Novel echinocandin derivatives, preparation method and use...

C - Chemistry – Metallurgy – 07 – K

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C07K 7/56 (2006.01) A61K 38/12 (2006.01) A61P 31/10 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2402219

The invention concerns compounds of general formula (I) wherein: R¿1? represents a hydrogen atom, a hydroxy radical, Ob or Ncd; A represents an oxygen atom, a CH¿2? radical or a NH radical; B represents the radical of a steroid; R¿3? represents a hydrogen atom, a methyl or hydroxyl radical; R¿4? represents a hydrogen atom or a hydroxyl radical; T represents a hydrogen atom, a methyl radical, a CH¿1?CONH¿2?, CH¿2?C.ident.N radical, a (CH¿2?)¿2?NH¿2? or (CH¿2?)2Nalk?+¿X?-¿radical; X being a halogen atom and alc an alkyl radical; Y represents a hydrogen atom, a hydroxyl radical or a halogen atom or a OSO¿3?H radical; W represents a hydrogen atom or a OH radical; Z represents a hydrogen atom or a methyl radical. The compounds of formula (I) exhibit antifungal properties.

L'invention a pour objet les composés de formule générale (I) dans lesquels: R1 représente un atome d'hydrogène, un radical hydroxy, Ob ou Ncd; A représente un atome d'oxygène, un radical CH2 ou un radical NH; B représente le reste d'un stéroïde; R3 représente un atome d'hydrogène, un radical méthyle ou hydroxyle; R4 représente un atome d'hydrogène ou un radical hydroxyle; T représente un atome d'hydrogène, un radical méthyle, un radical CH1CONH2, CH2C.ident.N, un radical (CH2)2NH2 ou (CH2)2Nalc+X-; X étant un atome d'halogène et alc un radical alkyle; Y représente un atome d'hydrogène, un radical hydroxyle ou un atome d'halogène ou un radical OSO3H; W représente un atome d'hydrogène ou un radical OH; Z représente un atome d'hydrogène ou un radical méthyle. Les composés de formule (I) sont doués de propriétés antifongiques.

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