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91. 发明授权

US07879890B2 Compounds for the treatment of inflammatory disorders 有权
标题翻译：用于治疗炎性疾病的化合物
公开(公告)号：US07879890B2
公开(公告)日：2011-02-01
申请号：US12338445
申请日：2008-12-18
申请人： Wensheng Yu , Ling Tong , Lei Chen , Joseph A. Kozlowski , Brian J. Lavey , Neng-Yang Shih , Vincent S. Madison , Guowei Zhou , Peter Orth , Zhuyan Guo , Michael K. C. Wong , De-Yi Yang , Seong Heon Kim , Bandarpalle B. Shankar , M. Arshad Siddiqui , Kristin E. Rosner , Chaoyang Dai , Janeta Popovici-Muller , Vinay M. Girijavallabhan , Dansu Li , Razia Rizvi , Aneta M. Micula , Robert Feltz
发明人： Wensheng Yu , Ling Tong , Lei Chen , Joseph A. Kozlowski , Brian J. Lavey , Neng-Yang Shih , Vincent S. Madison , Guowei Zhou , Peter Orth , Zhuyan Guo , Michael K. C. Wong , De-Yi Yang , Seong Heon Kim , Bandarpalle B. Shankar , M. Arshad Siddiqui , Kristin E. Rosner , Chaoyang Dai , Janeta Popovici-Muller , Vinay M. Girijavallabhan , Dansu Li , Razia Rizvi , Aneta M. Micula , Robert Feltz
IPC分类号： A61K31/416 , A61K31/428
CPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/00 , C07D473/34 , C07D487/04 , C07D491/04 , C07D495/04
摘要： This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，溶剂化物，酯或异构体，其可用于治疗由MMP，ADAM，TACE，聚集蛋白聚糖酶，TNF-或组合介导的疾病或病症其中。

92. 发明授权

US07879838B2 Heteroaryl substituted pyrazinyl-piperazine-piperidines with CXCR3 antagonist activity 有权
标题翻译：具有CXCR3拮抗活性的杂芳基取代的吡嗪基 - 哌嗪 - 哌啶
公开(公告)号：US07879838B2
公开(公告)日：2011-02-01
申请号：US11353474
申请日：2006-02-14
申请人： Qingbei Zeng , De-Yi Yang , Stuart B. Rosenblum , Michael K. C. Wong , Gopinadhan N. Anilkumar , Seong Heon Kim , Wensheng Yu , Joseph A. Kozlowski , Neng-Yang Shih , Brian F. McGuinness , Lisa Guise Zawacki , Doublas W. Hobbs
发明人： Qingbei Zeng , De-Yi Yang , Stuart B. Rosenblum , Michael K. C. Wong , Gopinadhan N. Anilkumar , Seong Heon Kim , Wensheng Yu , Joseph A. Kozlowski , Neng-Yang Shih , Brian F. McGuinness , Lisa Guise Zawacki , Doublas W. Hobbs
IPC分类号： A01N43/00 , A61K31/00 , A61K31/535 , A61K31/497 , C07D413/00 , C07D403/00 , C07D241/02
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D487/04
摘要： The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts or solvates of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: and the pharmaceutically acceptable salts, solvates or 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药的所述化合物或其对映异构体，立体异构体，旋转异构体，互变异构体，外消旋体或前药，或所述前药的所述化合物，所述化合物具有式1所示的一般结构：和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。

93. 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。

94. 发明授权

US07781437B2 Substituted heterocyclic compounds with CXCR3 antagonist activity 有权
标题翻译：取代的具有CXCR3拮抗剂活性的杂环化合物
公开(公告)号：US07781437B2
公开(公告)日：2010-08-24
申请号：US11545201
申请日：2006-10-10
申请人： Seong Heon Kim , Bandarpalle B. Shankar , Joseph A. Kozlowski , Stuart B. Rosenblum , Neng-Yang Shih
发明人： Seong Heon Kim , Bandarpalle B. Shankar , Joseph A. Kozlowski , Stuart B. Rosenblum , Neng-Yang Shih
IPC分类号： A61K31/497
CPC分类号： C07D401/14 , C07D401/08 , 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, 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, 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，I型糖尿病，病毒性脑膜炎和使用式1的化合物的肿瘤。

