Gem difluorinated c-glycopeptides, their preparation and...

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 9/00 (2006.01) A01N 1/02 (2006.01) A61K 38/14 (2006.01)

Patent

CA 2588801

The invention concerns a gem-difluorinated C-glycopeptide compound of formula (I) in which N is an integer between 1 and 5, R4= H, AA1, AA1-AA2 and R5= OH, AA1, AA1.AA2, with AA1, and AA2 are independents and representing amino acids with a non-functionalised side chain and R1, R2, R3 are independent groups and one of them is egal to formula (II), in which n is an integer between 3 and 4, Y, Y' are independent groups in which Y, Y'= H, OR, N3, NR'R", SR~", where R = H, benzyl, trimethylsilyl, tert-butyldimethylsilyl, tert-butyldiphenylsilyl, acetate group, R', R" = H, alkyl, allyl, benzyl, tosylate group, C(=0)-alkyl, C(=O)-Bn, R"' = H, alkyl, acetate group, R6 is notably a group H, CH3, CH2OH, CH2-Glycoside group, CH2-OGP in which GP is a protector group such as an alkyl, benzyl, trimethylsilyl, tert-butyldimethylsilyl, tert~butyldiphenylsilyl, acetate group, and R7 = OH, OGP', NH2, N3, NHGP', NGP'GP" in which GP' and GP" is or not a protector group such as an alkyl, benzyl, trimethylsilyl, tert~butyldimethylsilyl, tert-butyldiphenylsilyl, acetate group, and RB is a hydrogen atom H or a free or protected alcohol function. It applies notably to preservation of biological materials and to cryosurgery.

L'invention concerne un composé de C-glycopeptide gem-difluoré représenté par la formule (I), dans laquelle N représente un nombre entier allant de 1 à 5, R4= H, AA1, AA1-AA2 et R5= OH, AA1, AA1-AA2, AA1, et AA2 étant indépendants et représentant des acides aminés comportant une chaîne latérale non fonctionnalisée, et R1, R2, R3 sont des groupes indépendants, dont l'un correspond à la formule (II), dans laquelle n représente un nombre entier entre 3 et 4, Y, Y' sont des groupes indépendants dans lesquels Y, Y'= H, OR, N3, NR'R", SR'", où R = un groupe H, benzyle, triméthylsilyle, tert-butyldiméthylsilyle, tert-butyldiphénylsilyle, acétate, R', R" = H ou un groupe alkyle, allyle, benzyle, tosylate, C(=0)-alkyle, C(=O)-Bn, R"' = H ou un groupe alkyle, acétate, R6 représente notamment un groupe H, CH3, CH2OH, CH2-glycoside, CH2-OGP dans lequel GP est un groupe protecteur tel qu'un groupe alkyle, benzyle, triméthylsilyle, tert-butyldiméthylsilyle, tert-butyldiphénylsilyle, acétate, et R7 = OH, OGP', NH2, N3, NHGP', NGP'GP", GP' et GP" pouvant éventuellement être un groupe protecteur tel qu'un groupe alkyle, benzyle, triméthylsilyle, tert-butyldiméthylsilyle, tert-butyldiphénylsilyle, ou acétate, et R8 représentant un atome d'hydrogène, H, ou une fonction alcool libre ou protégée. Les applications de ce composé comprennent notamment la conservation de matières biologiques, et la cryochirurgie.

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