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公开(公告)号：EP0828488B1
公开(公告)日：2003-02-12
申请号：EP96913177.0
申请日：1996-04-26
发明人： BOLTON, Gary, Louis , DOMAGALA, John, Michael , ELSLAGER, Edward, Faith , GOGLIOTTI, Rocco, Dean , PURCHASE, Terri, Stoeber , SANCHEZ, Joseph, Peter , TRIVEDI, Bharat, Kalidas
IPC分类号： A61K31/425 , A61K31/435 , A61K31/505 , C07D275/06 , C07D513/04 , C07D417/04 , C07D513/14
CPC分类号： C07D275/04 , C07D513/04 , C07D513/14
摘要： Isothiazolones having general structure (I) where A is a monocyclic or bicyclic ring which may contain up to 3 heteroatoms selected from O, S, and N; R?1 and R2¿ are substituent groups such as alkyl, alkoxy, hydroxy, nitro, cyano, amino, and carboxy; and R5 is alkyl, cycloalkyl, phenyl, and Het. The isothiazolones are useful as anti-retroviral agents, anti-inflammatory agents, and anti-atherosclerotic agents.
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公开(公告)号：EP0927167A1
公开(公告)日：1999-07-07
申请号：EP97938148.0
申请日：1997-08-06
发明人： CONNOR, David, Thomas , GLASE, Shelly, Ann , PURCHASE, Terri, Stoeber , ROTH, Bruce, David , TRIVEDI, Bharat, Kalidas
CPC分类号： C07D235/02 , C07D235/18
摘要： Benzimidazole derivatives of formula (I) or a pharmaceutically acceptable salt thereof are MCP-1 antagonists and are thus useful in the treatment of inflammation, artherosclerosis, restenosis, and immune disorders such as arthritis and transplant rejection wherein A is N or CH; where W, X, Y and Z can be independently C-R2, C-R3, C-R4, C-R5, or N; no more than two of W, X, Y and Z can be N in any one structure, R2, R3, R4 and R5 can be independently H, C1-20 alkyl, halogen, nitro, -SO2NR8R9, alkoxy of from 1-4 carbon atoms; -S(O)pR where p is an integer from 0 to 2; -(CH2)mOR, -(CH2)mCOOR, -(CH2)mNR8R9, -(CH2)mCONR8R9, -(CH2)mCOR, or -CF3; m is an integer of from 0 to 4, R is hydrogen, lower alkyl of from 1-4 carbon atoms, aryl of from 6-10 carbon atoms, or benzyl; R1 can be H, lower alkyl of from 1-4 carbon atoms, or -(CH2)m-Ph; R6 is alkyl of from 1-6 carbon atoms or R7; R7 is (CH2)nNR10R11; n is an integer from 2 to 6; R8 and R9 can be independently hydrogen, lower alkyl of from 1-4 carbon atoms, or can be taken together to form a ring of from 3-8 atoms having up to one additional heteroatom as O, S, SO2, or N-R12; R10 and R11 can independently be lower alkyl, -(CH2)mPh, unsubstituted or substituted with up to three R2 substituents, or R10 and R11 can be taken together to form a ring of from 3-8 atoms which may contain oxygen or NR12; R12 is hydrogen, lower alkyl, -(CH2)tPh, where Ph is phenyl unsubstituted or substituted with up to three R2 substituents; t is an integer of from 0 to 2.
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3.发明公开
公开(公告)号：EP1192144A1
公开(公告)日：2002-04-03
申请号：EP00939472.7
申请日：2000-05-31
IPC分类号： C07D277/36 , C07D417/06 , C07D417/10 , C07D417/14 , A61K31/426 , A61K31/427 , A61K51/04 , A61P25/28
CPC分类号： C07D417/14 , A61K51/0453 , A61K51/0455 , A61K51/0459 , C07D277/20 , C07D417/06 , C07D417/10
摘要： The present invention provides a method of treating Alzheimer's disease using a compound of Formula (I). Also provided is a method of inhibiting the aggregation of amyloid proteins using a compound of Formula (I) and a method of imaging amyloid deposits using substituted rhodanine derivatives.
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公开(公告)号：EP0828488A1
公开(公告)日：1998-03-18
申请号：EP96913177.0
申请日：1996-04-26
发明人： BOLTON, Gary, Louis , DOMAGALA, John, Michael , ELSLAGER, Edward, Faith , GOGLIOTTI, Rocco, Dean , PURCHASE, Terri, Stoeber , SANCHEZ, Joseph, Peter , TRIVEDI, Bharat, Kalidas
CPC分类号： C07D275/04 , C07D513/04 , C07D513/14
摘要： Isothiazolones having general structure (I) where A is a monocyclic or bicyclic ring which may contain up to 3 heteroatoms selected from O, S, and N; R?1 and R2¿ are substituent groups such as alkyl, alkoxy, hydroxy, nitro, cyano, amino, and carboxy; and R5 is alkyl, cycloalkyl, phenyl, and Het. The isothiazolones are useful as anti-retroviral agents, anti-inflammatory agents, and anti-atherosclerotic agents.
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