摘要 |
<p>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)<SUB>2</SUB> or -SO<SUB>2</SUB>OH ; each R<SUP>1</SUP> is the same or different and is halogen, hydroxy, C<SUB>1-6</SUB> alkyl, C<SUB>2-6</SUB> alkenyl, C<SUB>2-6</SUB> alkynyl, C<SUB>1-6</SUB> alkoxy, C<SUB>1-6</SUB> alkylthio, thio, amino, mono(C<SUB>1-6</SUB> alkyl)amino, di(C<SUB>1-6</SUB> alkyl)amino, nitro, cyano or -CO<SUB>2</SUB>R<SUP>/</SUP>, wherein R<SUP>/</SUP> represents hydrogen or C<SUB>1-6</SUB> alkyl; n is 0, 1, 2 or 3; R<SUP>2</SUP> is hydrogen, C<SUB>1-6</SUB> alkyl, C<SUB>2-6</SUB> alkenyl or C<SUB>2-6</SUB> alkynyl; Y is a linking group; and X is C<SUB>1-6</SUB> alkyl, C<SUB>2-6</SUB> alkenyl, C<SUB>2-6</SUB> alkynyl, aryl, heteroaryl, carbocyclyl, heterocyclyl, -M-aryl, -M-heteroaryl, -M-carbocyclyl or -M-heterocyclyl, wherein M is C<SUB>1-6</SUB> alkylene, C<SUB>2-6</SUB> alkenylene, C<SUB>2-6</SUB> alkynylene, -Q-Het-Q'- or -Q-Het- wherein Q and Q' are the same or different and are C<SUB>1-6</SUB> alkylene, C<SUB>2-6</SUB> alkenylene or C<SUB>2-6</SUB> alkynylene and Het is selected from -NR<SUP>/</SUP>-, -O-, -S-, -SO<SUB>2</SUB>-, -SO-, -C(O)-O-, -OC(O), -CO-, -C(O)-NR<SUP>/</SUP>- or -NR<SUP>/</SUP>-C(O)- wherein R<SUP>/</SUP> is as defined above, provided that: when n is 0, Z is -COOH, R<SUP>2</SUP> is hydrogen and Y is -N=N-, X is other than 2-pyridyl.</p> |
申请人 |
UNIVERSITY OF SOUTHAMPTON;PACKHAM, GRAHAM, KEITH;GANESAN, ARASU;MANN, DEREK, A.;OAKLEY, FIONA;NATARAJAN, SRINIVASAN |
发明人 |
PACKHAM, GRAHAM, KEITH;GANESAN, ARASU;MANN, DEREK, A.;OAKLEY, FIONA;NATARAJAN, SRINIVASAN |