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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

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

3. 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。

4. 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。

5. 发明授权

US07393844B2 Tetrahydropyranyl cyclopentyl heterocyclic amide 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杂环酰胺调节剂
公开(公告)号：US07393844B2
公开(公告)日：2008-07-01
申请号：US10550111
申请日：2004-03-12
申请人： Stephen D. Goble , Alexander Pasternak , Sander G. Mills , Changyou Zhou , Lihu Yang
发明人： Stephen D. Goble , Alexander Pasternak , Sander G. Mills , Changyou Zhou , Lihu Yang
IPC分类号： C07D491/02 , C07D413/02 , A61K31/538
CPC分类号： C07D413/12 , C07D405/12 , C07D417/12 , C07D471/04
摘要： The present invention is directed to compounds of the formula (1) Wherein A, B, D, X, Y, n, R1, R3, R4, R5, R15, R16, R17, R18 and the dashed line 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（1）的化合物，其中A，B，D，X，Y，n，R 1，R 3， R 4，R 5，R 15，R 16，R 17，R 16， 18和虚线如本文所定义，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

6. 发明授权

US07410961B2 2,6-disubstituted piperiddines as modulators 失效
标题翻译： 2,6-二取代的哌啶作为调节剂
公开(公告)号：US07410961B2
公开(公告)日：2008-08-12
申请号：US10586765
申请日：2005-01-14
申请人： Lihu Yang , Sander G. Mills , Changyou Zhou , Stephen D. Goble , Alexander Pasternak
发明人： Lihu Yang , Sander G. Mills , Changyou Zhou , Stephen D. Goble , Alexander Pasternak
IPC分类号： C07D401/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00 , C07D421/00 , C07D223/16 , A01N43/00 , A61K31/553 , A61K31/554
CPC分类号： C07D519/00 , C07D451/02 , C07D451/04 , C07D451/06
摘要： The present invention is further directed to compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R16, R17, R18, R19, R20, R21 and R22 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）的化合物：其中R 1，R 2，R 3，R 4， R 5，R 6，R 7，R 8，R 9，R 9， R 10，R 16，R 17，R 18，R 19，R 16， R 20，R 21，R 22和R 22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，以及自身免疫病态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。

7. 发明授权

US07700591B2 Benzoxazinyl-amidocyclopentyl-heterocyclic modulators of chemokine receptors 有权
标题翻译：趋化因子受体的苯并恶嗪基酰胺基环戊基 - 杂环调节剂
公开(公告)号：US07700591B2
公开(公告)日：2010-04-20
申请号：US11129512
申请日：2005-05-13
申请人： Stephen D. Goble , Sander G. Mills , Lihu Yang , Alexander Pasternak , Celine Bonnefous , Theodore M Kamenecka , Jean-Michel Vernier , John H. Hutchinson , Essa Hu , Steven Govek
发明人： Stephen D. Goble , Sander G. Mills , Lihu Yang , Alexander Pasternak , Celine Bonnefous , Theodore M Kamenecka , Jean-Michel Vernier , John H. Hutchinson , Essa Hu , Steven Govek
IPC分类号： A61K31/535 , C07D265/12 , C07D498/00
CPC分类号： C07D413/08 , C07D413/14 , C07D417/14
摘要： Cyclopentyl compounds linked to a benzoxazinyl group through an amido moiety utilizing the ring nitrogen of the benzoxazine, and further substituted with a heterocyclic moiety, such compounds represented by formula I: which are used to modulate the CCR-2 chemokine receptor to prevent or treat 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; and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions.
摘要翻译：通过使用苯并恶嗪的环氮通过酰胺部分连接到苯并恶嗪基的环戊基化合物，并进一步被杂环部分取代，由式I表示的化合物：其用于调节CCR-2趋化因子受体以预防或治疗炎症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，以及自身免疫性病态如类风湿性关节炎和动脉粥样硬化; 和包含这些化合物的药物组合物以及这些化合物和组合物的用途。

8. 发明授权

US07566726B2 3,3-disubstituted tetrahydropyranyl cyclopentyl amide modulators of chemokine receptor activity 失效
标题翻译：趋化因子受体活性的3,3-二取代四氢吡喃基环戊基酰胺调节剂
公开(公告)号：US07566726B2
公开(公告)日：2009-07-28
申请号：US11587448
申请日：2005-04-22
申请人： Lihu Yang , Sander G. Mills , Kothandaraman Shankaran
发明人： Lihu Yang , Sander G. Mills , Kothandaraman Shankaran
IPC分类号： C07D217/02 , C07D471/02 , A61K31/4375
CPC分类号： C07D471/04
摘要： (wherein n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, Y and Z are 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：（其中n，R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9，R 10，R 15，R 16，R 17，R 18，Y和Z在本文中定义），其是趋化因子受体活性的调节剂，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，以及自身免疫病态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。

9. 发明授权

US07700772B2 Amino heterocyclic modulators of chemokine receptor activity 失效
标题翻译：趋化因子受体活性的氨基杂环调节剂
公开(公告)号：US07700772B2
公开(公告)日：2010-04-20
申请号：US10589406
申请日：2005-02-08
申请人： Lihu Yang , Alexander Pasternak , Sander G. Mills
发明人： Lihu Yang , Alexander Pasternak , Sander G. Mills
IPC分类号： C07D401/04 , C07D407/04 , A61K31/445 , A61K31/438
CPC分类号： C07D307/24 , C07D207/16 , C07D401/04 , C07D405/04 , C07D405/12 , C07D405/14 , C07D471/04
摘要： Compounds of Formula I and Formula II: (wherein n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, R19, R24, R25, R26, R27, R28, R29, R30, R33, R34, R35, R36, R37, R38, A, j, k, m, n, X, Y and Z 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：式I和式II化合物（其中n，R1，R2，R3，R4，R5，R6，R7，R8，R9，R10，R15，R16，R17，R18，R19，R24，R25，R26， R28，R29，R30，R33，R34，R35，R36，R37，R38，A，j，k，m，n，X，Y和Z如本文所定义），其是趋化因子受体活性的调节剂，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，以及自身免疫性病态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。

10. 发明授权

US06248755B1 Pyrrolidine modulators of chemokine receptor activity 失效
标题翻译：趋化因子受体活性的吡咯烷调节剂
公开(公告)号：US06248755B1
公开(公告)日：2001-06-19
申请号：US09542617
申请日：2000-04-04
申请人： Kevin Chapman , Jeffrey Hale , Dooseop Kim , Christopher Lynch , Shrenik Shah , Kothandaraman Shankaran , Dong-Ming Shen , Christopher Willoughby , Malcolm MacCoss , Sander G. Mills , Jennifer L. Loebach , Ravindra N. Guthikonda
发明人： Kevin Chapman , Jeffrey Hale , Dooseop Kim , Christopher Lynch , Shrenik Shah , Kothandaraman Shankaran , Dong-Ming Shen , Christopher Willoughby , Malcolm MacCoss , Sander G. Mills , Jennifer L. Loebach , Ravindra N. Guthikonda
IPC分类号： A61K3150
CPC分类号： C07D401/06 , C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4, R5, R6, R14 and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.
摘要翻译：本发明涉及可用作趋化因子受体活性调节剂的式I的吡咯烷化合物（其中R 1，R 2，R 3，R 4，R 5，R 6，R 14和n如本文所定义）。特别地，这些化合物可用作趋化因子受体CCR-5和/或CCR-3的调节剂。

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