Patent ID: 6034118
Filing Date: 2000-03-07
Classification: C07D

Abstract:
A composition comprising a compound of the formula: ##STR515## wherein: Y is independently --O--, --S--, --SO--, --SO.sub.2 --, --N(R.sub.1)--, --N(R.sub.1)--SO.sub.2 --, --N(R.sub.1)--CO--, or --O--SO.sub.2 --,E and U are independently H, or --CR.sub.1 R.sub.1).sub.m1 --W.sub.1, with the proviso that at least one of E and U is --CR.sub.1 R.sub.1).sub.m1 --W.sub.1 ;G and T are independently --CR.sub.1 R.sub.1).sub.m1 --W.sub.1, or --CR.sub.1 R.sub.1).sub.m1 --C(R.sub.1)(W.sub.1)(W.sub.2), with the provisos that:when E is --CR.sub.1 R.sub.1).sub.m1 --W.sub.1, then G is --CR.sub.1 R.sub.1).sub.m1 --W.sub.1 ;when U is --CR.sub.1 R.sub.1).sub.m1 --W.sub.1, then T is --CR.sub.1 R.sub.1).sub.m1 --W.sub.1 ; and G and T may be the same or different;J and L are independently H, N.sub.3, --OR.sub.2, --N(R.sub.2)(R.sub.2), or --N(R.sub.2)(R.sub.3), wherein R.sub.2 is H, or PRT, with the proviso that at least one of J and L is --OR.sub.2, or J and L are taken together to form an epoxide, or a cyclic protecting group;W.sub.1 is W.sub.2 or W.sub.3 ;W.sub.2 is carbocycle or heterocycle, with the proviso that each W.sub.2 is independently substituted with 0 to 3 R.sub.5 groups;W.sub.3 is alkyl, alkenyl, or alkynyl, with the proviso that each W.sub.3 is independently substituted with 0 to 3 R.sub.6 groups;R.sub.1 is R.sub.3 or R.sub.6 ;R.sub.3 is H or R.sub.4 ;R.sub.4 is alkyl;R.sub.5 is R.sub.6, or R.sub.7, with the proviso that each R.sub.7 is independently substituted with 0 to 3 R.sub.6 groups;R.sub.6 is --O-(antigenic polypeptide), --N(R.sub.3)-(antigenic polypeptide), --C(O)O-(antigenic polypeptide), --C(O)N(R.sub.3)-(antigenic polypeptide), --S-- (antigenic polypeptide), --S--S-(antigenic polypeptide), --O-(label), --N(R.sub.3)-(label), --C(O)O-(label), --C(O)N(R.sub.3)-(label), --S-(label), --S--S-(label), F, Cl, Br, I, --CN, N.sub.3, --NO.sub.2, --OR.sub.3, --OPRT, --O--C(O)R.sub.4, .dbd.O, --N(R.sub.3)(R.sub.3), --N(R.sub.3)(PRT), --N(PRT).sub.2, --N(R.sub.3)--C(O)R.sub.4, .dbd.N(R.sub.3), .dbd.N(PRT), --N(OR.sub.3)(R.sub.3), --N(OPRT)(R.sub.3), --N(OR.sub.3)(PRT), --N(OPRT)(R.sub.3), --N(N(R.sub.3)(R.sub.3))(R.sub.3), --N(N(PRT)(R.sub.3))(R.sub.3), --N(N(R.sub.3)(R.sub.3))(PRT), --N(N(PRT)(PRT))(R.sub.3), --N(N(PRT)(R.sub.3))(PRT), --N(N(PRT)(PRT))(PRT), --N(R.sub.3)--C(N(R.sub.3))(N(R.sub.3).sub.2), --N(PRT)--C(N(R.sub.3))(N(R.sub.3).sub.2), --N(R.sub.3)--C(N(PRT))(N(R.sub.3).sub.2), --N(R.sub.3)--C(N(R.sub.3))(N(R.sub.3)(PRT)), --N(PRT)--C(N(PRT))(N(R.sub.3).sub.2), --N(PRT)--C(N(R.sub.3))(N(R.sub.3)(PRT)), --N(R.sub.3)--C(N(PRT))(N(R.sub.3)(PRT)), --N(R.sub.3)--C(N(R.sub.3))(N(PRT).sub.2), --N(PRT)--C(N(PRT))(N(R.sub.3)(PRT)), --N(PRT)--C(N(R.sub.3))(N(PRT).sub.2), --N(R.sub.3)--C(N(PRT))(N(PRT).sub.2), --N(PRT)--C(N(PRT))(N(PRT).sub.2), --C(NR.sub.3)(N(R.sub.3).sub.2), --C(N(R.sub.3))(N(R.sub.3)(PRT)), --C(NPRT)(N(R.sub.3).sub.2), --C(N(PRT))(N(R.sub.3)(PRT)), --C(N(R.sub.3))(N(PRT).sub.2), --C(N(PRT))(N(PRT).sub.2), --SR.sub.3, --S(PRT), .dbd.S, --S(O)--R.sub.3, --S(O)--OR.sub.3, --S(O)--OPRT, --O--S(O)--R.sub.3, --S(O).sub.2 --R.sub.3, --S(O).sub.2 --OR.sub.3, --S(O).sub.2 --OPRT, --O--S(O).sub.2 --R.sub.3, --C(O)OR.sub.3, --C(O)OPRT, --C(O)N(R.sub.3).sub.2, --C(O)N(R.sub.3)(PRT), --C(O)N(PRT).sub.2, --C(S)N(R.sub.3).sub.2, --C(S)N(R.sub.3)(PRT), --C(S)N(PRT).sub.2, --N(R.sub.3)--S(O).sub.2 --R.sub.3, --N(PRT)--S(O).sub.2 --R.sub.3, --S(O).sub.2 --N(R.sub.3)--R.sub.3, --S(O)2--N(PRT)--R.sub.3, carbocycle, or heterocycle;R.sub.7 is alkyl, alkenyl, or alkynyl;each m1 is independently an integer from 0 to 3; and with the proviso that the compound, taken as a whole, contains 0 to 16 R.sub.6 groups, and that each E, G, T, and U, taken individually, contain 0 to 8 R.sub.6 groups.