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Enantioselective Total Synthesis of Quadrigemine C and Psycholeine

Journal of the American Chemical Society, 2002-08, Vol.124 (31), p.9008-9009

2002

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Characterization of 2-(2,6-dichloro-benzyl)-thiazolo[5,4- d]pyrimidin-7-yl]-(4-trifluoromethyl-phenyl)-amine (JNJ-39729209) as a novel TRPV1 antagonist

European journal of pharmacology, 2011-08, Vol.663 (1), p.40-50

2011

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Structural Basis of Small-Molecule Aggregate Induced Inhibition of a Protein–Protein Interaction

Journal of medicinal chemistry, 2017-04, Vol.60 (8), p.3511-3517

2017

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Accelerating Lead Identification by High Throughput Virtual Screening: Prospective Case Studies from the Pharmaceutical Industry

Journal of chemical information and modeling, 2019-05, Vol.59 (5), p.2046-2062

2019

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Enantioselective Total Synthesis of Shahamin K

Journal of the American Chemical Society, 2001-05, Vol.123 (20), p.4851-4852

2001

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Stereocontrolled enantioselective total synthesis of the [2+2] quadrigemine alkaloids

Tetrahedron, 2015-09, Vol.71 (37), p.6424-6436

2015

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A Single Amino Acid Difference between Mouse and Human 5-Lipoxygenase Activating Protein (FLAP) Explains the Speciation and Differential Pharmacology of Novel FLAP Inhibitors

The Journal of biological chemistry, 2016-06, Vol.291 (24), p.12724-12731

2016

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The discovery and preclinical characterization of 6-chloro-N-(2-(4,4-difluoropiperidin-1-yl)-2-(2-(trifluoromethyl)pyrimidin-5-yl)ethyl)quinoline-5-carboxamide based P2X7 antagonists

Bioorganic & medicinal chemistry letters, 2016-10, Vol.26 (19), p.4781-4784

2016

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Polypharmacology of Small-Molecule Modulators of the 5-Lipoxygenase Activating Protein (FLAP) Observed via a High-throughput Lipidomics Platform

Journal of biomolecular screening, 2016-02, Vol.21 (2), p.127-135

2016

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Scale-Up Synthesis of a TRPV1 Antagonist Featuring a Facile Thiazolo[5,4-d]pyrimidine Formation

Organic process research & development, 2011-03, Vol.15 (2), p.382-388

2011

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Discovery and synthesis of 6,7,8,9-tetrahydro-5H-pyrimido-[4,5-d]azepines as novel TRPV1 antagonists

Bioorganic & medicinal chemistry letters, 2010-12, Vol.20 (23), p.7137-7141

2010

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Identification and synthesis of [1,2,4]triazolo[3,4-a]phthalazine derivatives as high-affinity ligands to the α2δ-1 subunit of voltage gated calcium channel

Bioorganic & medicinal chemistry letters, 2004-05, Vol.14 (10), p.2463-2467

2004

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Identification and synthesis of 2,7-diamino-thiazolo[5,4- d]pyrimidine derivatives as TRPV1 antagonists

Bioorganic & medicinal chemistry letters, 2009, Vol.19 (1), p.40-46

2009

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Discovery of N-{ N-[(3-cyanobenzene) sulfonyl]-4( R)-(3,3-difluoropiperidin-1-yl)-( l)-prolyl}-4-[(3′,5′-dichloro-isonicotinoyl) amino]-( l)-phenylalanine (MK-0617), a highly potent and orally active VLA-4 antagonist

Bioorganic & medicinal chemistry letters, 2009-10, Vol.19 (19), p.5803-5806

2009

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1,2-Diamino-ethane-substituted-6,7,8,9-tetrahydro-5H-pyrimido[4,5-d]azepines as TRPV1 antagonists with improved properties

Bioorganic & medicinal chemistry letters, 2010-12, Vol.20 (23), p.7142-7146

2010

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The discovery and preclinical characterization of 6-chloro-N-(2-(4,4-difluoropiperidin-1-yl)-2-(2-(trifluoromethyl)p y rimidin-5-yl)ethyl)quinoline-5-carboxamide based P2X7 antagonists

Bioorganic & medicinal chemistry letters, 2016-10, Vol.26 (19), p.4781-4784

2016

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PHARMACOLOGICAL CHARACTERIZATION OF A PURINERGIC RECEPTOR (P2X7) ANTAGONIST IN‐VITRO AND IN‐VIVO

The FASEB journal, 2010-04, Vol.24 (S1), p.lb460-lb460

2010

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Discovery and synthesis of 6,7,8,9-tetrahydro-5 H-pyrimido-[4,5- d]azepines as novel TRPV1 antagonists

Bioorganic & medicinal chemistry letters, 2010, Vol.20 (23), p.7137-7141

2010

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1,2-Diamino-ethane-substituted-6,7,8,9-tetrahydro-5 H-pyrimido[4,5- d]azepines as TRPV1 antagonists with improved properties

Bioorganic & medicinal chemistry letters, 2010, Vol.20 (23), p.7142-7146

2010

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Scope and Limitations of the Thionium Ion-Initiated Prins-Pinacol Synthesis of Carbocycles

Synlett, 2004-07, Vol.2004 (8), p.1387-1393

2004

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Identification and synthesis of [1,2,4]triazolo[3,4-a]phthalazine derivatives as high-affinity ligands to the alpha 2 delta-1 subunit of voltage gated calcium channel

Bioorganic & medicinal chemistry letters, 2004-05, Vol.14 (10), p.2463

2004

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Identification and synthesis of [1,2,4]triazolo[3,4- a]phthalazine derivatives as high-affinity ligands to the α 2δ-1 subunit of voltage gated calcium channel

Bioorganic & medicinal chemistry letters, 2004, Vol.14 (10), p.2463-2467

2004

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Identification and Synthesis of [1,2,4]Triazolo[3,4‐a]phthalazine Derivatives as High‐Affinity Ligands to the α 2 δ‐1 Subunit of Voltage Gated Calcium Channel

ChemInform, 2004-09, Vol.35 (37)

Lebsack, Alec D.

