Method of treating HIV infections with anti-viral formulations
AssigneeMerrell Pharmaceuticals Inc.
InventorsAlan D. Cardin, Richard L. Jackson, Michael J. Mullins
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Abstract
The preferred oligomers of the present invention are polyureas, polycarbonates, polyesters or polyamides having a number average molecular weight of <10,000. These oligomers are water-soluble, have a rigid backbone, have recurring units coupled by carbonyl linking moieties which have anionic groups, display predominantly linear geomentry such that regular spacing between anionic groups exists in an aqueous medium, and are pharmaceutically-acceptable. The oligomers are useful for the treatment and/or diagnosis of AIDS and ARC.
Claims25
A method of treating an HIV infection in a patient in need thereof which comprises administering to the patient an effective amount of a pharmaceutical formulation comprising a pharmaceutically acceptable carrier and a rigid backbone, water soluable oligomer, having a molecular weight less than 10,000, recurring units coupled by carbonyl linking moieties, anionic groups and predominantly linear geometry in an aqueous medium and which is represented by any one of the following formula:
- ##STR37## wherein:
- R represents hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl, or phenyl substituted with from 1 to 2 R.sup.1 moieties and up to 3 substituents independently selected from chloro, bromo or C.sub.1 -C.sub.4 alkyl;
- R.sup.1 represents --SO.sub.3 R.sup.2, --CO.sub.2 R.sup.2, --PO.sub.3 (R.sup.2).sub.2, or --OPO.sub.3 R.sup.2 ;
- R.sup.2 represents hydrogen or a pharmaceutically-acceptable cation;
- m is an integer 0 or 1, with the proviso that when m is O ,R is hydrogen;
- X represents ##STR38## Y represents --CO.sub.2 --, --C.tbd.C--, --N.dbd.N--, ##STR39## n is an integer from 3 to 50;
- and R.sup.3 represents --R or --X--NH.sub.2, where R and X are defined as before;
- B) a polycarbonate of the formula:
- ##STR40## wherein:
- X and n are defined as in Formula I, above;
- X.sup.1 represents a HO--X--, where X is defined as in Formula I, above, C.sub.1 -C.sub.4 alkyl, phenyl, or phenyl substituted with from 1 to 2 R.sup.1 moieties and up to 3 substituents independently selected from chloro, bromo or C.sub.1 -C.sub.4 alkyl;
- and
- X.sup.2 represents hydrogen, or --CO.sub.2 X.sup.1, where X.sup.1 is defined as above;
- C) a polyester of the formula ##STR41## wherein:
- X and n are defined as in Formula I, above;
- R.sup.4 represents --R.sup.2, as defined in Formula I, above, or --X.sup.1, as defined in Formula II, above;
- R.sup.5 represents ##STR42## where R.sup.4 is defined as in Formula III, above, or --R.sup.2, where R.sup.2 is defined as in Formula I, above;
- X.sup.3 represents ##STR43## wherein R.sup.1 and Y are defined as in Formula I, above;
- or D) a polyamide of the formula:
- ##STR44## wherein:
- X and n are defined as in Formula I, above;
- X.sup.3 is defined as in Formula III, above;
- R.sup.6 represents H.sub.2 N--X--NH--, R.sup.2 O--, RNH-- or R--C(O)--NH--X--NH--, where R, R.sup.2 and X are defined as in Formula I, above;
- R.sup.7 represents hydrogen, ##STR45## where R and R.sup.2 are defined as in Formula I, above;
- and
- X.sup.3 is defined as in Formula III, above.
A method of treating an HIV infection in a patient in need thereof which comprises administering to the patient an effective amount of a pharmaceutical formulation comprising a mixture of oligomers which are water soluble, have a rigid backbone, a molecular weight <10,000, and recurring units coupled by carbonyl linking moieties, and which have anionic groups and predominantly linear geometry in an aqueous medium and which are represented by, the formula:
- ##STR61## wherein:
- R represents hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl, or phenyl substituted with from 1 to 2 R.sup.1 moieties and up to 3 substituents independently selected from chloro, bromo or C.sub.1 -C.sub.4 alkyl;
- R.sup.1 represents --SO.sub.3 R.sup.2, --CO.sub.2 R.sup.2,--PO.sub.3 (R.sup.2).sub.2, or--OPO.sub.3 R.sup.2 ;
- R.sup.2 represents hydrogen or a pharmaceutically acceptable cation;
- m is an integer 0 or 1, with the proviso that when m is 0, R is hydrogen;
- X represents:
- ##STR62## Y represents:
- --CO.sub.2 --, --C.dbd.C--, --N.dbd.N--, ##STR63## n is an integer from 3 to 50;
- and R.sup.3 represents --R or--X--NH.sub.2, where R and X are defined as before;
- B) a polycarbonate of the formula:
- ##STR64## wherein:
- X and n are defined as in Formula I, above;
- X.sup.1 represents HO--X--, where X is defined as in Formula I, above, C.sub.1 -C.sub.4 alkyl, phenyl, or phenyl substituted with from 1 to 2R.sup.1 moieties and up to 3 substituents independently selected from chloro, bromo or C.sub.1 -C.sub.4 alkyl;
- and
- X .sup.2 represents hydrogen or --CO.sub.2 X.sup.1, where X is defined as above;
- c) a polyester of the formula:
- ##STR65## wherein X and n are defined as in Formula I, above;
- R.sup.4 represents --R.sup.2, as defined in Formula I, above, or X.sup.1, as defined in Formula II, above;
- R.sup.5 represents ##STR66## where R.sup.4 is defined as in Formula III, above, or--R.sup.2, where R.sup.2 is defined as in Formula I, above;
- X.sup.3 represents ##STR67## wherein R.sup.1 and Y are defined as in Formula I, above;
- or D) a polyamide of the formula:
- ##STR68## wherein:
- X and n are defined as in Formula I, above;
- X.sup.3 is defined as in Formula III, above;
- R.sup.6 represents H.sub.2 N--X--NH--, R.sup.2 O, RNH-- or R--C(O) --NH--X--NH, wherein R, R.sup.2 and X are defined as in Formula I, above;
- R.sup.7 represents hydrogen, ##STR69## where R ans R.sup.2 are defined as in Formula I, above;
- and
- X.sup.3 is defined as in Formula III, above.
A method of treating an HIV infection in a patient in need thereof which comprises administering to the patient an effective amount of a pharmaceutical formulation comprising a pharmaceutically acceptable carrier and a water-soluble, rigid backbone oligomer having a molecular weight less than 10,000 comprising recurring units coupled by carbonyl linking moieties, anionic groups and predominantly linear geometry such that regular spacing between the anionic groups exists in an aqueous medium.
Dependencies are inferred from the claim text.