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11. 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。

12. 发明授权

US08143305B2 2,3-substituted indole derivatives for treating viral infections 失效
标题翻译：用于治疗病毒感染的2,3-取代的吲哚衍生物
公开(公告)号：US08143305B2
公开(公告)日：2012-03-27
申请号：US12675897
申请日：2008-08-27
申请人： Gopinadhan N. Anilkumar , Frank Bennett , Tin-Yau Chan , Kevin X. Chen , Mousumi Sannigrahi , Francisco Velazquez , Srikanth Venkatraman , Qingbei Zeng , Jose S. Duca , Charles A. Lesburg , Joseph A. Kozlowski , F. George Njoroge , Stuart B. Rosenblum , Neng-Yang Shih , Stephen J. Gavalas , Yueheng Jiang , Patrick A. Pinto , Haiyan Pu , Oleg B. Selyutin , Bancha Vibulbhan , Li Wang , Wanli Wu , Weiying Yang , Yuhua Huang , Hsueh-Cheng Huang , Robert Palermo , Boris Feld
发明人： Gopinadhan N. Anilkumar , Frank Bennett , Tin-Yau Chan , Kevin X. Chen , Mousumi Sannigrahi , Francisco Velazquez , Srikanth Venkatraman , Qingbei Zeng , Jose S. Duca , Charles A. Lesburg , Joseph A. Kozlowski , F. George Njoroge , Stuart B. Rosenblum , Neng-Yang Shih , Stephen J. Gavalas , Yueheng Jiang , Patrick A. Pinto , Haiyan Pu , Oleg B. Selyutin , Bancha Vibulbhan , Li Wang , Wanli Wu , Weiying Yang , Yuhua Huang , Hsueh-Cheng Huang , Robert Palermo , Boris Feld
IPC分类号： A01N43/38 , A61K31/40 , C07D209/04
CPC分类号： C07D417/14 , C07D209/42 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention relates to 2,3-Substituted Indole Derivatives, compositions comprising at least one 2,3-Substituted Indole Derivative, and methods of using the 2,3-Substituted 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2,3-取代的吲哚衍生物，包含至少一种2,3-取代的吲哚衍生物的组合物和使用2,3-取代的吲哚衍生物用于治疗或预防病毒感染或病毒相关的方法病人无序。

13. 发明申请

US20110033417A1 2,3-SUBSTITUTED INDOLE DERIVATIVES FOR TREATING VIRAL INFECTIONS 失效
标题翻译：用于治疗病毒感染的2,3-取代的吲哚衍生物
公开(公告)号：US20110033417A1
公开(公告)日：2011-02-10
申请号：US12675897
申请日：2008-08-27
申请人： Gopinadhan N. Anilkumar , Frank Bennett , Tin-Yau Chan , Kevin X. Chen , Mousumi Sannigrahi , Francisco Velazquez , Srikanth Venkatraman , Qingbei Zeng , Jose S. Duca , Charles A. Lesburg , Joseph A. Kozlowski , F. George Njoroge , Stuart B. Rosenblum , Neng-Yang Shih , Stephen J. Gavalas , Yueheng Jiang , Patrick A. Pinto , Haiyan Pu , Oleg B. Selyutin , Bancha Vibulbhan , Li Wang , Wanli Wu , Weiying Yang , Yuhua Huang , Hsueh-Cheng Huang , Robert Palermo , Boris Feld
发明人： Gopinadhan N. Anilkumar , Frank Bennett , Tin-Yau Chan , Kevin X. Chen , Mousumi Sannigrahi , Francisco Velazquez , Srikanth Venkatraman , Qingbei Zeng , Jose S. Duca , Charles A. Lesburg , Joseph A. Kozlowski , F. George Njoroge , Stuart B. Rosenblum , Neng-Yang Shih , Stephen J. Gavalas , Yueheng Jiang , Patrick A. Pinto , Haiyan Pu , Oleg B. Selyutin , Bancha Vibulbhan , Li Wang , Wanli Wu , Weiying Yang , Yuhua Huang , Hsueh-Cheng Huang , Robert Palermo , Boris Feld
IPC分类号： A61K38/21 , C07D401/04 , C07D413/14 , C07D209/42 , C07D401/14 , C07D417/14 , C07D407/14 , C07D409/14 , A61K31/4439 , A61K31/444 , A61K31/404 , A61K31/4545 , A61K31/513 , A61K31/443 , A61K31/4709 , A61K31/4436 , A61K31/5377 , A61K31/538 , A61K31/5415 , A61K31/7088 , A61K31/7052 , A61K39/12 , A61K39/42 , A61P31/12 , A61P31/14
CPC分类号： C07D417/14 , C07D209/42 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention relates to 2,3-Substituted Indole Derivatives, compositions comprising at least one 2,3-Substituted Indole Derivative, and methods of using the 2,3-Substituted 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2,3-取代的吲哚衍生物，包含至少一种2,3-取代的吲哚衍生物的组合物和使用2,3-取代的吲哚衍生物用于治疗或预防病毒感染或病毒相关的方法病人无序。

