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公开(公告)号:EP2089416A1
公开(公告)日:2009-08-19
申请号:EP07848705.5
申请日:2007-11-23
CPC分类号: C07K5/0205
摘要: Compounds which are Spiruchostatin analogues of the general formula (I) or (I'), isosteres thereof and pharmaceutically acceptable salts thereof are found to inhibit HDAC wherein R1, R2, R3 and R4 are the same or different and represent an amino acid side chain moiety and each R6 is the same or different and represents hydrogen or C1-C4 alkyl.
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公开(公告)号:EP1888097B1
公开(公告)日:2014-03-05
申请号:EP06744076.8
申请日:2006-06-02
发明人: GANESAN, Arasu , PACKHAM, Graham Keith , YUREK-GEORGE, Alexander , CECIL, Alexander, Richard, Liam
CPC分类号: A61K38/15
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公开(公告)号:EP1888097A1
公开(公告)日:2008-02-20
申请号:EP06744076.8
申请日:2006-06-02
发明人: GANESAN, Arasu , PACKHAM, Graham Keith , YUREK-GEORGE, Alexander , CECIL, Alexander, Richard, Liam
CPC分类号: A61K38/15
摘要: Compounds which are FK228 analogues of the general formula (I) or (I/), isosteres thereof and pharmaceutically acceptable salts thereof are found to inhibit HDAC wherein R1, R2, R3 and R4 are the same or different and represent an amino acid side chain moiety and each R6 is the same or different and represents hydrogen or C1-C4 alkyl.
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5.
公开(公告)号:EP1835900A1
公开(公告)日:2007-09-26
申请号:EP06700183.4
申请日:2006-01-05
发明人: PACKHAM, Graham, Keith , GANESAN, Arasu , MANN, Derek, A. , OAKLEY, Fiona , NATARAJAN, Srinivasan
CPC分类号: A61K31/63 , A61K31/192
摘要: Use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use as a Nuclear Factor-kB (NF-kB) inhibitor formula (I), wherein: A has the following structure; formula (i) Z is -COOH5 -P(O)(OH)2 or -SO2OH ; each R1 is the same or different and is halogen, hydroxy, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, C1-6 alkylthio, thio, amino, mono(C1-6 alkyl)amino, di(C1-6 alkyl)amino, nitro, cyano or -CO2R/, wherein R/ represents hydrogen or C1-6 alkyl; n is 0, 1, 2 or 3; R2 is hydrogen, C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl; Y is a linking group; and X is C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, aryl, heteroaryl, carbocyclyl, heterocyclyl, -M-aryl, -M-heteroaryl, -M-carbocyclyl or -M-heterocyclyl, wherein M is C1-6 alkylene, C2-6 alkenylene, C2-6 alkynylene, -Q-Het-Q'- or -Q-Het- wherein Q and Q' are the same or different and are C1-6 alkylene, C2-6 alkenylene or C2-6 alkynylene and Het is selected from -NR/-, -O-, -S-, -SO2-, -SO-, -C(O)-O-, -OC(O), -CO-, -C(O)-NR/- or -NR/-C(O)- wherein R/ is as defined above, provided that: when n is 0, Z is -COOH, R2 is hydrogen and Y is -N=N-, X is other than 2-pyridyl.
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