Treatment and prevention of benign pigmented moles (naevi)...

A - Human Necessities – 61 – K

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A61K 31/357 (2006.01) A61K 9/70 (2006.01) A61K 31/366 (2006.01) A61L 15/44 (2006.01) A61P 17/00 (2006.01) C07D 493/18 (2006.01)

Patent

CA 2626704

Benign pigmented moles or athlete's foot or ringworm of the nails can be treated with locally applicable, especially topically formulated active ingredients of formula (I) wherein X represents CO, CHOZ or CHNRZ, Z is selected from hydrogen, linear or branched (C1-C6) alkyl, linear or branched (C2-C6) alkenyl, linear or branched (C2-C6) alkynyl, (C3-C8) cycloalkyl, (C6- C24) aryl, (C7-C24) aralkyl, m- und p- represent CH2(C6H4)COOM; COR3; CSR3; C (NR6) R3; SOR4; SO2OM; SO2NR7R8; SO2O- artemisinyl; SO2NH-artemisinyl; POR4R5 and PSR4R5; R3 represents a linear or branched (C1-C6) alkyl, a linear or branched (C1-C6) alkoxy; a linear or branched (C2-C6) alkenyl; a linear or branched (C2-C6) alkynyl; (C3-C8) cycloalkyl; (C6-C24) aryl; (C6-C10) aryloxy; (C7-C24) aralkyl; -(CH2)n-COOM, where n represents a whole number between 1 and 6; or 10a-dihydroartemisinyl; R4 and R5 are independently selected from linear or branched (C1-C6) alkyl; linear or branched (C2-C6) alkenyl; linear or branched (C2-C6) alkynyl; (C3-C8) cycloalkyl; (C6-C24) aryl; (C7-C24) aralkyl; OM; linear or branched (C1-C6) alkoxy; (C6-C10) aryloxy and NR7R8; R6 is selected from linear or branched (C1-C6) alkyl; linear or branched (C2-C6) alkenyl; linear or branched (C2-C6) alkynyl; (C3-C8) cycloalkyl; (C6-C24) aryl and (C7-C24) aralkyl; M represents hydrogen or a pharmaceutically acceptable cation; and R7 and R8 independnetly represent hydrogen or a linear or branched (C1-C6) alkyl, or R7 and R8 together form am alkylene bridge (C4-C6); and R is selected from hydrogen and the groups cited for R6. Said compounds are also effective in the prevention of acquired Naevus cell naevi.

L'invention concerne des manifestations pigmentaires bénignes de la peau ou des champignons des pieds ou des ongles pouvant être traités par des agents, de formule (I), formulés sous forme topique et pouvant être appliqués localement. Dans cette formule, X représente CO, CHOZ ou CHNRZ, Z est sélectionné parmi hydrogène, alkyle (C1-C6) ramifié ou linéaire, alcényle (C2-C6) ramifié ou linéaire, alcynyle (C2-C6) ramifié ou linéaire, cycloalkyle (C3-C8), aryle (C6-C24), aralkyle (C7-C24) ; m et p représentent CH2(C6H4)COOM; COR3; CSR3; C (NR6) R3; SOR4; SO2OM; SO2NR7R8; SO2O- Artémisinyle; SO2NH-Artémisinyle; POR4R5 et PSR4R5 ; R3 représente alkyle (C1-C6) ramifié ou linéaire, alcoxy (C1-C6) ramifié ou linéaire, alcényle (C2-C6) ramifié ou linéaire, alcynyle (C2-C6) ramifié ou linéaire, cycloalkyle (C3-C8), aryle (C6-C24), aryloxy (C6-C10), aralkyle (C7-C24), -(CH2)n-COOM comprenant n représentant un nombre entier compris entre 1 et 6 ou 10a-Dihydroartémisinyle ; R4 et R5 représentent indépendamment l'un de l'autre alkyle (C1-C6) ramifié ou linéaire, alcényle (C2-C6) ramifié ou linéaire, alcynyle (C2-C6) ramifié ou linéaire, cycloalkyle (C3-C8) ramifié ou linéaire, aryle (C6-C24), aralkyle (C7-C24) ; OM, alcoxy (C1-C6) ramifié ou linéaire, aryloxy (C6-C10) et NR7R8 ; R6 est sélectionné parmi alkyle (C1-C6) ramifié ou linéaire, alcynyle (C2-C6), cycloalkyle (C3-C8), aryle (C6-C24), aralkyle (C7-C24) ; M représente hydrogène ou un cation pharmaceutiquement acceptable ; et R7 et R8 représentent ensemble un pont alcylène (C4-C6) ; et R est sélectionné entre hydrogène et les groupes constituant R6. Les composés de l'invention sont également utilisés dans la prévention de naevus comportant des cellules naevus acquis.

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