Aminobiguanides and the use thereof to disinfect contact lenses and preserve pharmaceutical compositions
First Claim
Patent Images
1. 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.
3 Assignments
0 Petitions
Accused Products
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.
41 Citations
56 Claims
-
1. 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. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11)
R1, R2, R3 and R4 are selected from the group consisting of hydrogen, alkyl (C1 to C20) and cycloalkyl (C3 to C20); and
X is selected from the group consisting of alkyl (C2 to C10) and alkyl (C2 to C10) substituted with cycloalkyl (C3 to C20).
-
-
10. A composition according to any one of claims 1 to 9, wherein the composition contains one or more compounds of formula (I) at a concentration in the range of 0.0001 to 0.1 w/v %.
-
11. A composition according to claim 10, wherein the solution has an osmolality of 220 to 320 mOsm/kg.
-
12. 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. - View Dependent Claims (13, 14, 15, 16, 17, 18, 19, 20, 21, 22)
R1, R2, R3 and R4 are selected from consisting of hydrogen, alkyl (C1 to C20) and cycloalkyl (C3 to C20); and
X is selected from the group consisting of alkyl (C2 to C10) and alkyl (C2 to C10) substituted with cycloalkyl (C3 to C20).
-
-
21. A method according to any one of claims 12-20, wherein the solution contains one or more compounds of formula (I) at a concentration in the range of 0.0001 to 0.1 w/v %.
-
22. A method according to claim 21, wherein the solution has an osmolality of 220 to 320 mOsm/kg.
-
23. 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. - View Dependent Claims (24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39)
R1, R2, R3 and R4 are selected from the group consisting of hydrogen, alkyl (C1 to C20) and cycloalkyl (C3 to C20); and
X is selected from the group consisting of alkyl (C2 to C10) and alkyl (C2 to C10) substituted with cycloalkyl (C3 to C20).
-
-
32. A pharmaceutical composition according to any one of claims 23 to 31, wherein the composition contains one or more compounds of formula (I) at a concentration of 0.00001 to 0.01 w/v %.
-
33. A pharmaceutical composition according to claim 32, wherein the composition is an ophthalmic composition.
-
34. A pharmaceutical composition according to claim 33, wherein the composition is utilized to treat contact lenses.
-
35. A pharmaceutical composition according to claim 32, wherein the composition is an aqueous ophthalmic composition.
-
36. A pharmaceutical composition according to any one of claims 23-31, wherein the composition is an aqueous ophthalmic composition.
-
37. A pharmaceutical composition according to any one of claims 23 to 31, wherein the composition is an aqueous solution and is utilized to treat contact lenses.
-
38. A pharmaceutical composition according to any one of claims 23 to 31, wherein the composition is an otic composition.
-
39. A pharmaceutical composition according to any one of claims 23 to 31, wherein the composition is a dermatological composition.
-
40. 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. - View Dependent Claims (41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56)
R1, R2, R3 and R4 are selected from the group consisting of hydrogen, alkyl (C1 to C20) and cycloalkyl (C3 to C20); and
X is selected from the group consisting of alkyl (C2 to C10) and alkyl (C2 to C10) ted with cycloalkyl (C3 to C20).
-
-
49. A method according to any one of claims 40 to 48, wherein the composition contains one or more compounds of formula (I) at a concentration of 0.00001 to 0.01 w/v %.
-
50. A method according to claim 49, wherein the composition is an ophthalmic composition.
-
51. A method according to claim 50, wherein the composition is utilized to treat contact lenses.
-
52. A method according to claim 50, wherein the composition is an aqueous ophthalmic composition.
-
53. A method according to any one of claims 40 to 48, wherein the composition is an aqueous ophthalmic composition.
-
54. A method according to any one of claims 40 to 48, wherein the composition is an aqueous solution and is utilized to treat contact lenses.
-
55. A method according to any one of claims 40 to 48, wherein the composition is an otic composition.
-
56. A method according to any one of claims 40 to 48, wherein the composition is a dermatological composition.
Specification
-
- Resources
Litigation Campaign Assessment
Thank you for your request. You will receive a custom alert email when the Litigation Campaign Assessment is available.
×
-
Current AssigneeAlcon Research Limited (Nestle SA)
-
Original AssigneeAlcon Manufacturing Limited (Alcon Incorporated)
-
InventorsMcQueen, Nathaniel D., Schlitzer, Ronald L., Park, Joonsup, Dassanayake, Nissanke L.
-
Primary Examiner(s)FAY, ZOHREH A
-
Application NumberUS09/581,952Time in Patent Office1,230 DaysField of Search514/635, 514/912US Class Current514/635CPC Class CodesA01N 47/44 Guanidine; Derivatives thereofA61L 12/141 Biguanides, e.g. chlorhexidineA61L 2/0088 Liquid substancesA61P 27/02 Ophthalmic agentsC07C 279/26 X and Y being nitrogen atom...
