Polyalkoxy copolymers as lipase inhibitors and their...

Drug – bio-affecting and body treating compositions – Solid synthetic organic polymer as designated organic active...

Reexamination Certificate

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C424S078310

Reexamination Certificate

active

06461601

ABSTRACT:

The invention relates to copolymeric compounds and compositions containing these compounds which inhibit lipase enzymes or reduce the lipase enzyme activity.
BACKGROUND
Various types of lipase enzymes are present on our skin, including enzymes from micro-organisms, enzymes derived from our diet and enzymes produced by the body. It is known that these enzymes can have undesirable effects. For example, these enzymes are believed to cause skin rash and possibly infections of the body, which for example, is a problem encountered by the users of articles which are in contact with the skin and the lipase enzymes thereon, such as bandages, plaster, diapers, incontinence articles, sanitary towels, training pants etc. Also, it is believed that the enzymes can be responsible for the (further) development of dandruff and acne.
It has also been found that lipase enzymes can be responsible for development of malodour of the body, which can be (partially) due to the production by the enzymes of fatty acids, which are partially eliminated from the body in the body exudates, which can cause a malodour of the body.
In other situations, the presence of lipase enzymes is essential but may have negative side-effects. For example, lipase enzymes are present in detergents to improve the removal of greasy stains, but the presence of active enzyme on the washed fabrics is not desirable. Lipase enzymes are present in our digestive system, but it may be desirable that their activity is limited, for example to reduce obesity.
In recent years, manufacturers of skin and health care products have developed products over the past decades which help reduce the occurrence of problems caused by enzymes, in particular skin rash. The main focus thereby has been to reduce the exposure of the skin to the enzymes.
Various lipase enzyme inhibitors are known in the art. For example, antibodies which are specific to certain lipase enzymes are used, such as described in WO 95/24896 and WO 95101155. EP 0117632-B relates to disposable articles which comprise lipase inhibiting agents, preferably zinc containing components, and a vehicle material. U.S. Pat. No. 3,091,241 relates to the use of triacetin in vaginal tampons to inhibit lipase enzyme activity. U.S. Pat. No. 3,961,486 teaches the use of adipic acid to reduce the lipase enzyme activity and to reduce the skin rash.
The inventors have now found that certain copolymeric compounds, having a backbone comprising one or more linear alkoxy units and one or more branched alkoxy units, can very effectively inhibit lipase enzymes, or reduce the lipolytic enzyme activity. The compounds have been found to be useful in various applications where reduction of the lipolytic enzyme activity is desired. In particular, the inventors have found that the compounds can inhibit lipase enzymes from various micro-organisms, including bacteria, and that the compounds can thus reduce the activity of the micro-organisms and reduce the problems caused by these micro organisms. For example, it has been found that the use on the skin of the compounds or compositions containing the compounds results in a very effective reduction or a prevention of skin rash or skin irritation and also of acne; it has also been found that the compositions or compounds can reduce the irritation of the eyes; it has been found that the compounds or compositions thereof are also able to reduce or prevent malodour of the body; it has been found that the compounds or compositions containing the compound are capable of reducing or preventing dandruff; it has also been found that the compositions or compounds can improve the longevity of a perfume, e.g. protect the perfume esters from degradation by the enzymes; it has also been found that the compositions or compounds can improve the preservation of food and beverage products; it has also been found that the compositions or compounds can improve the healing of wounds.
SUMMARY OF THE INVENTION
The invention provides specific compositions for the reduction of the lipase enzyme activity, comprising a copolymeric compound of average molecular weight of at least 400, having a polyalkoxy backbone which comprises at least one branched C
1
-C
30
alkoxy unit and at least one linear C
1
-C
30
alkoxy unit.
The invention also relates to the use of these copolymeric compounds for preparation of compositions for reduction of the lipolytic enzyme activity, in particular of lipase enzymes derived from micro-organisms, in particular of micro-organisms in contact with the hair or skin.


REFERENCES:
patent: 5362425 (1994-11-01), Schrier
patent: 5725872 (1998-03-01), Stamm et al.
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patent: 117613 (1984-09-01), None
patent: 117613 (1990-06-01), None
patent: 61012616 (1986-01-01), None
patent: 61-012616 (1986-01-01), None
patent: 8053337 (1996-02-01), None
patent: 08053337 (1996-02-01), None
patent: 8268882 (1996-10-01), None
patent: 9516433 (1995-06-01), None
Thomas P. Johnston et al.: “Mechanism of Poloxamer 407-Induced Hypertriglyceridemia in the Rat” Biochem. Pharmacology vol. 46, No. 6, 1993.
Comai, Karen et al., “Antiobesity Activity of Pluronic L-101,” International Journal of Obesity, vol. 4, No. 1, 1980, pp. 33-42.
Johnston et al. (“Mechanism of Poloxamer 407-Induced Hypertriglyceridemia in the Rat,” Biochemical Pharmacology, vol. 46, No. 6, pp. 1037-1042, 1993).*
Comai et al. (“Antiobesity activity of Pluronic L-101,” International Journal of Obesity, vol. 4, No. 1.*
Derwent Abstract of JP 08-053337, Feb., 1996.*
Derwent Abstract of JP 05-317393, Dec., 1993.

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