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公开(公告)号：EP1363897B1
公开(公告)日：2005-12-21
申请号：EP02709746.8
申请日：2002-02-28
发明人： LABORDE, Edgardo , ROBINSON, Louise , MENG, Fanying , PETERSON, Brian, T. , VILLAR, Hugo, O. , ANUSKIEWICZ, Steven, E. , ISHIWATA, Yoshiro , YOKOCHI, Shoji , MATSUMOTO, Yukiharu , KAKIGAMI, Takuji , INAGAKI, Hideaki , JOMORI, Takahito , MATSUSHIMA, Kouji
IPC分类号： C07D319/18 , C07D405/12 , C07D409/12 , C07D407/12 , C07D241/42 , C07D417/12 , C07D401/12 , C07D265/36 , C07D215/48 , A61K31/357 , A61P29/00
CPC分类号： C07D401/12 , C07D215/48 , C07D241/42 , C07D265/36 , C07D319/18 , C07D405/12 , C07D407/12 , C07D409/12 , C07D417/12
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公开(公告)号：EP1358188A2
公开(公告)日：2003-11-05
申请号：EP02707672.8
申请日：2002-01-30
发明人： LABORDE, Edgardo , ROBINSON, Louise , MENG, Fanying , PETERSON, Brian, T. , VILLAR, Hugo, O. , ANUSKIEWICZ, Steven, E. , ISHIWATA, Yoshiro , YOKOCHI, Shoji , MATSUMOTO, Yukiharu , KAKIGAMI, Takuji , INAGAKI, Hideaki , JOMORI, Takahito , MATSUSHIMA, Kouji
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , A61K31/437 , A61K31/496 , A61K31/5377 , A61K31/5513 , A61K45/06 , A61K2300/00
摘要： The present invention relates to chemical compounds of Formula (I) or (II) (wherein Y, Z and R1 - R6 are defined herein), pharmaceutical compositions comprising said compounds, uses of said compounds and compositions, methods of treatment employing said compounds and compositions, and processes for preparing said compounds. Specifically, this invention relates to novel compounds which are antagonists of MCP-1 function and are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases. More specifically, the invention is related to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases.
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公开(公告)号：EP1383757B1
公开(公告)日：2006-09-27
申请号：EP02763877.4
申请日：2002-03-28
发明人： LABORDE, Edgardo , ROBINSON, Louise , MENG, Fanying , PETERSON, Brian, T. , VILLAR, Hugo O. , ANUSKIEWICZ, Steven E. , ISHIWATA, Yoshiro, 1-2 Nagakute Aza-arata , YOKOCHI, Shoji , MATSUMOTO, Yukiharu , KAKIGAMI, Takuji , INAGAKI, Hideaki , JOMORI, Takahito , MATSUSHIMA, Kouji
IPC分类号： C07D317/54 , C07D307/81 , C07D209/14 , C07D249/18 , C07D235/14 , C07D263/14 , C07D413/12 , C07D411/12 , C07D407/12 , A61K31/36 , A61P29/00
CPC分类号： C07D235/06 , C07D209/08 , C07D249/18 , C07D263/56 , C07D307/79 , C07D317/68 , C07D405/12 , C07D407/12 , C07D409/12 , C07D417/12
摘要： The present invention relates to chemical compounds Ia, IIa and IIIa, pharmaceutical compositions comprising said compounds, uses of said compounds and compositions, methods of treatment employing said compounds and compositions, and processes for preparing said compounds. Specifically, this invention relates to novel compounds which are antagonists of Monocyte Chemoattractant Protein-1 (MCP-1) function and are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection. More specifically, the invention is related to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases.
