Patent ID: 6103711
Filing Date: 2000-08-15
Classification: A61K,A61P,C07K

Abstract:
A compound represented by the formula: ##STR168## wherein: X.sub.1 is --CH;g is 0 or 1;each J is independently --H, --OH, or --F, provided that when a first and second J are bound to a C and said first J is --OH, said second J is --H;m is 0, 1, or 2;T is --OH, --CO--CO.sub.2 H, --CO.sub.2 H, --CO--CH.sub.2 OH, --CO--NHOH, --SO.sub.2 --NHR, --SO.sub.3 H, --PO(OH)NH.sub.2, --CONHCN, --OSO.sub.3 H, --CO--NHSO.sub.2 R.sub.16, --PO(OH).sub.2, --PO(OH) (OR.sub.16), --PO(OH) (R.sub.16), --OPO(OH).sub.2, --OPO(OH) (OR.sub.16), --OPO(OH) (R.sub.16), --NHPO(OH).sub.2, --NHPO(OH) (OR.sub.16), --NHPO(OH) (R.sub.16), ##STR169## R.sub.15 is --H, a --C.sub.1-6 alkyl group, or the bond linking T to (CJ.sub.2).sub.m ;R.sub.16 is a --C.sub.1-6 alkyl group;R.sub.1 is selected from the group consisting of the following formulae, in which any ring may optionally be singly or multiply substituted at any carbon by Q.sub.1 at any nitrogen by R.sub.5, or at any atom by .dbd.O, --OH, --CO.sub.2 H, or halogen; any saturated ring may optionally be unsaturated at one or two bonds; and wherein R.sub.1 (e) is optionally benzofused; ##STR170## R.sub.3 is: --CN,--CH.dbd.CH--R.sub.9,--CH.dbd.N--O--R.sub.9,--(CH.sub.2).sub.1-3 --T.sub.1 --R.sub.9,--CJ.sub.2 --R.sub.9,--CO--R.sub.13, or ##STR171## each R.sub.4 is independently: --H,--Ar.sub.1,--R.sub.9,--T.sub.1 --R.sub.9, or--(CH.sub.2).sub.1,2,3 --T.sub.1 --R.sub.9 ;each T.sub.1 is independently:CH.dbd.CH--,--O--,--S--,--SO--,--SO.sub.2,--NR.sub.10 --,--NR.sub.10 --CO--,--CO--,--O--CO--,--CO--O--,--CO--NR.sub.10 --,--O--CO--NR.sub.10 --,--NR.sub.10 --CO--O--,--NR.sub.10 --CO--NR.sub.10 --,--SO.sub.2 --NR.sub.10 --,--NR.sub.10 --SO.sub.2 --, or--NR.sub.10 --SO.sub.2 --NR.sub.10 --;each R.sub.5 is independently:--H,--Ar.sub.1,--CO--Ar.sub.1,--SO.sub.2 Ar.sub.1,--CO--NH.sub.2,--SO.sub.2 NH.sub.2,--R.sub.9,--CO--R.sub.9,--CO--O--R.sub.9,--SO.sub.2 --R.sub.9, ##STR172## each R.sub.9 is a C.sub.1-6 straight or branched alkyl group optionally singly or multiply substituted by --OH, --F, or .dbd.O and optionally substituted with one or two Ar.sub.1 groups;each R.sub.10 is independently --H or a C.sub.1-6 straight or branched alkyl group;each R.sub.13 is independently --Ar.sub.2, --R.sub.4 or ##STR173## each Ar.sub.1 is a cyclic group independently selected from an aryl group which contains 6, 10, 12, or 14 carbon atoms and between 1 and 3 rings, a cycloalkyl group which contains between 3 and 15 carbon atoms and between 1 and 3 rings, said cycloalkyl group being optionally benzofused, or a heterocycle group containing between 5 and 15 ring atoms and between 1 and 3 rings, said heterocycle group containing at least one heteroatom group selected from --O--, --S--, --SO--, --SO.sub.2 --, .dbd.N--, and --NH--, said heterocycle group optionally containing one or more double bonds, said heterocycle group optionally comprising one or more aromatic rings, and said cyclic group optionally being singly or multiply substituted by --NH.sub.2, --CO.sub.2 H, --Cl, --F, --Br, --I, --NO.sub.2, --CN, .dbd.O, --OH, -perfluoro C.sub.1-3 alkyl, ##STR174## each Ar.sub.2 is independently selected from the following group, in which any ring may optionally be singly or multiply substituted by --Q.sub.1 and --Q.sub.2 : ##STR175## each Q.sub.1 is independently: --Ar.sub.1,--O--Ar.sub.1,--R.sub.9,--T.sub.1 --R.sub.9, or--(CH.sub.2).sub.1,2,3 --T.sub.1 --R.sub.9 ;each Q.sub.2 is independently --OH, --NH.sub.2 --CO.sub.2 H, --Cl, --F, --Br, --I, --NO.sub.2, --CN, --CF.sub.3, or ##STR176## provided that when --Ar.sub.1 is substituted with a Q.sub.1 group which comprises one or more additional --Ar.sub.1 groups, said additional --Ar.sub.1 groups are not substituted with Q.sub.1 ;each X is independently .dbd.N-- or .dbd.CH--;each X.sub.2 is independently --O--, --CH.sub.2 --, --NH--, --S--, --SO--, or --SO.sub.2 --;each X.sub.5 is independently ##STR177## each Y is independently --O--, --S--, or --NH; each Z is independently CO or SO.sub.2 ;each a is independently 0 or 1;each d is independently 0, 1, or 2; andeach e is independently 0, 1, 2, or 3; provided that whenR.sub.1 is: ##STR178## then R.sub.5 cannot be: --Ar.sub.1,--SO.sub.2 --Ar.sub.1,--CO--R.sub.9,--SO.sub.2 --R.sub.9,--CO--NH.sub.2,--SO.sub.2 --NH.sub.2, ##STR179## when R.sub.1 is ##STR180## g is 0; J is --H;m is 1;T is --CO.sub.2 H; andR.sub.3 is --CO--R.sub.13, wherein R.sub.13 is:--H, ##STR181## then R.sub.5 cannot be: ##STR182## and provided that when R.sub.1 is: ##STR183## g is 0; J is --H;m is 1;T is --CO.sub.2 H; andR.sub.3 is --CO--R.sub.13, wherein R.sub.13 is H;then R.sub.5 may not be --C(O)--CH.sub.2 CH.sub.2 Ph.