Agents acting against hyperreactive and hypoactive,...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C514S457000, C514S152000, C514S858000, C514S859000, C514S860000, C514S861000, C514S863000, C514S864000

Reexamination Certificate

active

06180662

ABSTRACT:

DESCRIPTION
Agents against hyperreactive and hypoactive, deficiency states of the skin and manifest dermatitis.
The present invention particularly relates to active compounds and formulations, in particular for topical use, which are used for prophylaxis and treatment of hyperreactive skin predisposed to dermatitis, and of deficient hypoactive skin and for prophylaxis and treatment of the manifest dermatoses mentioned under I. to XIII., such as, for example, atopic dermatitis, neurodermatitis, atopic eczema and seborrhoeic dermatitis, photoinduced dermatoses (for example Mallorca acne and in particular polymorphic photodermatosis and photodermatitis), rosacea, prurigo forms, pruritus, psoriasis forms, ichthyosis, decubitus, ulcus cruris and microbial and viral infections, such as, for example, herpes simplex, h.zoster or h.labialis.
The skin states according to the invention are explained below in more detail.
Various pathological mechanisms which characterize the clinical picture of hypoactive skin or hyperreactive skin and the dermatoses mentioned under I. to XIII., such as, for example, forms of acne, atopic dermatitis, prurigo forms, psoriasis, photodermatoses, decubitus, ulcus cruris and ichthyosis, are described in the literature. However, the causal pathological mechanisms and the chronology thereof are not sufficiently known for any of the dermatoses mentioned. The treatment methods and active compounds administered which are known to date lead in the most favourable case to a brief improvement in the symptoms. UV treatment and/or chemotherapy (psoralen, PUVA, cyclosporin A, corticosteroids, acyclovir and the like), for example, are used for treatment, with the known adverse side effects on repeated administration.
The object of the invention is to improve this unsatisfactory prior art and to provide cosmetic, dermatological and/or pharmaceutical active compounds and formulations which are used for prophylaxis and treatment of deficient, hypoactive skin or for prophylaxis and treatment of hyperreactive skin with a propensity to dermatitis, and for prophylaxis and treatment of the manifest dermatoses mentioned under sections I. to XIII. below, without inducing the side effects of known agents, even during long-term use.
These objects are achieved according to the invention.
The invention relates to the use of
a) a compound or several compounds from the group consisting of flavonoids, or
b) an active compound combination comprising a compound or several compounds chosen from the group consisting of flavonoids, in combination with a compound or several compounds chosen from the group consisting of cinnamic acid derivatives, and if appropriate additionally in each case a compound or several compounds from one of the groups or several of the groups
c) of the antioxidants or
d) of the endogenous energy metabolism metabolites or
e) of the endogenous enzymatic antioxidant systems and synthetic derivatives thereof (mimics) or
f) of the antimicrobial action systems or
g) of the antiviral action systems or
h) active compounds of the known, conventional treatment forms
in each case for the treatment or prophylactic treatment of hyperreactive skin predisposed to dermatitis or deficient, hypoactive skin or dermatoses.
Active compound combinations b), their use and formulations which comprise these are preferred.
The invention also relates to cosmetic and dermatological formulations, in particular topical formulations and pharmaceutical preparations, having a content of the abovementioned active compounds for treatment and prophylactic treatment of the abovementioned states of the skin or diseases.
The invention also relates to cosmetic and dermatological, in particular topical formulations and pharmaceutical preparations having a content of the abovementioned active compounds according to the invention.
The manifest dermatoses or skin diseases (dermatitis) according to the invention and the most important forms and names thereof are, in particular:
