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1.发明授权N-(BENZYL)AMINOALKYL CARBOXYLATE, PHOSPHINATES, PHOSPHONATES AND TETRAZOLES AS EDG RECEPTOR AGONISTS 有权“N-（苄基）氨基烷基羧酸盐，膦酸盐，膦酸酯和四唑AS EDG受体激动剂”
公开(公告)号：EP1575964B1
公开(公告)日：2009-11-11
申请号：EP03702110.2
申请日：2003-01-14
申请人： Merck & Co., Inc.
IPC分类号： C07C229/14 , C07C229/20 , C07C229/22 , C07D333/16 , C07F9/30 , C07F9/38 , C07F9/48 , A61K31/16 , A61K31/44 , A61K31/165 , A61K31/17 , A61K31/18 , A61K31/495 , C07D413/04 , C07F9/59 , C07F9/6553 , C07F9/6558 , A61P37/06
CPC分类号： C07D413/04 , C07C229/14 , C07C229/20 , C07C229/22 , C07D333/16 , C07F9/301 , C07F9/307 , C07F9/3808 , C07F9/4816 , C07F9/591 , C07F9/655345 , C07F9/65586
摘要： The present invention encompasses compounds of Formula (I) as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.
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2.发明授权TETRAHYDROPYRANYL CYCLOPENTYL TETRAHYDROPYRIDOPYRIDINE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 有权趋化因子受体活性的四氢环戊TETRAHYDROPYRIDOPYRIDIN调节剂
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
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.
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3.发明公开OCTAHYDROPYRANO[3,4-C]PYRROLE TACHYKININ RECEPTOR ANTAGONISTS 审中-公开OCTAHYDROPYRANO [3,4-c]吡咯的速激肽受体拮抗剂
公开(公告)号：EP1827420A2
公开(公告)日：2007-09-05
申请号：EP05853689.7
申请日：2005-12-12
申请人： Merck & Co., Inc.
IPC分类号： A61K31/401 , C07D491/052
CPC分类号： C07D491/04
摘要： The present invention is directed to certain hydropyranopyrrolidine compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depresssion, and anxiety.
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公开(公告)号：EP1819342A1
公开(公告)日：2007-08-22
申请号：EP05852416.6
申请日：2005-11-29
申请人： Merck & Co., Inc.
IPC分类号： A61K31/535 , C07D207/04 , C07D211/70
CPC分类号： C07D215/20 , C07D215/38 , C07D215/48 , C07D215/60 , C07D453/06
摘要： The present invention is directed to certain quinoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
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5.发明公开3,3-DISUBSTITUTED TETRAHYDROPYRANYL CYCLOPENTYL AMIDE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 审中-公开趋化因子受体活性的3,3-二取代环戊基四氢吡喃酰胺调节剂
公开(公告)号：EP1755603A2
公开(公告)日：2007-02-28
申请号：EP05741852.7
申请日：2005-04-22
申请人： Merck & Co., Inc.
IPC分类号： A61K31/4745
CPC分类号： C07D471/04
摘要： Compounds of Formula I (wherein n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, 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.
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6.发明公开TETRAHYDROPYRANYL CYCLOPENTYL 1-SUBSTITUTED AND 1,1-DISUBSTITUTED TETRAHYDROISOQUINOLINE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 审中-公开四氢环戊基1-取代的和1,1-二取代的四氢趋化因子受体调节剂
公开(公告)号：EP1742919A2
公开(公告)日：2007-01-17
申请号：EP05779916.5
申请日：2005-04-22
申请人： Merck & Co., Inc.
发明人： YANG, Lihu , MILLS, Sander, G. , MORRIELLO, Gregori, J. , GUIADEEN, Deodialsingh , SHANKARAN, Kothandaraman
IPC分类号： C07D217/00 , A61K31/47
CPC分类号： C07D471/04 , C07D405/12
摘要： Compounds of Formula I: I (wherein n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, 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.
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7.发明公开TETRAHYDROPYRANYL CYCLOPENTYL TETRAHY-DROPYRIDOPYRIDINE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 审中-公开趋化因子受体的四氢环戊TETRAHYDROPYRIDOPYRIDIN调节剂
公开(公告)号：EP1742915A2
公开(公告)日：2007-01-17
申请号：EP05784477.1
申请日：2005-04-22
申请人： Merck & Co., Inc.
发明人： YANG, Lihu , MILLS, Sander, G. , JIAO, Richard
IPC分类号： C07D213/02 , C07D217/00 , A61K31/47 , A61K31/4375 , A61K31/44
CPC分类号： C07D309/14 , C07D405/12
摘要： Compounds of Formula I (wherein n, R1, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, 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.
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8.发明公开ALKYLAMINO, ARYLAMINO, AND SULFONAMIDO CYCLOPENTYL AMIDE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 审中-公开氨基亚氨基 - 亚氨基 - 磺酰氨基戊二酰氨基二异氰酸酯四环维生素VEM CHEMOKINREZEPTOREN
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。
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9.发明公开TETRAHYDROPYRANYL CYCLOPENTYL HETEROCYLIC AMIDE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 审中-公开趋化因子受体活性的四氢吡喃环戊基异戊酰胺类调节剂
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.
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。
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10.发明公开N-(BENZYL)AMINOALKYL CARBOXYLATE, PHOSPHINATES, PHOSPHONATES AND TETRAZOLES AS EDG RECEPTOR AGONISTS 有权“N-（BENZYL）AMINOALKYL CARBOXYLATE，PHOSPHINATE，PHOSPHONATE UND TETRAZOLE ALS EDG REZEPTORAGONISON”
公开(公告)号：EP1575964A2
公开(公告)日：2005-09-21
申请号：EP03702110.2
申请日：2003-01-14
申请人： Merck & Co., Inc.
IPC分类号： C07F1/00
CPC分类号： C07D413/04 , C07C229/14 , C07C229/20 , C07C229/22 , C07D333/16 , C07F9/301 , C07F9/307 , C07F9/3808 , C07F9/4816 , C07F9/591 , C07F9/655345 , C07F9/65586
摘要： The present invention encompasses compounds of Formula (I) as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.
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