Aminobiguanides and the use thereof to disinfect contact lenses and preserve pharmaceutical compositions
AssigneeAlcon Manufacturing, Ltd.
InventorsJoonsup Park, Nissanke L. Dassanayake, Nathaniel D. McQueen, Ronald L. Schlitzer
Life of this patent
Estimating the term…
Abstract
Aminobiguanides and the use of same as antimicrobial agents in pharmaceutical compositions are disclosed. The aminobiguanides are useful in the preservation of pharmaceutical compositions, particularly ophthalmic pharmaceutical compositions and compositions for treating contact lenses. The compounds are especially useful for disinfecting contact lenses.
Claims56
A pharmaceutical composition for disinfecting a contact lens, comprising:
- a compound of the following formula, in an amount effective to disinfect the lens:
- wherein:
- R1 and R2 are the same or different and are selected from the group consisting of hydrogen, alkyl (C1 to C20), aminoalkyl (C1 to C20), aryl, arylalkyl (C3 to C20), aryloxyalkyl (C3 to C20) and cycloalkyl (C3 to C20);
- R3 and R4 are the same or different and are selected from the group consisting of hydrogen, alkyl (C1 to C20), aryl, arylalkyl (C3 to C20), aryloxyalkyl (C3 to C20) and cycloalkyl (C3 to C20);
- and
- X is alkyl (C2 to C20), optionally containing one or more substituents selected from the group consisting of cycloalkyl (C3 to C20), aryl, arylalkyl (C3 to C20) and aryloxyalkyl (C3 to C20);
- provided that at least one of R1, R2, R3 and R4 is a substituent other than hydrogen;
- or a pharmaceutically acceptable salt thereof;
- and
- an aqueous vehicle therefor.
A method of disinfecting a contact lens which comprises soaking the lens in an aqueous disinfecting solution for a time sufficient to disinfect the lens, said solution comprising:
- a compound of the following formula, in an amount effective to disinfect the lens:
- wherein:
- R1 and R2 are the same or different and are selected from the group consisting of hydrogen, alkyl (C1 to C20), aminoalkyl (C1 to C20), aryl, arylalkyl (C3 to C20), aryloxyalkyl (C3 to C20) and cycloalkyl (C3 to C20);
- R3 and R4 are the same or different and are selected from the group consisting of hydrogen, alkyl (C1 to C20), aryl, arylalkyl (C3 to C20), aryloxyalkyl (C3 to C20) and cycloalkyl (C3 to C20);
- and
- X is alkyl (C2 to C20), optionally containing one or more substituents selected from the group consisting of cycloalkyl (C3 to C20), aryl, arylalkyl (C3 to C20) and aryloxyalkyl (C3 to C20);
- provided that at least one of R1, R2, R3 and R4 is a substituent other than hydrogen;
- or a pharmaceutically acceptable salt thereof;
- and
- an aqueous vehicle therefor.
A pharmaceutical composition comprising a compound of the following formula, in an amount effective to preserve the composition from microbial contamination:
- wherein:
- R1 and R2 are the same or different and are selected from the group consisting of hydrogen, alkyl (C1 to C20), aminoalkyl (C1 to C20), aryl, arylalkyl (C3 to C20), aryloxyalkyl (C3 to C20) and cycloalkyl (C3 to C20);
- R3 and R4 are the same or different and are selected from the group consisting of hydrogen, alkyl (C1 to C20), aryl, arylalkyl (C3 to C20), aryloxyalkyl (C3 to C20) and cycloalkyl (C3 to C20);
- and
- X is alkyl (C2 to C20), optionally containing one or more substituents selected from the group consisting of cycloalkyl (C3 to C20), aryl, arylalkyl (C3 to C20) and aryloxyalkyl (C3 to C20);
- provided that at least one of R1, R2, R3 and R4 is a substituent other than hydrogen;
- or a pharmaceutically acceptable salt thereof;
- and
- a pharmaceutically acceptable vehicle therefor.
A method of preserving a pharmaceutical composition from microbial contamination, which comprises including a compound of the following formula in the composition, in an amount effective to preserve the composition:
- wherein:
- R1 and R2 are the same or different and are selected from the group consisting of hydrogen, alkyl (C1 to C20), aminoalkyl (C1 to C20), aryl, arylalkyl (C3 to C20), aryloxyalkyl (C3 to C20) and cycloalkyl (C3 to C20);
- R3 and R4 are the same or different and are selected from the group consisting of hydrogen, alkyl (C1 to C20), aryl, arylalkyl (C3 to C20), aryloxyalkyl (C3 to C20) and cycloalkyl (C3 to C20);
- and
- X is alkyl (C2 to C20), optionally containing one or more substituents selected from the group consisting of cycloalkyl (C3 to C20), aryl, arylalkyl (C3 to C20) and aryloxyalkyl (C3 to C20);
- provided that at least one of R1, R2, R3 and R4 is a substituent other than hydrogen;
- or a pharmaceutically acceptable salt thereof;
- and
- a pharmaceutically acceptable vehicle therefor.
Dependencies are inferred from the claim text.