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Potent and selective nonpeptidic inhibitors of procollagen C-proteinase.
Sulfonamide 56 (UK-421,045) was selected as a candidate for further preclinical evaluation as a topically applied, dermal anti-scarring agent and demonstrates excellent selectivity over MMPs involved in wound healing (>10 000-fold).
Role of hydrogen bonding in ligand interaction with the N-methyl-D-aspartate receptor ion channel.
Analysis of the binding of a series of the 10 available structurally rigid dibenzoazabicyclo[x.y.z]alkanes uncovered a highly significant correlation between affinity and a proposed ligand-active site hydrogen bonding vector.
Succinyl hydroxamates as potent and selective non-peptidic inhibitors of procollagen C-proteinase: design, synthesis, and evaluation as topically applied, dermal anti-scarring agents.
Discovery of Potent, Selective, and Peripherally Restricted Pan-Trk Kinase Inhibitors for the Treatment of Pain.
Two potent, selective, peripherally restricted, efficacious, and well-tolerated series of pan-Trk inhibitors are discussed which successfully delivered three candidate quality compounds and all three compounds are predicted to possess low metabolic clearance in human that does not proceed via aldehyde oxidase-catalyzed reactions, thus addressing the potential clearance prediction liability associated with the current pan- Trk development candidate PF-06273340.
Absorption, distribution, metabolism, and excretion considerations in selection of orally active indole-containing endothelin antagonist.
- D. K. Walker, K. Dack, D. Smith
- Chemistry, BiologyDrug metabolism and disposition: the biological…
- 1 November 2001
A series of potent indole-containing endothelin antagonists evaluated in rat pharmacokinetic studies showed a correlation between calculated H-bonding capacity and rate of permeability across Caco-2 monolayers for this series of compounds, indicating that reducing the overall H-Bonding potential, through a reduction in the number of H- bond donors and acceptors, could increase absorption of the molecules.
Inhalation by design: novel ultra-long-acting β(2)-adrenoreceptor agonists for inhaled once-daily treatment of asthma and chronic obstructive pulmonary disease that utilize a sulfonamide agonist…
A novel series of potent and selective sulfonamide derived β(2)-adrenoreceptor agonists are described that exhibit potential as inhaled ultra-long-acting bronchodilators for the treatment of asthma…
The discovery of long acting β2-adrenoreceptor agonists
The discovery of adamantyl-derived, inhaled, long acting beta(2)-adrenoreceptor agonists.
Inhalation by design: novel tertiary amine muscarinic M₃ receptor antagonists with slow off-rate binding kinetics for inhaled once-daily treatment of chronic obstructive pulmonary disease.
- P. Glossop, Christine A L Watson, F. Spence
- Biology, MedicineJournal of medicinal chemistry
- 20 September 2011
A novel tertiary amine series of potent muscarinic M(3) receptor antagonists are described that exhibit potential as inhaled long-acting bronchodilators for the treatment of chronic obstructive pulmonary disease, with in vivo duration of action studies confirming its potential for once-daily use in humans.