摘要 |
<p>A compound which is a biphenyl derivative of formula (I), or a pharmaceutically acceptable salt thereof wherein: R<SUB>1</SUB> is a C<SUB>1</SUB>-C<SUB>6</SUB> alkyl group or a moiety -A<SUB>1</SUB>, -L<SUB>1</SUB>-A<SUB>1</SUB>, -A<SUB>1</SUB>-A<SUB>1</SUB>', -L<SUB>1</SUB>-A<SUB>1</SUB>-A<SUB>1</SUB>', -A<SUB>1</SUB>-L<SUB>1</SUB>-A<SUB>1</SUB>', -A<SUB>1</SUB>-Y<SUB>1</SUB>-A<SUB>1</SUB>', -A<SUB>1</SUB>-Het<SUB>1</SUB>-A<SUB>1</SUB>', -L<SUB>1</SUB>-A<SUB>1</SUB>-Y<SUB>1</SUB>-A<SUB>1</SUB>', -L<SUB>1</SUB>-A<SUB>1</SUB>-Het<SUB>1</SUB>-A<SUB>1</SUB>', -L<SUB>1</SUB>-Het<SUB>1</SUB>-A<SUB>1</SUB>, -L<SUB>1</SUB>-Y<SUB>1</SUB>-A<SUB>1</SUB>, -L<SUB>1</SUB>-Y<SUB>1</SUB>-Het<SUB>1</SUB>-A<SUB>1</SUB>, -L<SUB>1</SUB>-Het<SUB>1</SUB>-Y<SUB>1</SUB>-A<SUB>1</SUB>, -L<SUB>1</SUB>-Y<SUB>1</SUB>-Het<SUB>1</SUB>-L<SUB>1</SUB>', -A<SUB>1</SUB>-Y<SUB>1</SUB>-Het<SUB>1</SUB>-A<SUB>1</SUB>', -A<SUB>1</SUB>-Het<SUB>1</SUB>-Y<SUB>1</SUB>-A<SUB>1</SUB>', -A<SUB>1</SUB>-Het<SUB>1</SUB>-L<SUB>1</SUB>-A<SUB>1</SUB>', -A<SUB>1</SUB>-L<SUB>1</SUB>-Het<SUB>1</SUB>-A<SUB>1</SUB>' or -L<SUB>1</SUB>-Het<SUB>1</SUB>-L<SUB>1</SUB>'; - A and B are the same or different and each represent a direct bond or a -CO- NR'-, -NR'-CO-, -NR'-CO<SUB>2</SUB>-, -CO-, -NR'-CO-NR''-, -NR'-S(O)<SUB>2</SUB>-, -S(O)<SUB>2</SUB>-NR'-, -SO<SUB>2</SUB>-, -NR'-, -NR'-CO-CO-, -CO-O-, -O-CO-, -(C<SUB>1</SUB>-C<SUB>2</SUB> alkylene)-NR'- or -(C<SUB>1</SUB>-C<SUB>2</SUB> hydroxyalkylene)-NR' - moiety, wherein R' and R'' are the same or different and each represent hydrogen or C<SUB>1</SUB>-C<SUB>4</SUB> alkyl; - R<SUB>2</SUB> and R<SUB>3</SUB> are the same or different and each represent C<SUB>1</SUB>-C<SUB>4</SUB> alkyl, C<SUB>1</SUB>-C<SUB>4</SUB> alkoxy, C<SUB>1</SUB>-C<SUB>4</SUB> haloalkyl, C<SUB>1</SUB>-C<SUB>4</SUB> haloalkoxy or halogen; n and m are the same or different and each represent 0 or 1 ; R<SUB>4</SUB> is a C<SUB>1</SUB>-C<SUB>6</SUB> alkyl group or a moiety -A<SUB>4</SUB>, -L<SUB>4</SUB>-A<SUB>4</SUB>, -A<SUB>4</SUB>-A<SUB>4</SUB>', -L<SUB>4</SUB>-A<SUB>4</SUB>-A<SUB>4</SUB>' , -A<SUB>4</SUB>-L<SUB>4</SUB>-A<SUB>4</SUB>', -A<SUB>4</SUB>-Y<SUB>4</SUB>-A<SUB>4</SUB>', -A<SUB>4</SUB>-Het<SUB>4</SUB>-A<SUB>4</SUB>', -L<SUB>4</SUB>-A<SUB>4</SUB>-Y<SUB>4</SUB>-A<SUB>4</SUB>', -L<SUB>4</SUB>-A<SUB>4</SUB>-Het<SUB>4</SUB>-A<SUB>4</SUB>', -L<SUB>4</SUB>-Het<SUB>4</SUB>-A<SUB>4</SUB>, -L<SUB>4</SUB>-Y<SUB>4</SUB>-A<SUB>4</SUB>, -L<SUB>4</SUB>-Y<SUB>4</SUB>-Het<SUB>4</SUB>-A<SUB>4</SUB>, -L<SUB>4</SUB>-Het<SUB>4</SUB>-Y<SUB>4</SUB>-A<SUB>4</SUB>, -L<SUB>4</SUB>-Y<SUB>4</SUB>-Het<SUB>4</SUB>-L<SUB>4</SUB>', -A<SUB>4</SUB>-Y<SUB>4</SUB>-Het<SUB>4</SUB>-A<SUB>4</SUB>', -A<SUB>4</SUB>-Het<SUB>4</SUB>-Y<SUB>4</SUB>-A<SUB>4</SUB>', -A<SUB>4</SUB>-Het<SUB>4</SUB>-L<SUB>4</SUB>-A<SUB>4</SUB>', -A<SUB>4</SUB>-L<SUB>4</SUB>-Het<SUB>4</SUB>-A<SUB>4</SUB>' or -L<SUB>4</SUB>-Het<SUB>4</SUB>-L<SUB>4</SUB>', each A<SUB>1</SUB>, A<SUB>4</SUB>, A<SUB>1</SUB>' and A<SUB>4</SUB>' are the same or different and represent a phenyl, 5- to 10- membered heteroaryl, 5- to 10- membered heterocyclyl or C<SUB>3</SUB>-C<SUB>8</SUB> carbocyclyl moiety; each L<SUB>1</SUB> and L<SUB>4</SUB> is the same or different and represents a C<SUB>1</SUB>-C<SUB>4</SUB> alkylene or a C<SUB>1</SUB>-C<SUB>4</SUB> hydroxyalkylene group; each Y<SUB>1</SUB> and Y<SUB>4</SUB> is the same or different and represents -CO-, -SO- or -S(O)<SUB>2</SUB>-; each L<SUB>1</SUB>' and L<SUB>4</SUB>' is the same or different and represents hydrogen or a C<SUB>1</SUB>-C<SUB>4</SUB> alkyl group; and each Het<SUB>1</SUB> and Het<SUB>4</SUB> is the same or different and represents -O-, -S- or -NR'-, wherein R' is hydrogen or a C<SUB>1</SUB>-C<SUB>4</SUB> alkyl group, the phenyl, heteroaryl, heterocyclyl and carbocyclyl moieties in R<SUB>1</SUB> and R<SUB>4</SUB> being optionally fused to a phenyl, 5- to 10- membered heteroaryl or 5- to 10- membered heterocyclyl ring; and the phenyl, heteroaryl, heterocyclyl and carbocyclyl moieties in R<SUB>1</SUB> and R<SUB>4</SUB> being unsubstituted or substituted by (a) a single unsubstituted substituent selected from -(C<SUB>1</SUB>-C<SUB>4</SUB> alkyl)-X<SUB>1</SUB>, -CO<SUB>2</SUB>R', -SO<SUB>2</SUB>NR'R'', -S(O)<SUB>2</SUB>-R', -CONR'R'', -NR'-CO-R''', -NR'-S(O)<SUB>2</SUB>-R''', -CO-NR'-(C<SUB>1</SUB>-C<SUB>4</SUB> alkyl)-NR'R'' and -CO-O-(C<SUB>1</SUB>-C<SUB>4</SUB> alkyl)-NR'R'' and/or (b) 1, 2 or 3 unsubstituted substituents selected from -(C<SUB>1</SUB>-C<SUB>4</SUB> alkyl)-X<SUB>2</SUB>, halogen, C<SUB>1</SUB>-C<SUB>4</SUB> alkyl, C<SUB>1</SUB>-C<SUB>4</SUB> alkoxy, C<SUB>1</SUB>-C<SUB>4</SUB> haloalkyl, C<SUB>1</SUB>-C<SUB>4</SUB> haloalkoxy, C<SUB>1</SUB>-C<SUB>4</SUB> hydroxyalkyl, hydroxy, cyano, nitro and -NR'R'', wherein X<SUB>1</SUB> is -CO<SUB>2</SUB>R', -SO<SUB>2</SUB>-R', -NR'-CO<SUB>2</SUB>-R'', -NR'-S(O)<SUB>2</SUB>-R''', -CONR'R'' or -SO<SUB>2</SUB>-NR'R'', each X<SUB>2</SUB> is the same or different and is cyano, nitro or -NR'R'', each R' and R'' is the same or different and represents hydrogen or C<SUB>1</SUB>-C<SUB>4</SUB> alkyl and each R''' is the same or different and represents C<SUB>1</SUB>-C<SUB>4</SUB> alkyl.</p> |
申请人 |
ARROW THERAPEUTICS LIMITED;WHEELHOUSE, CHRISTOPHER, JAMES;THOMAS, ALEXANDER, JAMES, FLOYD;BUSHNELL, DAVID, JOHN;LUMLEY, JAMES;SALTER, JAMES, IAIN;CARTER, MALCOLM, CLIVE;MATHEWS, NEIL;PILKINGTON, CHRISTOPHER, JOHN;ANGELL, RICHARD, MARTYN |
发明人 |
WHEELHOUSE, CHRISTOPHER, JAMES;THOMAS, ALEXANDER, JAMES, FLOYD;BUSHNELL, DAVID, JOHN;LUMLEY, JAMES;SALTER, JAMES, IAIN;CARTER, MALCOLM, CLIVE;MATHEWS, NEIL;PILKINGTON, CHRISTOPHER, JOHN;ANGELL, RICHARD, MARTYN |