C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 1/04 (2006.01) C07K 1/10 (2006.01)
Patent
CA 2579631
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 more 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 hydroxymethylobenzoic acid, or esters formed by carboxy groups of aspartic or glutamic acid.
La présente invention a trait à des lieurs faisant intervenir des liaisons ester, en particulier des liaisons de l'ester d'acide iminodiacétique, destinés à des utilisations dans la synthèse peptidique en phase solide. De manière plus précise, l'invention concerne des lieurs clivables pouvant libérer les peptides d'un support en phase solide dans des conditions relativement douces par formation d'une dicétopipérazine ou d'une autre structure cyclique, de telle sorte que la structure cyclique demeure sur le support solide, puis par un second clivage dans des conditions plus rigoureuses, à pH élevé. L'invention a en outre trait à des supports en phase solide préparés avec de multiples lieurs clivables, dont un lieur qui est clivé par formation d'un produit cyclique. Ces lieurs peuvent être des esters d'acide hydroxyméthylbenzoïque, ou des esters formés à partir des groupements carboxy de l'acide aspartique ou de l'acide glutamique.
Kocis Petr
Krchnak Viktor
Lam Kit S.
Lebl Michal
Aventis Pharmaceuticals Inc.
Aventisub II Inc.
Osler Hoskin & Harcourt Llp
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