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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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Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors

ACS medicinal chemistry letters, 2017-09, Vol.8 (9), p.975-980

2017

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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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Preclinical pharmacokinetics and metabolism of MAK683, a clinical stage selective oral embryonic ectoderm development (EED) inhibitor for cancer treatment

Xenobiotica, 2022-01, Vol.52 (1), p.65-78

2022

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Discovery and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors

ACS medicinal chemistry letters, 2016-08, Vol.7 (8), p.762-767

2016

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Evaluation of relative MS response factors of drug metabolites for semi‐quantitative assessment of chemical liabilities in drug discovery

Journal of mass spectrometry., 2017-04, Vol.52 (4), p.210-217

2017

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Discovery of Imidazoquinolines as a Novel Class of Potent, Selective, and in Vivo Efficacious Cancer Osaka Thyroid (COT) Kinase Inhibitors

Journal of medicinal chemistry, 2016-08, Vol.59 (16), p.7544-7560

2016

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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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Design of A Metabolically Stable Tritium‐Tracer of the PI 3K δ ‐Inhibitor CDZ 173 (Leniolisib) as a Tool to Study Liver Metabolites

Helvetica chimica acta, 2018-06, Vol.101 (6)

2018

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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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Identification and optimisation of 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole and 4,5-dihydrothiazolo[4,5-h]quinazoline series of selective phosphatidylinositol-3 kinase alpha inhibitors

Bioorganic & medicinal chemistry letters, 2015-09, Vol.25 (17), p.3575-3581

2015

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Orally bioavailable Syk inhibitors with activity in a rat PK/PD model

Bioorganic & medicinal chemistry letters, 2015-10, Vol.25 (20), p.4642-4647

2015

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Design of A Metabolically Stable Tritium‐Tracer of the PI3Kδ‐Inhibitor CDZ173 (Leniolisib) as a Tool to Study Liver Metabolites

Helvetica chimica acta, 2018-06, Vol.101 (6), p.n/a

2018

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Syk inhibitors with high potency in presence of blood

Bioorganic & medicinal chemistry letters, 2014-05, Vol.24 (10), p.2278-2282

2014

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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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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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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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Abstract 1922: 2-Aminothiazoles as potent and selective PI3Kalpha inhibitors: Discovery of NVP-BYL719 and structural basis for the isoform selectivity

Cancer research (Chicago, Ill.), 2012-04, Vol.72 (8_Supplement), p.1922-1922

2012

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Benzimidazoles as Potent and Orally Active mGlu5 Receptor Antagonists with an Improved PK Profile

ACS medicinal chemistry letters, 2011-01, Vol.2 (1), p.58-62

2011

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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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Cytochrome P-450-induced cytotoxicity of mitoxantrone by formation of electrophilic intermediates

Cancer research (Chicago, Ill.), 1993-11, Vol.53 (21), p.5135-5142

1993

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13C-Markierung der Seitenketten von Mitoxantrone

Journal of labelled compounds & radiopharmaceuticals, 1989-01, Vol.27 (1), p.91-101

1989

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Pharmacokinetics and metabolism of mitoxantrone : a review

Clinical pharmacokinetics, 1990-05, Vol.18 (5), p.365-380

1990

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

Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors

Discovery and Profiling of a Selective and Efficacious Syk Inhibitor

Discovery of the Clinical Candidate MAK683: An EED-Directed, Allosteric, and Selective PRC2 Inhibitor for the Treatment of Advanced Malignancies

Preclinical pharmacokinetics and metabolism of MAK683, a clinical stage selective oral embryonic ectoderm development (EED) inhibitor for cancer treatment

Discovery and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors

Evaluation of relative MS response factors of drug metabolites for semi‐quantitative assessment of chemical liabilities in drug discovery

Discovery of Imidazoquinolines as a Novel Class of Potent, Selective, and in Vivo Efficacious Cancer Osaka Thyroid (COT) Kinase Inhibitors

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

Design of A Metabolically Stable Tritium‐Tracer of the PI 3K δ ‐Inhibitor CDZ 173 (Leniolisib) as a Tool to Study Liver Metabolites

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

Identification and optimisation of 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole and 4,5-dihydrothiazolo[4,5-h]quinazoline series of selective phosphatidylinositol-3 kinase alpha inhibitors

Orally bioavailable Syk inhibitors with activity in a rat PK/PD model

Design of A Metabolically Stable Tritium‐Tracer of the PI3Kδ‐Inhibitor CDZ173 (Leniolisib) as a Tool to Study Liver Metabolites

Syk inhibitors with high potency in presence of blood

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]

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

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

Abstract 1922: 2-Aminothiazoles as potent and selective PI3Kalpha inhibitors: Discovery of NVP-BYL719 and structural basis for the isoform selectivity

Benzimidazoles as Potent and Orally Active mGlu5 Receptor Antagonists with an Improved PK Profile

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

Cytochrome P-450-induced cytotoxicity of mitoxantrone by formation of electrophilic intermediates

13C-Markierung der Seitenketten von Mitoxantrone

Pharmacokinetics and metabolism of mitoxantrone : a review

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