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Last Updated: April 18, 2024

Claims for Patent: 5,665,727


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Summary for Patent: 5,665,727
Title: Use of 11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]octacos-18-ene derivatives and pharmaceutical compositions containing them
Abstract:The compounds of formula I, ##STR1## have been found to have excellent topical activity. They are thus indicated for use in the topical treatment of inflammatory and hyperpoliferative skin diseases and of cutaneous manifestations of immunologically-induced illnesses, such as psoriasis.
Inventor(s): Grassberger; Maximilian (Vienna, AT), Meingassner; Josef Gottfried (Perchtoldsdorf, AT), Stutz; Anton (Vienna, AT), Stutz; Peter (Vienna, AT)
Assignee: Sandoz Ltd. (Basel, CH)
Application Number:08/291,010
Patent Claims: 1. A method of topically treating inflammatory or hyperproliferative skin diseases or cutaneous manifestations of immunologically-mediated illnesses, in a mammal in need of said treatment, which comprises administering topically to said mammal in an amount effective for the treatment of inflammatory or hyperproliferative skin diseases or cutaneous manifestations of immunologically mediated illnesses a compound of formula I ##STR4## wherein R.sup.1 is optionally protected hydroxy,

R.sup.2 is hydrogen or optionally protected hydroxy,

R.sup.3 is methyl, ethyl, propyl or allyl,

n is 1 or 2 and

the symbol of a line and dotted line is a single bond or a double bond,

in free form or in pharmaceutically acceptable salt form.

2. A method according to claim 1, wherein

R.sup.3 is propyl or allyl,

in free form or in pharmaceutically acceptable salt form.

3. A method according to claim 1,

wherein R.sup.1 and R.sup.2 are hydroxy,

R.sup.3 is allyl,

n is 2, and

the symbol of a line and dotted line is a single bond,

in free form.

4. A method according to claim 1 in which the compound is ##STR5## in free form.

5. A method according to claim 1 in which the compound is administered 2 to 5 times daily in the form of a lotion, gel, or cream comprising 1 to 3% of the compound.

6. A method of topically treating atopical dermatitis, contact dermatitis, eczematous dermatitises, seborrhoeic dermatitis, Lichen planus, Pemphigus, bullous Pemphigoid, Epidermolysis bullosa, urticaria, angioedemas, vasculitides, erythemas, cutaneous eosinophilias, or Alopecia areata in a mammal in need of said treatment, which comprises administering topically to said mammal in an amount effective for the treatment of atopical dermatitis, contact dermatitis, eczematous dermatitises, seborrhoeic dermatitis, Lichen planus, Pemphigus, bullous Pemphigoid, Epidermolyeis bulloea, urticaria, angioedemaes, vasculitides, erythomas, cutaneous eosinophilias, or Alopecia areata a compound of formula I ##STR6## wherein R.sup.1 is optionally protected hydroxy,

R.sup.2 is hydrogen or optionally protected hydroxy,

R.sup.3 is methyl ethyl, propyl or allyl,

n is 1 or 2 and

the symbol of a line and dotted line is a single bond or a double bond,

in free form or in pharmaceutically acceptable salt form.

7. A method according to claim 6, wherein

R.sup.3 is propyl or allyl,

in free form or in pharmaceutically acceptable salt form.

8. A method according to claim 6,

wherein

R.sup.1 and R.sup.2 are hydroxy,

R.sup.3 is allyl,

n is 2, and

the symbol of a line and dotted line is a single bond,

in free form.

9. A method according to claim 6 in which the compound is ##STR7## in free form.

10. A method according to claim 6 in which the compound is administered 2 to 3 times daily in the form of a lotion, gel, or cream comprising 1 to 3% of the compound.

11. A method of topically treating atopical dermatitis, contact dermatitis, eczematous dermatitises, or seborrhoeic dermatitis in a mammal in need of said treatment, which comprises administering topically to said mammal in an amount effective for the treatment of atopical dermatitis, contact dermatitis, eczematous dermatitises, or seborrhoeic dermatitis a compound of formula I ##STR8## wherein R.sup.1 is optionally protected hydroxy,

R.sup.2 is hydrogen or optionally protected hydroxy,

R.sup.3 is methyl, ethyl, propyl or allyl,

n is 1 or 2 and

the symbol of a line and dotted line is a single bond or a double bond,

in free form or in pharmaceutically acceptable salt form.

12. A method according to claim 11, wherein

R.sup.3 is propyl or allyl

in free form or in pharmaceutically acceptable salt form.

13. A method according to claim 11,

wherein

R.sup.1 and R.sup.2 are hydroxy,

R.sup.3 is allyl,

n is 2, and

the symbol of a line and dotted line is a single bond,

in free form.

14. A method according to claim 11 in which the compound is ##STR9## in free form.

15. A method according to claim 11 in which the compound is administered 2 to 5 times daily in the form of a lotion, gel, or cream comprising 1 to 3% of the compound.

16. A method according to claim 11 of topically treating atopical dermatitis.

17. A method according to claim 11 of topically treating contact dermatitis or eczematous dermatitises.

18. A method according to claim 11 of topically treating seborrhoeic dermatitis.

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