Apoptolidin analogs and derivatives for inducing apoptosis...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C549S271000, C548S431000

Reexamination Certificate

active

07151116

ABSTRACT:
The invention provides novel apoptosis-inducing compounds that include isolated, purified isoapoptolidin, and selectively functionalized isoapoptolidin derivatives and stereoisomers thereof; selectively functionalized apoptolidin derivatives and stereoisomers thereof; and deglycosylated isoapoptolidin and selectively functionalized derivatives and stereoisomers thereof. The isoapoptolidin, apoptolidin, and deglycosylated isoapoptolidin derivatives may be functionalized by substituting any or all of the methoxyl or hydroxyl groups of the parent molecule. Pharmaceutical compositions and methods for using the compounds are also provided.

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Salmon et al, Understanding and exploiting the mechanistic basis for selectivity of polyketide inhibitors of F0F1-ATPase, PNAS, 97(26), pp. 14766-14771, Dec. 19, 2000.
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Pennington, et al., “Toward a stable apoptolidin derivative: identification of isoapoptolidin and selective deglycosylation of apoptolidin,” Org. Lett. (2002) 4:3823-3825.
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