I. Atopic eczema:
neurodermatitis
atopic dermatitis, dermatitis atopica
atopic eczema with type I and type IV contact
eczema,
aggravated by occupation,
nappy dermatitis
milk crust
eczematous erythroderma
II. Contact eczema:
toxic/irritating contact eczema,
occupation-related (for example oil/tar; halogens)
allergic contact eczema, type I or type IV
photoallergic contact eczema
contact urticaria
dyshidrosiform eczema
III. Acne:
acne vulgaris, juvenile and adult (acne with comedones, papulous, pustulous, nodose, i.e. nodular, nodulocystic acne)
acne conglobata (special form: hidradenitis suppurativa)
acne fulminans
acne tetrad
acne neonatorum
senile acne (M. Favre-Racouchot)
mechanical acne forms (excoriated acne)
acne cosmetica
folliculitis with superinfected acne (Staphylococci)
occupation-related acne forms (for example chlorine acne)
IV. Herpes virus infections:
herpes simplex (HSV I+II)
herpes zoster (varicella virus)
herpes labialis (gingivostomatitis herpetica, mouth-rot, aphthae,
stomatitis aphthosa,
paronychia herpetica, eczema herpeticatum aphthoid of posphiscill and Feyrter, vulvovaginitis herpetica, keratoconjunctivitis herpetica, herpes simplex recidivans, herpes genitalis recidivans, herpes glutaelis recidivans, dermatitis herpetiformis)
varicella virus (herpes zoster, acute posterior ganglionitis, shingles, zona)
V. Bacterial infections:
non-follicular pyodermas, vulgaris or bullous (impetigo contagiosa, Streptococci, Staphylococci) follicular pyodermas (cocci), furuncles, carbuncles,
folliculitis, for example f. barbae
mycobacterioses (Corynebacteria, Spirochaeta, anaerobic organisms)
erysipelas (Gram-pos. cocci, Gram-neg. rod-shaped organisms)
ecthyma forms
leprosy forms
erythrasma (
Coryneb. minutissimum
)
trichomycosis axillaris (
Coryneb. tenuis
)
VI. Psoriasis:
psoriasis vulgaris
flaking eczema
psoriasis pustulosa
psoriasis arthropatica
psoriatic erythroderma
VII. Rosacea
VIII. Perioral dermatitis
IX. Prurigo:
p. simplex acuta (strophulus, urticaria papulosa),
subacuta, chronica,
p. nodularis Hyde
X. Eczema:
seborrhoeic eczema (p. ovale)
microbial eczema (nappy dermatitis-Bacillus ammonia-genase,
B. proteus, B. subtilis, E. coli, S. aureus
)
numular eczema
dyshidrotic eczema
desiccating eczema (asteatotic eczema, xerosis, eczema craquele)
lichen simplex chronicus (neurodermatitis circumscripta)
XI. Photodermatosis:
radiodermatitis acuta and chronica (UV and ionizing radiation therapy)
chronic actinic dermatitis
photourticaria (urticaria solaris)
polymorphic photodermatosis (other names for polymorphic photodermatosis are PPD, PPE and a large number of other names such as are mentioned in the literature (for example A. Voelckel et al., Zentralblatt Haut- und Geschlechtskrankheiten (1989), 156, page 2))
XII. Decubitus
XIII. Ulcus cruris
In the following text, the flavonoids according to the invention are also designated A), the cinnamic acid derivatives are also designated B), the antioxidants are also designated C), the endogenous energy metabolism metabolites are also designated D), the endogenous enzymatic antioxidant systems or substances and synthetic derivatives thereof (mimics) are also designated E), the antimicrobial action systems or active compounds are also designated F), the antiviral action systems for substances are also designated G) and the known conventional treatment forms or substances are also designated H).
Preferred flavonoids according to the invention are, for example, hydroxylated flavones, flavonones, isoflavones or chalcones, and in each case also glycosides thereof, as well as these non-hydroxylated base structures or parent substances.
According to the invention, the flavonoids A) are preferably chosen from the group of substances having the generic structural formulae:
wherein Z
1
-Z
5
independently of one another are chosen from the group consisting of H, OH and O-alkyl, wherein the alkyl groups can be branched and unbranched and can contain 1-18 C atoms, and wherein Gly is chosen from the group consisting of mono- and oligoglycoside radicals, or can also be H. Preferred glycoside

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