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Discovery Process and Pharmacological Characterization of 2-(S)-(4-Fluoro-2-methylphenyl)piperazine-1-carboxylic Acid [1-(R)-(3,5-Bis-trifluoromethylphenyl)ethyl]methylamide (Vestipitant) as a Potent, Selective, and Orally Active NK1 Receptor Antagonist

Journal of medicinal chemistry, 2009-05, Vol.52 (10), p.3238-3247

2009

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Quality by Design in lead optimization: a new strategy to address productivity in drug discovery

Current opinion in pharmacology, 2011-10, Vol.11 (5), p.515-520

2011

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Drug efficiency: a new concept to guide lead optimization programs towards the selection of better clinical candidates

Expert opinion on drug discovery, 2010-07, Vol.5 (7), p.609-618

2010

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Stereoselective Synthesis of a Key Intermediate of Sanfetrinem by Means of a Chelated Tin(IV) Enolate

Journal of organic chemistry, 1997-03, Vol.62 (6), p.1653-1661

1997

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Solution phase library of perhydrooxazin-4-ones

Tetrahedron letters, 1998-09, Vol.39 (36), p.6585-6588

1998

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1,2,4-Triazol-3-yl-thiopropyl-tetrahydrobenzazepines: A Series of Potent and Selective Dopamine D 3 Receptor Antagonists

Journal of medicinal chemistry, 2007-10, Vol.50 (21), p.5076-5089

2007

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Application of drug efficiency index in drug discovery: a strategy towards low therapeutic dose

Expert opinion on drug discovery, 2011-09, Vol.6 (9), p.913-920

2011

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The synthesis of a key intermediate of tricyclic beta-lactam antibiotics

Tetrahedron letters, 1995-06, Vol.36 (24), p.4283-4286

1995

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Analogues of 4,5-bis(3,5-dichlorophenyl)-2-trifluoromethyl-1H-imidazole as potential antibacterial agents

Bioorganic & medicinal chemistry letters, 1999-04, Vol.9 (7), p.1023-1028

1999

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Dopamine D 3 receptor antagonists: The quest for a potentially selective PET ligand. Part 3: Radiosynthesis and in vivo studies

Bioorganic & medicinal chemistry letters, 2009-09, Vol.19 (17), p.5056-5059

2009

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Application of LC-NMR to the identification of bulk drug impurities in NK1 antagonist GW597599 (vestipitant)

Magnetic resonance in chemistry, 2010-07, Vol.48 (7), p.523-530

2010

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Dopamine D3 receptor antagonists: The quest for a potentially selective PET ligand. Part 3: Radiosynthesis and in vivo studies

Bioorganic & medicinal chemistry letters, 2009-09, Vol.19 (17), p.5056-5059

2009

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Dopamine D sub(3) receptor antagonists: The quest for a potentially selective PET ligand. Part 3: Radiosynthesis and in vivo studies

Bioorganic & medicinal chemistry letters, 2009-09, Vol.19 (17), p.5056-5059

2009

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1,2,4-triazol-3-yl-thiopropyl-tetrahydrobenzazepines: a series of potent and selective dopamine D(3) receptor antagonists

Journal of medicinal chemistry, 2007-10, Vol.50 (21), p.5076

2007

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Highly Diastereoselective Synthesis of 4- N-Methylformamidino Trinem (GV129606), a Potent Antibacterial Agent

Tetrahedron, 2000-07, Vol.56 (31), p.5649-5655

2000

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Nitrate ester derivatives from epoxides using CAN: Efficient preparation of key intermediates in the synthesis of 4-alkoxytrinems

Tetrahedron letters, 1997-05, Vol.38 (20), p.3587-3590

1997

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Solid-phase/solution-phase combinatorial synthesis of neuroimmunophilin ligands

Bioorganic & medicinal chemistry letters, 2000-05, Vol.10 (10), p.1007-1010

2000

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The stereoselective synthesis of 4-formyltrinem, a key intermediate for novel trinems

Tetrahedron letters, 1997-05, Vol.38 (20), p.3569-3572

1997

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Novel Amidoalkylation of 4-Acetoxyazetidinones with Allylic Boranes. A Stereoselective Entry into the Tribactams

