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- Publications
- Influence
Early pharmaceutical profiling to predict oral drug absorption: current status and unmet needs.
- Christel A S Bergström, R. Holm, +15 authors A. Mullertz
- Medicine
- European journal of pharmaceutical sciences…
- 16 June 2014
Preformulation measurements are used to estimate the fraction absorbed in vivo for orally administered compounds and thereby allow an early evaluation of the need for enabling formulations. As part… Expand
Potent, selective, and orally active adenosine A2A receptor antagonists: arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines.
- B. Neustadt, Jinsong Hao, +12 authors Kung-I Feng
- Chemistry, Medicine
- Bioorganic & medicinal chemistry letters
- 1 March 2007
Antagonism of the adenosine A2A receptor offers great promise in the treatment of Parkinson's disease. Employing the known pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine A2A antagonist SCH 58261 as… Expand
Discovery of Ruzasvir (MK-8408): A Potent, Pan-Genotype HCV NS5A Inhibitor with Optimized Activity against Common Resistance-Associated Polymorphisms.
- Ling Tong, Wensheng Yu, +29 authors J. Kozlowski
- Chemistry, Medicine
- Journal of medicinal chemistry
- 12 January 2017
We describe the research that led to the discovery of compound 40 (ruzasvir, MK-8408), a pan-genotypic HCV nonstructural protein 5A (NS5A) inhibitor with a "flat" GT1 mutant profile. This NS5A… Expand
Analyzing the Potential Root Causes of Variability of Pharmacokinetics in Preclinical Species.
- Pierre Daublain, Kung-I Feng, +7 authors Caroline McGregor
- Chemistry, Medicine
- Molecular pharmaceutics
- 3 April 2017
The purpose of this research was to assess variability in pharmacokinetic profiles (PK variability) in preclinical species and identify the risk factors associated with the properties of a drug… Expand
The discovery of N-((2H-tetrazol-5-yl)methyl)-4-((R)-1-((5r,8R)-8-(tert-butyl)-3-(3,5-dichlorophenyl)-2-oxo-1,4-diazaspiro[4.5]dec-3-en-1-yl)-4,4-dimethylpentyl)benzamide (SCH 900822): a potent and…
- Duane Demong, Xing Dai, +34 authors H. Zhao
- Chemistry, Medicine
- Journal of medicinal chemistry
- 26 February 2014
A novel series of spiroimidazolone-based antagonists of the human glucagon receptor (hGCGR) has been developed. Our efforts have led to compound 1,… Expand
Effect of composition of simulated intestinal media on the solubility of poorly soluble compounds investigated by design of experiments
- C. Madsen, Kung-I Feng, +4 authors T. Rades
- Chemistry, Medicine
- European journal of pharmaceutical sciences…
- 1 January 2018
ABSTRACT The composition of the human intestinal fluids varies both intra‐ and inter‐individually. This will influence the solubility of orally administered drug compounds, and hence, the absorption… Expand
Discovery of oral and inhaled PDE4 inhibitors.
- P. Ting, J. Lee, +15 authors C. S. Celly
- Chemistry, Medicine
- Bioorganic & medicinal chemistry letters
- 15 October 2013
The optimization of oxazole-based PDE4 inhibitor 1 has led to the identification of both oral (compound 16) and inhaled (compound 34) PDE4 inhibitors. Selectivity against PDE10/PDE11, off target… Expand
Discovery of MK-6169, a Potent Pan-Genotype Hepatitis C Virus NS5A Inhibitor with Optimized Activity against Common Resistance-Associated Substitutions.
- Wensheng Yu, Ling Tong, +22 authors J. Kozlowski
- Chemistry, Medicine
- Journal of medicinal chemistry
- 21 April 2018
We describe the discovery of MK-6169, a potent and pan-genotype hepatitis C virus NS5A inhibitor with optimized activity against common resistance-associated substitutions. SAR studies around the… Expand
Assessing the Utility of In Vitro Screening Tools for Predicting Bio-Performance of Oral Peptide Delivery
- Prajakta Gadgil, Candice Alleyne, +10 authors Nicole Buist
- Chemistry, Medicine
- Pharmaceutical Research
- 26 August 2019
In this study we evaluated the utility of in-vitro screening tools for predicting the in-vivo behavior of six cyclic peptides with different solubility and permeability properties (BCS class II and… Expand
Pharmacological Characterization of a Novel α2C-Adrenoceptor Agonist N-[3,4-dihydro-4-(1H-imidazol-4-ylmethyl)-2H-1, 4-benzoxazin-6-yl]-N-ethyl-N′-methylurea (Compound A)
- M. Corboz, M. Rivelli, +18 authors J. Hey
- Chemistry, Medicine
- Journal of Pharmacology and Experimental…
- 1 April 2011
We define the pharmacological and pharmacokinetic profiles of a novel α2C-adrenoceptor agonist, compound A [N-[3,4-dihydro-4-(1H-imidazol-4-ylmethyl)-2H-1,4-benzoxazin-6-yl]-N-ethyl-N′-methylurea].… Expand