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公开(公告)号：US06498161B1
公开(公告)日：2002-12-24
申请号：US09543019
申请日：2000-04-04
申请人： Charles G. Caldwell , Kevin T. Chapman , Jeffrey Hale , Dooseop Kim , Christopher Lynch , Malcolm MacCoss , Sander G. Mills , Christopher Willoughby , Scott Berk , Ronald M. Kim
发明人： Charles G. Caldwell , Kevin T. Chapman , Jeffrey Hale , Dooseop Kim , Christopher Lynch , Malcolm MacCoss , Sander G. Mills , Christopher Willoughby , Scott Berk , Ronald M. Kim
IPC分类号： A61K31165
CPC分类号： C07D401/14 , C07D401/06 , C07D409/14 , C07D413/14 , C07D417/14 , C07D491/10 , C07F9/59 , C07F9/65583
摘要： The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4, R5, R6 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的调节剂的式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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公开(公告)号：US06399619B1
公开(公告)日：2002-06-04
申请号：US09542898
申请日：2000-04-04
申请人： Scott Berk , Charles G. Caldwell , Kevin T. Chapman , Jeffrey Hale , Christopher Lynch , Malcolm MacCoss , Sander G. Mills , Christopher Willoughby
发明人： Scott Berk , Charles G. Caldwell , Kevin T. Chapman , Jeffrey Hale , Christopher Lynch , Malcolm MacCoss , Sander G. Mills , Christopher Willoughby
IPC分类号： A61K31495
CPC分类号： C07D401/06 , C07C259/06 , C07C2601/02 , C07C2601/04 , C07D401/14 , C07D405/14
摘要： The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4, R5, R6 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.
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公开(公告)号：US06265434B1
公开(公告)日：2001-07-24
申请号：US09543024
申请日：2000-04-04
申请人： Charles Caldwell , Kevin T. Chapman , Jeffrey Hale , Dooseop Kim , Christopher Lynch , Malcolm MacCoss , Sander G. Mills , Keith Rosauer , Christopher Willoughby , Scott Berk
发明人： Charles Caldwell , Kevin T. Chapman , Jeffrey Hale , Dooseop Kim , Christopher Lynch , Malcolm MacCoss , Sander G. Mills , Keith Rosauer , Christopher Willoughby , Scott Berk
IPC分类号： A61K3140
CPC分类号： C07D401/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D495/04
摘要： The present invention is directed to pyrrolidine compounds of the formula 1: (wherein R1, R2, R3, R4, R5, R6 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1的吡咯烷化合物（其中R 1，R 2，R 3，R 4，R 5，R 6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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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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公开(公告)号：US5750549A
公开(公告)日：1998-05-12
申请号：US730277
申请日：1996-10-15
申请人： Charles G. Caldwell , Ping Chen , Philippe L. Durette , Paul Finke , Jeffrey Hale , Edward Holson , Ihor Kopka , Malcolm MacCoss , Laura Meurer , Sander G. Mills , Albert Robichaud
发明人： Charles G. Caldwell , Ping Chen , Philippe L. Durette , Paul Finke , Jeffrey Hale , Edward Holson , Ihor Kopka , Malcolm MacCoss , Laura Meurer , Sander G. Mills , Albert Robichaud
IPC分类号： C07C69/757 , C07C217/52 , C07C237/06 , C07C255/59 , C07D207/08 , C07D207/16 , C07D207/26 , C07D213/30 , C07D213/38 , C07D213/61 , C07D215/18 , C07D215/20 , C07D233/70 , C07D239/26 , C07D249/08 , C07D249/12 , C07D257/04 , C07D261/08 , C07D271/06 , C07D271/10 , C07D277/28 , C07D277/64 , C07D307/12 , C07D307/82 , C07D333/20 , C07D333/32 , C07D333/64 , C07D401/04 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D513/04 , C07D521/00 , A61K31/41
CPC分类号： C07D207/26 , C07C217/52 , C07C237/06 , C07C255/59 , C07C69/757 , C07D207/08 , C07D207/16 , C07D213/30 , C07D213/38 , C07D213/61 , C07D215/18 , C07D215/20 , C07D231/12 , C07D233/56 , C07D233/70 , C07D239/26 , C07D249/08 , C07D249/12 , C07D257/04 , C07D261/08 , C07D271/06 , C07D271/10 , C07D277/28 , C07D277/64 , C07D307/12 , C07D307/82 , C07D333/20 , C07D333/32 , C07D333/64 , C07D401/04 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D513/04 , C07C2101/08 , C07C2101/14
摘要： The present invention is directed to certain novel compounds represented by structural formula I: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.11, R.sup.12, R.sup.13, A, Q, W, X, Y, Z and n are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis.
