Patent ID: 6110896
Filing Date: 2000-08-29
Classification: A61K,A61P,C07K,Y10S

Abstract:
A compound of the formula (I): ##STR16## wherein: R.sup.1 is a C.sub.1-6 alkyl, C.sub.2-6 alkenyl, (C.sub.1-6 alkyl) aryl, aryl, (C.sub.1-6 alkyl) heteroaryl, heteroaryl or C.sub.1-6 alkyl AR.sup.9 group where A is O, NR.sup.9 or S(O).sub.m where m=0-2, and R.sup.9 is H, C.sub.1-4 alkyl, aryl, heteroaryl, C.sub.1-4 alkyl-aryl or C.sub.1-4 alkyl-heteroaryl; if A=NR.sup.9 the R.sup.9 groups may be the same or different;R.sup.2 is hydrogen or C.sub.1-6 alkyl;R.sup.3 is a (Alk).sub.n R.sup.6 group where Alk is a C.sub.1-6 alkyl or C.sub.2-6 alkenyl group and n is zero or 1;X is a group NR.sup.4 R.sup.5 where R.sup.4 is hydrogen, aryl, heteroaryl, C.sub.1-6 alkyl-heteroaryl, cyclo(C.sub.3-6)alkyl, C.sub.1-6 alkyl-cyclo(C.sub.3-6)alkyl, heterocyclo(C.sub.3-6)alkyl or C.sub.1-6 alkyl-heterocyclo(C.sub.3-6)alkyl, or the group C.sub.1-6 alkyl optionally substituted by amino (NH.sub.2), aryl, arylamino, protected amino, di (C.sub.1-6 alkyl) amino, mono (C.sub.1-6 alkyl) amino, CO.sub.2 H, protected carboxyl, carbamoyl, mono (C.sub.1-6 alkyl) carbamoyl, di (C.sub.1-6 alkyl) carbamoyl, and R.sup.5 is hydrogen or a C.sub.1-6 alkyl group; or NR.sup.4 R.sup.5 forms a ring;R.sup.7 is hydrogen or the group R.sup.10 CO where R.sup.10 is a group C.sub.1-4 alkyl, C.sub.1-4 alkyl-aryl, C.sub.1-4 alkyl-heteroaryl, cyclo (C.sub.3-6 ) alkyl, C.sub.1-4 alkyl-cyclo (C.sub.3-6) alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkenyl-aryl, aryl or heteroaryl;R.sup.14 is OH, NH.sub.2, OR.sup.8, NHR.sup.8 or R.sup.8 ;R.sup.8 is aryl (optionally substituted with R.sup.11), heteroaryl (optionally substituted with R.sup.11), C.sub.1-4 alkyl substituted with R.sup.11, C.sub.1-4 alkyl-aryl (optionally substituted with R.sup.11), C.sub.1-4 alkyl-heteroaryl (optionally substituted with R.sup.11), cyclo (C.sub.3-6) alkyl (optionally substituted with R.sup.11), cyclo (C.sub.3-6) alkenyl (optionally substituted with R.sup.11), C.sub.1-4 alkyl-cyclo (C.sub.3-6) alkyl (optionally substituted with R.sup.11), the groups: ##STR17## where p=1-2, or the group: ##STR18## where B and C may be selected from the groups O,S,C(R.sup.9).sub.2, or NR.sup.9 and these may be the same or different;R.sup.6 is an optionally substituted cyclo(C.sub.3-6)alkyl, cyclo(C.sub.3-6) alkenyl, C.sub.1-6 alkyl, aryl, C.sub.1-6 alkoxyaryl, benzyloxyaryl, heteroaryl, COR.sup.9, C.sub.1-3 alkyl-aryl, C.sub.1-3 alkyl-heteroaryl, alkyl-CO.sub.2 R.sup.9, C.sub.1-6 alkyl-NHR.sup.9, AR.sup.9, CO.sub.2 R.sup.9, CONHR.sup.10, NHCOR.sup.10, NHCO.sub.2 R.sup.10 or NHSO.sub.2 R.sup.10 group, an amidine or guanidine group;R.sup.11 is SR.sup.7, COR.sup.13, SO.sub.2 R.sup.9 (when R.sup.9 is not H), SO.sub.2 N(R.sup.9).sub.2, N(R.sup.9).sub.2, NR.sup.9 R.sup.12, OR.sup.9, COR.sup.9, phthalimido or succinimido;R.sup.12 is hydrogen, COR.sup.9, CO.sub.2 R.sup.9, CONHR.sup.9 or SO.sub.2 R.sup.9 (where R.sup.9 is not H); andR.sup.13 is OH, OC.sub.1-4 alkyl, O(C.sub.1-4 alkyl)-aryl or N(R.sup.9).sub.2 (in which R.sup.9 is the same or different);and the salts, solvates and hydrates thereof.