abstract |
1. The compound of formula I:! ! where R1 is H, R4, haloalkyl, CHN2, CH2Cl, CH2F, —CH2OPO (R4) 2, —CH2OPO (OR4) 2, or —C1-2 alkyl-R3R4; ! R2 is a P4-P3-P2, P3-P2 or P2 fragment of a caspase inhibitor; ! R3 is —O—, —NH—, —NR4—, —S— or —O (C = O) -; ! R4 is a C1-12 aliphatic radical, C6-10 aryl, (5-10) membered heterocyclyl, (5-10) membered heteroaryl, C3-10 cycloaliphatic radical, - (C1-6 alkyl) -C6-10 aryl, - ( C1-6alkyl) - ((5-10) membered heteroaryl), - (C1-6alkyl) - ((5-10) membered heterocyclyl) or - (C1-6alkyl) C3-10cycloaliphatic; wherein said R4 group is optionally substituted with 0-5 groups J and 0-2 groups J2; ! or two R4 groups together with the atom to which they are attached form a (3-8) membered monocyclic or (8-12) membered bicyclic ring optionally substituted with 0-5 groups J and 0-2 groups J2; ! J represents halogen, -OR ', -NO2, -CN, -CF3, -OCF3, -R', 1,2-methylenedioxy, 1,2-ethylenedioxy, -N (R ') 2, -SR', - SOR ', -SO2R', -SO2N (R ') 2, -SO3R', -C (O) R ', -C (O) C (O) R', -C (O) C (O) OR ' , -C (O) C (O) N (R ') 2, -C (O) CH2C (O) R', -C (S) R ', -C (S) OR', -C (O) OR ', -OC (O) R', -C (O) N (R ') 2, -OC (O) N (R') 2, -C (S) N (R ') 2, - (CH2 ) 0-2NHC (O) R ', -N (R') N (R ') COR', -N (R ') N (R') C (O) OR ', -N (R') N ( R ') CON (R') 2, -N (R ') SO2R', -N (R ') SO2N (R') 2, -N (R ') C (O) OR', -N (R ' ) C (O) R ', -N (R') C (S) R ', -N (R') C (O) N (R ') 2, -N (R') C (S) N ( R ') 2, -N (COR') COR ', -N (OR') R ', -CN, -C (= NR') N (R ') 2, -C (O) N (OR') R ', -C (= NOR') R ', -OP (O) (OR') 2, -P (O) (R ') 2, -P (O) (OR') 2 or -P (O ) (H) (OR '); ! J2 represents = NR ', = N (OR'), = O or = S; ! R 'represents H, C1-12 aliphatic radical, C6-10 aryl, (5-10) membered heterocyclyl, (5-10) membered heteroaryl, C3-10 cycloaliphatic radical, - (C1-6 alkyl) -C6-10 aryl , - (C1-6alkyl) - ((5-10) membered heteroaryl), - (C1-6alkyl) - ((5-10) membered heterocyclyl) or - (C1-6alkyl) C3-10cycloaliphatic; ! each R 'is independently and optionally substituted with 0-5 substituents selected from H, C1-6 alkyl, CF3, halogen, —NO2, OCF3, CN, OH, O (C1-6 alkyl), NH2, N (C1-6 alkyl), N (C1-6alkyl) 2, C (= O) CH3 or C1-6alkyl, optional |