摘要翻译： 本发明涉及由结构式I表示的某些新化合物：其中R3，R6，R7，R8，R11，R12，R13，A，Q，W，X，Y，Z和n如本文所定义。 本发明还涉及包含这些新化合物作为活性成分的药物制剂，以及新型化合物及其制剂在治疗某些疾病中的用途。 本发明化合物是速激肽受体拮抗剂，可用于治疗炎性疾病，疼痛或偏头痛，哮喘和呕吐。
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公开(公告)号：US06593346B2
公开(公告)日：2003-07-15
申请号：US10075163
申请日：2002-02-14
申请人： Paul E. Finke , Kerry A. Hilfiker , Malcolm MacCoss , Kevin T. Chapman , Jennifer L. Loebach , Sander G. Mills , Ravi N. Guthikonda , Shrenik K. Shah , Dooseop Kim , Dong-Ming Shen , Bryan Oates
发明人： Paul E. Finke , Kerry A. Hilfiker , Malcolm MacCoss , Kevin T. Chapman , Jennifer L. Loebach , Sander G. Mills , Ravi N. Guthikonda , Shrenik K. Shah , Dooseop Kim , Dong-Ming Shen , Bryan Oates
IPC分类号： A61K31445
CPC分类号： C07D401/04 , C07D211/14 , C07D211/18 , C07D211/20 , C07D211/24 , C07D211/34 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/04 , C07D413/06 , C07D417/04 , C07D471/04 , Y02P20/582
摘要： The present invention is directed to compounds of the formula I: (wherein R1, R3, R4, R5, R6, R7, R8, X, n, x and y 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.
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公开(公告)号：US06358979B1
公开(公告)日：2002-03-19
申请号：US09590750
申请日：2000-06-08
申请人： Paul E. Finke , Kerry A. Hilfiker , Malcolm MacCoss , Kevin T. Chapman , Jennifer L. Loebach , Sander G. Mills , Ravi N. Guthikonda , Shrenik K. Shah , Dooseop Kim , Dong-Ming Shen , Bryan Oates
发明人： Paul E. Finke , Kerry A. Hilfiker , Malcolm MacCoss , Kevin T. Chapman , Jennifer L. Loebach , Sander G. Mills , Ravi N. Guthikonda , Shrenik K. Shah , Dooseop Kim , Dong-Ming Shen , Bryan Oates
IPC分类号： A61K31445
CPC分类号： C07D401/04 , C07D211/14 , C07D211/18 , C07D211/20 , C07D211/24 , C07D211/34 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/04 , C07D413/06 , C07D417/04 , C07D471/04 , Y02P20/582
摘要： The present invention is directed to compounds of the formula I: (wherein R1, R3, R4, R5, R6, R7, R8, X, n, x and y 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化合物（其中R 1，R 3，R 4，R 5，R 6，R 7，R 8，X，n，x和y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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公开(公告)号：US5637699A
公开(公告)日：1997-06-10
申请号：US445489
申请日：1995-05-22
申请人： Conrad P. Dorn , Jeffrey J. Hale , Paul E. Finke , Malcolm MacCoss , Sander G. Mills , Shrenik K. Shah , Mark S. Chambers , Timothy Harrison , Tamara Ladduwahetty , Brian J. Williams
发明人： Conrad P. Dorn , Jeffrey J. Hale , Paul E. Finke , Malcolm MacCoss , Sander G. Mills , Shrenik K. Shah , Mark S. Chambers , Timothy Harrison , Tamara Ladduwahetty , Brian J. Williams
IPC分类号： C07D265/30 , C07D265/32 , C07D279/12 , C07D413/04 , C07D413/06 , C07D413/14 , C07D413/02 , C07D265/28 , C07D265/34
CPC分类号： C07D265/30 , C07D265/32 , C07D279/12 , C07D413/04 , C07D413/06 , C07D413/14
摘要： Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
摘要翻译： 取代的通式结构式的杂环：
是可用于治疗炎性疾病，疼痛或偏头痛，哮喘和呕吐的速激肽受体拮抗剂，以及可用于治疗心血管疾病如心绞痛，高血压或缺血的钙通道阻滞剂。 -
公开(公告)号：US5387595A
公开(公告)日：1995-02-07
申请号：US935754
申请日：1992-08-26
IPC分类号： C07C235/34 , C07C275/24 , C07D213/40 , C07D249/08 , C07D249/12 , C07C57/46 , C07C235/26
CPC分类号： C07D213/40 , C07C235/34 , C07C275/24 , C07D249/08 , C07D249/12 , C07C2101/14
摘要： Substituted alicyclic compounds of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, and asthma.
摘要翻译： 取代的通式结构式的脂环化合物：
是可用于治疗炎性疾病，疼痛或偏头痛和哮喘的速激肽受体拮抗剂。 -
公开(公告)号：US5344830A
公开(公告)日：1994-09-06
申请号：US988514
申请日：1992-12-10
申请人： Sander G. Mills , Richard J. Budhu , Conrad P. Dorn , William J. Greenlee , Malcolm MacCoss , Mu T. Wu
发明人： Sander G. Mills , Richard J. Budhu , Conrad P. Dorn , William J. Greenlee , Malcolm MacCoss , Mu T. Wu
IPC分类号： C07D241/04 , A61K31/495 , C07D401/12 , C07D413/12
CPC分类号： C07D241/04
摘要： Diacylpiperazines of general structure ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, and asthma, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
摘要翻译： 一般结构的二酰基哌嗪可以用于治疗炎性疾病，疼痛或偏头痛，哮喘和钙通道阻滞剂，可用于治疗心血管疾病如心绞痛，高血压或局部缺血。
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