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    Drug resistance and multidrug resistance modulators
    3.
    发明授权
    Drug resistance and multidrug resistance modulators 失效
    耐药性和多药耐药调节剂

    公开(公告)号：US06180633B2

    公开(公告)日：2001-01-30

    申请号：US09345255

    申请日：1999-06-30

    申请人： Julian Stanley Kroin ,  Bryan Hurst Norman

    发明人： Julian Stanley Kroin ,  Bryan Hurst Norman

    IPC分类号： A61K31495

    CPC分类号： C07D295/088 ,  C07B2200/07 ,  C07C2603/40

    摘要： Drug and multidrug resistant modulators of the formula: where R1 and R2 are independently hydrogen or halo; A is —CH2—CH2—, —CH2—CHR4—CH2—, or —CH2—CHR5—CHR6—CH2—, where R4 is —H, —OH, or acyloxy; one of R5 or R6 is —H, —OH, or acyloxy, and the other is —H; R3 is a polyaryl; and pharmaceutically acceptable salts and solvates thereof, are described and claimed. Use of the new compounds in the preparation of pharmaceutical compositions is described and claimed. In addition, methods for treating drug and multidrug resistance in various diseases using a compound, or pharmaceutically acceptable salt or solvate thereof, of this invention are described and claimed. Also, methods of enhancing oral bioavailability of a drug and methods of enhancing bioavailability of a drug to the brain using a compound, or pharmaceutically acceptable salt or solvate thereof, of this invention are described and claimed.

    摘要翻译： 具有下式的药物和多药耐药调节剂：其中R 1和R 2独立地是氢或卤素; A是-CH 2 -CH 2 - ， - CH 2 -CHR 4 -CH 2 - 或-CH 2 -CHR 5 -CHR 6 -CH 2 - ，其中R 4是-H，-OH或酰氧基; R5或R6中的一个是-H，-OH或酰氧基，另一个是-H; R3是多芳基; 和其药学上可接受的盐和溶剂化物。 描述和要求保护新化合物在制备药物组合物中的用途。 此外，描述并要求保护本发明化合物或其药学上可接受的盐或溶剂化物在各种疾病中治疗药物和多药耐药性的方法。 此外，描述并要求保护药物的口服生物利用度的方法和使用本发明的化合物或其药学上可接受的盐或溶剂化物向大脑提高药物生物利用度的方法。

    Drug resistance and multidrug resistance modulators
    4.
    发明授权
    Drug resistance and multidrug resistance modulators 失效
    耐药性和多药耐药调节剂

    公开(公告)号：US5776939A

    公开(公告)日：1998-07-07

    申请号：US873583

    申请日：1997-06-12

    申请人： Julian Stanley Kroin ,  Bryan Hurst Norman

    发明人： Julian Stanley Kroin ,  Bryan Hurst Norman

    IPC分类号： A61K31/495 ,  C07D215/14 ,  A01N43/60 ,  C07D241/04

    CPC分类号： C07D215/14 ,  A61K31/495

    摘要： Drug and multidrug resistant modulators of Formula (C): ##STR1## where Z is selected from the group consisting of --S--, --S(O).sub.w --, and --CH.sub.2 --, where w is 1 or 2; and pharmaceutically acceptable salts or solvates thereof are described and claimed. Use of the new compounds in the preparation of pharmaceutical compositions is described and claimed. In addition, methods for treating drug and multidrug resistance in various diseases using a compound of this invention are described and claimed. Also, methods of enhancing oral bioavailability of a drug and methods of enhancing bioavailability of a drug to the brain using a compound of this invention are described and claimed.

