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Development of targeted protein degradation therapeutics

Nature chemical biology, 2019-10, Vol.15 (10), p.937-944

2019

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Discovery of CRBN E3 Ligase Modulator CC-92480 for the Treatment of Relapsed and Refractory Multiple Myeloma

Journal of medicinal chemistry, 2020-07, Vol.63 (13), p.6648-6676

2020

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Discovery of Small Molecule Splicing Modulators of Survival Motor Neuron‑2 (SMN2) for the Treatment of Spinal Muscular Atrophy (SMA)

Journal of medicinal chemistry, 2018-12, Vol.61 (24), p.11021-11036

2018

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Intermolecular Crossed [2 + 2] Cycloaddition Promoted by Visible-Light Triplet Photosensitization: Expedient Access to Polysubstituted 2‑Oxaspiro[3.3]heptanes

Journal of the American Chemical Society, 2021-03, Vol.143 (10), p.4055-4063

2021

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Expedient access to saturated nitrogen heterocycles by photoredox cyclization of imino-tethered dihydropyridines

Chemical science (Cambridge), 2019-11, Vol.1 (41), p.9591-9596

2019

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Use of Intramolecular 1,5-Sulfur–Oxygen and 1,5-Sulfur–Halogen Interactions in the Design of N‑Methyl-5-aryl‑N‑(2,2,6,6-tetramethylpiperidin-4-yl)-1,3,4-thiadiazol-2-amine SMN2 Splicing Modulators

Journal of medicinal chemistry, 2021-04, Vol.64 (8), p.4744-4761

2021

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Evolution of Cereblon-Mediated Protein Degradation as a Therapeutic Modality

ACS medicinal chemistry letters, 2019-12, Vol.10 (12), p.1592-1602

2019

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Non-directed allylic C–H acetoxylation in the presence of Lewis basic heterocycles

Chemical science (Cambridge), 2014-01, Vol.5 (6), p.2352

2014

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Discovery of a Brain-Penetrant ATP-Competitive Inhibitor of the Mechanistic Target of Rapamycin (mTOR) for CNS Disorders

Journal of medicinal chemistry, 2020-02, Vol.63 (3), p.1068-1083

2020

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Discovery of a novel indole pharmacophore for the irreversible inhibition of myeloperoxidase (MPO)

Bioorganic & medicinal chemistry, 2020-06, Vol.28 (12), p.115548-115548, Article 115548

2020

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Die Erschließung von Wirkstoffmetaboliten durch übergangsmetallkatalysierte C-H-Oxidation: die Leber als Inspiration für die Synthese

Angewandte Chemie, 2016-11, Vol.128 (46), p.14430-14451

2016

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Potent, Selective, and Orally Bioavailable Inhibitors of VPS34 Provide Chemical Tools to Modulate Autophagy in Vivo

ACS medicinal chemistry letters, 2016-01, Vol.7 (1), p.72-76

2016

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A scalable synthesis of (1R,3S,5R)-2-(tert-butoxycarbonyl)-2-azabicyclo[3.1.0]hexane-3-carboxylic acid

Tetrahedron letters, 2013-12, Vol.54 (49), p.6722-6724

2013

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Natural products on demand

Nature chemistry, 2014-05, Vol.6 (6), p.460-461

Hamann, Lawrence G.

2014

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Palladium-Catalyzed Microwave-Assisted Amination of 1-Bromonaphthalenes and 5- and 8-Bromoquinolines

Organic letters, 2003-03, Vol.5 (6), p.897-900

2003

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Pyridine amides as potent and selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1

Bioorganic & medicinal chemistry, 2008-06, Vol.18 (11), p.3168-3172

2008

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An Efficient, Stereospecific Synthesis of the Dimer-Selective Retinoid X Receptor Modulator (2E,4E,6Z)-7-[5,6,7,8- Tetrahydro-5,5,8,8-tetramethyl-2- (n-propyloxy)naphthalen-3-yl]-3- methylocta-2,4,6-trienoic Acid

Journal of organic chemistry, 2000-05, Vol.65 (10), p.3233-3235

Hamann, Lawrence G

2000

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Expedient access to saturated nitrogen heterocycles by photoredox cyclization of imino-tethered dihydropyridines† †Electronic supplementary information (ESI) available: Supplementary substrate scope. Supplementary optimizations table. BDFE calculations. Detailed experimental procedures and compound characterization. See DOI: 10.1039/c9sc03429c

Chemical science (Cambridge), 2019-08, Vol.10 (41), p.9591-9596

2019

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Small molecule allosteric inhibitors of ROR[gamma]t block Th17-dependent inflammation and associated gene expression in vivo

