Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Reexamination Certificate
2001-12-21
2004-07-20
Wang, Shengjun (Department: 1617)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
C514S169000, C514S170000, C514S180000, C514S177000, C514S178000, C514S179000, C514S769000, C514S785000, C424S400000
Reexamination Certificate
active
06765001
ABSTRACT:
FIELD OF THE INVENTION
Topical corticosteroids are useful for their anti-inflammatory, anti-pruritic and vasoconstrictive actions. Corticosteroids (or corticoids) are any steroids (lipids that contain a hydrogenated cyclopentoperhydrophenanthrene ring system) elaborated by the adrenal cortex (except sex hormones of adrenal origin) in response to the release of adrenocorticotrophin or adrenocorticotropic hormone by the pituitary gland, or to any synthetic equivalent, or to angiotensin II. Corticosteroids include but are not limited to alclometasone dipropionate, amcinonide, amcinafel, amcinafide, beclamethasone, betamethasone, betamethasone dipropionate, betamethasone valerate, clobetasone propionate, chloroprednisone, clocortelone, cortisol, cortisone, cortodoxone, difluorosone diacetate, descinolone, desonide, defluprednate, dihydroxycortisone, desoximetasone, dexamethasone, deflazacort, diflorasone diacetate, dichlorisone, esters of betamethasone, flucetonide, flucloronide, fluorocortisone, flumethasone, flunisolide, fluocinonide, fluocinolone acetonide, flucortolone, fluperolone, fluprednisolone, fluroandrenolone acetonide, fluocinolone acetonide, flurandrenolide, fluorametholone, fluticasone propionate, hydrocortisone, hydrocortisone butyrate, hydrocortisone valerate, hydrocortamate, medrysone, meprednisone, methylprednisone, methylprednisolone, mometasone furoate, paramethasone, prednisone, prednisolone, prednidone, triamcinolone acetonide, and triamcinolone.
Hydrocortisone was the first corticosteroid found to be topically effective. Other more potent glucocorticoids, which are a subset of corticosteroids that affect carbohydrate metabolism, inhibit corticotropin secretion, and possess pronounced anti-inflammatory activity, have since been developed. Currently, topical steroids are among the most frequently prescribed of all dermatological drug products.
It is believed that glucocorticoids exert their potent anti-inflammatory effects by inhibiting the formation of prostaglandins and other derivatives of the arachidonic acid pathway. It is known that glucocorticoids inhibit the release of phospholipase A2, the enzyme responsible for liberating arachidonic acid from cell membranes, thus inhibiting the arachidonic acid pathway. Currently, it is believed that glucocorticoids inhibit phospholipase A2, in cells by directly inducing phosphorylation of the enzyme.
Steroids are commonly divided into two classes, fluorinated and nonfluorinated. Fluorinated steroids have been chemically modified to increase potency. These modifications, such as halogenation and methylation, can result in improved activity within the target cell and in decreased breakdown to inactive metabolites. These modifications can also lead to more systemic side effects. However, modification of the chemical structure of the steroid is not the only way to increase potency.
The potency of topical steroid preparations is strongly correlated to their absorption through the skin. Treatment of the skin prior to application of the topical steroid may also affect the absorption of the compounds into the skin. Treatments with keratolytics or with fat solvents (such as acetone) disrupt the epidermal barrier and increase penetration. Hydrating the skin has also been shown to increase the penetration of the corticosteroids.
Once absorbed through the skin, topical corticosteroids are handled through pharmacokinetic pathways similar to systemically administered corticosteroids. The potencies of corticosteroids vary greatly and it is a challenge to increase the potency of any particular steroid.
BACKGROUND OF THE INVENTION
The clinical effectiveness of corticoids is related to four basic properties: vasoconstriction, antiproliferative effects, immunosuppression, and anti-inflammatory effects. Topical steroids cause the capillaries in the superficial dermis to constrict, thus reducing erythema. The ability of a given glucocorticoid agent to cause vasoconstriction usually correlates with its anti-inflammatory potency. Vasoconstrictor assays are used in the art and by the U.S. Food and Drug Administration for determining the potency of topical corticosteroid preparations. Topical glucocorticoid preparations have been divided in the field into seven classes based on potency based on double-blind clinical studies and vasoconstrictor assays. Class 1 includes the most potent, while class 7 contains the least potent.
The following glucocorticoid preparations were designated in Fitzpatrick,
Dermatology in General Medicine,
5
th
edition, CD-ROM, 1999, Table 243-1, with the following classes.
TABLE 1
Corticosteroid
Preparation
Corticosteroid
Class
Source
Temovate ® Cream
Clobetasone
1
Glaxo
0.05%
propionate
Wellcome
Temovate ® ointment
Clobetasone
1
Glaxo
0.05%
propionate
Wellcome
Diprolene ® cream
Betamethasone
1
Schering Corp.
