IP Library Granted Patent US 8,013,011
Granted Patent B2
US 8,013,011 · App. 12/089,773 · Granted Sep 6, 2011

Treatment and prevention of benign pigmented moles (naevi) using artemisinine and the derivatives thereof

Assignee: EPIPHARM GmbH
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Quick Facts
Patent No.
US 8,013,011
App. No.
12/089,773
Granted
Sep 6, 2011
Kind
B2
Abstract

A method of treating a benign pigmented mole or a dermatomycosis. The method comprises locally applying to a subject in need thereof artemisinine and/or one or more structurally related compounds. Also disclosed is a plaster which comprises a topical formulation comprising artemisinine and/or one or more structurally related compounds.

Claims (22)

1. A method of treating at least one benign pigmented mole, wherein the method comprises locally applying to a subject in need thereof one or more compounds of formula (I):

wherein:

X represents CO, CHOZ or CHNRZ;

Z is selected from hydrogen; straight-chain and branched (C 1 -C 6 ) alkyl; straight-chain or branched (C 2 -C 6 ) alkenyl; straight-chain or branched (C 2 -C 6 ) alkynyl; (C 3 -C 8 ) cycloalkyl; (C 6 -C 24 ) aryl; (C 7 -C 24 ) aralkyl; m- and p-CH 2 (C 6 H 4 )COOM; COR 3 ; CSR 3 ; C(NR 6 )R 3 ; SOR 4 ; SO 2 OM; SO 2 NR 7 R 8 ; SO 2 O-artemisinyl; SO 2 NH-artemisinyl; POR 4 R 5 ; and PSR 4 R 5 ;

R 3 is selected from straight-chain or branched (C 1 -C 6 ) alkyl; straight-chain or branched (C 1 -C 6 ) alkoxy; straight-chain or branched (C 2 -C 6 ) alkenyl; straight-chain or branched (C 2 -C 6 ) alkynyl; (C 3 -C 8 ) cycloalkyl; (C 6 -C 24 ) aryl; (C 6 -C 10 ) aryloxy; (C 7 -C 24 ) aralkyl; —(CH 2 ) n —COOM, with n being an integer of from 1 to 6; and 10α-di-hydroartemisinyl;

R 4 and R 5 are independently selected from straight-chain or branched (C 1 -C 6 ) alkyl; straight-chain or branched (C 2 -C 6 ) alkenyl; straight-chain or branched (C 2 -C 6 ) alkynyl; (C 3 -C 8 ) cycloalkyl; (C 6 -C 24 ) aryl; (C 7 -C 24 ) aralkyl; OM; straight-chain or branched (C 1 -C 6 ) alkoxy; (C 6 -C 10 ) aryloxy; and NR 7 R 8 ;

R 6 is selected from straight-chain or branched (C 1 -C 6 ) alkyl; straight-chain or branched (C 2 -C 6 ) alkenyl; straight-chain or branched (C 2 -C 6 ) alkynyl; (C 3 -C 8 ) cycloalkyl; (C 6 -C 24 ) aryl; and (C 7 -C 24 ) aralkyl;

M represents hydrogen or a pharmaceutically acceptable cation;

R 7 and R 8 are independently selected from straight-chain or branched (C 1 -C 6 ) alkyl, or R 7 and R 8 together form a (C 4 -C 6 ) alkylene bridge; and

R is selected from hydrogen; straight-chain or branched (C 1 -C 6 ) alkyl; straight-chain or branched (C 2 -C 6 ) alkenyl; straight-chain or branched (C 2 -C 6 ) alkynyl; (C 3 -C 8 ) cycloalkyl; (C 6 -C 24 ) aryl; and (C 7 -C 24 ) aralkyl.

2. The method of claim 1 , wherein the one or more compounds of formula (I) are applied in a form of a topical formulation.

3. The method of claim 2 , wherein the topical formulation comprises at least one of a paste, an ointment, a suspension, a solution, a gel, a spray, and a cream.

4. The method of claim 3 , wherein the topical formulation comprises an ointment and loss of moisture from skin is prevented by application of the ointment.

5. The method of claim 2 , wherein the topical formulation is applied in conjunction with a plaster.

6. The method of claim 1 , wherein the at least one benign pigmented mole is selected from one or more of acquired nevus cell nevi; congenital nevus cell nevi, disorders of melanin pigmentation, and pigmented moles of the mucous membranes.

7. The method of claim 6 , wherein the at least one benign pigmented mole comprises an acquired nevus cell nevi.

8. The method of claim 6 , wherein the at least one benign pigmented mole comprises a congenital nevus cell nevi.

9. The method of claim 6 , wherein the at least one benign pigmented mole is selected from one or more of birthmarks, liver spots, sun spots and age spots.

10. The method of claim 1 , wherein the one or more compounds of formula (I) comprise at least one compound wherein X is CHOZ, Z is selected from m- and p-CH 2 (C 6 H 4 )COOM and COR 3 ; and R 3 represents —(CH 2 ) n —COOM.

11. The method of claim 1 , wherein the one or more compounds of formula (I) comprise at least one compound selected from artemisinine; dihydroartemisinine; carboxyl group containing derivatives of formula (I); artemether; arteether; propyl carbonate of dihydroartemisinine, and artelinic acid.

12. The method of claim 11 , wherein the one or more compounds of formula (I) comprise at least one compound selected from artemisinine, dihydroartemisinine, and artesunate.

13. The method of claim 11 , wherein the one or more compounds of formula (I) comprise artesunate.

Assignments (2)
CHANGE OF NAME Recorded Jul 18, 2012
From: EPIPHARM GMBH
To: EPIPHARM AG
Reel/Frame 028584/0329 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 2, 2008
From: SIFT CARTER, ROSEMARIE
To: EPIPHARM GMBH
Reel/Frame 021182/0151 →
Priority Claims (2)
CH 1686/05 · Oct 20, 2005 · national
CH 0514/06 · Mar 30, 2006 · national
Continuity (1)
Related Publication 20080255223A1 · Oct 16, 2008