95. 发明授权

US07776862B2 Pyridyl and phenyl substituted piperazine-piperidines with CXCR3 antagonist activity 有权
标题翻译：具有CXCR3拮抗活性的吡啶基和苯基取代的哌嗪 - 哌啶
公开(公告)号：US07776862B2
公开(公告)日：2010-08-17
申请号：US11353697
申请日：2006-02-14
申请人： Brian F. McGuinness , Stuart B. Rosenblum , Joseph A. Kozlowski , Gopinadhan N. Anilkumar , Seong Heon Kim , Neng-Yang Shih , Chung-Her Jenh , Paul J. Zavodny , Douglas W. Hobbs , Guizhen Dong , Yuefei Shao , Lisa Guise Zawacki , Cangmeng Yang , Carolyn Dilanni Carroll
发明人： Brian F. McGuinness , Stuart B. Rosenblum , Joseph A. Kozlowski , Gopinadhan N. Anilkumar , Seong Heon Kim , Neng-Yang Shih , Chung-Her Jenh , Paul J. Zavodny , Douglas W. Hobbs , Guizhen Dong , Yuefei Shao , Lisa Guise Zawacki , Cangmeng Yang , Carolyn Dilanni Carroll
IPC分类号： A61K31/497 , C07D401/00
CPC分类号： C07D401/12 , C07D211/58 , C07D401/14 , C07D405/14 , 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。

96. 发明授权

US07772263B2 Compounds for the treatment of inflammatory disorders 有权
公开(公告)号：US07772263B2
公开(公告)日：2010-08-10
申请号：US12364845
申请日：2009-02-03
申请人： Brian J. Lavey , Joseph A. Kozlowski , Guowei Zhou , Ling Tong , Wensheng Yu , Michael K. C. Wong , Bandarpalle B. Shankar , Neng-Yang Shih , M. Arshad Siddiqui , Kristin E. Rosner , Chaoyang Dai , Janeta Popovici-Muller , Vinay M. Girijavallabhan , Dansu Li , Razia Rizvi , Lei Chen , De-Yi Yang , Robert Feltz , Seong Heon Kim
发明人： Brian J. Lavey , Joseph A. Kozlowski , Guowei Zhou , Ling Tong , Wensheng Yu , Michael K. C. Wong , Bandarpalle B. Shankar , Neng-Yang Shih , M. Arshad Siddiqui , Kristin E. Rosner , Chaoyang Dai , Janeta Popovici-Muller , Vinay M. Girijavallabhan , Dansu Li , Razia Rizvi , Lei Chen , De-Yi Yang , Robert Feltz , Seong Heon Kim
IPC分类号： A61K31/427 , A61K31/4164 , A61K31/4375
CPC分类号： C07D403/14 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/00
摘要： This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-α or combinations thereof.

97. 发明申请

US20100168124A1 NOVEL HETEROCYCLIC SUBSTITUTED PYRIDINE COMPOUNDS WITH CXCR3 ANTAGONIST ACTIVITY 有权
标题翻译：具有CXCR3拮抗剂活性的新型杂环取代的吡啶化合物
公开(公告)号：US20100168124A1
公开(公告)日：2010-07-01
申请号：US12642931
申请日：2009-12-21
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 , C07D413/14 , C07D401/14 , C07D417/14 , A61P19/02 , A61P17/06 , A61P11/00
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, 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。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。

98. 发明申请

US20100145048A1 COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISORDERS 失效
标题翻译：用于治疗炎症性疾病的化合物
公开(公告)号：US20100145048A1
公开(公告)日：2010-06-10
申请号：US12582341
申请日：2009-10-20
申请人： Zhuyan Guo , Peter Orth , Zhaoning Zhu , Robert D. Mazzola , Tin-Yau Chan , Henry A. Vaccaro , Brian McKittrick , Joseph A. Kozlowski , Brian J. Lavey , Guowei Zhou , Sunil Paliwal , Shing-Chun Wong , Neng-Yang Shih , Pauline C. Ting , Kristin E. Rosner , Gerald W. Shipps, JR. , M. Arshad Siddiqui , David B. Belanger , Chaoyang Dai , Dansu Li , Vinay M. Girijavallabhan , Janeta Popovici-Muller , Wensheng Yu , Lianyun Zhao
发明人： Zhuyan Guo , Peter Orth , Zhaoning Zhu , Robert D. Mazzola , Tin-Yau Chan , Henry A. Vaccaro , Brian McKittrick , Joseph A. Kozlowski , Brian J. Lavey , Guowei Zhou , Sunil Paliwal , Shing-Chun Wong , Neng-Yang Shih , Pauline C. Ting , Kristin E. Rosner , Gerald W. Shipps, JR. , M. Arshad Siddiqui , David B. Belanger , Chaoyang Dai , Dansu Li , Vinay M. Girijavallabhan , Janeta Popovici-Muller , Wensheng Yu , Lianyun Zhao
IPC分类号： C07D405/12 , C07D417/12 , C07D413/14 , C07D409/12
CPC分类号： C07D409/14 , C07C235/06 , C07C235/08 , C07C235/10 , C07C2601/08 , C07D207/20 , C07D207/26 , C07D209/44 , C07D215/14 , C07D217/06 , C07D263/32 , C07D295/185 , C07D307/52 , C07D333/20 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D513/04
摘要： This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF-α or combinations thereof.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，溶剂合物或异构体，其可用于治疗由MMP，ADAM，TACE，TNF-α或其组合介导的疾病或病症。

