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Title:
BIOMIMETIC COMBINATORIAL SYNTHESIS
Document Type and Number:
WIPO Patent Application WO1999064379
Kind Code:
A3
Abstract:
The present invention provides biomimetic compounds and libraries thereof, as well as methods for their production. In general, the inventive method involves the selection of a desired biological synthetic pathway and mimics that synthetic pathway utilizing modern synthetic tools. The structures formed from this method are preferably generated in fewer than four steps. These scaffold structures can than be functionalized to yield biomimetic compounds and libraries of compounds. In preferred embodiments, biomimetic compounds and libraries are generated from an oxidative phenolic coupling reaction. In other particularly preferred embodiments, the compounds and libraries of compounds are generated from cascade reactions to yield bicyclo [n.3.1] ring systems, medium ring systems, and fused ring systems. In addition to compounds, libraries and methods for their production, the present invention also provides pharmaceutical compositions and methods and kits for determining one or more biological activities of the library members.

Inventors:
LINDSLEY CRAIG W
CHEN CHUO
SHAIR MATTHEW D
WESTWOOD NICHOLAS J
CHAN LAWRENCE K
PELISH HENRY EFRAM
SHEEHAN SCOTT M
GOESS BRIAN C
LAYTON MARK E
Application Number:
PCT/US1999/012942
Publication Date:
August 03, 2000
Filing Date:
June 11, 1999
Export Citation:
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Assignee:
HARVARD COLLEGE (US)
International Classes:
C07B61/00; C07D311/78; C07D498/12; (IPC1-7): C07B61/00; A61K31/00; C07D311/78; C07D313/00; C07D471/06; C07D493/10; G01N33/50
Domestic Patent References:
WO1997035199A11997-09-25
Other References:
CORNIA, MARA ET AL: "Oxygen heterocycles by oxidation of ortho-alkylphenols. Oxidation of ortho-propenylphenols", GAZZ. CHIM. ITAL. (1977), 107(5-6), 299-304, XP000874250
JAKUPOVIC, J. ET AL: "Benzoxanthenone derivatives from Polemannia montana", PHYTOCHEMISTRY (1987), 26(8), 2427-9, XP000874710
IYER, MEERA R. ET AL: "Silver(I) oxide catalyzed oxidation of o-allyl- and o-(1-propenyl)phenols", BULL. CHEM. SOC. JPN. (1992), 65(6), 1662-4, XP002132445
MATSUMOTO, MASAKATSU ET AL: "Transition metal(II) Schiff's base complexes catalyzed oxidation of trans-2-(1-propenyl)-4,5-methylenedioxyphenol to carpanone by molecular oxygen", TETRAHEDRON LETT. (1981), 22(44), 4437-40, XP002132446
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