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Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation

Bioorganic & medicinal chemistry letters, 2013-07, Vol.23 (13), p.3741-3748

2013

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ADAM17 is the main sheddase for the generation of human triggering receptor expressed in myeloid cells (hTREM2) ectodomain and cleaves TREM2 after Histidine 157

Neuroscience letters, 2017-11, Vol.660, p.109-114

2017

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The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588

Bioorganic & medicinal chemistry, 2013-06, Vol.21 (11), p.3231-3239

2013

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Discovery and Profiling of a Selective and Efficacious Syk Inhibitor

Journal of medicinal chemistry, 2015-02, Vol.58 (4), p.1950-1963

2015

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Discovery and Characterization of the Topical Soft JAK Inhibitor CEE321 for Atopic Dermatitis

Journal of medicinal chemistry, 2023-02, Vol.66 (3), p.2161-2168

2023

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Optimization of the In Vivo Potency of Pyrazolopyrimidine MALT1 Protease Inhibitors by Reducing Metabolism and Increasing Potency in Whole Blood

Journal of medicinal chemistry, 2020-12, Vol.63 (23), p.14594-14608

2020

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Discovery of the First Potent, Selective, and Orally Bioavailable Signal Peptide Peptidase-Like 2a (SPPL2a) Inhibitor Displaying Pronounced Immunomodulatory Effects In Vivo

Journal of medicinal chemistry, 2018-02, Vol.61 (3), p.865-880

2018

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Micropreparative isolation and NMR structure elucidation of metabolites of the drug candidate 1-isopropyl-4-(4-isopropylphenyl)-6-(prop-2-yn-1-yloxy) quinazolin-2(1H)-one from rat bile and urine

Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, 2015-05, Vol.989, p.1-10

2015

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Complementary use of ion trap/time-of-flight mass spectrometry in combination with capillary high-pressure liquid chromatography: early characterization of in vivo metabolites of the cathepsin K inhibitor NVP-AAV490 in rat

Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, 2003-04, Vol.787 (2), p.255-270

2003

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Increasing metabolic stability via the deuterium kinetic isotope effect: An example from a proline-amide-urea aminothiazole series of phosphatidylinositol-3 kinase alpha inhibitors

Bioorganic & medicinal chemistry letters, 2016-10, Vol.26 (19), p.4729-4734

2016

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Orthoamides and Iminium Salts LXXIV. Reactions of N,N,N',N'-Tetramethyl-chloroformamidinium Chloride with Metals

Zeitschrift für Naturforschung. B, A journal of chemical sciences, 2012-04, Vol.67, p.305

2012

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Orthoamide und Iminiumsalze, LXXIV [1]. Umsetzung von N,N,N´,N´-Tetramethyl-chlorformamidiniumchlorid mit Metallen: Orthoamides and Iminium Salts LXXIV [1]. Reactions of N,N,N´,N´-Tetramethyl-chloroformamidiniumChloride with Metals

Zeitschrift für Naturforschung. B, A journal of chemical sciences, 2012-04, Vol.67 (4), p.305-319

2012

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Orthoamide und Iminiumsalze, LXXIV [1]. Umsetzung von N,N,N´,N´-Tetramethyl-chlorformamidiniumchlorid mit Metallen

Zeitschrift für Naturforschung. B, A journal of chemical sciences, 2012-04, Vol.67 (4), p.305-319

2012

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Biocatalytic synthesis and structure elucidation of cyclized metabolites of the deacetylase inhibitor panobinostat (LBH589)

Drug metabolism and disposition, 2012-05, Vol.40 (5), p.1041-1050

2012

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In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part II

Bioorganic & medicinal chemistry letters, 2010-08, Vol.20 (15), p.4719-4723

2010

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Corrigendum to “Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation” [Bioorg. Med. Chem. Lett. 23 (2013) 3741–3748]

Bioorganic & medicinal chemistry letters, 2013-08, Vol.23 (16), p.4723-4723

2013

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2-Cyano-pyrimidines: A New Chemotype for Inhibitors of the Cysteine Protease Cathepsin K

Journal of medicinal chemistry, 2007-02, Vol.50 (4), p.591-594

2007

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Exploring subtype selectivity and metabolic stability of a novel series of ligands for the benzodiazepine binding site of the GABA A receptor

Bioorganic & medicinal chemistry letters, 2011-03, Vol.21 (5), p.1523-1526

2011

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Exploring subtype selectivity and metabolic stability of a novel series of ligands for the benzodiazepine binding site of the GABAA receptor

