TREATMENT AND PREVENTION OF BENIGN PIGMENTED MOLES (NAEVI) USING ARTEMISININE AND THE DERIVATIVES THEREOF

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Patent No.: US None
App. No.: 13/223,776

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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 (35)

1 . A plaster comprising a topical formulation which comprises one or more active agents, wherein the one or more active agents comprise at least one compound 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-hydro artemisinyl;

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 plaster of claim 1 , wherein X represents CHOZ, Z is selected from m- and p-CH 2 (C 6 H 4 )COOM and COR 3 ; and R 3 represents —(CH 2 ), —COOM.

3 . The plaster 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.

4 . The plaster of claim 1 , wherein the one or more compounds of formula (I) comprise at least one compound selected from artemisinine, dihydroartemisinine, and artesunate.

5 . The plaster of claim 1 , wherein the one or more compounds of formula (I) comprise artesunate.

6 . The plaster of claim 1 , wherein the topical formulation comprises at least one of a paste, an ointment, a suspension, a solution, a gel, a spray, and a cream.

7 . A method of treating a benign pigmented mole or a dermatomycosis, 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;

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

8 . The method of claim 7 , wherein the topical formulation is applied in conjunction with a plaster.

9 . The method of claim 7 , wherein mycosis pedis or nail fungus is treated.

10 . The method of claim 7 , wherein the method further comprises a prevention of cancer.

11 . The method of claim 7 , 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.

12 . The method of claim 7 , 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.

13 . The method of claim 7 , wherein the one or more compounds of formula (I) comprise at least one compound selected from artemisinine, dihydroartemisinine, and artesunate.

14 . The method of claim 7 , wherein the one or more compounds of formula (I) comprise artesunate.

15 . The method of claim 7 , wherein the one or more compounds of formula (I) are applied in a form of a topical formulation.

16 . The method of claim 15 , wherein the topical formulation comprises at least one of a paste, an ointment, a suspension, a solution, a gel, a spray, and a cream.

17 . The method of claim 16 , wherein the topical formulation comprises an ointment and loss of moisture from skin is prevented by application of the ointment.

Assignments (1)

CHANGE OF NAME Recorded Jul 18, 2012

From: EPIPHARM GMBH

To: EPIPHARM AG

Reel/Frame 028584/0329 →