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1. 发明授权

US07390803B2 Tetrahydropyranyl cyclopentyl benzylamide modulators of chemokine receptor activity 失效
标题翻译：趋化因子受体活性的四氢吡喃基环戊基苄基酰胺调节剂
公开(公告)号：US07390803B2
公开(公告)日：2008-06-24
申请号：US10533326
申请日：2003-10-24
申请人： Gabor Butora , Sander G. Mills , Alexander Pasternak , Kothandaraman Shankaran , Lihu Yang , Changyou Zhou , Stephen D. Goble
发明人： Gabor Butora , Sander G. Mills , Alexander Pasternak , Kothandaraman Shankaran , Lihu Yang , Changyou Zhou , Stephen D. Goble
IPC分类号： A61K31/351 , A61K31/4523 , A61K31/5365 , C07D257/04 , C07D231/56
CPC分类号： C07D311/00 , C07C237/24 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/08 , C07C2602/10 , C07D211/58 , C07D211/96 , C07D305/08 , C07D307/22 , C07D309/14 , C07D311/02 , C07D311/68 , C07D311/74 , C07D313/04 , C07D319/06 , C07D333/36 , C07D335/02 , C07D405/04 , C07D405/12 , C07D409/12 , C07D417/12 , C07D491/04 , C07D491/107 , C07D493/08
摘要： The present invention is directed to compounds of the formula (I) (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R27, R28, R29, R30, R31, X, m, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2
摘要翻译：本发明涉及式（I）化合物（其中R 1，R 2，R 3，R 3，R 4， R 5，R 6，R 7，R 8，R 9，R 9， R 10，R 11，R 27，R 28，R 29， R 30，R 30，R 31，X，m，n，虚线在本文中定义），其可用作趋化因子受体活性的调节剂。特别地，这些化合物可用作趋化因子受体CCR-2的调节剂

2. 发明授权

US06812234B2 Tetrahydropyranyl cyclopentyl tetrahydropyridopyridine modulators of chemokine receptor activity 有权
标题翻译：趋化因子受体活性的四氢吡喃基环戊基四氢吡啶并吡啶调节剂
公开(公告)号：US06812234B2
公开(公告)日：2004-11-02
申请号：US10425167
申请日：2003-04-29
申请人： Richard Jiao , Gregori Morriello , Lihu Yang , Stephen D. Goble , Sander G. Mills , Alexander Pasternak , Changyou Zhou , Gabor Butora , Shankaran Kothandaraman , Deodialsingh Guiadeen , Christopher Moyes , Cheng Tang
发明人： Richard Jiao , Gregori Morriello , Lihu Yang , Stephen D. Goble , Sander G. Mills , Alexander Pasternak , Changyou Zhou , Gabor Butora , Shankaran Kothandaraman , Deodialsingh Guiadeen , Christopher Moyes , Cheng Tang
IPC分类号： A61K314375
CPC分类号： C07D471/04
摘要： The present invention is directed to compounds of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
摘要翻译：本发明涉及式I化合物：其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 7， R 9，R 10，X，n和虚线在本文中定义），其可用作趋化因子受体活性的调节剂。特别地，这些化合物可用作趋化因子受体CCR-2的调节剂。

3. 发明授权

US07166614B2 Tetrahydropyranyl cyclopentyl tetrahydroisoquinoline modulators of chemokine receptor activity 失效
标题翻译：趋化因子受体活性的四氢吡喃基环戊基四氢异喹啉调节剂
公开(公告)号：US07166614B2
公开(公告)日：2007-01-23
申请号：US10512925
申请日：2003-04-25
申请人： Richard Jiao , Stephen D. Goble , Sander G. Mills , Gregori Morriello , Alexander Pasternak , Lihu Yang , Changyou Zhou , Gabor Butora , Shankaran Kothandaraman , Deodialsingh Guiadeen , Christopher Moyes
发明人： Richard Jiao , Stephen D. Goble , Sander G. Mills , Gregori Morriello , Alexander Pasternak , Lihu Yang , Changyou Zhou , Gabor Butora , Shankaran Kothandaraman , Deodialsingh Guiadeen , Christopher Moyes
IPC分类号： C07D217/02 , A61K31/47
CPC分类号： C07D231/12 , C07D217/06 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D491/04 , C07D491/052
摘要： The present invention is directed to compounds of the formula I: I(wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2
摘要翻译：本发明涉及式I化合物（其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R10，X，n和虚线在本文中定义）趋化因子受体活性的调节剂。特别地，这些化合物可用作趋化因子受体CCR-2的调节剂

