公开(公告)号：US07754718B2

公开(公告)日：2010-07-13

申请号：US11579284

申请日：2005-05-02

申请人： Hosup Yeo ,  David J. Austin ,  Ling Li ,  Yung-chi Cheng

发明人： Hosup Yeo ,  David J. Austin ,  Ling Li ,  Yung-chi Cheng

IPC分类号： A61K31/502 ,  C07D237/26

CPC分类号： A61K31/365 ,  A61K31/36 ,  A61K31/517 ,  C07D405/04 ,  C07D407/04 ,  C07D491/04 ,  C07D493/04

摘要： The present invention relates to novel antiviral helioxanthin analogs. These compounds may particularly be used alone or in combination with other drugs for the treatment of the following: hepadnaviruses, flaviviruses, herpesviruses and human immunodeficiency virus. In addition, compounds according to the present invention can be used to prevent or reduce the likelihood of the occurrence of tumors secondary to virus infection as well as other infections or disease states that are secondary to the virus infection.

摘要翻译： 本发明涉及新的抗病毒螺甲黄素类似物。 这些化合物可以单独使用或与其他药物组合使用，用于治疗以下物质：肝素病毒，黄病毒，疱疹病毒和人类免疫缺陷病毒。 此外，根据本发明的化合物可用于预防或减少继发于病毒感染的肿瘤以及其它感染或继发于病毒感染的疾病状态的可能性。

公开(公告)号：US20080167353A1

公开(公告)日：2008-07-10

申请号：US11579284

申请日：2005-05-02

申请人： Hosup Yeo ,  David J. Austin ,  Ling Li ,  Yung-Chi Cheng

发明人： Hosup Yeo ,  David J. Austin ,  Ling Li ,  Yung-Chi Cheng

IPC分类号： C07D285/02 ,  A61K31/335

CPC分类号： A61K31/365 ,  A61K31/36 ,  A61K31/517 ,  C07D405/04 ,  C07D407/04 ,  C07D491/04 ,  C07D493/04

摘要： The present invention relates to novel antiviral helioxanthin analogs. These compounds may particularly be used alone or in combination with other drugs for the treatment of the following: hepadnaviruses, flaviviruses, herpesviruses and human immunodeficiency virus. In addition, compounds according to the present invention can be used to prevent or reduce the likelihood of the occurrence of tumors secondary to virus infection as well as other infections or disease states that are secondary to the virus infection.

摘要翻译： 本发明涉及新的抗病毒螺甲黄素类似物。 这些化合物可以单独使用或与其他药物组合使用，用于治疗以下物质：肝素病毒，黄病毒，疱疹病毒和人类免疫缺陷病毒。 此外，根据本发明的化合物可用于预防或减少继发于病毒感染的肿瘤以及其它感染或继发于病毒感染的疾病状态的可能性。

公开(公告)号：US20070161605A1

公开(公告)日：2007-07-12

申请号：US10586822

申请日：2005-01-31

申请人： Yung-chi Cheng ,  Yashang Lee ,  Hosup Yeo

发明人： Yung-chi Cheng ,  Yashang Lee ,  Hosup Yeo

IPC分类号： A61K31/353 ,  A61K31/665 ,  C07D311/02

CPC分类号： C07D311/32 ,  C07D311/30

摘要： The present invention is directed to analogs of baicalein according to formula (I): where R5 is H, (C1-C12)alkyl, (C2-C13)acyl, or an optionally substituted phenyl or benzyl group, an acyl group, a C1-C20 alkyl or ether group, a phosphate, diphosphate, triphosphate or phosphodiester group; R6 and R7 are 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 R1 and R2 is independently H, a C1-C3 alkyl group or an optionally substituted phenyl or benzyl group; and R8 is H, OH, an O-acyl group, a C1,-C4 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是H，（C 1 -C 12） 烷基，（C 2 -C 13）酰基或任选取代的苯基或苄基，酰基，C 1 -C 3烷基 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 1 -C 12） 酰基或任选取代的苯基或苄基，或一起形成-OCR 1 R 12， O-基团，其中R 1和R 2各自独立地为H，C 1 -C 3 - 基团或任选取代的苯基或苄基; 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，其通过抑制P-糖蛋白170（P-gp 170）和/或其衍生物来显示抗P-糖蛋白活性和增强活性化合物，特别是口服给药化合物的生物利用度的方法， 或CYP450酶，特别是CYP450 3A4酶。 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。

公开(公告)号：US07875650B2

公开(公告)日：2011-01-25

申请号：US10586822

申请日：2005-01-31

申请人： Yung-chi Cheng ,  Yashang Lee ,  Hosup Yeo

发明人： Yung-chi Cheng ,  Yashang Lee ,  Hosup Yeo

IPC分类号： A61K31/35

CPC分类号： C07D311/32 ,  C07D311/30

摘要： The present invention is directed to analogs of baicalein according to formula (I): where R5 is H, (C1-C12)alkyl, (C2-C13)acyl, or an optionally substituted phenyl or benzyl group, an acyl group, a C1-C20 alkyl or ether group, a phosphate, diphosphate, triphosphate or phosphodiester group; R6 and R7 are 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 R1 and R2 is independently H, a C1-C3 alkyl group or an optionally substituted phenyl or benzyl group; and R8 is H, OH, an O-acyl group, a C1,-C4 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是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，C1 -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， C3烷基或任选取代的苯基或苄基; R8为H，OH，O-酰基，C1-C4烷基或烷氧基，F，Cl，Br或I或其药学上可接受的盐，其具有抗P-糖蛋白活性和增强的方法 通过抑制P-糖蛋白170（P-gp 170）和/或CYP450酶，特别是CYP450 3A4酶，活性化合物，特别是口服给药化合物的生物利用度。 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。