公开(公告)号：US06326391B1

公开(公告)日：2001-12-04

申请号：US09454258

申请日：1999-12-02

申请人： Penelope N. Markham ,  Debbie C. Mulhearn ,  Alexander A. Neyfakh ,  David Crich ,  Mohamad-Rami Jaber ,  Michael E. Johnson

发明人： Penelope N. Markham ,  Debbie C. Mulhearn ,  Alexander A. Neyfakh ,  David Crich ,  Mohamad-Rami Jaber ,  Michael E. Johnson

IPC分类号： A61K31404

CPC分类号： C07D215/00 ,  A61K31/403 ,  A61K31/404 ,  A61K31/495 ,  C07D209/08 ,  C07D209/12 ,  Y02A50/473 ,  A61K31/475 ,  A61K31/47 ,  A61K31/17 ,  A61K31/165 ,  A61K2300/00

摘要： The present invention relates generally to the fields of bacteriology and mycology. More particularly, the present invention provides novel inhibitors of multidrug transport proteins that may be used in combination with existing antibacterial agent and/or antifungal agents to increase the toxic effects of the antimicrobial agents. More specifically the present invention provides methods and compositions for enhancing the antibacterial action of fluoroquinolones by administering fluoroquinolones in combination with an inhibitor of multidrug transporters and of enhancing the antifungal action of azole antifungal agents by administering an azole antifungal agent in combination with an inhibitor of multidrug transporters. Compositions comprising indole, urea, quinoline or aromatic amide based inhibitors also are disclosed.

摘要翻译： 本发明一般涉及细菌学和真菌学领域。 更具体地说，本发明提供了可与现有的抗菌剂和/或抗真菌剂组合使用以增加抗微生物剂的毒性作用的多药转运蛋白的新型抑制剂。 更具体地说，本发明提供了通过与多药物转运蛋白抑制剂组合施用氟喹诺酮和通过将唑类抗真菌剂与多药物抑制剂联合来增强唑类抗真菌药物的抗真菌作用来提高氟喹诺酮类抗菌作用的方法和组合物 运输商 还公开了包含吲哚，脲，喹啉或芳族酰胺的抑制剂的组合物。

公开(公告)号：US06362229B1

公开(公告)日：2002-03-26

申请号：US09640890

申请日：2000-08-17

申请人： Penelope N. Markham ,  Debbie C. Mulhearn ,  Alexander A. Neyfakh ,  David Crich ,  Mohamad-Rami Jaber ,  Michael E. Johnson

发明人： Penelope N. Markham ,  Debbie C. Mulhearn ,  Alexander A. Neyfakh ,  David Crich ,  Mohamad-Rami Jaber ,  Michael E. Johnson

IPC分类号： A61K3117

CPC分类号： C07D215/00 ,  A61K31/403 ,  A61K31/404 ,  A61K31/495 ,  C07D209/08 ,  C07D209/12 ,  Y02A50/473 ,  A61K31/475 ,  A61K31/47 ,  A61K31/17 ,  A61K31/165 ,  A61K2300/00

摘要： The present invention relates generally to the fields of bacteriology and mycology. More particularly, the present invention provides novel inhibitors of multidrug transport proteins that may be used in combination with existing antibacterial agent and/or antifungal agents to increase the toxic effects of the antimicrobial agents. More specifically, the present invention provides methods and compositions for enhancing the antibacterial action of fluoroquinolones by administering fluoroquinolones in combination with an inhibitor of multidrug transporters and of enhancing the antifungal action of azole antifungal agents by administering an azole antifungal agent in combination with an inhibitor of multidrug transporters. Compositions comprising indole, urea, quinoline or aromatic amide based inhibitors also are disclosed.

摘要翻译： 本发明一般涉及细菌学和真菌学领域。 更具体地说，本发明提供了可与现有的抗菌剂和/或抗真菌剂组合使用以增加抗微生物剂的毒性作用的多药转运蛋白的新型抑制剂。 更具体地说，本发明提供了通过与多药物转运蛋白抑制剂组合施用氟喹诺酮类药物来提高氟喹诺酮类药物的抗菌作用的方法和组合物，并且通过将唑类抗真菌药物与唑类抗真菌药物 多药转运蛋白 还公开了包含吲哚，脲，喹啉或芳族酰胺的抑制剂的组合物。