Use of amide derivative of GE 2270 factor A
Use of the compound of formula (I) and the pharmaceutically acceptable addition salts thereof for the manufacture of a medicament for topical treatment or 5 prevention of acne formula (I) wherein: R represents methoxymethyl, R1 represents methyl, Rz represents methyl, Y represents the group formula (II) The compound of formula (I) and the pharmaceutically acid addition salts thereof show selective activity against propionibacterium acne and are suitable for use in a method of treatment or prevention of acne.
1. A medicament for use in the topical treatment of acne which comprises a compound of formula (I)
wherein:
R represents methoxymethyl,
R 1 represents methyl,
R 2 represents methyl,
Y represents the group
and the pharmaceutically acceptable acid addition salts thereof, wherein said compound inhibits the growth of Propionibacterium acnes strain at dosages that are inactive against gram-positive bacteria that normally colonize the skin surface.
2. The medicament as in claim 1 , wherein the gram-positive bacteria that normally colonize the skin surface are selected from the group consisting of Staphylococcus aureus, Staphylococcus epidermis , and Streptococcus pyogenes.
3. The medicament as in claim 1 , wherein the gram-positive bacteria that normally colonize the skin surface are resistant to a broader spectrum antibiotic.
4. A method for treating acne which comprises topically administering a compound of formula (I)
wherein:
R represents methoxymethyl,
R 1 represents methyl,
R 2 represents methyl,
Y represents the group
or a pharmaceutically acceptable acid addition salt thereof to a patient affected by or exposed to said skin disorder, in an amount sufficient to provide inhibitory activity or proliferation of Propionibacterium acne , wherein said compound inhibits the growth of Propionibacterium acnes strain at dosages that are inactive against other gram-positive bacteria that normally colonize the skin surface.
5. The method as in claim 4 , wherein the gram-positive bacteria that normally colonize the skin surface are selected from the group consisting of Staphylococcus aureus, Staphylococcus epidermis , and Streptococcus pyogenes.
6. The method as in claim 4 , wherein the gram-positive bacteria that normally colonize the skin surface are resistant to a broader spectrum antibiotic.
7. The method as in claim 6 , wherein the broader spectrum antibiotic is selected from the group consisting of erythromycin, tetracycline, and clindamycin.
8. The method as in claim 4 , further comprising the step of administering an additional component that has auxiliary action in the treatment of acne or provides skin benefits.
9. The method as in claim 8 , wherein the additional component that has auxiliary action in the treatment of acne or provides skin benefits is selected from the group consisting of an antibiotic, antimicrobial, comedolytic agent, non-steroidal anti-inflammatory agent, steroidal anti-inflammatory agent, vitamin, oil or sebum control agent, skin healing agent, and skin conditioning agent.
10. The method as in claim 9 , wherein the antibiotic is selected from the group consisting of erythromycin, tetracycline, and clindamycin.
11. The method as in claim 9 , wherein the antimicrobial is selected from the group consisting of chlorexidine, benzoylperoxide, 1-pentadecanol, cedrene, caryophyllene, longifolene, thujopsene, and derivatives thereof.
12. The method as in claim 9 , wherein the comedolytic agent is selected from the group consisting of tretinoin, adapalene, azelaic acid, tazarotene, salicylic acid, and derivatives thereof.
13. The method as in claim 9 , wherein the non-steroidal anti-inflammatory agent is selected from the group consisting of acetylsalicylic acid, ibuprofen, naproxen, and sulfacetamide.
14. The method as in claim 9 , wherein the steroidal anti-inflammatory agent is hydrocortisone.
15. The method as in claim 9 , wherein the vitamin is retinoic acid.
16. The method as in claim 9 , wherein the oil or sebum control agent is clay silicone.
17. The method as in claim 4 , wherein the compound of formula (I) or a pharmaceutically acceptable acid addition salt thereof is incorporated into a pharmaceutical composition suitable for topical administration in an amount ranging from about 0.1 to 10 percent by weight of said pharmaceutical composition.
18. The method as in claim 17 , wherein the pharmaceutical composition is in the form of a cream, lotion, mousse, spray, emulsion or gel.
19. The method as in claim 4 , wherein the pharmaceutically acceptable acid addition salts are salts with hydrochloric acid or lactic acid.
20. The method as in claim 17 , wherein the pharmaceutical composition includes a pharmaceutically acceptable excipient.