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公开(公告)号：EP2044068A1
公开(公告)日：2009-04-08
申请号：EP07796862.6
申请日：2007-07-13
申请人： Merck & Co., Inc.
发明人： WILLIAMS, Peter, D. , VENKATRAMAN, Shankar , LANGFORD, H. Marie , KIM, Boyoung , BOOTH, Theresa, M. , GROBLER, Jay, A. , STAAS, Donnette , RUZEK, Rowena, D. , EMBREY, Mark, W. , WISCOUNT, Catherine, M. , LYLE, Terry, A.
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： 1-Hydroxy naphthyridine compounds (e.g., 1-hydroxy naphthyridin-2(1H)-one compounds of Formula I are inhibitors of HIV integrase and/or HIV RNase H and inhibitors of HIV replication: (I) wherein X and R1-R6 are as defined herein. The compounds are useful in the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other anti-HIV agents such as HIV antivirals, immunomodulators, antibiotics and vaccines.
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2.发明公开TRIAZOLO-PYRIDAZINE COMPOUNDS AND DERIVATIVES THEREOF USEFUL IN THE TREATMENT OF NEUROPATHIC PAIN 审中-公开三唑并哒嗪化合物及其衍生物，疼痛神经病的治疗
公开(公告)号：EP1677799A1
公开(公告)日：2006-07-12
申请号：EP04795608.1
申请日：2004-10-15
申请人： Merck & Co., Inc.
发明人： LEBSACK, Alec D. , MUNOZ, Benito , PRACITTO, Richard , VENKATRAMAN, Shankar , WANG, Bowei , GUNZNER, Janet
IPC分类号： A61K31/5025 , C07D237/32 , C07D237/34 , C07D487/04
CPC分类号： C04B35/632 , C07D401/12 , C07D401/14 , C07D413/14 , C07D471/04 , C07D487/04
摘要： The present invention is directed to a method of use of triazolo-pyridazine compounds in the treatment of neuropathic pain. The present invention is also directed to the use of triazolo-pyridazine compounds in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, bipolar disorders, and panic, as well as in the treatment of pain, Parkinson’s disease, cognitive dysfunction, epilepsy, circadian rhythm and sleep disorders - such as shift-work induced sleep disorder and jet-lag, drug addiction, drug abuse, drug withdrawal and other diseases. The present invention is also directed to novel triazolo-pyridazine compounds that selectively bind to α2δ-1 subunit of Ca channels.
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公开(公告)号：EP1781686B1
公开(公告)日：2009-05-06
申请号：EP05808535.8
申请日：2005-08-12
申请人： Merck & Co., Inc.
CPC分类号： C07K5/06139 , C07K5/06191
摘要： Compounds of Formula (I) are antagonists of VLA-4, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of inflammatory bowel disease including ulcerative colitis and Crohn's disease, multiple sclerosis, asthma, and rheumatoid arthritis.
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公开(公告)号：EP1781686A2
公开(公告)日：2007-05-09
申请号：EP05808535.8
申请日：2005-08-12
申请人： Merck & Co., Inc.
CPC分类号： C07K5/06139 , C07K5/06191
摘要： Compounds of Formula (I) are antagonists of VLA-4, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of inflammatory bowel disease including ulcerative colitis and Crohn’s disease, multiple sclerosis, asthma, and rheumatoid arthritis.
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5.发明公开PYRIDIN-4-YLAMINE COMPOUNDS USEFUL IN THE TREATMENT OF NEUROPATHIC PAIN 审中-公开疼痛神经病SUITABLE吡啶-4- YLAMINVERBINDUNGEN的治疗
公开(公告)号：EP1687275A1
公开(公告)日：2006-08-09
申请号：EP04811391.4
申请日：2004-11-18
申请人： Merck & Co., Inc.
发明人： LIM, Jongwon , BOUERES, Julia, K. , MUNOZ, Benito , PRACITTO, Richard , STOCK, Nicholas , VENKATRAMAN, Shankar
IPC分类号： C07D215/00 , C07D219/00 , A61K31/435 , A61K31/47
CPC分类号： C07D219/12 , C07D215/46
摘要： The present invention is directed to a method of use of triazolo-pyridazine compounds in the treatment of neuropathic pain. The present invention is also directed to the use of triazolo-pyridazine compounds in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, bipolar disorders, and panic, as well as in the treatment of pain, Parkinson’s disease, cognitive dysfunction, epilepsy, circadian rhythm and sleep disorders - such as shift-work induced sleep disorder and jet-lag, drug addiction, drug abuse, drug withdrawal and other diseases. The present invention is also directed to novel triazolo-pyridazine compounds that selectively bind to α2δ-1 subunit of Ca channels.
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