. Hobbs
发明人： Qingbei Zeng , Stuart B. Rosenblum , Joseph A. Kozlowski , Neng-Yang Shih , Brian F. McGuinness , Douglas W. Hobbs
IPC分类号： A61K31/519 , C07D401/14 , C07D473/32 , A61K31/52 , A61K31/496 , A61P29/00 , A61P37/00 , C07D471/04 , A61K31/506
CPC分类号： C07D401/14
摘要： The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1 or Formula 5: or a pharmaceutically acceptable salt, solvate or ester thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non limiting example(s) include, psoriasis), autoimmune diseases (non limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non limiting example(s) include, allograft rejection, zenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.
摘要翻译：本申请公开了所述化合物或所述前体药物的所述化合物或其药学上可接受的盐，溶剂合物或酯的化合物或对映异构体，立体异构体，旋转异构体，互变异构体或前药，所述化合物具有式1所示的一般结构或式5：或其药学上可接受的盐，溶剂合物或酯。还公开了治疗趋化因子介导的疾病的方法，例如姑息治疗，治疗疗法，某些疾病和疾病如炎性疾病的预防性治疗（非限制性实例，包括牛皮癣），自身免疫疾病（非限制性实例（传染性疾病（例如结核性麻风病），固定药物爆发，皮肤迟发型超敏反应，眼部炎症反应（例如，类风湿性关节炎，多发性硬化症），移植物排斥反应（非限制性实例包括同种异体移植物排斥反应，，I型糖尿病，病毒性脑膜炎和使用式1的化合物的肿瘤。

37. 再颁专利

USRE42461E1 Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents 失效
标题翻译：用作降胆固醇药的羟基取代的氮杂环丁酮化合物
公开(公告)号：USRE42461E1
公开(公告)日：2011-06-14
申请号：US12797341
申请日：1994-09-14
申请人： Stuart B. Rosenblum , Sundeep Dugar , Duane A. Burnett , John W. Clader , Brian A. McKittrick
发明人： Stuart B. Rosenblum , Sundeep Dugar , Duane A. Burnett , John W. Clader , Brian A. McKittrick
IPC分类号： C07D205/08 , A61P9/10 , A61P3/06 , A61K31/395
CPC分类号： C07D205/08 , A61K9/2018 , A61K9/4858 , A61K31/21 , A61K31/35 , A61K31/395 , A61K31/40 , A61K45/06 , Y02P20/55 , Y10S514/824 , A61K2300/00
摘要： Hydroxy-substituted azetidinone hypocholesterolemic agents of the formula or a pharmaceutically acceptable salt thereof, wherein: Ar1 and Ar2 are aryl or R4-substituted aryl; Ar3 is aryl or R5-substituted aryl; X, Y and Z are —CH2—, —CH(lower alkyl)— or —C(dilower alkyl)—; R and R2 are —OR6, —O(CO)R6, —O(CO)OR9 or —O(CO)NR6R7; R1 and R3 are H or lower alkyl; q is 0 or 1; r is 0 or 1; m, n and p are 0-4; provided that at least one of q and r is 1, and the sum of m, n, p, q and r is 1-6; and provided that when p is O and r is 1, the sum of m, q and n is 1-5; R4 is selected from lower alkyl, R5, —CF3, —CN, —NO2 and halogen R5 is selected from —OR6, —O(CO)R6, —O(CO)OR9, —O(CH2)1-5OR6, —O(CO)NR6R7, —NR6R7, —NR6(CO)R7, —NR6(CO)OR9, —NR6(CO)NR7R8, —NR6SO2R9, —COOR6, —CONR6R7, —COR6, —SO2NR6R7, S(O)0-2R9, —O(CH2)1-10—COOR6, —O(CH2)1-10CON6R7, —(lower alkylene)COOR6 and —CH═CH—COOR6; R6, R7 and R8 are H, lower alkyl or aryl-substituted Ic R9 is lower alkyl, aryl or aryl-substituted lower alkyl; are disclosed, as well as a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor, pharmaceutical compositions containing them; and a process for preparing them.
摘要翻译：羟基取代的氮杂环丁酮低胆固醇血药剂或其药学上可接受的盐，其中：Ar 1和Ar 2是芳基或R 4取代的芳基; Ar 3是芳基或者R 5取代的芳基; X，Y和Z是-CH 2 - ， - CH（低级烷基） - 或-C（二卤代烷基） - 。 R和R 2为-OR 6，-O（CO）R 6，-O（CO）OR 9或-O（CO）NR 6 R 7; R1和R3是H或低级烷基; q为0或1; r为0或1; m，n和p为0-4; 条件是q和r中的至少一个为1，m，n，p，q和r的和为1-6; 并且条件是当p为O且r为1时，m，q和n的和为1-5; R4选自低级烷基，R5，-CF3，-CN，-NO2，卤素R5选自-OR6，-O（CO）R6，-O（CO）OR9，-O（CH2）1-5OR6， - O（CO）NR6R7，-NR6R7，-NR6（CO）R7，-NR6（CO）OR9，-NR6（CO）NR7R8，-NR6SO2R9，-COOR6，-CONR6R7，-COR6，-SO2NR6R7，S（O） -2R9，-O（CH2）1-10-COOR6，-O（CH2）1-10CON6R7， - （低级亚烷基）COOR6和-CH = CH-COOR6; R6，R7和R8是H，低级烷基或芳基取代的Ic R9是低级烷基，芳基或芳基取代的低级烷基; 以及通过单独或与胆固醇生物合成抑制剂组合含有它们的药物组合物来施用所述化合物来降低血清胆固醇的方法; 和一个准备它们的过程。

