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    Amine-linked pyridyl and phenyl substituted piperazine-piperidines with CXCR3 antagonist activity
    1.
    发明授权
    Amine-linked pyridyl and phenyl substituted piperazine-piperidines with CXCR3 antagonist activity 有权
    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。

    Heterocyclic substituted piperazines with CXCR3 antagonist activity
    3.
    发明授权
    Heterocyclic substituted piperazines with CXCR3 antagonist activity 有权
    具有CXCR3拮抗剂活性的杂环取代哌嗪

    公开(公告)号：US08207170B2

    公开(公告)日：2012-06-26

    申请号：US12952994

    申请日：2010-11-23

    申请人： Seong Heon Kim ,  Gopinadhan N. Anilkumar ,  Michael K. C. Wong ,  Qingbei Zeng ,  Stuart B. Rosenblum ,  Joseph A. Kozlowski ,  Yuefei Shao ,  Brian F. McGuinness ,  Douglas W. Hobbs

    发明人： Seong Heon Kim ,  Gopinadhan N. Anilkumar ,  Michael K. C. Wong ,  Qingbei Zeng ,  Stuart B. Rosenblum ,  Joseph A. Kozlowski ,  Yuefei Shao ,  Brian F. McGuinness ,  Douglas W. Hobbs

    IPC分类号： A61K31/497

    CPC分类号： 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: 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。

    HETEROCYCLIC SUBSTITUTED PIPERAZINES WITH CXCR3 ANTAGONIST ACTIVITY
    4.
    发明申请
    HETEROCYCLIC SUBSTITUTED PIPERAZINES WITH CXCR3 ANTAGONIST ACTIVITY 有权
    具有CXCR3拮抗剂活性的杂环取代的哌啶

    公开(公告)号：US20110065651A1

    公开(公告)日：2011-03-17

    申请号：US12952994

    申请日：2010-11-23

    申请人： Seong Heon Kim ,  Gopinadhan N. Anilkumar ,  Michael K. C. Wong ,  Qingbei Zeng ,  Stuart B. Rosenblum ,  Joseph A. Kozlowski ,  Yuefei Shao ,  Brian F. McGuinness ,  Douglas W. Hobbs

    发明人： Seong Heon Kim ,  Gopinadhan N. Anilkumar ,  Michael K. C. Wong ,  Qingbei Zeng ,  Stuart B. Rosenblum ,  Joseph A. Kozlowski ,  Yuefei Shao ,  Brian F. McGuinness ,  Douglas W. Hobbs

    IPC分类号： A61K38/13 ,  A61K31/497 ,  A61K31/56 ,  A61P19/02

    CPC分类号： 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: 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。

    Heterocyclic substituted piperazines with CXCR3 antagonist activity
    5.
    发明授权
    Heterocyclic substituted piperazines with CXCR3 antagonist activity 有权
    具有CXCR3拮抗剂活性的杂环取代哌嗪

    公开(公告)号：US07868006B2

    公开(公告)日：2011-01-11

    申请号：US11353641

    申请日：2006-02-14

    申请人： Seong Heon Kim ,  Gopinadhan N. Anilkumar ,  Michael K. C. Wong ,  Qingbei Zeng ,  Stuart B. Rosenblum ,  Joseph A. Kozlowski ,  Yuefei Shao ,  Brian F. McGuinness ,  Douglas W. Hobbs

    发明人： Seong Heon Kim ,  Gopinadhan N. Anilkumar ,  Michael K. C. Wong ,  Qingbei Zeng ,  Stuart B. Rosenblum ,  Joseph A. Kozlowski ,  Yuefei Shao ,  Brian F. McGuinness ,  Douglas W. Hobbs

    IPC分类号： A61K31/497 ,  C07D241/02

    CPC分类号： 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: 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。

    Heterocyclic substituted pyridine or phenyl compounds with CXCR3 antagonist activity
    8.
    发明授权
    Heterocyclic substituted pyridine or phenyl compounds with CXCR3 antagonist activity 有权
    杂环取代的吡啶或具有CXCR3拮抗剂活性的苯基化合物

    公开(公告)号：US07417045B2

    公开(公告)日：2008-08-26

    申请号：US11353609

    申请日：2006-02-14

    申请人： Gopinadhan N. Anilkumar ,  Qingbei Zeng ,  Stuart B. Rosenblum ,  Joseph A. Kozlowski ,  Brian F. McGuinness ,  Douglas W. Hobbs

    发明人： Gopinadhan N. Anilkumar ,  Qingbei Zeng ,  Stuart B. Rosenblum ,  Joseph A. Kozlowski ,  Brian F. McGuinness ,  Douglas W. Hobbs

    IPC分类号： A61K31/497 ,  C07D403/00 ,  C07D295/00 ,  C07D241/04

    CPC分类号： C07D417/14 ,  C07D401/04 ,  C07D401/14 ,  C07D413/14

    摘要： The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prod rug 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药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，产物，所述化合物具有式 1：或其药学上可接受的盐，溶剂化物或酯。 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。

    NOVEL HETEROCYCLIC SUBSTITUTED PYRIDINE OR PHENYL COMPOUNDS WITH CXCR3 ANTAGONIST ACTIVITY
    9.
    发明申请
    NOVEL HETEROCYCLIC SUBSTITUTED PYRIDINE OR PHENYL COMPOUNDS WITH CXCR3 ANTAGONIST ACTIVITY 有权
    具有CXCR3拮抗剂活性的新型杂环取代的吡啶或苯基化合物

    公开(公告)号：US20080292589A1

    公开(公告)日：2008-11-27

    申请号：US12147140

    申请日：2008-06-26

    申请人： Gopinadhan N. Anilkumar ,  Qingbei Zeng ,  Stuart B. Rosenblum ,  Joseph A. Kozlowski ,  Brian F. McGuinness ,  Douglas W. Hobbs

    发明人： Gopinadhan N. Anilkumar ,  Qingbei Zeng ,  Stuart B. Rosenblum ,  Joseph A. Kozlowski ,  Brian F. McGuinness ,  Douglas W. Hobbs

    IPC分类号： A61K38/21 ,  C07D401/14 ,  A61K31/496 ,  A61K38/13 ,  A61K31/573 ,  A61P29/00 ,  A61K31/505 ,  A61K31/606

    CPC分类号： C07D417/14 ,  C07D401/04 ,  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，包括同种异体移植物排斥，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。

    HETEROCYCLIC COMPOUNDS WITH CXCR3 ANTAGONIST ACTIVITY
    10.
    发明申请
    HETEROCYCLIC COMPOUNDS WITH CXCR3 ANTAGONIST ACTIVITY 审中-公开
    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。