Patent ID: 6017768
Filing Date: 2000-01-25
Classification: A61P,C07B,C07C,C07D,C12Q,C40B,G01N

Abstract:
A combinatorial chemical library comprising a plurality of members of the formula: ##STR190## wherein: ##STR191## is a solid support; --L' is a linker; and--II' is a compound residue of the formula: ##STR192## wherein: R.sup.1a is --CH.sub.2 --O--, --CH.sub.2 --CH.sub.2 --O--, --C(.dbd.O)--CH.sub.2 --O--, --C(.dbd.O)--, or when L' terminates in N(CH.sub.2).sub.1-6 R.sup.17, R.sup.1a may additionally be --C(.dbd.O)--Z--O-- or --C(.dbd.O)-4-Phe--CH.sub.2 --O--;R.sup.2 is H or lower alkyl;R.sup.3 is H, alkyl, aryl or arylalkyl;R.sup.4 and R.sup.5 are each independently H, lower alkyl, or substituted lower alkyl where the substituents are 1-3 alkoxy, aryl, substituted aryl, carboalkoxy, carboxamido, diloweralkylamido, or ##STR193## or R.sup.4 and R.sup.5 taken together are --(CH.sub.2).sub.n --, --(CH.sub.2).sub.2 --O--(CH.sub.2).sub.2 --, --CH.sub.2 --O--(CH.sub.2).sub.3 --, --(CH.sub.2).sub.2 --NR.sup.8 --CH.sub.2).sub.2 --, --CH.sub.2 --NR.sup.8 --(CH.sub.2).sub.m --, --(CH.sub.2).sub.2 XH(NHR.sup.8)(CH.sub.2).sub.2 --, --(CH.sub.2).sub.2 --S(O).sub.0-2 (CH.sub.2).sub.2 --, or ##STR194## one of R.sup.6 and R.sup.7 is H and the other is H, OH, or N(CH.sub.2).sub.1-6 R.sup.14 R.sup.15, or R.sup.6 and R.sup.7 taken together are ##STR195## R.sup.8 is H, COOR.sup.9, CONHR.sup.10, CSNHR.sup.11, COR.sup.12, SO.sub.2 R.sup.13, lower alkyl,aryl lower alkyl, heteroaryl, or heteroaryl lower alkyl, wherein aryl is optionally substituted with 1-3 substituents selected from lower alkyl, lower alkoxy, halo, CN, NH.sub.2, COOH, CONH.sub.2, carboalkoxy, and mono- or di-lower alkylamino and wherein heteroaryl is a mono- or bicyclic heteroaromatic ring system of 5 to 10 members including 1 to 3 heteroatoms selected from O, N, and S and 0-3 substituents selected from halo, amino, cyano, lower alkyl, carboalkoxy, CONH.sub.2, and S-lower alkyl;R.sup.9 is lower alkyl, aryl, aryl lower alkyl, heteroaryl, aryl substituted by 1-3 substituents selected from alkyl, alkenyl, alkoxy, methylene dioxy, and halo, or a 5- to 6-membered heterocyclic ring wherein the hetero atom is O or N, wherein heteroaryl is a heteroaromatic ring of 5 to 6 members including 1 to 2 heteroatoms selected from O, N, and S and 0-2 substituents selected from lower alkyl, dialkylamino, lower alkoxy, and halo;R.sup.10 and R.sup.11 are each independently lower alkyl, aryl, aryl loweralkyl, or aryl substituted by 1-3 substituents selected from lower alkyl, halo, alkoxy and haloalkyl;R.sup.12 is lower alkyl, aryl, heteroaryl, aryl lower alkyl, heteroaryl lower alkyl, a 5- or 6-membered heterocyclic ring containing 1-2 heteroatoms selected from O, S, and N lower alkyl, or aryl substituted with 1-3 substituents selected from lower alkyl, alkoxy, halo, sulfamoyl, lower alkyl sulfamoyl, cyano, and phenyl;R.sup.13 is lower alkyl, aryl or aryl substituted with 1-3 substituents selected from lower alkyl, alkoxy, halo, CN, and haloalkyl;R.sup.14 is H; alkyl; alkyl substituted by 1-3 alkoxy, S-loweralkyl, sulfamoyl, halo, alkylsulphonamido, or arylsulphonamido; alkenyl; alkynyl; aryl; substituted aryl; heteroaryl; substituted heteroaryl; heterocycloalkyl; --CH.sub.2 NR.sup.16 C(O)R.sup.16 ; --C(O)NR.sup.16 R.sup.16 ; --CH.sub.2 OC(O)R.sup.16 ; or --CH.sub.2 SC(O)R.sup.16 ;R.sup.15 is H, alkyl, --C(O)X, --C(S)X, or --C(NCN)NR.sup.3 R.sup.3 ;R.sup.16 is lower alkyl, substituted lower alkyl, aryl, or substituted aryl;R.sup.17 is H, alkyl, alkyl substituted by 1-3 alkoxy, S-loweralkyl, sulfamoyl, halo, alkylsulphonamide, or arylsulphonamido; alkenyl; alkynyl; aryl; substituted aryl; heteroaryl; substituted heteroaryl; heterocycloalkyl; substituted heterocycloalkyl; diphenylmethyl; --CH.sub.2 NR.sup.16 C(O)R.sup.16 ; --C(O)NR.sup.16 ; R.sup.16 --CH.sub.2 OC(O)R.sup.16, or --CH.sub.2 SC(O)R.sup.16 ;X is alkyl, aryl, arylalkyl, O-loweralkyl, or --NR.sup.3 R.sup.3 ;Z is --(CH.sub.2).sub.1-6 -, optionally substituted with 1-3 lower alkyl; --CHR.sup.2 --; --Phe--CH.sub.2 --, where Phe is optionally mono-substituted with halogen, lower alkyl, or alkoxy; or heteroarylene-(CH.sub.2)--;m is 2or 3; andn is 4-9.