38. 发明授权

US07868005B2 Pyrazinyl substituted piperazine-piperidines with CXCR3 antagonist activity 有权
标题翻译：吡嗪基取代的哌嗪 - 哌啶与CXCR3拮抗剂活性
公开(公告)号：US07868005B2
公开(公告)日：2011-01-11
申请号：US11354138
申请日：2006-02-14
申请人： Stuart B. Rosenblum , Seong Heon Kim , Qingbei Zeng , Michael K. C. Wong , Gopinadhan N. Anilkumar , Yueheng Jiang , Wensheng Yu , Joseph A. Kozlowski , Neng-Yang Shih , Bandarpalle B. Shankar , Brian F. McGuinness , Guizhen Dong , Lisa Guise Zawacki , Douglas W. Hobbs , John J. Baldwin , Yuefei Shao
发明人： Stuart B. Rosenblum , Seong Heon Kim , Qingbei Zeng , Michael K. C. Wong , Gopinadhan N. Anilkumar , Yueheng Jiang , Wensheng Yu , Joseph A. Kozlowski , Neng-Yang Shih , Bandarpalle B. Shankar , Brian F. McGuinness , Guizhen Dong , Lisa Guise Zawacki , Douglas W. Hobbs , John J. Baldwin , Yuefei Shao
IPC分类号： C07D241/04 , C07D401/14 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/444 , A61K31/4436 , A61K31/695 , C07F7/18 , A61P25/28 , A61P35/00 , A61P29/00
CPC分类号： C07D405/14 , C07D401/12 , C07D401/14 , C07D413/14 , C07D417/14
摘要： The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: and the pharmaceutically acceptable salts, solvates and esters thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.
摘要翻译：本申请公开了所述化合物或所述前体药物的所述化合物或其药学上可接受的盐，溶剂合物或酯的化合物或对映异构体，立体异构体，旋转异构体，互变异构体或前药，所述化合物具有式1所示的一般结构：及其药学上可接受的盐，溶剂化物和酯。还公开了治疗趋化因子介导的疾病的方法，例如姑息治疗，疗效治疗，某些疾病和疾病如炎性疾病的预防性治疗（非限制性实例，牛皮癣），自身免疫性疾病（非限制性的例如，类风湿性关节炎，多发性硬化症），移植排斥反应（非限制性实例包括，同种异体移植排斥反应，异种移植物排斥），感染性疾病（例如结核性麻风病），固定药物爆发，皮肤迟发型超敏反应应答，眼部炎症，I型糖尿病，病毒性脑膜炎和使用式1的化合物的肿瘤。