4. 发明授权

US07589085B2 Tetrahydropyran heterocyclic cyclopentyl heteroaryl modulators of chemokine receptor activity 失效
标题翻译：趋化因子受体活性的四氢吡喃杂环环戊基杂芳基调节剂
公开(公告)号：US07589085B2
公开(公告)日：2009-09-15
申请号：US10567516
申请日：2004-08-06
申请人： Gabor Butora , Lihu Yang , Stephen D. Goble
发明人： Gabor Butora , Lihu Yang , Stephen D. Goble
IPC分类号： C07D401/02 , A61K31/44
CPC分类号： C07D405/12 , C07D417/12
摘要： The present invention is further directed to compounds of the formulas: (I) (II) (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, R19, R24 and R25 are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.
摘要翻译：本发明还涉及式（I）（II）（其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R10，R15，R16，R17，R18，R19， R24和R25如本文所定义），其是趋化因子受体活性的调节剂，并且可用于预防或治疗某些炎性和免疫调节性疾病和疾病，过敏性疾病，特应性病症，包括过敏性鼻炎，皮炎，结膜炎和哮喘，以及作为自身免疫性病变如类风湿性关节炎和动脉粥样硬化。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及趋化因子受体的疾病中的用途。

5. 发明授权

US07598243B2 Heterocyclic cyclopentyl tetrahydroisoquinoline and tetrahydropyridopyridine modulators of chemokine receptor activity 失效
标题翻译：杂环环四氢异喹啉和四氢吡啶并吡啶调节剂的趋化因子受体活性
公开(公告)号：US07598243B2
公开(公告)日：2009-10-06
申请号：US10260008
申请日：2004-10-15
申请人： Gabor Butora , Stephen D. Goble , Alexander Pasternak , Lihu Yang , Changyou Zhou , Christopher R. Moyes
发明人： Gabor Butora , Stephen D. Goble , Alexander Pasternak , Lihu Yang , Changyou Zhou , Christopher R. Moyes
IPC分类号： A61K31/5377 , C07D413/08 , C07D413/14
CPC分类号： C07D401/08 , C07D217/06 , C07D401/12 , C07D401/14 , C07D413/08 , C07D471/04 , C07D491/08 , C07D519/00
摘要： The present invention is directed to compounds of the formula I: Wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X, n and the broken lines are as defined herein which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
摘要翻译：本发明涉及式I化合物：其中R1，R2，R3，R4，R5，R6，R7，R8，R9，X，n和虚线如本文所定义，其可用作趋化因子受体的调节剂活动。特别地，这些化合物可用作趋化因子受体CCR-2的调节剂。

6. 发明申请

US20080081803A1 Heterocyclic cyclopentyl tetrahydroisoquinoline and tetrahydropyridopyridine modulators of chemokine receptor activity 失效
标题翻译：杂环环四氢异喹啉和四氢吡啶并吡啶调节剂的趋化因子受体活性
公开(公告)号：US20080081803A1
公开(公告)日：2008-04-03
申请号：US10260008
申请日：2004-10-15
申请人： Gabor Butora , Stephen D. Goble , Alexander Pastemak , Lihu Yang , Changyou Zhou , Christopher R. Moyes
发明人： Gabor Butora , Stephen D. Goble , Alexander Pastemak , Lihu Yang , Changyou Zhou , Christopher R. Moyes
IPC分类号： A61K31/4725 , A61K31/4709 , A61K31/496 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/553 , A61P19/02 , A61P29/00 , A61P35/00 , A61P37/00 , C07D401/08 , C07D401/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D491/08
CPC分类号： C07D401/08 , C07D217/06 , C07D401/12 , C07D401/14 , C07D413/08 , C07D471/04 , C07D491/08 , C07D519/00
摘要： The present invention is directed to compounds of the formula I: Wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X, n and the broken lines are as defined herein which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
摘要翻译：本发明涉及式I化合物：其中R 1，R 2，R 3，R 4， R 5，R 6，R 7，R 8，R 9， SUB，X，n，虚线如本文所定义，其可用作趋化因子受体活性的调节剂。特别地，这些化合物可用作趋化因子受体CCR-2的调节剂。

