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Discovery of Potent Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 Using a Novel Growth-Based Protocol of in Silico Screening and Optimization in CONTOUR

Journal of chemical information and modeling, 2019-08, Vol.59 (8), p.3422-3436

2019

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Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR) β Agonist

Journal of medicinal chemistry, 2016-04, Vol.59 (7), p.3264-3271

2016

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Pharmacological characterization of the selective 11β-hydroxysteroid dehydrogenase 1 inhibitor, BI 135585, a clinical candidate for the treatment of type 2 diabetes

European journal of pharmacology, 2015-01, Vol.746, p.50-55

2015

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Discovery of BI 135585, an in vivo efficacious oxazinanone-based 11β hydroxysteroid dehydrogenase type 1 inhibitor

Bioorganic & medicinal chemistry, 2017-07, Vol.25 (14), p.3649-3657

2017

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Influence of sub-chronic selective 11β-hydroxysteroid dehydrogenase 1 inhibition on the hypothalamic-pituitary-adrenal axis in female cynomolgus monkeys

European journal of pharmacology, 2016-10, Vol.789, p.68-74

2016

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Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core

Bioorganic & medicinal chemistry letters, 2016-10, Vol.26 (20), p.5044-5050

2016

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Structure-Based Design and Synthesis of 1,3-Oxazinan-2-one Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1

Journal of medicinal chemistry, 2011-09, Vol.54 (17), p.6050-6062

2011

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An electronic environment and contact direction sensitive scoring function for predicting affinities of protein–ligand complexes in Contour

Journal of molecular graphics & modelling, 2014-09, Vol.53, p.118-127

2014

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Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility

ACS medicinal chemistry letters, 2011-10, Vol.2 (10), p.747-751

2011

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Spirocyclic ureas: Orally bioavailable 11β-HSD1 inhibitors identified by computer-aided drug design

Bioorganic & medicinal chemistry letters, 2010-02, Vol.20 (3), p.881-886

2010

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Identification and Characterization of 4-Methylbenzyl 4-[(Pyrimidin-2-ylamino)methyl]piperidine-1-carboxylate, an Orally Bioavailable, Brain Penetrant NR2B Selective N-Methyl-d-Aspartate Receptor Antagonist

Journal of medicinal chemistry, 2007-02, Vol.50 (4), p.807-819

2007

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Cyclic benzamidines as orally efficacious NR2B-selective NMDA receptor antagonists

Bioorganic & medicinal chemistry letters, 2007-07, Vol.17 (14), p.3997-4000

2007

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Discovery and optimization of adamantyl carbamate inhibitors of 11β-HSD1

Bioorganic & medicinal chemistry letters, 2010-11, Vol.20 (22), p.6725-6729

2010

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NR2B-Selective N-Methyl-d-aspartate Antagonists: Synthesis and Evaluation of 5-Substituted Benzimidazoles

Journal of medicinal chemistry, 2004-04, Vol.47 (8), p.2089-2096

2004

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Synthesis and evaluation of novel tricyclic benzo[4.5]cyclohepta[1.2]pyridine derivatives as NMDA/NR2B antagonists

Bioorganic & medicinal chemistry letters, 2009-09, Vol.19 (17), p.5132-5135

2009

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Nonpeptide glycoprotein IIb/IIIa inhibitors: Substituted quinazolinediones and quinazolinones as potent fibrinogen receptor antagonists

Bioorganic & medicinal chemistry letters, 1998-03, Vol.8 (5), p.483-486

1998

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Abstract 3187: Pediatric Preclinical Testing Consortium evaluation of the menin inhibitor, VTP-50469, against xenograft models of MLL-rearranged infant acute lymphoblastic leukemia

Cancer research (Chicago, Ill.), 2018-07, Vol.78 (13_Supplement), p.3187-3187

2018

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Pyridazine based inhibitors of p38 MAPK

Bioorganic & medicinal chemistry letters, 2002-02, Vol.12 (4), p.689-692

2002

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Transglutaminase Inhibition by 2-[(2-Oxopropyl)thio]imidazolium Derivatives: Mechanism of Factor XIIIa Inactivation

