Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Reexamination Certificate
1999-01-15
2002-04-23
Qazi, Sabiha (Department: 1616)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
C510S161000, C510S131000, C510S382000, C510S384000, C510S386000, C424S405000, C424S238100, C424S409000, C514S579000, C514S663000, C514S667000, C514S670000
Reexamination Certificate
active
06376547
ABSTRACT:
FIELD OF THE INVENTION
The present invention relates to the use of N,N′-substituted glycine and derivatives of glycine in disinfectants, in particular in aldehyde-free liquid disinfectants with activity against mycobacteria, which are particularly suitable for the disinfection of surfaces and instruments.
BACKGROUND OF THE INVENTION
Mycobacteria are still a great problem in the clinical area. Therefore, a tuberculocidal activity is demanded of disinfectants in this area in addition to a bactericidal, fungicidal and virucidal activity.
The trend in the field of surface and instrument disinfectants is increasingly in the direction of aldehyde-free preparations. On account of their toxicological properties and the odour problems which occur, aldehyde—containing disinfectants known in the prior art suffer from decreased user acceptance. Moreover, only a few biocides having tuberculocidal activity are known in the sector of aldehyde-free disinfectants.
These include, for example, N,N′-bis(3-amino-propyl)laurylamine from the amines group, which is employed in various surface and instrument disinfectants. As is known, formulations which have been prepared using this active compound have a raised pH. This leads to an increased risk in skin and material compatibility.
Of the aromatic alcohols which also have tuberculocidal activity, such as phenoxypropanols (e.g. 1-and 2-phenoxypropanol), markedly larger amounts must be employed in order to achieve a corresponding action. This leads to an increased risk of build-up of an undesired layer on the disinfected materials.
SUMMARY OF THE INVENTION
It was thus the object of the invention to make available disinfectants which have a good activity against mycobacteria, without having the abovementioned disadvantages.
Surprisingly, it has been found that, in addition to the activity against the bacterial spectrum known until now, N,N′-substituted glycine and N,N′-substituted derivatives of glycine are active against mycobacteria and, in particular in admixtures with cationic compounds, even act synergistically against mycobacteria.
The present invention thus relates to the use of an N,N′-substituted glycine and of derivatives of glycine (a) of the general formula I
in which R
1
is hydrogen or a straight-chain or branched, saturated or unsaturated alkyl, alkaryl or aralkyl radical having 1 to 30 C atoms, which can optionally contain heteroatoms such as O, S and N, R
2
is a straight-chain or branched, saturated or unsaturated alkyl, alkaryl or aralkyl radical having 1 to 30 C atoms containing at least one primary, secondary or tertiary amino group and X is OH, OR
3
, NH
2
, NHR
4
, NR
4
R
5
or O
−
M
30
, where R
3
, R
4
and R
5
are straight-chain or branched, saturated or unsaturated alkyl, alkaryl or aralkyl radicals which can be identical to or different from one another, and M is a metal cation, as active compound in a tuberculocidal disinfectant.
The present invention further relates to a tuberculocidal disinfectant, which is characterized in that it contains at least one N,N′-substituted glycine or derivative of glycine (a) in the form of the free acid or of a salt thereof, an ester or an amide of the above general formula I, where R
1
, R
2
, R
3
, R
4
, R
5
and X have the meanings indicated above, and at least one further active compound (b) selected from quaternary ammonium compounds, guanidinium derivatives, biguanides, aromatic alcohols and amines.
Preferred embodiments of the invention are the subject of the subclaims.
The tuberculocidal disinfectant is preferably aldehyde-free and is present as a liquid concentrate.
Preferably, R
1
is hydrogen and R
2
is an amino-substituted C
2
- to C
4
-alkyl radical, in particular an amino-substituted C
3
-alkyl radical, preferably a 3-aminopropyl group which is substituted on the nitrogen atom by a radical R, where R is a C
8
- to C
18
-alkyl radical, in particular a C
10
- to C
16
-alkyl radical. Thus N-(3-aminopropyl)-N′-C
(8-18)
-alkylglycine derivatives and N-(3-aminopropyl)-N′-C
(10-16)
-alkyl-glycine derivatives are particularly preferred.