0.05%
dipropionate
Diprolene ® ointment
Betamethasone
1
Schering Corp.
0.05%
dipropionate
Psorcon ® ointment
Diflorasone diacetate
1
Dermik
Laboratories,
Inc.
Cyclocort ® ointment
Amcinonide
2
Fujisawa
0.1%
Diprolene ® cream AF
Betamethasone
2
Schering Corp.
0.05%
dipropionate
Diprosone ® ointment
Betamethasone
2
Schering Corp.
0.05%
dipropionate
Elocon ® ointment 0.1%
Mometasone furoate
2
Schering Corp.
Florone ® ointment
Diflorasone diacetate
2
Dermik
0.05%
Halog ® cream 0.1%
Halcinonide
2
Westwood-
Squibb
Lidex ® gel 0.05%
Fluocinonide
2
Medicis
Pharma-
ceuticals
Corp.
Lidex ® cream 0.05%
Fluocinonide
2
Medicis
Pharma-
ceuticals
Corp.
Lidex ® ointment 0.05%
Fluocinonide
2
Medicis
Pharma-
ceuticals
Corp.
Maxiflor ® ointment
Diflorasone diacetate
2
Allergan
0.05%
Herbert
Topicort ® cream 0.25%
Desoximetasone
2
Medicis
Pharma-
ceuticals
Corp.
Topicort ® gel 0.05%
Desoximetasone
2
Medicis
Pharma-
ceuticals
Corp.
Topicort ® ointment
Desoximetasone
2
Medicis
0.25%
Pharma-
ceuticals
Corp.
Aristocort A ® ointment
Triamcinolone
3
Fujisawa
0.1%
acetonide
Cutivate ® ointment
Fluticasone propionate
3
Glaxo
0.005%
Wellcome
Cyclocort ® cream 0.1%
Amcinonide
3
Fujisawa
Cyclocort ® Lotion
Amcinonide
3
Fujisawa
0.1%
Diprosone ® cream
Betamethasone
3
Schering Corp.
0.05%
dipropionate
Florone ® cream 0.05%
Diflorasone diacetate
3
Dermik
Halog ® ointment 0.1%
Halcinonide
3
Westwood-
Squibb
Lidex ® E cream 0.05%
Fluocinonide
3
Medicis
Pharma-
ceutical
Corp.
Maxiflor ® cream 0.05%
Diflorasone diacetate
3
Allergan
Herbert
Valisone ® ointment
Betamethasone
3
Schering Corp.
0.1%
valerate
Cordran ® ointment
Flurandrenolide
4
Oclassen
0.05%
Elocon ® cream 0.1%
Mometasone furoate
4
Schering Corp.
Kenalog ® cream 0.1%
Triamcinolone
4
Westwood-
acetonide
Squibb
Synalar ® ointment
Fluocinolone acetonide
4
Medicis
0.025%
Pharma-
ceuticals
Corp.
Westcort ® ointment
Hydrocortisone
4
Westwood-
0.2%
valerate
Squibb
Cordran ® cream 0.05%
Flurandrenolide
5
Oclassen
Cutivate ® cream 0.05%
Fluticasone propionate
5
Glaxo
Wellcome
Diprosone ® lotion
Betamethasone
5
Schering Corp.
0.05%
dipropionate
Kenalog ® lotion 0.1%
Triamcinolone
5
Westwood-
acetonide
Squibb
Locoid ® cream 0.1%
Hydrocortisone
5
Ferndale
butyrate
Synalar ® cream 0.025%
Flucinolone acetonide
5
Medicis
Pharma-
ceuticals
Corp.
Valisone ® cream 0.1%
Betamethasone
5
Schering Corp.
valerate
Westcort ® cream 0.2%
Hydrocortisone
5
Westwood-
valerate
Squibb
Aclovate ® cream
Alclometasone
6
Glaxo
0.05%
dipropionate
Wellcome
Aclovate ® ointment
Alclometasone
6
Glaxo
0.05%
dipropionate
Wellcome
Aristocort ® cream 0.1%
Triamcinolone
6
Fujisawa
acetonide
Desowen ® cream
Desonide
6
Galderma
0.05%
Synalar ® solution
Fluocinolone acetonide
6
Medicis
0.01%
Pharma-
ceuticals
Corp.
Synalar ® cream 0.01%
Fluocinolone acetonide
6
Medicis
Pharma-
ceuticals
Corp.
Tridesilon ® cream
Desonide
6
Miles
0.05%
Valisone ® lotion 0.1%
Betamethasone
6
Schering Corp.
vale
Gans Eugene H.
Wortzman Mitchell S.
Feehery Maryellen
McNichol, Jr. William J.
Medicis Pharmaceutical Corporation
Smith LLP Reed
Wang Shengjun
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