Novel echinocandin derivatives, method for preparing same...

Details Novel echinocandin derivatives, method for preparing same... Novel echinocandin derivatives, method for preparing same...

C - Chemistry, Metallurgy

07

K

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

Patent

CA 2376490

The invention concerns compounds of formula (I) wherein: either R¿1? and R¿2? = H, OH, alkyl optionally substituted, or NR¿1? forms with the carbon bearing NR¿1?R¿2? a double bond and R¿2? is XRa, X being O, NH or N-alkyl and Ra being H, alkyl optionally substituted, or R¿2? is e-N = C(-N-d)-N(f)-g; R¿3? = H, OH, CH¿3?; R¿4? = H, OH; R = chain containing up to 30 carbon atoms, optionally containing one or several heteroatoms, one or several heterocycles; T = H, CH¿3?, CH¿2?CONH¿2?, CH¿2?C≡N, (CH¿2?)¿2?NH¿2?, (CH¿2?)¿2?Nalk?+¿X?-¿; Y = H, OH, halogen, OSO¿3?H; W = H, OH; Z = H or CH¿3?. The products have antifungal properties.

L'invention a pour objet les composés de formule (I), dans lesquels ou bien R1 et R2 = H, OH, alkyle éventuellement substitué, ou bien NR1 forme avec le carbone portant NR1R2 une double liaison et R2 est XRa, X étant O, NH ou N- alkyle et Ra étant H, alkyle éventuellement substitué, ou R2 est e-N=C(-N-d)- N(f)-g; R3 = H, OH, CH3; R4 = H, OH; R = chaîne renfermant jusqu'à 30 atomes de carbone, renfermant éventuellement un ou plusieurs hétéroatomes, un ou plusieurs hétérocycles, T = H, CH3, CH2CONH2, CH2C≡N, (CH2)2NH2, (CH2)2Nalc+X-; Y = H, OH, Halogène, OSO3H; W = H, OH; Z = H ou CH3. Les produits présentent des propriétés antifongiques.

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