7. 发明授权

US07230008B2 Tetrahydropyranyl cyclopentyl tetrahydropyridopyridine modulators of chemokine receptor activity 有权
标题翻译：趋化因子受体活性的四氢吡喃基环戊基四氢吡啶并吡啶调节剂
公开(公告)号：US07230008B2
公开(公告)日：2007-06-12
申请号：US10923594
申请日：2004-08-20
申请人： Richard Jiao , Gabor Butora , Stephen D. Goble , Deodialsingh Guiadeen , Sander G. Mills , Gregori Morriello , Alexander Pasternak , Cheng Tang , Lihu Yang , Changyou Zhou , Shankaran Kothandaraman , Christopher Moyes
发明人： Richard Jiao , Gabor Butora , Stephen D. Goble , Deodialsingh Guiadeen , Sander G. Mills , Gregori Morriello , Alexander Pasternak , Cheng Tang , Lihu Yang , Changyou Zhou , Shankaran Kothandaraman , Christopher Moyes
IPC分类号： A61K31/47 , C07D471/02
CPC分类号： A61K31/4375
摘要： The present invention is directed to methods for treating, preventing, ameliorating, controlling or reducing the risk of an inflammatory or immunoregulatory disorder or disease, which method comprises the administration to a patient of an effective amount of the compound of formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
摘要翻译：本发明涉及用于治疗，预防，改善，控制或降低炎性或免疫调节性疾病或疾病风险的方法，该方法包括向患者施用有效量的式I化合物：（其中R R 1，R 2，R 3，R 4，R 5，R 5，R 5， R 6，R 7，R 8，R 9，R 10，X 10，，n和虚线在本文中定义），其可用作趋化因子受体活性的调节剂。特别地，这些化合物可用作趋化因子受体CCR-2的调节剂。

8. 发明申请

US20060030582A1 Tetrahydropyranyl cyclopentyl tetrahydropyridopyridine modulators of chemokine receptor activity 审中-公开
标题翻译：趋化因子受体活性的四氢吡喃基环戊基四氢吡啶并吡啶调节剂
公开(公告)号：US20060030582A1
公开(公告)日：2006-02-09
申请号：US11102417
申请日：2005-04-08
申请人： Julie DeMartino , Taro Akiyama , Mary Struthers , Lihu Yang , Joel Berger , Gregori Morriello , Alexander Pastemak , Changyou Zhou , Sander Mills , Gabor Butora , Shankaran Kothandaraman , Deodialsingh Guiadeen , Cheng Tang , Richard Jiao , Stephen Goble , Christopher Moyes
发明人： Julie DeMartino , Taro Akiyama , Mary Struthers , Lihu Yang , Joel Berger , Gregori Morriello , Alexander Pastemak , Changyou Zhou , Sander Mills , Gabor Butora , Shankaran Kothandaraman , Deodialsingh Guiadeen , Cheng Tang , Richard Jiao , Stephen Goble , Christopher Moyes
IPC分类号： A61K31/4745
CPC分类号： A61K31/4745 , A61K31/495 , A61K31/55
摘要： The present invention is directed to methods for treating, preventing, ameliorating, controlling or reducing the risk of a disorder or disease, which method comprises the administration to a patient of an effective amount of the compound of formula I: I (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
摘要翻译：本发明涉及治疗，预防，改善，控制或降低病症或疾病风险的方法，该方法包括向患者施用有效量的式I化合物：其中R为 R 1，R 2，R 3，R 4，R 5，R 4， R 6，R 7，R 8，R 9，R 10，X，n，并且虚线在本文中定义），其可用作趋化因子受体活性的调节剂。特别地，这些化合物可用作趋化因子受体CCR-2的调节剂。

