公开(公告)号：EP1718152A2

公开(公告)日：2006-11-08

申请号：EP05722554.2

申请日：2005-01-26

申请人： Merck & Co., Inc.

发明人： BUTORA, Gabor ,  GUIADEEN, Deodialsingh ,  KOTHANDARAMAN, Shankaran ,  MACCOSS, Malcolm ,  MILLS, Sander, G. ,  YANG, Lihu

IPC分类号： A01N43/64 ,  A01N43/66 ,  A01N43/58 ,  A01N43/60 ,  A61K31/53 ,  A61K31/495 ,  A61K31/50 ,  C07D253/08 ,  C07D487/00 ,  C07D241/36

CPC分类号： C07D471/04

摘要： Compounds of Formula I and Formula II (wherein A, E, j, k, m, n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, R19, R24, R25, R26, R27, R28, R29, R30, R31, R32, R33, R34, 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.

公开(公告)号：EP1501507A2

公开(公告)日：2005-02-02

申请号：EP03724241.9

申请日：2003-04-25

申请人： Merck & Co., Inc. ,  MERCK SHARP & DOHME LTD.

发明人： JIAO, Richard ,  MORRIELLO, Gregori ,  YANG, Lihu ,  GOBLE, Stephen, D. ,  MILLS, Sander, G. ,  PASTERNAK, Alexander ,  ZHOU, Changyou ,  BUTORA, Gabor ,  KOTHANDARAMAN, Shankaran ,  GUIADEEN, Deodialsingh ,  TANG, Cheng ,  MOYES, Christopher

IPC分类号： A61K31/4375 ,  C07D471/04

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.

公开(公告)号：EP1501803B1

公开(公告)日：2008-08-13

申请号：EP03719958.5

申请日：2003-04-25

申请人： Merck & Co., Inc. ,  MERCK SHARP & DOHME LTD.

发明人： JIAO, Richard ,  GOBLE, Stephen, D. ,  MILLS, Sander, G. ,  MORRIELLO, Gregori ,  PASTERNAK, Alexander ,  YANG, Lihu ,  ZHOU, Changyou ,  BUTORA, Gabor ,  KOTHANDARAMAN, Shankaran ,  GUIADEEN, Deodialsingh ,  MOYES, Christopher

IPC分类号： C07D217/00 ,  A61K31/47 ,  C07D405/12 ,  C07D401/12 ,  C07D217/06 ,  A61P29/00

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R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9，R 10，X，n和虚线在本文中定义） 趋化因子受体活性调节剂。 特别是，这些化合物可用作趋化因子受体CCR-2的调节剂。

公开(公告)号：EP1052992A1

公开(公告)日：2000-11-22

申请号：EP99906697.0

申请日：1999-02-01

申请人： MERCK & CO., INC.

发明人： CALDWELL, Charles, G. ,  FINKE, Paul, E. ,  MACCOSS, Malcolm ,  MILLS, Sander, G. ,  OATES, Bryan ,  KIM, Dooseop ,  KOTHANDARAMAN, Shankaran ,  WANG, Liping

IPC分类号： A61K31/445 ,  A61K31/535 ,  A61K31/54 ,  A61K31/55 ,  C07D211/18 ,  C07D211/32 ,  C07D211/36 ,  C07D211/96 ,  C07D401/06 ,  C07D401/14 ,  C07D407/14 ,  C07D409/10 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/10 ,  C07D491/107

CPC分类号： C07D231/12 ,  C07D211/56 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06

摘要： The present invention is directed to cyclic amines of formula I (wherein R?1, R2, R3¿, m 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-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.

公开(公告)号：EP2136810A1

公开(公告)日：2009-12-30

申请号：EP08742873.6

申请日：2008-04-14

申请人： Merck & Co., Inc.

发明人： GUIADEEN, Deodialsingh ,  HALE, Jeffrey, J. ,  KOTHANDARAMAN, Shankaran

IPC分类号： A61K31/535

CPC分类号： C07D471/04

摘要： The present invention relates to naphthyridine compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.

公开(公告)号：EP1501803A2

公开(公告)日：2005-02-02

申请号：EP03719958.5

申请日：2003-04-25

申请人： Merck & Co., Inc. ,  MERCK SHARP & DOHME LTD.

发明人： JIAO, Richard ,  GOBLE, Stephen, D. ,  MILLS, Sander, G. ,  MORRIELLO, Gregori ,  PASTERNAK, Alexander ,  YANG, Lihu ,  ZHOU, Changyou ,  BUTORA, Gabor ,  KOTHANDARAMAN, Shankaran ,  GUIADEEN, Deodialsingh ,  MOYES, Christopher

IPC分类号： C07D217/00 ,  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.

公开(公告)号：EP1501507B1

公开(公告)日：2008-05-28

申请号：EP03724241.9

申请日：2003-04-25

申请人： Merck & Co., Inc. ,  MERCK SHARP & DOHME LTD.

发明人： JIAO, Richard ,  MORRIELLO, Gregori ,  YANG, Lihu ,  GOBLE, Stephen, D. ,  MILLS, Sander, G. ,  PASTERNAK, Alexander ,  ZHOU, Changyou ,  BUTORA, Gabor ,  KOTHANDARAMAN, Shankaran ,  GUIADEEN, Deodialsingh ,  TANG, Cheng ,  MOYES, Christopher

IPC分类号： C07D471/04 ,  A61K31/4375 ,  A61P29/00

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.

公开(公告)号：EP1701724A2

公开(公告)日：2006-09-20

申请号：EP04815779.6

申请日：2004-12-29

申请人： Merck & Co., Inc.

发明人： GOBLE, Stephen, D. ,  YANG, Lihu ,  ZHOU, Changyou ,  KOTHANDARAMAN, Shankaran ,  GUIADEEN, Deodialsingh ,  BUTORA, Gabor ,  PASTERNAK, Alexander ,  MILLS, Sander, G.

IPC分类号： A61K31/4375

CPC分类号： C07D405/12 ,  C07C237/24 ,  C07C311/37 ,  C07C311/43 ,  C07C313/04 ,  C07C2601/08 ,  C07D213/53 ,  C07D217/06 ,  C07D265/14 ,  C07D267/14 ,  C07D277/46 ,  C07D317/58 ,  C07D471/04

摘要： Compounds of the formula (I) which are modulators of chemokine receptor activity 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, and 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： 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，特应性疾病，包括过敏性鼻炎，皮炎，结膜炎和哮喘以及自身免疫病理学的趋化因子受体活性调节剂的式（I）化合物 例如类风湿性关节炎和动脉粥样硬化，以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。