公开(公告)号：EP1846379B1

公开(公告)日：2009-08-19

申请号：EP06719898.6

申请日：2006-01-30

申请人： Merck & Co., Inc.

发明人： GE, Min ,  YANG, Lihu ,  ZHOU, Changyou ,  LIN, Songnian ,  TANG, Haifeng ,  CLINE, Eric, Dean ,  MALKANI, Sunita

IPC分类号： C07D263/44 ,  C07D277/34 ,  C07D413/04 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  A61K31/421 ,  A61K31/422 ,  A61K31/426 ,  A61K31/427 ,  A61P3/10

CPC分类号： C07D263/44 ,  C07D233/74 ,  C07D271/07 ,  C07D277/34 ,  C07D413/04 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12

摘要： Bicyclic compounds containing a phenyl or pyridyl ring fused to a cycloalkyl or heterocyclic ring, to which is attached a 5-membered heterocyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

公开(公告)号：EP2079467A2

公开(公告)日：2009-07-22

申请号：EP07839789.0

申请日：2007-10-26

申请人： Merck & Co., Inc.

发明人： GE, Min ,  LIN, Songnian ,  WALSH, Shawn P. ,  YANG, Lihu ,  ZHOU, Changyou

IPC分类号： A61K31/426 ,  A61K31/421 ,  C07D339/02 ,  C07D277/14

CPC分类号： C07D333/60 ,  C07C59/72 ,  C07C59/90 ,  C07C235/46 ,  C07C255/54 ,  C07C2602/08 ,  C07C2602/10 ,  C07D207/34 ,  C07D209/34 ,  C07D209/46 ,  C07D213/61 ,  C07D215/233 ,  C07D217/24 ,  C07D307/80 ,  C07D311/58 ,  C07D333/48 ,  C07D405/12 ,  C07D487/04

摘要： Diaryl ethers in which one of the aryl groups is a phenyl fused to a cycloalkyl or heterocyclic ring, to which is attached an acetic acid group, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that often accompany this disease, including insulin resistance, obesity and lipid disorders.

摘要翻译： 其中一个芳基为与环烷基或杂环稠合的苯基的二芳基醚是G蛋白偶联受体40（GPR40）的激动剂，并且可用作治疗化合物，特别是 2型糖尿病的治疗以及常伴有这种疾病的病症，包括胰岛素抵抗，肥胖和脂质紊乱。

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：EP1846379A1

公开(公告)日：2007-10-24

申请号：EP06719898.6

申请日：2006-01-30

申请人： Merck & Co., Inc.

发明人： GE, Min ,  YANG, Lihu ,  ZHOU, Changyou ,  LIN, Songnian ,  TANG, Haifeng ,  CLINE, Eric, Dean ,  MALKANI, Sunita

IPC分类号： C07D263/44 ,  C07D277/34 ,  C07D413/04 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  A61K31/421 ,  A61K31/422 ,  A61K31/426 ,  A61K31/427 ,  A61P3/10

CPC分类号： C07D263/44 ,  C07D233/74 ,  C07D271/07 ,  C07D277/34 ,  C07D413/04 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12

摘要： Bicyclic compounds containing a phenyl or pyridyl ring fused to a cycloalkyl or heterocyclic ring, to which is attached a 5-membered heterocyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

公开(公告)号：EP1732552A2

公开(公告)日：2006-12-20

申请号：EP05711338.3

申请日：2005-01-14

申请人： Merck & Co., Inc.

发明人： YANG, Lihu ,  MILLS, Sander, G. ,  ZHOU, Changyou ,  GOBLE, Stephen, D. ,  PASTERNAK, Alexander

IPC分类号： A61K31/454

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.

公开(公告)号：EP1558243A2

公开(公告)日：2005-08-03

申请号：EP03777911.3

申请日：2003-10-24

申请人： Merck & Co., Inc.

发明人： BUTORA, Gabor ,  MILLS, Sander, G. ,  PASTERNAK, Alexander ,  SHANKARAN, Kothandaraman ,  YANG, Lihu ,  ZHOU, Changyou ,  GOBLE, Stephen, D.

IPC分类号： A61K31/351 ,  C07D257/04 ,  C07D263/48 ,  C07D309/14 ,  C07D491/02

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.

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：EP1753740A2

公开(公告)日：2007-02-21

申请号：EP05785401.0

申请日：2005-05-20

申请人： Merck & Co., Inc.

发明人： YANG, Lihu ,  LIN, Songnian ,  MORRIELLO, Gregori ,  GUO, Liangqin ,  ZHOU, Changyou

IPC分类号： C07D401/04 ,  C07D221/20 ,  C07D209/02 ,  C07D235/04 ,  A61K31/44 ,  A61K31/4523 ,  A61K31/438 ,  A61K31/415

CPC分类号： C07D211/14 ,  C07D211/18 ,  C07D211/52 ,  C07D211/64 ,  C07D221/20 ,  C07D295/155 ,  C07D309/14 ,  C07D401/10 ,  C07D405/12 ,  C07D471/04

摘要： Compounds of the formulae (I) and (II): (wherein Q, X, E, G1, G2, R2, R3, R4, R5, R6 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：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。

公开(公告)号：EP1606280A2

公开(公告)日：2005-12-21

申请号：EP04720505.9

申请日：2004-03-12

申请人： Merck & Co. Inc.

发明人： GOBLE, Stephen, D. ,  PASTERNAK, Alexander ,  MILLS, Sander, G. ,  ZHOU, Changyou ,  YANG, Lihu

IPC分类号： C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14

CPC分类号： C07D413/12 ,  C07D405/12 ,  C07D417/12 ,  C07D471/04

摘要： The present invention is directed to compounds of the formula (I) 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（I）化合物，其中A，B，D，X，Y，n，R1，R3，R4，R5，R15，R16，R17，R18和虚线如本文所定义， 可用作趋化因子受体活性的调节剂。 特别是，这些化合物可用作趋化因子受体CCR-2的调节剂。