| abstract |
A pharmaceutical compound having the formulan nin whichn R 1 is alkyl, -SO 2 R 14 where R 14 is alkyl, optionallynsubstituted aryl or optionally substituted heteroaryl, R 2 is hydrogen, alkyl optionally substituted with one ornmore hydroxy or C 1-4 alkoxy groups, optionally substitutednaryl, optionally substituted heteroaryl, -OR 15 , -P(O)(OR 15 )(OR 16 ) or -NR 15 R 16 where R 15 and R 16 are eachnhydrogen or alkyl, or -SO 2 R 17 where R 17 is hydrogen, alkyl,noptionally substituted aryl or optionally substitutednheteroaryl, R 3 is hydrogen, -CN, -CO 2 R 18 , -CONR 18 R 19 ,-CH 18 ≡CHR 19 , -C≡CR 18 ,n-OCH 2 CO.R 18 , -SO 2 R 18 , -CH 2 OR 18 , -CH 2 OCO.R 18 , -CH 2 NHCOR 18 ,n-CH 2 N(COR 18 ) 2 , -CHO, -OR 18 , -CH 2 NR 18 R 19 , -CH 2 OR 18 , -CH=NR 18 orn-CH=N-OR 18 , where R 18 and R 19 are each hydrogen or alkyl, X is a bond or -SO 2 -, R 4 , R 5 , R 6 , R 8 , R 9 and R 10 are each hydrogen or alkyl, n is 1 to 4, A is -CH 2 - or -YCO- where Y is a bond, -O-, optionallynsubstituted phenylene, -CH=CH-, or -NR 20 - where R 20 isnhydrogen or alkyl, R 7 is the C-α substituent of an amino acid or an esternthereof, or R 6 and R 7 together form a C 3-5 alkylene chainnoptionally substituted by C 1-4 alkyl or hydroxyl, or angroup of the formula -CH 2 -Z-CH 2 - where Z is -CO-, -S-, -SO-nor -SO 2 -, or R 7 and R 8 together form a C 3 to C 5 alkylene chainnoptionally substituted by C 1-4 alkyl or hydroxyl, B is -CON(R 21 )-, -CON(R 21 )N(R 22 )- orn nwhere -x=y- is -C(R 22 )=N-, -N=C(R 22 )- or -N=N-, where R 21 is hydrogen, alkyl orn-NR 23 R 24 where R 23 and R 24 are each hydrogen or alkyl, andnwhere R 22 is hydrogen or alkyl, or R 8 and R 21 together formna C 2-4 alkylene chain, m is 0 to 2, R 11 is hydrogen or alkyl, R 12 is hydrogen, alkyl, optionally substituted aryl,noptionally substituted heteroaryl, -CN, -OH, -CO 2 R 25 , n-CONR 25 R 26 , where R 25 and R 26 are each hydrogen or alkyl,nand R 13 is alkyl, optionally substituted aryl or optionallynsubstituted heteroaryl, or R 12 and R 13 together form a C 3-8 ncycloalkyl group or C 3-8 cycloalkyl fused to optionallynsubstituted phenyl; nor a salt or ester thereof. |