Synthesis of derivatives of ginkgolide C

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C514S443000

Reexamination Certificate

active

07429670

ABSTRACT:
The subject invention provides ginkgolide C derivatives compounds having the structure:wherein R is H or -A-Ar,where A is an alkyl group; andAr is an aryl group, which may contain heteroatoms and may be unsubstituted or substituted by one to five substituents each selected from the group consisting of hydrogen, alkoxy, —CH2CO2R4, and —CH2CONR5R6;where R4is an alkyl group; andR5and R6are each, independently, hydrogen or a branched or unbranched alkyl group;wherein R1is H or —COR7,where R7is alkyl, aryl or amino;wherein R2is present or absent, and when present is H, —COR8or —CO—Z—R8;where R8is alkyl, aryl or amino; andZ is oxygen;wherein R3is present or absent, and when present is —COR9;where R9is alkyl or aryl;wherein only one of R2or R3is present in the compound;wherein only two of R, R1, R2and R3are H; andwherein each of a and b designates a single covalent bond which is present or absent,where bond a is present when R3is absent and bond b is present when R2is absent;or an optically pure enantiomer of the compound. Additionally, the subject invention provides methods of inhibiting the activity of a glycine receptor using these compounds.

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