Biochemistry (Easton), 1994-08, Vol.33 (33), p.10109-10119

1994

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Orally Efficacious NR2B-Selective NMDA Receptor Antagonists

Bioorganic & medicinal chemistry letters, 2003-02, Vol.13 (4), p.697-700

2003

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The potent, selective RORγt blocker, VTP-43742, suppresses Th17 production in vivo and provides greater benefit than IL-17 blockade in the EAE model of autoimmunity (THER3P.968)

The Journal of immunology (1950), 2015-05, Vol.194 (1_Supplement), p.68-68.1

2015

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Abstract 334: The LXRβ Selective Agonist, VTP-38443, Significantly Decreases Plaque Cholesterol Ester Content and Inflammation in a Murine Model of Accelerated Atherosclerosis

Arteriosclerosis, thrombosis, and vascular biology, 2015-05, Vol.35 (suppl_1)

2015

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Discovery of Potent Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 Using a Novel Growth-Based Protocol of in Silico Screening and Optimization in CONTOUR

Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR) β Agonist

Pharmacological characterization of the selective 11β-hydroxysteroid dehydrogenase 1 inhibitor, BI 135585, a clinical candidate for the treatment of type 2 diabetes

Discovery of BI 135585, an in vivo efficacious oxazinanone-based 11β hydroxysteroid dehydrogenase type 1 inhibitor

Influence of sub-chronic selective 11β-hydroxysteroid dehydrogenase 1 inhibition on the hypothalamic-pituitary-adrenal axis in female cynomolgus monkeys

Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core

Structure-Based Design and Synthesis of 1,3-Oxazinan-2-one Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1

An electronic environment and contact direction sensitive scoring function for predicting affinities of protein–ligand complexes in Contour

Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility

Spirocyclic ureas: Orally bioavailable 11β-HSD1 inhibitors identified by computer-aided drug design

Identification and Characterization of 4-Methylbenzyl 4-[(Pyrimidin-2-ylamino)methyl]piperidine-1-carboxylate, an Orally Bioavailable, Brain Penetrant NR2B Selective N-Methyl-d-Aspartate Receptor Antagonist

A Menin-MLL Inhibitor Induces Specific Chromatin Changes and Eradicates Disease in Models of MLL-Rearranged Leukemia

Cyclic benzamidines as orally efficacious NR2B-selective NMDA receptor antagonists

Discovery and optimization of adamantyl carbamate inhibitors of 11β-HSD1

NR2B-Selective N-Methyl-d-aspartate Antagonists: Synthesis and Evaluation of 5-Substituted Benzimidazoles

Synthesis and evaluation of novel tricyclic benzo[4.5]cyclohepta[1.2]pyridine derivatives as NMDA/NR2B antagonists

Nonpeptide glycoprotein IIb/IIIa inhibitors: Substituted quinazolinediones and quinazolinones as potent fibrinogen receptor antagonists

Abstract 3187: Pediatric Preclinical Testing Consortium evaluation of the menin inhibitor, VTP-50469, against xenograft models of MLL-rearranged infant acute lymphoblastic leukemia

Process Development of the BACE Inhibitors BI 1147560 BS and BI 1181181 MZ

Class III Antiarrhythmic Activity in Vivo by Selective Blockade of the Slowly Activating Cardiac Delayed Rectifier Potassium Current I Ks by (R)-2-(2,4- Trifluoromethyl)-N-[2-oxo-5-phenyl- 1-(2,2,2-trifluoroethyl)-2,3-dihydro- 1H-benzo[e][1,4]diazepin-3-yl]acetamide

Pyridazine based inhibitors of p38 MAPK

Transglutaminase Inhibition by 2-[(2-Oxopropyl)thio]imidazolium Derivatives: Mechanism of Factor XIIIa Inactivation

Orally Efficacious NR2B-Selective NMDA Receptor Antagonists

The potent, selective RORγt blocker, VTP-43742, suppresses Th17 production in vivo and provides greater benefit than IL-17 blockade in the EAE model of autoimmunity (THER3P.968)

Abstract 334: The LXRβ Selective Agonist, VTP-38443, Significantly Decreases Plaque Cholesterol Ester Content and Inflammation in a Murine Model of Accelerated Atherosclerosis

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