Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2011-01-25
2011-01-25
Henley, III, Raymond J (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
Reexamination Certificate
active
07875650
ABSTRACT:
The present invention is directed to analogs of baicalein according to formula (I): where R5is H, (C1-C12)alkyl, (C2-C13)acyl, or an optionally substituted phenyl or benzyl group, an acyl group, a C1-C20alkyl or ether group, a phosphate, diphosphate, triphosphate or phosphodiester group; R6and R7are each independently H, (C1-C12)alkyl, (C2-C13)acyl, or an optionally substituted phenyl or benzyl or together form a —OCR1R2O— group wherein each of R1and R2is independently H, a C1-C3alkyl group or an optionally substituted phenyl or benzyl group; and R8is H, OH, an O-acyl group, a C1,-C4alkyl or alkoxy group, F, Cl, Br or I, or a pharmaceutically acceptable salt thereof, which exhibit anti-P-glycoprotein activity and methods of enhancing the bioavailability of active compounds, especially orally administered compounds, by inhibition of P-glycoprotein 170 (P-gp 170) and/or CYP450 enzyme, especially CYP450 3A4 enzyme. Pharmaceutical compositions based upon these novel derivatives according to the present invention are also described herein.
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Callaghan, R
Cheng Yung-Chi
Lee Yashang
Yeo Hosup
Coleman Henry D.
Henley, III Raymond J
Sapone William J.
Sudol R. Neil
Yale University
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