    摘要翻译： 式（C）的药物和多药耐药调节剂：其中Z选自-S-，-S（O）w - 和-CH 2 - ，其中w为1或2; 并描述和要求保护其药学上可接受的盐或溶剂合物。 描述和要求保护新化合物在制备药物组合物中的用途。 此外，描述并要求保护使用本发明化合物治疗各种疾病药物和多药耐药性的方法。 此外，描述并要求保护药物的口服生物利用度的方法和使用本发明的化合物向大脑提高药物的生物利用度的方法。

    Drug resistance and multidrug resistance modulators
    6.
    发明授权
    Drug resistance and multidrug resistance modulators 失效
    耐药性和多药耐药调节剂

    公开(公告)号：US6130219A

    公开(公告)日：2000-10-10

    申请号：US343379

    申请日：1999-06-30

    申请人： Julian Stanley Kroin ,  Bryan Hurst Norman

    发明人： Julian Stanley Kroin ,  Bryan Hurst Norman

    IPC分类号： C07D295/08 ,  A61K31/495 ,  C07D295/092

    CPC分类号： C07D295/088 ,  C07B2200/07 ,  C07C2103/40

    摘要： Drug and multidrug resistant modulators of the formula: ##STR1## where R.sup.1 and R.sup.2 are independently hydrogen or halo; A is --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CHR.sup.4 --CH.sub.2 --, or --CH.sub.2 --CHR.sup.5 --CHR.sup.6 --CH.sub.2 --, where R.sup.4 is --H, --OH, or acyloxy; one of R.sup.5 or R.sup.6 is --H, --OH, or acyloxy, and the other is --H; R.sup.3 is a polyaryl; and pharmaceutically acceptable salts and solvates thereof, are described and claimed. Use of the new compounds in the preparation of pharmaceutical compositions is described and claimed. In addition, methods for treating drug and multidrug resistance in various diseases using a compound, or pharmaceutically acceptable salt or solvate thereof, of this invention are described and claimed. Also, methods of enhancing oral bioavailability of a drug and methods of enhancing bioavailability of a drug to the brain using a compound, or pharmaceutically acceptable salt or solvate thereof, of this invention are described and claimed.

    摘要翻译： 具有下式的药物和多药耐药调节剂：其中R 1和R 2独立地是氢或卤素; A是-CH 2 -CH 2 - ， - CH 2 -CHR 4 -CH 2 - 或-CH 2 -CHR 5 -CHR 6 -CH 2 - ，其中R 4是-H，-OH或酰氧基; R5或R6中的一个是-H，-OH或酰氧基，另一个是-H; R3是多芳基; 和其药学上可接受的盐和溶剂化物。 描述和要求保护新化合物在制备药物组合物中的用途。 此外，描述并要求保护本发明化合物或其药学上可接受的盐或溶剂化物在各种疾病中治疗药物和多药耐药性的方法。 此外，描述并要求保护药物的口服生物利用度的方法和使用本发明的化合物或其药学上可接受的盐或溶剂化物向大脑提高药物生物利用度的方法。

    Drug resistance and multidrug resistance modulators
    7.
    发明授权
    Drug resistance and multidrug resistance modulators 失效

    公开(公告)号：US6025359A

    公开(公告)日：2000-02-15

    申请号：US873782

    申请日：1997-06-12

    申请人： Julian Stanley Kroin ,  Bryan Hurst Norman

    发明人： Julian Stanley Kroin ,  Bryan Hurst Norman

    IPC分类号： C07D295/08 ,  A61K31/495 ,  C07D295/092 ,  C07D295/088

    CPC分类号： C07D295/088 ,  C07B2200/07 ,  C07C2103/40

    摘要： Drug and multidrug resistant modulators of the formula: ##STR1## where R.sup.1 and R.sup.2 are independently hydrogen or halo; A is --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CHR.sup.4 --CH.sub.2 --, or --CH.sub.2 --CHR.sup.5 --CHR.sup.6 --CH.sub.2 --, where R.sup.4 is --H, --OH, or acyloxy; one of R.sup.5 or R.sup.6 is --H, --OH, or acyloxy, and the other is --H; R.sup.3 is a polyaryl; and pharmaceutically acceptable salts and solvates thereof, are described and claimed. Use of the new compounds in the preparation of pharmaceutical compositions is described and claimed. In addition, methods for treating drug and multidrug resistance in various diseases using a compound, or pharmaceutically acceptable salt or solvate thereof, of this invention are described and claimed. Also, methods of enhancing oral bioavailability of a drug and methods of enhancing bioavailability of a drug to the brain using a compound, or pharmaceutically acceptable salt or solvate thereof, of this invention are described and claimed.