14. 发明授权

US08614229B2 Substituted indole derivatives and methods of use thereof 有权
标题翻译：取代的吲哚衍生物及其使用方法
公开(公告)号：US08614229B2
公开(公告)日：2013-12-24
申请号：US12675891
申请日：2008-08-27
申请人： Gopinadhan N. Anilkumar , Frank Bennett , Tin-Yau Chan , Kevin X. Chen , Mousumi Sannigrahi , Francisco Velazquez , Srikanth Venkatraman , Qingbei Zeng , Jose S. Duca , Charles A. Lesburg , Joseph A. Kozlowski , F. George Njoroge , Stuart B. Rosenblum , Neng-Yang Shih
发明人： Gopinadhan N. Anilkumar , Frank Bennett , Tin-Yau Chan , Kevin X. Chen , Mousumi Sannigrahi , Francisco Velazquez , Srikanth Venkatraman , Qingbei Zeng , Jose S. Duca , Charles A. Lesburg , Joseph A. Kozlowski , F. George Njoroge , Stuart B. Rosenblum , Neng-Yang Shih
IPC分类号： A61K31/47 , A61K31/4402 , A61K31/426 , A61K31/428 , A61K31/4184 , A61K31/404 , C07D239/96 , C07D239/88 , C07D241/44 , C07D471/04 , C07D215/18 , C07D401/04 , C07D211/88 , C07D277/18 , C07D487/04 , C07D275/04 , C07D249/18
CPC分类号： C07D403/04 , C07D401/04
摘要： The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
摘要翻译：本发明涉及取代的吲哚衍生物，包含至少一种取代的吲哚衍生物的组合物，以及使用这些取代的吲哚衍生物来治疗或预防患者的病毒感染或病毒相关病症的方法。

15. 发明授权

US08557848B2 4,5-ring annulated indole derivatives for treating or preventing of HCV and related viral infections 有权
标题翻译：用于治疗或预防HCV和相关病毒感染的4,5环环状吲哚衍生物
公开(公告)号：US08557848B2
公开(公告)日：2013-10-15
申请号：US12519715
申请日：2007-12-17
申请人： Kevin X. Chen , Srikanth Venkatraman , F. George Njoroge , Stuart B. Rosenblum , Charles A. Lesburg , Jose S. Duca , Neng-Yang Shih , Francisco Velazquez , Gopinadhan N. Anilkumar , Qingbei Zeng , Joseph A. Kozlowski
发明人： Kevin X. Chen , Srikanth Venkatraman , F. George Njoroge , Stuart B. Rosenblum , Charles A. Lesburg , Jose S. Duca , Neng-Yang Shih , Francisco Velazquez , Gopinadhan N. Anilkumar , Qingbei Zeng , Joseph A. Kozlowski
IPC分类号： A61K31/497 , A61K31/4353 , A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/498 , A61K31/517 , C07D215/12 , C07D401/14 , C07D241/44 , C07D239/88
CPC分类号： C07D491/04 , C07D401/04 , C07D487/04 , C07D495/04 , C07D513/04
摘要： The present invention relates to 4,5-ring annulated indole derivatives, 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 a cyclopentyl, cyclopentenyl, 5-membered heterocycloalkyl, 5-membered heterocycloalkenyl or 5-membered heteroaryl ring.
摘要翻译：本发明涉及4,5-环环状吲哚衍生物，包含至少一种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病毒感染或患者病毒相关疾病。其中式（I）的Z环是环戊基，环戊烯基，5元杂环烷基，5元杂环烯基或5元杂芳基环。

16. 发明申请

US20110104109A1 TETRACYCLIC INDOLE DERIVATIVES AND THEIR USE FOR TREATING OR PREVENTING VIRAL INFECTIONS 审中-公开
标题翻译：四环素衍生物及其用于治疗或预防病毒感染的用途
公开(公告)号：US20110104109A1
公开(公告)日：2011-05-05
申请号：US12675277
申请日：2008-08-27
申请人： Frank Bennett , Qingbei Zeng , Srikanth Venkatraman , Mousumi Sannigrahi , Kevin X. Chen , Gopinadhan N. Anilkumar , Stuart B. Rosenblum , Joseph A. Kozlowski , F. George Njoroge
发明人： Frank Bennett , Qingbei Zeng , Srikanth Venkatraman , Mousumi Sannigrahi , Kevin X. Chen , Gopinadhan N. Anilkumar , Stuart B. Rosenblum , Joseph A. Kozlowski , F. George Njoroge
IPC分类号： A61K31/437 , C07D498/22 , C07D491/147 , C07D491/22 , C07D513/22 , C07D495/04 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/536 , A61K38/21 , A61K39/12 , A61K39/42 , A61K31/7088 , A61P31/12 , A61P37/04
CPC分类号： C07D491/147 , A61K38/21 , C07D491/22 , C07D498/22 , C07D513/22 , C07D519/00 , A61K2300/00
摘要： The present invention relates to Tetracyclic Indole Derivatives, compositions comprising at least one Tetracyclic Indole Derivative, and methods of using the Tetracyclic Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
摘要翻译：本发明涉及四环吲哚衍生物，包含至少一种四环吲哚衍生物的组合物，以及使用四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。

