Amg 517
| Title | Journal |
|---|---|
| 7-tert-Butyl-6-(4-chloro-phenyl)-2-thioxo-2,3-dihydro-1H-pyrido[2,3-d]pyrimidin-4-one, a classic polymodal inhibitor of transient receptor potential vanilloid type 1 with a reduced liability for hyperthermia, is analgesic and ameliorates visceral hypersensitivity. | The Journal of pharmacology and experimental therapeutics 20120801 |
| Aging reverses the role of the transient receptor potential vanilloid-1 channel in systemic inflammation from anti-inflammatory to proinflammatory. | Cell cycle (Georgetown, Tex.) 20120115 |
| TRPV1 antagonists: clinical setbacks and prospects for future development. | Progress in medicinal chemistry 20120101 |
| Application of automated serial blood sampling and dried blood spot technique with liquid chromatography-tandem mass spectrometry for pharmacokinetic studies in mice. | Journal of pharmaceutical and biomedical analysis 20111101 |
| Application of automated dried blood spot sampling and LC-MS/MS for pharmacokinetic studies of AMG 517 in rats. | Bioanalysis 20111001 |
| Improved pharmacokinetics of AMG 517 through co-crystallization part 2: analysis of 12 carboxylic acid co-crystals. | Journal of pharmaceutical sciences 20110701 |
| Improved pharmacokinetics of AMG 517 through co-crystallization. Part 1: comparison of two acids with corresponding amide co-crystals. | Journal of pharmaceutical sciences 20100901 |
| Discovery of novel 6,6-heterocycles as transient receptor potential vanilloid (TRPV1) antagonists. | Journal of medicinal chemistry 20100422 |
| Manufacture of pharmaceutical co-crystals using twin screw extrusion: a solvent-less and scalable process. | Journal of pharmaceutical sciences 20100401 |
| Analgesic potential of TRPV1 antagonists. | Biochemical pharmacology 20090801 |
| Characterization and optimization of AMG 517 supersaturatable self-emulsifying drug delivery system (S-SEDDS) for improved oral absorption. | Journal of pharmaceutical sciences 20090201 |
| Substituted aryl pyrimidines as potent and soluble TRPV1 antagonists. | Bioorganic & medicinal chemistry letters 20080915 |
| The co-crystal approach to improve the exposure of a water-insoluble compound: AMG 517 sorbic acid co-crystal characterization and pharmacokinetics. | Journal of pharmaceutical sciences 20080901 |
| Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists. | Journal of medicinal chemistry 20080508 |
| Pharmacological blockade of the vanilloid receptor TRPV1 elicits marked hyperthermia in humans. | Pain 20080501 |
| On the thermoregulatory perils of TRPV1 antagonism. | Pain 20080501 |
| 4-Aminopyrimidine tetrahydronaphthols: a series of novel vanilloid receptor-1 antagonists with improved solubility properties. | Bioorganic & medicinal chemistry letters 20080315 |
| Enhanced bioavailability of a poorly soluble VR1 antagonist using an amorphous solid dispersion approach: a case study. | Molecular pharmaceutics 20080101 |
| Trisubstituted pyrimidines as transient receptor potential vanilloid 1 (TRPV1) antagonists with improved solubility. | Bioorganic & medicinal chemistry letters 20071201 |
| Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade. | The Journal of pharmacology and experimental therapeutics 20071001 |
| Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. | Journal of medicinal chemistry 20070726 |
| Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties. | Journal of medicinal chemistry 20070726 |