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公开(公告)号：EP1383757A1
公开(公告)日：2004-01-28
申请号：EP02763877.4
申请日：2002-03-28
发明人： LABORDE, Edgardo , ROBINSON, Louise , MENG, Fanying , PETERSON, Brian, T. , VILLAR, Hugo O. , ANUSKIEWICZ, Steven E. , ISHIWATA, Yoshiro,1-2 Nagakute Aza-arata , YOKOCHI, Shoji , MATSUMOTO, Yukiharu , KAKIGAMI, Takuji , INAGAKI, Hideaki , JOMORI, Takahito , MATSUSHIMA, Kouji
IPC分类号： C07D317/54 , C07D307/81 , C07D209/14 , C07D249/18 , C07D235/14 , C07D263/14 , C07D413/12 , C07D411/12 , C07D407/12 , A61K31/36 , A61P29/00
CPC分类号： C07D235/06 , C07D209/08 , C07D249/18 , C07D263/56 , C07D307/79 , C07D317/68 , C07D405/12 , C07D407/12 , C07D409/12 , C07D417/12
摘要： The present invention relates to chemical compounds Ia, IIa and IIIa, pharmaceutical compositions comprising said compounds, uses of said compounds and compositions, methods of treatment employing said compounds and compositions, and processes for preparing said compounds. Specifically, this invention relates to novel compounds which are antagonists of Monocyte Chemoattractant Protein-1 (MCP-1) function and are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection. More specifically, the invention is related to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases.
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公开(公告)号：EP1363897A2
公开(公告)日：2003-11-26
申请号：EP02709746.8
申请日：2002-02-28
发明人： LABORDE, Edgardo , ROBINSON, Louise , MENG, Fanying , PETERSON, Brian, T. , VILLAR, Hugo, O. , ANUSKIEWICZ, Steven, E. , ISHIWATA, Yoshiro , YOKOCHI, Shoji , MATSUMOTO, Yukiharu , KAKIGAMI, Takuji , INAGAKI, Hideaki , JOMORI, Takahito , MATSUSHIMA, Kouji
IPC分类号： C07D319/18 , C07D405/12 , C07D409/12 , C07D407/12 , C07D241/42 , C07D417/12 , C07D401/12 , C07D265/36 , C07D215/48 , A61K31/357 , A61P29/00
CPC分类号： C07D401/12 , C07D215/48 , C07D241/42 , C07D265/36 , C07D319/18 , C07D405/12 , C07D407/12 , C07D409/12 , C07D417/12
摘要： The present invention relates to chemical compounds, pharmaceutical compositions comprising said compounds, uses of said compounds and compositions, methods of treatment employing said compounds and compositions, and processes for preparing said compounds. Specifically, this invention relates to novel compounds which are antagonists of MCP-1 function and are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection. More specifically, the invention is related to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases.
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6.发明公开
公开(公告)号：EP1357913A1
公开(公告)日：2003-11-05
申请号：EP02714858.4
申请日：2002-02-08
申请人： TELIK, INC.
发明人： LABORDE, Edgardo , VILLAR, Hugo, O.
IPC分类号： A61K31/41 , C07D417/04 , C07D409/12 , C07D405/04 , C07D249/12 , C07D271/10 , A61P25/28
CPC分类号： C07D271/113 , A61K31/41 , A61K31/4196 , A61K31/4245 , A61K31/433 , C07D403/04 , C07D409/12 , C07D417/04
摘要： The invention provides compounds, compositions and methods for inhibiting the glycine transporter (2) and for affecting glycine transporter mediated neuronal activity. Useful compounds comprise compounds of Formula I : wherein n is (0, 1, 2 or 3) and R is independently halogen, hydroxy, lower alkyl optionally substituted with halogen or lower alkoxy optionally substituted with halogen; X is O, S or N-R' (wherein R's is lower alkyl, aryl, heteroaryl, aryl-lower alkylene or heteroaryl-lower alkylene); Q may be absent or present, and when present, it is represented by the formula : in which n, R and X are as defined above; when Q is present, W is a lower alkylene and when Q is absent, W is optionally substituted lower alkyl, optionally substituted aryl, optionally substituted heteroaryl (optionally substituted aryl)-X-CH2-or (optionally substituted heteroaryl)-X-CH2-in which X is as defined above; or a pharmaceutically acceptable salt thereof. These compounds are particularly useful for treating diseases of the nerve and muscle, including psychoses, pain, epilepsy, neurodegenerative diseases, stroke, head trauma, multiple sclerosis and the like, and of muscle disorders, including diseases or conditions associated with increased muscle contraction, such as spasticity and myoclonus. In addition, the compounds may be used to discover other agents with improved activity in assays in which the compounds of the invention are active.
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