17. 发明申请

US20100098661A1 4,5-RING ANNULATED INDOLE DERIVATIVES FOR TREATING OR PREVENTING OF HCV AND RELATED VIRAL INFECTIONS 有权
标题翻译：用于治疗或预防HCV和相关病毒感染的4,5环结构吲哚类衍生物
公开(公告)号：US20100098661A1
公开(公告)日：2010-04-22
申请号：US12519715
申请日：2007-12-17
申请人： Kevin X. Chen , Srikanth Venkatraman , F. George Njoroge , Stuart B. Rosenblum , Charles A. Lesburg , Jose S. Duca , Neng-Yang Shih , Francisco Velazquez , Gopinadhan N. Anilkumar , Qingbei Zeng , Joseph A. Kozlowski
发明人： Kevin X. Chen , Srikanth Venkatraman , F. George Njoroge , Stuart B. Rosenblum , Charles A. Lesburg , Jose S. Duca , Neng-Yang Shih , Francisco Velazquez , Gopinadhan N. Anilkumar , Qingbei Zeng , Joseph A. Kozlowski
IPC分类号： A61K38/21 , C07D401/02 , A61K31/4439 , C07D417/14 , A61K31/4436 , C07D215/00 , A61K31/47 , C07D241/36 , A61K31/498 , C07D401/14 , A61K31/517 , A61K31/444 , A61K39/00 , A61K39/395 , A61P31/12
CPC分类号： C07D491/04 , C07D401/04 , C07D487/04 , C07D495/04 , C07D513/04
摘要： The present invention relates to 4,5-ring annulated indole derivatives, 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 a cyclopentyl, cyclopentenyl, 5-membered heterocycloalkyl, 5-membered heterocycloalkenyl or 5-membered heteroaryl ring.
摘要翻译：本发明涉及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病毒感染或患者病毒相关疾病。其中式（I）的Z环是环戊基，环戊烯基，5元杂环烷基，5元杂环烯基或5元杂芳基环。

18. 发明授权

US07566718B2 Amine-linked pyridyl and phenyl substituted piperazine-piperidines with CXCR3 antagonist activity 有权
标题翻译：胺连接的吡啶基和苯基取代的哌嗪 - 哌啶与CXCR3拮抗剂活性
公开(公告)号：US07566718B2
公开(公告)日：2009-07-28
申请号：US11354328
申请日：2006-02-14
申请人： Michael K. C. Wong , Youheng Shu , Wensheng Yu , Stuart B. Rosenblum , Joseph A. Kozlowski , Brian F. McGuinness , Yuefei Shao , Douglas W. Hobbs
发明人： Michael K. C. Wong , Youheng Shu , Wensheng Yu , Stuart B. Rosenblum , Joseph A. Kozlowski , Brian F. McGuinness , Yuefei Shao , Douglas W. Hobbs
IPC分类号： A61K31/497 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00
CPC分类号： C07D401/14 , C07D211/58 , C07D401/12 , C07D405/14 , C07D409/14 , 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，异种移植排斥），感染性疾病（例如结核性麻风病），固定药物喷发，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。

19. 发明授权

US07902199B2 Heterocyclic substituted piperazine compounds with CXCR3 antagonist activity 有权
标题翻译：具有CXCR3拮抗活性的杂环取代哌嗪化合物
公开(公告)号：US07902199B2
公开(公告)日：2011-03-08
申请号：US11776901
申请日：2007-07-12
申请人： Stuart B. Rosenblum , Joseph A. Kozlowski , Neng-Yang Shih , Brian F. McGuinness , Douglas W. Hobbs
发明人： Stuart B. Rosenblum , Joseph A. Kozlowski , Neng-Yang Shih , Brian F. McGuinness , Douglas W. Hobbs
IPC分类号： A61K31/496 , C07D401/12 , C07D401/14
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 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，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），移植物排斥（非限制性实例，包括同种异体移植排斥，移植排斥），感染性疾病（例如结核性麻风病），固定药物喷发，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。

20. 发明授权

US07786124B2 Heterocyclic substituted pyridine compounds with CXCR3 antagonist activity 有权
标题翻译：具有CXCR3拮抗活性的杂环取代的吡啶化合物
公开(公告)号：US07786124B2
公开(公告)日：2010-08-31
申请号：US11688014
申请日：2007-03-19
申请人： Stuart B. Rosenblum , Joseph A. Kozlowski , Neng-Yang Shih , Brian F. McGuinness , Douglas W. Hobbs
发明人： Stuart B. Rosenblum , Joseph A. Kozlowski , Neng-Yang Shih , Brian F. McGuinness , Douglas W. Hobbs
IPC分类号： C07D413/14 , A61K31/496
CPC分类号： C07D401/14 , C07D413/14
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 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，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），移植物排斥（非限制性实例，包括同种异体移植排斥，移植排斥），感染性疾病（例如结核性麻风病），固定药物喷发，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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