39. 发明申请

US20100196319A1 4, 5-RING ANNULATED INDOLE DERIVATIVES FOR TREATING OR PREVENTING OF HCV AND RELATED VIRAL INFECTIONS 失效
标题翻译： 4，用于治疗或预防HCV和相关病毒感染的5环结合吲哚类衍生物
公开(公告)号：US20100196319A1
公开(公告)日：2010-08-05
申请号：US12519728
申请日：2007-12-17
申请人： Gopinadhan N. Anilkumar , Yueheng Jiang , Stuart B. Rosenblum , Srikanth Venkatraman , Francisco Velazquez , Neng-Yang Shih , F. George Njoroge , Joseph A. Kozlowski
发明人： Gopinadhan N. Anilkumar , Yueheng Jiang , Stuart B. Rosenblum , Srikanth Venkatraman , Francisco Velazquez , Neng-Yang Shih , F. George Njoroge , Joseph A. Kozlowski
IPC分类号： A61K38/21 , A61P31/12 , A61K39/395 , A61K31/437 , A61K31/444 , A61K31/403 , C07D471/04 , C07D401/14 , C07D209/58
CPC分类号： C07D209/60 , C07D401/06 , C07D401/14 , C07D403/06 , C07D471/04 , C07D491/04
摘要： The present invention relates to 4,5-ring annulated indole derivatives of formula (I), compositions comprising at least one 4,5-ring annulated indole derivatives, and methods of using the 4,5-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient, wherein ring Z of formula (I), is cyclohexyl, cyclohexenyl, 6-membered heterocycloalkyl, 6-membered heterocycloalkenyl, 6-membered aryl or 6-membered heteroaryl, wherein R1, R2, R3, R6, R7 and R10 are as described herein.
摘要翻译：本发明涉及式（I）的4,5-环环状吲哚衍生物，包含至少一个4,5-环环状吲哚衍生物的组合物，以及使用4,5-环环状吲哚衍生物治疗或预防的方法病毒感染或病毒相关疾病，其中式（I）的环Z为环己基，环己烯基，6-元杂环烷基，6-元杂环烯基，6-元芳基或6-元杂芳基，其中R1， R2，R3，R6，R7和R10如本文所述。

40. 发明授权

US07763616B2 Piperazine-piperidines with CXCR3 antagonist activity 有权
标题翻译：哌嗪 - 哌啶与CXCR3拮抗剂活性
公开(公告)号：US07763616B2
公开(公告)日：2010-07-27
申请号：US11353806
申请日：2006-02-14
申请人： Wensheng Yu , Seong Heon Kim , Gopinadhan N. Anilkumar , Stuart B. Rosenblum , Bandarpalle B. Shankar , Brian F. McGuinness , Douglas W. Hobbs , Yuefei Shao
发明人： Wensheng Yu , Seong Heon Kim , Gopinadhan N. Anilkumar , Stuart B. Rosenblum , Bandarpalle B. Shankar , Brian F. McGuinness , Douglas W. Hobbs , Yuefei Shao
IPC分类号： A61K31/5025 , A61K31/4985 , C07D245/02 , C07D255/02 , C07D257/08 , C07D259/00 , C07D239/04 , C07D239/70 , C07D471/04 , C07D487/04 , A61K31/497 , C07D241/36 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , A61P29/00 , A61P17/06 , A61P19/02 , A61P3/10 , A61P31/08
CPC分类号： C07D487/04 , C07D401/12
摘要： The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: or a pharmaceutically acceptable salt, solvate or ester thereof, wherein the various moieties are defined herein. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.
摘要翻译：本申请公开了所述化合物或所述前体药物的所述化合物或其药学上可接受的盐，溶剂合物或酯的化合物或对映异构体，立体异构体，旋转异构体，互变异构体或前药，所述化合物具有式1所示的一般结构：或其药学上可接受的盐，溶剂合物或酯，其中各种部分在本文中定义。还公开了治疗趋化因子介导的疾病的方法，例如姑息治疗，疗效治疗，某些疾病和疾病如炎性疾病的预防性治疗（非限制性实例，牛皮癣），自身免疫性疾病（非限制性的例如，类风湿性关节炎，多发性硬化症），移植排斥反应（非限制性实例包括，同种异体移植排斥反应，异种移植物排斥），感染性疾病（例如结核性麻风病），固定药物爆发，皮肤迟发型超敏反应应答，眼部炎症，I型糖尿病，病毒性脑膜炎和使用式1的化合物的肿瘤。

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