Patent ID: 6057314
Filing Date: 2000-05-02
Classification: C07D

Abstract:
A compound of formula (VIII): ##STR270## wherein R.sub.1 is selected from the group consisting of formula VIa to VId: ##STR271## wherein: R.sub.11 is hydrogen or C.sub.1-6 alkyl;K is a bond or a --NH--;G is C.sub.1-4 alkoxy; cyano; --NH.sub.2 ; --CH.sub.2 --NH.sub.2 ; --C(NH)--NH.sub.2 ; --NH--C(NH)--NH.sub.2 ; --C(NH)--C(NH)--NH.sub.2 ; a C.sub.6 cycloalkyl or aryl substituted with cyano, --NH.sub.2, --CH.sub.2, --NH.sub.2, --C(NH)--NH.sub.2, --NH--C(NH)--NH.sub.2 or --CH.sub.2 --NH--C(NH)--NH.sub.2 ; or a 5 or 6 member, saturated or unsaturated heterocycle optionally substituted with cyano, --NH.sub.2 ; --CH.sub.2 --NH.sub.2 ; --C(NH)--NH.sub.2 ; --NH--C(NH)--NH.sub.2 ; or --CH.sub.2 --NH--C--(nh)--NH.sub.2 ;U is cyano, --NH.sub.2 ; --C(NH)--NH.sub.2 or --NH--C--(NH)--NH.sub.2 ;P is a bond, --C(O)--or a bivalent group; ##STR272## J is C.sub.1-6 alkylene optionally substituted with OH, NH.sub.2 or C.sub.1-6 alkyl and optionally interrupted by a heteroatom selected from O, S, and N;n is 0 or 1; andT is selected from the group consisting of H, OH, amino, a peptide chain, C.sub.1-16 alkyl, C.sub.1-16 alkoxy, C.sub.6-20 aralkyl, and a moiety selected from the group consisting of: ##STR273## wherein X.sub.5, X.sub.10, X.sub.11 and X.sub.12 are each independently selected from the group consisting of N, and C--X.sub.7 where X.sub.7 is hydrogen, C.sub.1-4 alkyl, or C.sub.5-8 aryl;X.sub.6 and X.sub.13 are each independently selected from the group consisting of C, O, N, S, N--X.sub.7, and CH--X.sub.7 ;R' is hydrogen, C.sub.1-16 alkyl optionally carboxyl substituted, carboxyl, --C.sub.0-16 alkyl--CO.sub.2 --C.sub.1-16 alkyl, C.sub.6-20 aralkyl, C.sub.3-7 cycloalkyl, aryl, an aromatic, and a 5 to 10 element mono- or bi- cyclic saturated or unsaturated heterocycle group with 1 to 4 heteroatoms selected from the group consisting of N, O and S, optionally mono- or di-substituted with OH, SH, amino, halogen, CF.sub.3, oxo, and C.sub.1-6 alkyl;R.sub.2 is H or C1-6 alkyl;R.sub.3 is selected from H, NR.sub.6 R.sub.7 and C.sub.1-6 alkyl; andR.sub.4 and R.sub.5 are independently selected from H; NR.sub.6 R.sub.7 ; C.sub.6-16 aryl or C.sub.3-7 cycloalkyl optionally substituted with C.sub.1-6 alkyl; C.sub.1-16 alkyl optionally interrupted by one or more heteroatom or carbonyl group and optionally substituted with OH, SH, NR.sub.6 R.sub.7 or a C.sub.6-16 aryl, heterocycle or C.sub.3-7 cycloalkyl group optionally substituted with halogen, hydroxyl, C.sub.1-6 alkyl; an amino acid side chain; and a hydrophobic group selected from the group consisting of C.sub.1-20 alkyl, C.sub.2-20 alkynyl optionally interrupted by a carbonyl group C.sub.6-16 aryl, C.sub.3-7 cycloalkyl, C.sub.6-20 cycloalkyl substituted C.sub.1-20 alkyl, wherein the aliphatic portion is optionally interrupted by a carbonyl group and the ring portion is optionally interrupted by a carbonyl group and the ring portion is optionally substituted with C.sub.1-6 alkyl; and a hydrophobic amino acid side chain.