Search

Your search keyword '"Anna Ollerstam"' showing total 2 results
Start Over Author "Anna Ollerstam" Journal journal of medicinal chemistry
2 results on '"Anna Ollerstam"'

1. Discovery and Early Clinical Development of Isobutyl 1-[8-Methoxy-5-(1-oxo-3H-isobenzofuran-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxylate (LEO 39652), a Novel 'Dual-Soft' PDE4 Inhibitor for Topical Treatment of Atopic Dermatitis

Author

Thomas Vifian, Tatiana G Stilou, Simon Feldbaek Nielsen, Maja Lambert, Jens Christian Højland Larsen, Tine Skak-Nielsen, Anders Soehoel, Pontus Hegardt, Lene M. Hansen, Nina Østergaard Knudsen, Morten Dahl Sørensen, Mogens Larsen, Cecilia Eskilsson, Steen Laursen, Stefan Eirefelt, Henrik Pettersson, and Anna Ollerstam

Subjects
0303 health sciences, Isobenzofuran, Chemistry, Drug discovery, Human skin, Topical treatment, Atopic dermatitis, Pharmacology, medicine.disease, 01 natural sciences, 0104 chemical sciences, 010404 medicinal & biomolecular chemistry, 03 medical and health sciences, chemistry.chemical_compound, Drug Discovery, medicine, Molecular Medicine, Target organ, 030304 developmental biology
Abstract

We describe the design of a novel PDE4 scaffold and the exploration of the dual-soft concept to reduce systemic side effects via rapid elimination: introducing ester functionalities that can be inactivated in blood as well as by the liver (dual-soft) while being stable in human skin. Compound 40 was selected as a clinical candidate as it was potent and rapidly degraded by blood and liver to inactive metabolites and because in preclinical studies it showed high exposure at the target organ: the skin. Preclinical and clinical data are presented confirming the value of the dual-soft concept in reducing systemic exposure.

Published
2020
Full Text
View/download PDF

2. Discovery and Early Clinical Development of Isobutyl 1-[8-Methoxy-5-(1-oxo-3

Author

Jens, Larsen, Maja, Lambert, Henrik, Pettersson, Thomas, Vifian, Mogens, Larsen, Anna, Ollerstam, Pontus, Hegardt, Cecilia, Eskilsson, Steen, Laursen, Anders, Soehoel, Tine, Skak-Nielsen, Lene M, Hansen, Nina Ø, Knudsen, Stefan, Eirefelt, Morten D, Sørensen, Tatiana G, Stilou, and Simon F, Nielsen

Subjects
Drug Discovery, Animals, Humans, Phosphodiesterase 4 Inhibitors, Dermatitis, Atopic
Abstract

We describe the design of a novel PDE4 scaffold and the exploration of the dual-soft concept to reduce systemic side effects via rapid elimination: introducing ester functionalities that can be inactivated in blood as well as by the liver (dual-soft) while being stable in human skin. Compound

Published
2020

Catalog

Books, media, physical & digital resources
See catalog results