9. 发明授权

US07632821B2 Ribonucleoside cyclic acetal derivatives for the treatment of RNA-dependent RNA viral infection 失效
标题翻译：用于治疗RNA依赖性RNA病毒感染的核糖核苷环缩醛衍生物
公开(公告)号：US07632821B2
公开(公告)日：2009-12-15
申请号：US11990051
申请日：2006-08-04
申请人： Gabor Butora , Kenneth Alan Koeplinger , Malcolm MacCoss , Daniel R. McMasters , David B. Olsen , Lihu Yang
发明人： Gabor Butora , Kenneth Alan Koeplinger , Malcolm MacCoss , Daniel R. McMasters , David B. Olsen , Lihu Yang
IPC分类号： A01N43/04 , A61K31/70
CPC分类号： C07H19/06 , C07H19/16
摘要： The present invention provides ribonucleoside 2′,3′-cyclic acetals of structural formula I which are precursors or prodrugs of inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors of inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors or prodrugs of inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors or prodrugs of inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such ribonucleoside 2′,3′-cyclic acetals alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the ribonucleoside 2′,3′-cyclic acetals of the present invention.
摘要翻译：本发明提供结构式I的核糖核苷2'，3'-环状缩醛，其为RNA依赖性RNA病毒聚合酶抑制剂的前体或前药。这些化合物是RNA依赖性RNA病毒复制的抑制剂的前体，可用于治疗RNA依赖性RNA病毒感染。它们特别可用作丙型肝炎病毒（HCV）NS5B聚合酶抑制剂的前体或前药，作为HCV复制抑制剂的前体或前药，和/或用于治疗丙型肝炎感染。本发明还描述了含有这种核糖核苷2'，3'-环状缩醛单独或与其它对RNA依赖性RNA病毒感染，特别是HCV感染有活性的试剂组合的药物组合物。还公开了本发明的核糖核苷2'，3'-环状缩醛的抑制RNA依赖性RNA聚合酶，抑制RNA依赖性RNA病毒复制和/或治疗RNA依赖性RNA病毒感染的方法。

10. 发明申请

US20090099126A1 Ribonucleoside Cyclic Acetal Derivatives for the Treatment of RNA-Dependent RNA Viral Infection 失效
标题翻译：用于治疗RNA依赖性RNA病毒感染的核糖核苷环形缩醛衍生物
公开(公告)号：US20090099126A1
公开(公告)日：2009-04-16
申请号：US11990051
申请日：2006-08-04
申请人： Gabor Butora , Kenneth Alan Koeplinger , Malcolm MacCoss , Daniel R. McMasters , David B. Olsen , Lihu Yang
发明人： Gabor Butora , Kenneth Alan Koeplinger , Malcolm MacCoss , Daniel R. McMasters , David B. Olsen , Lihu Yang
IPC分类号： A61K31/7076 , C07H19/16 , A61K31/7064 , A61P31/12 , C07H19/06
CPC分类号： C07H19/06 , C07H19/16
摘要： The present invention provides ribonucleoside 2′,3′-cyclic acetals of structural formula I which are precursors or prodrugs of inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors of inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as pre-cursors or prodrugs of inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors or prodrugs of inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such ribonucleoside 2′,3′-cyclic acetals alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the ribonucleoside 2′,3′-cyclic acetals of the present invention.
摘要翻译：本发明提供结构式I的核糖核苷2'，3'-环状缩醛，其为RNA依赖性RNA病毒聚合酶抑制剂的前体或前药。这些化合物是RNA依赖性RNA病毒复制的抑制剂的前体，可用于治疗RNA依赖性RNA病毒感染。它们特别可用作丙型肝炎病毒（HCV）NS5B聚合酶的抑制剂的前体或前药，作为HCV复制抑制剂的前体或前药，和/或用于治疗丙型肝炎感染。本发明还描述了含有这种核糖核苷2'，3'-环状缩醛单独或与其它对RNA依赖性RNA病毒感染，特别是HCV感染有活性的试剂组合的药物组合物。还公开了本发明的核糖核苷2'，3'-环状缩醛的抑制RNA依赖性RNA聚合酶，抑制RNA依赖性RNA病毒复制和/或治疗RNA依赖性RNA病毒感染的方法。

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