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Title:
METHODS FOR PREPARATION OF MACROCYCLIC MOLECULES MACROCYCLIC MOLECULES PREPARED THEREBY AND SUBSTRATES AND SOLID SUPPORTS FOR USE THEREIN
Document Type and Number:
WIPO Patent Application WO2003040094
Kind Code:
A3
Abstract:
The invention features a new solid supports having at least one amino functionality and a linker bound to the solid support through at least a portion of the amino functional groups. The invention also features solid support bound substrates suitable for use in the formation of macrocycles by a TE domain catalyzed macrocyclization reaction. The invention features methods of making the solid supports and solid support bound substrates of the invention and methods of effecting macrocyclizations of solid support bound substrates. The invention further provides new macrocyclic molecules having one or more peptide domains and one or more polyketide domains in the macrocyclic ring. In another embodiment of the invention, libraries of macrocycles are provided as well as methods of forming libraries of macrocycles from libraries of solid support bound substrates are provided.

Inventors:
WALSH THOMAS CHRISTOPHER
KOHLI RAHUL MANU
BURKART MICHAEL D
BURKE MARTIN D
Application Number:
PCT/US2002/035487
Publication Date:
February 12, 2004
Filing Date:
November 06, 2002
Export Citation:
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Assignee:
HARVARD COLLEGE (US)
International Classes:
C07B61/00; C07H17/08; C07K1/04; C07K7/50; C07K7/64; C07K14/00; C08G63/48; C08G63/91; (IPC1-7): A61K31/15; A61K31/33; C07D233/00; C07D245/00; C07D267/22
Other References:
KOHLI ET AL.: "Biomimetic synthesis and optimization of cyclic peptide antibiotics", NATURE, vol. 418, 8 August 2002 (2002-08-08), pages 658 - 661, XP002966195
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