X is preferably OH. Thus HOOC-CH
2
-NH-(CH
2
)
3
-NH-R, where R has the previously indicated meaning, is a preferred compound in the sense of the present invention.
The use according to the invention of the N,N′-substituted glycine or of the derivatives described above in the tuberculocidal disinfectant is preferably effected in combination with at least one further active compound (b) selected from quaternary ammonium compounds, guanidine derivatives, biguanides, aromatic alcohols and amines.
The tuberculocidal disinfectant according to the invention can contain 0.01 to 40% by weight, preferably 0.05 to 30% by weight and in particular 1 to 15% by weight of the N,N′-substituted glycine or its derivative (a) and, if it is used in combination with one of the abovementioned active compounds (b), optionally 1 to 70% by weight, preferably 5 to 60% by weight and in particular 10 to 30% by weight, of the active compound (b).
Use solutions having tuberculocidal activity can also be prepared which contain 0.1 to 10% by volume and in particular 0.2 to 5% by volume of the abovementioned concentrate.
The solvent used is preferably water or a water—containing solvent mixture. If a solvent mixture is employed, this preferably contains one or more alcohols having 2 to 4 C atoms, such as ethanol, 1-propanol, 2-propanol, n-butanol, isobutanol, sec-butanol or tert-butyl alcohol, in particular ethanol, i-propanol and/or 2-propanol.
For better wetting of the surfaces and for assisting the action, one or more surfactants can be added to the disinfectants according to the invention. As surfactants, certain anionic surfactants, for example soaps such as sodium stearate, potassium stearate or triethanolamine soaps, sulphonated aromatic hydrocarbons such as N-alkylbenzenesulphonates, sulphonated aliphatic hydrocarbons such as secondary alkanesulphonates, sulphonated olefins, sulphated fatty alcohols such as sodium lauryl sulphate, sulphated fatty alcohol ethers such as sodium lauryl polyglycol ether sulphate, sulphonated maleic acid esters such as lauryl sulphosuccinate, carboxymethylated fatty alcohol polyglycol ethers such as lauryl polyglycol ether acetate and/or non-ionic surfactants such as alkyl alkoxylates, alkylphenol ethoxylates, fatty acid ethoxylates, fatty acid alkylolamides, fatty acid alkylolamide ethoxylates, fatty amine ethoxylates, alkyl polyglycosides such as cocoylpolyglucose, laurylpolyglucose, decylpolyglucose or polyalkylene oxide block copolymers and/or amphoteric surfactants such as alkylaminoalkylglycines, betaines or sulphobetaines can preferably be used. Combinations of surfactants which are compatible with one another can also be employed.
In addition, complexing agents such as ethylenediaminetetraacetic acid, nitrilotriacetic acid or their salts, and sequestering agents such as phosphonobutanetricarboxylic acids can be added. To adjust the pH, organic acids such as citric acid, malic acid or lactic acid and/or inorganic acids such as, for example, hydrochloric acid, phosphoric acid or sulphuric acid can be used. To improve the material compatibilities, corrosion inhibitors, such as, for example, 1H-benzotriazole, tolyltriazole or mercaptobenzoxazole can be employed. Fragrances and colourants can furthermore be added.
The spectrum of action of the disinfectants according to the invention can be extended by addition of further active compounds (b). Compounds suitable for this are preferably quaternary ammonium compounds such as alkylbenzyldimethylammonium chloride, dialkyl-dimethyl-ammonium chloride, alkyldimethylethyl ethosulphate and/or dialkylmethyloxyethylammonium propionate, guanidinium derivatives such as coconut propylenediamineguanidinium diacetate, biguanides such as polyhexamethylene biguanide, furthermore aliphatic amines such as N,N′-bis(3-aminopropyl)dodecylamine and/or aromatic alcohols such as phenoxypropanols (e.g. 1-phenoxypropanol, 2-phenox-propanol or mixt
Behrends Sabine
Dettmann Andreas
Mohr Michael
L'Air Liquide SANTE (International)
Qazi Sabiha
LandOfFree
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