Yale University

Yashang Lee

Yung-Chi Cheng

Hosup Yeo

The present invention is directed to analogs of baicalein according to formula (I): where Ris H, (C-C)alkyl, (C-C)acyl, or an optionally substituted phenyl or benzyl group, an acyl group, a C-Calkyl or ether group, a phosphate, diphosphate, triphosphate or phosphodiester group; Rand Rare each independently H, (C-C)alkyl, (C-C)acyl, or an optionally substituted phenyl or benzyl or together form a &#x2014;OCRRO&#x2014; group wherein each of Rand Ris independently H, a C-Calkyl group or an optionally substituted phenyl or benzyl group; and Ris H, OH, an O-acyl group, a C,-Calkyl 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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New Haven, CT, United States of America

Yashang Lee