C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 1/04 (2006.01)
Patent
CA 2165780
The present invention is directed to linkers based on ester bond linkages, especially iminodiacetic acid ester bond linkages, for use in solid phase peptide synthesis. In particular, the invention is directed to cleavable linkers that can release peptide from the solid phase support under relatively mild conditions by formation of a diketopiperazine or other cyclic structure, such that the cyclic structure remains on the solid phase support, and, in a second cleavage, under mole stringent conditions of high pH. The invention is further directed to solid phase supports prepared with multiple cleavable linkers, including a linker that is cleaved by formation of a cyclic product. One such second linker is an ester of hydroxymethylbenzoic acid, or esters formed by carboxy groups of aspartic or glutamic acid.
La présente invention concerne l'utilisation d'éléments de liaison faisant intervenir des liaisons ester, en particulier les liaisons ester de l'acide iminodiacétique, pour la synthèse de peptides en phase solide. En particulier, l'invention concerne des éléments de liaison pouvant subir une première scission pour libérer le peptide de la phase solide de support dans des conditions relativement douces avec formation d'une dicétopipérazine ou d'une autre structure cyclique où la structure cyclique reste sur la phase solide de support, et une seconde scission dans des conditions plus dures de pH élevé. L'invention concerne également des supports de phase solide préparés avec des éléments de liaison multiples pouvant être coupés, comprenant un élément de liaison qui est coupé avec formation d'un produit cyclique. Comme autres exemples de ces éléments de liaison, on peut citer un ester d'acide hydroxyméthylbenzoïque ou un ester formé par les groupes carboxy de l'acide aspartique ou glutamique.
Kocis Petr
Krchnak Viktor
Lam Kit S.
Lebl Michal
Aventisub II Inc.
Osler Hoskin & Harcourt Llp
Selectide Corporation
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