99. 发明申请

US20100120838A1 COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISORDERS 有权
标题翻译：用于治疗炎症性疾病的化合物
公开(公告)号：US20100120838A1
公开(公告)日：2010-05-13
申请号：US12690633
申请日：2010-01-20
申请人： Brian J. Lavey , Joseph A. Kozlowski , Guowei Zhou , Ling Tong , Wensheng Yu , Michael K. C. Wong , Shankar B. Bandarpalle , Neng-Yang Shih , M. Arshad Siddiqui , Kristin E. Rosner , Chaoyang Dai , Janeta Popovici-Muller , Vinay M. Girijavallabhan , Dansu Li , Aneta M. Micula , Seong Heon Kim , De-Yi Yang , Razia Rizvi
发明人： Brian J. Lavey , Joseph A. Kozlowski , Guowei Zhou , Ling Tong , Wensheng Yu , Michael K. C. Wong , Shankar B. Bandarpalle , Neng-Yang Shih , M. Arshad Siddiqui , Kristin E. Rosner , Chaoyang Dai , Janeta Popovici-Muller , Vinay M. Girijavallabhan , Dansu Li , Aneta M. Micula , Seong Heon Kim , De-Yi Yang , Razia Rizvi
IPC分类号： A61K31/4178 , A61K31/437 , A61K31/4439 , C07D491/048 , C07D471/04 , C07D401/14 , C07D403/06 , A61P3/00 , A61P29/00 , A61P11/00
CPC分类号： C07D403/14 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/00
摘要： This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-α or combinations thereof.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，溶剂合物或异构体，其可用于治疗由MMP，ADAM，TACE，聚集蛋白聚糖蛋白酶，TNF-α或其组合介导的疾病或病症。

100. 发明授权

US07705153B2 Bipiperdine derivatives useful as CCR3 antagonists 失效
标题翻译：双哌啶衍生物可用作CCR3拮抗剂
公开(公告)号：US07705153B2
公开(公告)日：2010-04-27
申请号：US11049460
申请日：2005-02-02
申请人： Pauline C. Ting , Jianhua Cao , Youhao Dong , Eric J. Gilbert , Ying Huang , Joseph M. Kelly , Stuart McCombie , Neng-Yang Shih
发明人： Pauline C. Ting , Jianhua Cao , Youhao Dong , Eric J. Gilbert , Ying Huang , Joseph M. Kelly , Stuart McCombie , Neng-Yang Shih
IPC分类号： A61K31/4709 , A61K31/4725 , C07D215/14
CPC分类号： C07D401/14 , C07D211/18 , C07D211/58 , C07D401/04 , C07D471/04
摘要： The use of CCR3 antagonists of the formula I or a pharmaceutically acceptable salt thereof for the treatment of asthma is disclosed, as well as novel compounds of the formula II, pharmaceutical compositions comprising them, and their use in the treatment of asthma, wherein R, Ra, X, Xa, R1, R2, R2a, R14, R14a, R16 and n are as defined in the specification.
摘要翻译：公开了使用式I的CCR3拮抗剂或其药学上可接受的盐治疗哮喘，以及式II的新型化合物，包含它们的药物组合物及其在治疗哮喘中的用途，其中R， Ra，X，Xa，R1，R2，R2a，R14，R14a，R16和n如说明书中所定义。

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