Journal of the American Chemical Society, 1995-09, Vol.117 (37), p.9604-9605

1995

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Synthesis of polymer-bound fischer chromium alkoxy and aminocarbene complexes

Tetrahedron letters, 1999-04, Vol.40 (18), p.3635-3638

1999

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Readily Prepared Resin-Bound Thioimidates as Reagents for the Synthesis of Amidines

Synlett, 2001, Vol.2001 (3), p.0388-0390

2001

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Synthesis and antibacterial activity of some thio trinems

Bioorganic & medicinal chemistry letters, 1997-08, Vol.7 (15), p.2061-2066

1997

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Polymer-supported silyl cyanide and silyl azide: Useful reagents for solid-phase applications

Biotechnology and bioengineering, 2000, Vol.71 (1), p.38-43

2000

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The use of zinc enolates in the synthesis of a key intermediate for the preparation of trinem antibiotics

Tetrahedron letters, 1996-10, Vol.37 (41), p.7441-7444

1996

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Discovery Process and Pharmacological Characterization of 2-(S)-(4-Fluoro-2-methylphenyl)piperazine-1-carboxylic Acid [1-(R)-(3,5-Bis-trifluoromethylphenyl)ethyl]methylamide (Vestipitant) as a Potent, Selective, and Orally Active NK1 Receptor Antagonist

Quality by Design in lead optimization: a new strategy to address productivity in drug discovery

Drug efficiency: a new concept to guide lead optimization programs towards the selection of better clinical candidates

Stereoselective Synthesis of a Key Intermediate of Sanfetrinem by Means of a Chelated Tin(IV) Enolate

Solution phase library of perhydrooxazin-4-ones

1,2,4-Triazol-3-yl-thiopropyl-tetrahydrobenzazepines: A Series of Potent and Selective Dopamine D 3 Receptor Antagonists

Application of drug efficiency index in drug discovery: a strategy towards low therapeutic dose

The synthesis of a key intermediate of tricyclic beta-lactam antibiotics

Analogues of 4,5-bis(3,5-dichlorophenyl)-2-trifluoromethyl-1H-imidazole as potential antibacterial agents

Dopamine D 3 receptor antagonists: The quest for a potentially selective PET ligand. Part 3: Radiosynthesis and in vivo studies

Application of LC-NMR to the identification of bulk drug impurities in NK1 antagonist GW597599 (vestipitant)

Dopamine D3 receptor antagonists: The quest for a potentially selective PET ligand. Part 3: Radiosynthesis and in vivo studies

Dopamine D sub(3) receptor antagonists: The quest for a potentially selective PET ligand. Part 3: Radiosynthesis and in vivo studies

Discovery Process and Pharmacological Characterization of 2-( S )-(4-Fluoro-2-methylphenyl)piperazine-1-carboxylic Acid [1-( R )-(3,5-Bis-trifluoromethylphenyl)ethyl]methylamide (Vestipitant) as a Potent, Selective, and Orally Active NK 1 Receptor Antagonist

1,2,4-triazol-3-yl-thiopropyl-tetrahydrobenzazepines: a series of potent and selective dopamine D(3) receptor antagonists

Highly Diastereoselective Synthesis of 4- N-Methylformamidino Trinem (GV129606), a Potent Antibacterial Agent

Nitrate ester derivatives from epoxides using CAN: Efficient preparation of key intermediates in the synthesis of 4-alkoxytrinems

Solid-phase/solution-phase combinatorial synthesis of neuroimmunophilin ligands

The stereoselective synthesis of 4-formyltrinem, a key intermediate for novel trinems

Novel Amidoalkylation of 4-Acetoxyazetidinones with Allylic Boranes. A Stereoselective Entry into the Tribactams

Synthesis of polymer-bound fischer chromium alkoxy and aminocarbene complexes

Readily Prepared Resin-Bound Thioimidates as Reagents for the Synthesis of Amidines

Synthesis and antibacterial activity of some thio trinems

Polymer-supported silyl cyanide and silyl azide: Useful reagents for solid-phase applications

The use of zinc enolates in the synthesis of a key intermediate for the preparation of trinem antibiotics

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