Bioorganic & medicinal chemistry letters, 2011-03, Vol.21 (5), p.1523-1526

2011

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Identification of natural ligands of retinoic acid receptor-related orphan receptor α ligand-binding domain expressed in Sf9 cells––a mass spectrometry approach

Analytical biochemistry, 2003-12, Vol.323 (1), p.139-149

2003

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Exploring subtype selectivity and metabolic stability of a novel series of ligands for the benzodiazepine binding site of the GABA sub(A receptor)

Bioorganic & medicinal chemistry letters, 2011-03, Vol.21 (5), p.1523-1526

2011

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In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part I

Bioorganic & medicinal chemistry letters, 2010-08, Vol.20 (15), p.4715-4718

2010

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2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors

Bioorganic & medicinal chemistry letters, 2010-03, Vol.20 (5), p.1724-1727

2010

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Dipeptide nitrile inhibitors of cathepsin K

Bioorganic & medicinal chemistry letters, 2006-05, Vol.16 (9), p.2549-2554

2006

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On the Importance of Metabolic Stability to Achieve High Oral Exposures for Cyclic Peptides

American Journal of Medicinal Chemistry, 2020-01, p.1-10

2020

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Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation

ADAM17 is the main sheddase for the generation of human triggering receptor expressed in myeloid cells (hTREM2) ectodomain and cleaves TREM2 after Histidine 157

The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588

Discovery and Profiling of a Selective and Efficacious Syk Inhibitor

Discovery and Characterization of the Topical Soft JAK Inhibitor CEE321 for Atopic Dermatitis

Optimization of the In Vivo Potency of Pyrazolopyrimidine MALT1 Protease Inhibitors by Reducing Metabolism and Increasing Potency in Whole Blood

Discovery of the First Potent, Selective, and Orally Bioavailable Signal Peptide Peptidase-Like 2a (SPPL2a) Inhibitor Displaying Pronounced Immunomodulatory Effects In Vivo

Micropreparative isolation and NMR structure elucidation of metabolites of the drug candidate 1-isopropyl-4-(4-isopropylphenyl)-6-(prop-2-yn-1-yloxy) quinazolin-2(1H)-one from rat bile and urine

Complementary use of ion trap/time-of-flight mass spectrometry in combination with capillary high-pressure liquid chromatography: early characterization of in vivo metabolites of the cathepsin K inhibitor NVP-AAV490 in rat

Increasing metabolic stability via the deuterium kinetic isotope effect: An example from a proline-amide-urea aminothiazole series of phosphatidylinositol-3 kinase alpha inhibitors

Orthoamides and Iminium Salts LXXIV. Reactions of N,N,N',N'-Tetramethyl-chloroformamidinium Chloride with Metals

Orthoamide und Iminiumsalze, LXXIV [1]. Umsetzung von N,N,N´,N´-Tetramethyl-chlorformamidiniumchlorid mit Metallen: Orthoamides and Iminium Salts LXXIV [1]. Reactions of N,N,N´,N´-Tetramethyl-chloroformamidiniumChloride with Metals

Orthoamide und Iminiumsalze, LXXIV [1]. Umsetzung von N,N,N´,N´-Tetramethyl-chlorformamidiniumchlorid mit Metallen

Biocatalytic synthesis and structure elucidation of cyclized metabolites of the deacetylase inhibitor panobinostat (LBH589)

In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part II

Corrigendum to “Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation” [Bioorg. Med. Chem. Lett. 23 (2013) 3741–3748]

2-Cyano-pyrimidines: A New Chemotype for Inhibitors of the Cysteine Protease Cathepsin K

Exploring subtype selectivity and metabolic stability of a novel series of ligands for the benzodiazepine binding site of the GABA A receptor

Exploring subtype selectivity and metabolic stability of a novel series of ligands for the benzodiazepine binding site of the GABAA receptor

Identification of natural ligands of retinoic acid receptor-related orphan receptor α ligand-binding domain expressed in Sf9 cells––a mass spectrometry approach

Exploring subtype selectivity and metabolic stability of a novel series of ligands for the benzodiazepine binding site of the GABA sub(A receptor)

In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part I

2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors

Dipeptide nitrile inhibitors of cathepsin K

On the Importance of Metabolic Stability to Achieve High Oral Exposures for Cyclic Peptides

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