PloS one, 2021-11, Vol.16 (11), p.e0248034

2021

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The 2nd Alpine Winter Conference on Medicinal and Synthetic Chemistry

ChemMedChem, 2021-08, Vol.16 (15), p.2417-2423

2021

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A scalable synthesis of (1R,3S,5R)-2-(tert-butoxycarbonyl)-2-azabicyclo[3.1.0]hexane-3-car b oxylic acid

Tetrahedron letters, 2013-12, Vol.54 (49), p.6722-6724

2013

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Effects of isosteric pyridone replacements in androgen receptor antagonists based on 1,2-dihydro- and 1,2,3,4-tetrahydro-2,2-dimethyl-6-trifluoromethyl-8-pyridono[5,6- g]quinolines

Bioorganic & medicinal chemistry letters, 2000-03, Vol.10 (5), p.411-414

2000

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ChemInform Abstract: Accessing Drug Metabolites via Transition‐Metal Catalyzed C—H Oxidation: The Liver as Synthetic Inspiration

ChemInform, 2016-12, Vol.47 (51), p.no-no

2016

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Development of targeted protein degradation therapeutics

Discovery of CRBN E3 Ligase Modulator CC-92480 for the Treatment of Relapsed and Refractory Multiple Myeloma

Discovery of Small Molecule Splicing Modulators of Survival Motor Neuron‑2 (SMN2) for the Treatment of Spinal Muscular Atrophy (SMA)

Intermolecular Crossed [2 + 2] Cycloaddition Promoted by Visible-Light Triplet Photosensitization: Expedient Access to Polysubstituted 2‑Oxaspiro[3.3]heptanes

Expedient access to saturated nitrogen heterocycles by photoredox cyclization of imino-tethered dihydropyridines

Use of Intramolecular 1,5-Sulfur–Oxygen and 1,5-Sulfur–Halogen Interactions in the Design of N‑Methyl-5-aryl‑N‑(2,2,6,6-tetramethylpiperidin-4-yl)-1,3,4-thiadiazol-2-amine SMN2 Splicing Modulators

Evolution of Cereblon-Mediated Protein Degradation as a Therapeutic Modality

Non-directed allylic C–H acetoxylation in the presence of Lewis basic heterocycles

Discovery of a Brain-Penetrant ATP-Competitive Inhibitor of the Mechanistic Target of Rapamycin (mTOR) for CNS Disorders

Identification of Brain-Penetrant ATP-Competitive mTOR Inhibitors for CNS Syndromes

Discovery of a novel indole pharmacophore for the irreversible inhibition of myeloperoxidase (MPO)

Die Erschließung von Wirkstoffmetaboliten durch übergangsmetallkatalysierte C-H-Oxidation: die Leber als Inspiration für die Synthese

Potent, Selective, and Orally Bioavailable Inhibitors of VPS34 Provide Chemical Tools to Modulate Autophagy in Vivo

A scalable synthesis of (1R,3S,5R)-2-(tert-butoxycarbonyl)-2-azabicyclo[3.1.0]hexane-3-carboxylic acid

Natural products on demand

Palladium-Catalyzed Microwave-Assisted Amination of 1-Bromonaphthalenes and 5- and 8-Bromoquinolines

Pyridine amides as potent and selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1

An Efficient, Stereospecific Synthesis of the Dimer-Selective Retinoid X Receptor Modulator (2E,4E,6Z)-7-[5,6,7,8- Tetrahydro-5,5,8,8-tetramethyl-2- (n-propyloxy)naphthalen-3-yl]-3- methylocta-2,4,6-trienoic Acid

Small molecule allosteric inhibitors of ROR[gamma]t block Th17-dependent inflammation and associated gene expression in vivo

The 2nd Alpine Winter Conference on Medicinal and Synthetic Chemistry

A scalable synthesis of (1R,3S,5R)-2-(tert-butoxycarbonyl)-2-azabicyclo[3.1.0]hexane-3-car b oxylic acid

Effects of isosteric pyridone replacements in androgen receptor antagonists based on 1,2-dihydro- and 1,2,3,4-tetrahydro-2,2-dimethyl-6-trifluoromethyl-8-pyridono[5,6- g]quinolines

Abstract ND02: Discovery of BMS-986365, a ligand-directed androgen receptor degrader (AR LDD) with a dual mechanism-of-action and best-in-class potential, for the treatment of advanced prostate cancer

ChemInform Abstract: Accessing Drug Metabolites via Transition‐Metal Catalyzed C—H Oxidation: The Liver as Synthetic Inspiration

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