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US 6,030,619 AGranted
Molecular mimetics of meningococcal B epitopes
AssigneeChiron Corporation
InventorsDan M. Granoff, Gregory R. Moe
Life of this patent
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Abstract
Molecular mimetics of unique epitopes of Neisseria meningitidis serogroup B ("MenB") are disclosed. Compositions containing such molecular mimetics can be used to prevent MenB or E. coli K1 disease without the risk of evoking autoantibody responses.
Claims19
A molecular mimetic of a unique epitope of Neisseria meningitidis serogroup B (MenB) having the following structure 1:
- ##STR10## wherein:
- R.sub.1 is --NR.sub.5 R.sub.6 ;
- R.sub.2 is --(CH.sub.2).sub.p --R.sub.11, wherein p is an integer from 0-8;
- R.sub.3 is H, 1-6C alkyl, aryl, alkyl-aryl, 2-6C alkenyl, or 2-6C alkynyl;
- R.sub.4 is --NH.sub.2, --NHOH, --NHNH.sub.2, --OH, --SH, or a multivalent linker moiety selected from the group of amines consisting of amino acids, peptoids, peptides, and --NH(CH.sub.2).sub.q SH, wherein q is an integer from 1-5;
- R.sub.5 is R.sub.2, H or R.sub.5 and R.sub.6 taken together form a carbocyclic or aryl ring, said ring optionally containing up to two heteroatoms selected from the group consisting of consisting of N, O and S;
- R.sub.6 is --CO--(CH.sub.2).sub.m --R.sub.7, wherein m is an integer from 1-6;
- ##STR11## wherein n is an integer from 0-5;
- R.sub.8 is H, 1-3C alkyl or acyl;
- R.sub.9 is --NH.sub.2, --NH--NH.sub.2, --CONH.sub.2, acyl, --COOH, --SH, --S-alkyl, --S-aryl, sulfonic acid or sulfonamide, with the proviso that when n=0, R.sub.9 is not --NH--NH.sub.2 ;
- R.sub.10 is H, 1-6C alkyl, halogen, OH, 1-6C alkoxy, acyl, amino, 1-5C alkylamino, amide, --COOH, --SH, --S-alkyl, --S-aryl, sulfonic acid or sulfonamide;
- and
- R.sub.11 is a carbocyclic ring or an aryl ring which is optionally substituted, --CH.dbd.CH--(CH.sub.2).sub.p --CH.sub.3, --CF.sub.3, --OH, 1-6C alkoxy, acyl, amino, --N(CH.sub.3).sub.2, --NH--NH.sub.2, amide, --COOH, --SH, --S-alkyl, --S-aryl, sulfonic acid or sulfonamide;
- with the proviso that when R.sub.3 is H;
- R.sub.4 is --NH.sub.2 ;
- and p is 0 or 1;
- R.sub.5 and R.sub.6 taken together do not form a bicyclic substituted carbocyclic or aryl ring, wherein one of the rings is a 7-membered ring.
14 more elements
A composition comprising a molecular mimetic of a unique epitope of Neisseria meningitidis serogroup B (MenB), in combination with a pharmaceutically acceptable excipient, having the following structure:
- wherein:
- R.sub.1 is --NR.sub.5 R.sub.6 ;
- R.sub.2 is --(CH.sub.2).sub.p --R.sub.11, wherein p is an integer from 0-8;
- R.sub.3 is H, 1-6C alkyl, aryl, alkyl-aryl, 2-6C alkenyl, or 2-6C alkynyl;
- R.sub.4 is --NH.sub.2, --NHOH, --NHNH.sub.2, --OH, --SH, or a multivalent linker moiety selected from the group of amines consisting of amino acids, peptoids, peptides, and --NH(CH.sub.2).sub.q SH, wherein q is an integer from 1-5;
- R.sub.5 is R.sub.2, H or R.sub.5 and R.sub.6 taken together form a carbocyclic or aryl ring, said ring optionally containing up to two heteroatoms selected from the group consisting of N, O and S;
- R.sub.6 is --CO--(CH.sub.2).sub.m --R.sub.7, wherein m is an integer from 1-6;
- ##STR18## wherein n is an integer from 0-5;
- R.sub.8 is H, 1-3C alkyl or acyl;
- R.sub.9 is --NH.sub.2, --NH--NH.sub.2, --CONH.sub.2, acyl, --COOH, --SH, --S-alkyl, --S-aryl, sulfonic acid or sulfonamide, with the proviso that when n=0, R.sub.9 is not --NH--NH.sub.2 ;
- R.sub.10 is H, 1-6C alkyl, halogen, OH, 1-6C alkoxy, acyl, amino, 1-5C alkylamino, amide, --COOH, --SH, --S-alkyl, --S-aryl, sulfonic acid or sulfonamide;
- and
- R.sub.11 is a carbocyclic ring or an aryl ring which is optionally substituted, --CH.dbd.CH--(CH.sub.2).sub.p --CH.sub.3, --CF.sub.3, --OH, 1-6C alkoxy, acyl, amino, --N(CH.sub.3).sub.2, --NH--NH.sub.2, amide, --COOH, --SH, --S-alkyl, --S-aryl, sulfonic acid or sulfonamide.
10 more elements
Dependencies are inferred from the claim text.