2004

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ChemInform Abstract: 1,2-Diamino-ethane-substituted-6,7,8,9-tetrahydro-5H-pyrimido [4,5-d]azepines as TRPV1 Antagonists with Improved Properties

ChemInform, 2011-04, Vol.42 (15), p.no-no

2011

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Scope and Limitations of the Thionium Ion-Initiated Prins-Pinacol Synthesis of Carbocycles

ChemInform, 2004-11, Vol.35 (45), p.no-no

2004

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Enantioselective Total Synthesis of Quadrigemine C and Psycholeine

Characterization of 2-(2,6-dichloro-benzyl)-thiazolo[5,4- d]pyrimidin-7-yl]-(4-trifluoromethyl-phenyl)-amine (JNJ-39729209) as a novel TRPV1 antagonist

Structural Basis of Small-Molecule Aggregate Induced Inhibition of a Protein–Protein Interaction

Accelerating Lead Identification by High Throughput Virtual Screening: Prospective Case Studies from the Pharmaceutical Industry

Enantioselective Total Synthesis of Shahamin K

Stereocontrolled enantioselective total synthesis of the [2+2] quadrigemine alkaloids

A Single Amino Acid Difference between Mouse and Human 5-Lipoxygenase Activating Protein (FLAP) Explains the Speciation and Differential Pharmacology of Novel FLAP Inhibitors

The discovery and preclinical characterization of 6-chloro-N-(2-(4,4-difluoropiperidin-1-yl)-2-(2-(trifluoromethyl)pyrimidin-5-yl)ethyl)quinoline-5-carboxamide based P2X7 antagonists

Polypharmacology of Small-Molecule Modulators of the 5-Lipoxygenase Activating Protein (FLAP) Observed via a High-throughput Lipidomics Platform

Scale-Up Synthesis of a TRPV1 Antagonist Featuring a Facile Thiazolo[5,4-d]pyrimidine Formation

Discovery and synthesis of 6,7,8,9-tetrahydro-5H-pyrimido-[4,5-d]azepines as novel TRPV1 antagonists

Identification and synthesis of [1,2,4]triazolo[3,4-a]phthalazine derivatives as high-affinity ligands to the α2δ-1 subunit of voltage gated calcium channel

Identification and synthesis of 2,7-diamino-thiazolo[5,4- d]pyrimidine derivatives as TRPV1 antagonists

Discovery of N-{ N-[(3-cyanobenzene) sulfonyl]-4( R)-(3,3-difluoropiperidin-1-yl)-( l)-prolyl}-4-[(3′,5′-dichloro-isonicotinoyl) amino]-( l)-phenylalanine (MK-0617), a highly potent and orally active VLA-4 antagonist

1,2-Diamino-ethane-substituted-6,7,8,9-tetrahydro-5H-pyrimido[4,5-d]azepines as TRPV1 antagonists with improved properties

The discovery and preclinical characterization of 6-chloro-N-(2-(4,4-difluoropiperidin-1-yl)-2-(2-(trifluoromethyl)p y rimidin-5-yl)ethyl)quinoline-5-carboxamide based P2X7 antagonists

PHARMACOLOGICAL CHARACTERIZATION OF A PURINERGIC RECEPTOR (P2X7) ANTAGONIST IN‐VITRO AND IN‐VIVO

Discovery and synthesis of 6,7,8,9-tetrahydro-5 H-pyrimido-[4,5- d]azepines as novel TRPV1 antagonists

1,2-Diamino-ethane-substituted-6,7,8,9-tetrahydro-5 H-pyrimido[4,5- d]azepines as TRPV1 antagonists with improved properties

Scope and Limitations of the Thionium Ion-Initiated Prins-Pinacol Synthesis of Carbocycles

Identification and synthesis of [1,2,4]triazolo[3,4-a]phthalazine derivatives as high-affinity ligands to the alpha 2 delta-1 subunit of voltage gated calcium channel

Identification and synthesis of [1,2,4]triazolo[3,4- a]phthalazine derivatives as high-affinity ligands to the α 2δ-1 subunit of voltage gated calcium channel

Identification and Synthesis of [1,2,4]Triazolo[3,4‐a]phthalazine Derivatives as High‐Affinity Ligands to the α 2 δ‐1 Subunit of Voltage Gated Calcium Channel

ChemInform Abstract: 1,2-Diamino-ethane-substituted-6,7,8,9-tetrahydro-5H-pyrimido [4,5-d]azepines as TRPV1 Antagonists with Improved Properties

Scope and Limitations of the Thionium Ion-Initiated Prins-Pinacol Synthesis of Carbocycles

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