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A new class of bradykinin B1 receptor antagonists with high oral bioavailability and minimal PXR activity |
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| Authors: | Feng Dong-Mei DiPardo Robert M Wai Jenny M Chang Ronald K Di Marco Christina N Murphy Kathy L Ransom Richard W Reiss Duane R Tang Cuyue Prueksaritanont Thomayant Pettibone Douglas J Bock Mark G Kuduk Scott D |
| Affiliation: | Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. |
| Abstract: | The design and synthesis of a novel class of human bradykinin B1 antagonists featuring difluoroethyl ether and isoxazole carboxamide moieties are disclosed. Compound 7g displayed excellent pharmacokinetic properties, efficient ex vivo receptor occupancy, and low potential for P450 induction via PXR activation. |
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