C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 17/00 (2006.01) C07B 61/00 (2006.01) C07H 3/06 (2006.01) C07H 21/00 (2006.01) C07K 1/04 (2006.01)
Patent
CA 2195321
The present invention relates to novel soluble combinatorial libraries, comprising a soluble phase in solution attached to a core molecule, and allowing the improved high-yield and efficient production of soluble combinatorial libraries. Some specific examples of the soluble combinatorial libraries claimed herein comprise one or more of the following: amino acids, .alpha.-azetide amino acids, triazine dione molecules, .gamma.-lactamtide molecules, .delta.-lactamthiotide molecules, .beta.-lactam nucleus containing molecules, lycoramine alkaloid nucleus containing molecules, and .beta.- blocker nucleus molecules. Further, a split synthesis technique for generating librairies of combinatorial molecules employs a biphasic macromolecular support which is soluble during the pooling, splitting, and coupling steps but which is insoluble during the washing step. The use of a biphasic macromolecular support in its soluble phase significantly enhances the efficiency and performance of the pooling, splitting, and coupling steps. The use of a biphasic macromolecular support in its insoluble phase significantly enhances the efficiency and performance of the washing step.
La présente invention concerne de nouvelles banques combinatoires solubles, comprenant une phase soluble en solution fixée à une molécule-coeur, et permettant la production efficace et à rendement élevé de banques combinatoires solubles. Des exemples spécifiques de banques combinatoires solubles comprennent un ou plusieurs des éléments suivants: acides aminés, acides aminés .alpha.-azétide, molécules de triazine dione, molécules de .gamma.-lactamtide, molécules de .sigma.-lactamthiotide, molécules contenant un noyau .beta.-lactam, des molécules contenant un noyau lycoramine alcaloïde, et des molécules à noyau .beta.-bloquant. En outre, une technique de synthèse par fractionnement pour générer des banques de molécules combinatoires utilise un support macromoléculaire biphasique qui est soluble pendant les étapes de groupement, division et couplage, mais insoluble pendant l'étape de lavage. L'utilisation d'un support macromoléculaire biphasique dans sa phase soluble améliore significativement l'efficacité et la performance des étapes de groupement, de division et de couplage, et améliore également l'efficacité et la performance de l'étape de lavage dans sa phase insoluble.
Hyunsoo Han
Janda Kim
Scripps Research Institute (the)
Smart & Biggar
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