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2. 发明申请

WO2005075449A1 COMPOUNDS AND METHODS TO INCREASE ANTI-P-GLYCOPROTEIN ACTIVITY OF BAICALEIN BY ALKYLATION ON THE A RING 审中-公开
标题翻译：化合物和方法通过在环上的烷基化来增加巴西汀的抗β-糖蛋白活性
公开(公告)号：WO2005075449A1
公开(公告)日：2005-08-18
申请号：PCT/US2005/002910
申请日：2005-01-31
申请人： YALE UNIVERSITY , CHENG, Yung-Chi , LEE, Yashang , YEO, Hosup
发明人： CHENG, Yung-Chi , LEE, Yashang , YEO, Hosup
IPC分类号： C07D311/32
CPC分类号： C07D311/32 , C07D311/30
摘要： The present invention is directed to analogs of baicalein according to formula (I): where R 5 is H, (C I -C 12 )alkyl, (C 2 -C 13 )acyl, or an optionally substituted phenyl or benzyl group, an acyl group, a C 1 -C 20 alkyl or ether group, a phosphate, diphosphate, triphosphate or phosphodiester group; R 6 and R 7 are each independently H, (C 1 -C 12 )alkyl, (C 2 -C 13 )acyl, or an optionally substituted phenyl or benzyl or together form a -OCR 1 R 2 0- group wherein each of R 1 and R 2 is independently H, a C 1 -C 3 alkyl group or an optionally substituted phenyl or benzyl group; and R 8 is H, OH, an O-acyl group, a C 1 ,-C 4 alkyl 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.
摘要翻译：本发明涉及式（I）的黄芩素类似物：其中R 5为H，（C 1 -C 12）烷基，（C 2 -C 13）酰基或任意取代的苯基或苄基，酰基，C 1 -C 20烷基或醚基，磷酸酯，二磷酸酯，三磷酸酯或磷酸二酯基; R 6和R 7各自独立地为H，（C 1 -C 12）烷基，（C 2 -C 13）酰基或任选取代的苯基或苄基，或一起形成-OCR 1 R 2 O- 基团，其中R 1和R 2各自独立地为H，C 1 -C 3烷基或任选取代的苯基或苄基; 和R 8是H，OH，O-酰基，C 1 -C 4烷基或烷氧基，F，Cl，Br或I或其药学上可接受的盐，它们具有抗P-糖蛋白活性，通过抑制P-糖蛋白170（P-gp 170）和/或CYP450酶，特别是CYP450 3A4酶，提高活性化合物，特别是口服给药化合物的生物利用度的方法。基于本发明的这些新型衍生物的药物组合物也在本文中描述。

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