Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2001-10-12
2002-06-04
Jarvis, William R. A. (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S859000
Reexamination Certificate
active
06399651
ABSTRACT:
FIELD OF THE INVENTION
The present invention relates to methods for treating various dermatoses including transient acantholytic dermatitis, acne miliaris necrotica, acne varoliformis, perioral dermatitis, and acneiform eruptions.
BACKGROUND OF THE INVENTION
Transient acantholytic dermatitis, acne miliaris necrotica, acne varoliformis, perioral dermatitis, and acneiform eruptions are common dermatological diseases. Each of the dermatoses has its own etiology and histology.
1. Transient Acantholytic Dermatosis
Transient acantholytic dermatosis, also called syn Grover's disease, is an acquired skin disease which is seen as itchy papules and vesicles resulting in soreness over the area. The lesions appear on the shoulders, neck, thighs, scalp rapidly. Some of the papules can become rough and may have crusting. The disease mostly occurs in meddle to old age, especially in men. Unlike the name of the disease, the condition is not transient, and can last for years.
The cause of the disease is unknown, however, various factors are thought to precipitate the disease, including sun exposure and sun burn, heat exposure, sweating, fever, radiation treatment, and cancers. There is no specific treatment for this disease. Currently, topical steroids, systemic steroids, oral vitamin A, etretinate, PUVA (psoralen and long-wave ultraviolet radiation) and Accutane® (isotretnoin, manufactured by Roche) have been used clinically.
2. Acne Miliaris Necrotica and Acne Varioliformis
Acne miliaris necrotica, also called scalp folliculitis, consists of follicular vesicopustules, frequently solitary, usually very itchy and tender, which appear anywhere in the scalp or adjacent areas. It can range from an occasional nuisance that many people experience to a chronic problem that can be quite troublesome. The severe form of the disease which leaves large scars is called acne varioliformis. The condition is more common in people who are doing activities that make them sweat or who wear occlusive head gear. Stress often seems to trigger outbreaks as well. Existing treatments range from antibiotic shampoos such as Capitrol® (a chloroxine shampoo), astringent compresses, topical antibiotics or steroids to oral antibiotics. In extreme cases, Accutane® has been used, which is well known for the severe adverse side effects that can cause.
3. Perioral Dermatitis
Perioral dermatitis is a chronic papulopustular facial dermatitis. It mostly occurs in younger women. The incidence is estimated as 0.5-1% in industrialized countries, independent of geographical factors. The disease is limited to the skin. Skin lesions occur as grouped follicular reddish papules, papulovesicles and papulopustules on erythematous base with a possible confluent aspect. In an extreme variant of the disease, called lupuslike perioral dermatitis, granulomatous infiltrates occur with a yellowish aspect in diascopy. Although perioral dermatitis is limited to the skin and not life threatening, emotional problems may occur due to the disfiguring character of the facial lesions and a possible prolonged course of the disease.
The etiology of perioral dermatitis is unknown. However, many causative factors have been suggested, including injudicious use of topical steroids, fluorinated toothpaste, skin care ointments and creams, especially with a petrolatum or paraffin base and the vehicle isopropyl myristate, and old or contaminated make-up or applicators. It is known that UV light, heat and wind worsen perioral dermatitis. Further, microbials such as fusiform spirilla bacteria, candida species and other fungi have been found from the lesions. Other microbiological factors, such as candidiasis have been reported to provoke perioral dermatitis. In addition, hormonal factors, and gastrointestinal disturbances have been considered as well.
Known treatments include oral tetracyclines, minocin and do3cycline, with discontinuing topical corticosteroids, and avoiding lauryl sulfate toothpaste. However, it is currently believed there is no medicine that one can apply directly to the skin which will help perioral dermatitis.
4. Acneiform Eruptions
Acneiform eruptions are characterized by papules and pustules resembling acne lesions, not necessarily confined to the usual sites of acne vulgaris. The eruptions are distinguished by their sudden onset, usually in a patient well past adolescence. Most of the acneiform eruptions originate from skin exposure to various industrial chemicals. Some eruptions may come from oral medications. Acneiform eruptions may be induced by exposure of the skin to the fumes generated in the manufacture of chlorine and its by-products. Cutting oils, lubricating oils, crude coal tar applied to the skin for medicinal purposes, have tar distillates, coal tar pitch, and corticosteroids applied to the skin under occlusive dressings, and asbestos are known substances that may produce acneiform eruptions. Some of the acneiform eruptions are induced by medications such as iodides in vitamins with mineral supplement, and bromides in drugs such as propantheline bromide, and corticosteroids.
Although commonly called “trade acne”, “bromine acne”, and “chloracne”, acneiform eruptions are not a true acne, even though they are often ushered in by open comedones. Current treatments of acneiform eruptions include massive keratinization-suppressing doses of vitamin A, 300,000 units daily, topical retinoids, such as Retin-A cream or gel, or even oral Accutane®.
The above-discussed dermatoses are commonly seen clinically. Some patients respond well to the existing treatments. However, many patients suffer from the diseases for many years without significant improvement after being treated with all existing treatments. Furthermore, some patients have adverse reactions to the existing medications, or can not tolerate antibiotics used for treating these dermatoses. Sometimes, it is not appropriate to use existing treatment methods or medications for certain patients. For example, antibiotics and Accutane® are effective for treating acute inflammation caused by these dermatoses, however, they should not be used for pregnant women and nursing mothers. Therefore, there is apparently a need for new and effective topical treatments for the above-menboned dermatoses.
The preferred compound that is used to illustrate the present invention is ivermectin. Ivermectin is a semi-synthetic derivative of avermectin and is generally produced as a mixture of at least 80% 22,23-dihydroavermectin B
1a
and less than 20% 22,23-dihydroavermectin B
1b
. The following molecular structure represents the avermectin series of compounds, which can be chemically converted to useful derivatives as discussed below.
wherein R is the 4′-(alpha-L-oleandrosyl)-alpha-L-oleandrose group of the structure:
wherein the broken line indicates a single or double bond; R
1
is hydroxy and is present only when said broken line indicates a double bond; R
2
is isopropyl or sec-butyl; and R
3
is methoxy or hydroxy.
The avermectins, of which ivermectin, a chemically produced along, is a member are a series of compounds isolated from the fermentation broth of a C-076 producing strain of
Streptomyces avermitillis
and also chemically produced derivatives thereof. There are eight different but closely related compounds are produced by
S. avermitillis
, designated as A
1a
, A
1b
, A
2a
, A
2b
, B
1a
, B
1b
, B
2a
, and B
2b
. The production of these compounds is described in U.S. Pat. No. 4,310,519. The preparation of ivermectin is disclosed in U.S. Pat. No. 4,199,569. The disclosures of each of the foregoing patents are incorporated herein by reference. The avermectin family of compounds is a series of very potent antiparasitic agents known to be useful against a broad spectrum of endoparasites and ectoparasites in mammals and also to have agricultural uses against various nematode and insect parasites found in and on crops and in soil.
Some of the avermectins contain a 22,23-double bond. This may be selectively reduced to prepare the ivermectin compounds. In addition, the avermectins poss
Jarvis William R. A.
Kim Vickie
Li Yi
Silverman M. K.
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