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Structural Optimization Affording 2-(R)-(1-(R)-3,5-Bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a Potent, Orally Active, Long-Acting Morpholine Acetal Human NK-1 Receptor Antagonist

Journal of medicinal chemistry, 1998-11, Vol.41 (23), p.4607-4614

1998

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Cyclopentane-based human NK1 antagonists. Part 2: Development of potent, orally active, water-soluble derivatives

Bioorganic & medicinal chemistry letters, 2006-09, Vol.16 (17), p.4504-4511

2006

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Combinatorial synthesis of 3-(Amidoalkyl) and 3-(Aminoalkyl)-2-arylindole derivatives: discovery of potent ligands for a variety of G-protein coupled receptors

Bioorganic & medicinal chemistry letters, 2002-01, Vol.12 (1), p.93-96

2002

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In vitro and in vivo predictors of the anti-emetic activity of tachykinin NK1 receptor antagonists

European journal of pharmacology, 1997-05, Vol.326 (2-3), p.201-209

1997

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Characterization of a Novel, Non-peptidyl Antagonist of the Human Glucagon Receptor

The Journal of biological chemistry, 1999-03, Vol.274 (13), p.8694-8697

1999

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Spirocyclic NK1 antagonists I:[4.5] and [5.5]-spiroketals

Bioorganic & medicinal chemistry letters, 2002-09, Vol.12 (18), p.2515-2518

2002

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Identification and isolation of a membrane protein necessary for leukotriene production

Nature (London), 1990-01, Vol.343 (6255), p.278-281

1990

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Tryptophan-Derived NK1 Antagonists: Conformationally Constrained Heterocyclic Bioisosteres of the Ester Linkage

Journal of medicinal chemistry, 1995-03, Vol.38 (6), p.923-933

1995

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Distinct Mechanism for Antidepressant Activity by Blockade of Central Substance P Receptors

Science (American Association for the Advancement of Science), 1998-09, Vol.281 (5383), p.1640-1645

1998

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Cyclopentane-based human NK1 antagonists. Part 1: Discovery and initial SAR

Bioorganic & medicinal chemistry letters, 2006-09, Vol.16 (17), p.4497-4503

2006

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An Orally Active, Water-Soluble Neurokinin-1 Receptor Antagonist Suitable for Both Intravenous and Oral Clinical Administration

Journal of medicinal chemistry, 2001-11, Vol.44 (24), p.4296-4299

2001

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Phosphorylated Morpholine Acetal Human Neurokinin-1 Receptor Antagonists as Water-Soluble Prodrugs

Journal of medicinal chemistry, 2000-03, Vol.43 (6), p.1234-1241

2000

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Characterization of the binding of a potent, selective, radioiodinated antagonist to the human neurokinin-1 receptor

Molecular pharmacology, 1992-09, Vol.42 (3), p.458-463

1992

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Characterization of the interaction of N-acyl-L-tryptophan benzyl ester neurokinin antagonists with the human neurokinin-1 receptor

The Journal of biological chemistry, 1994-03, Vol.269 (9), p.6587-6591

1994

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Pharmacological effects of non-steroidal antiinflammatory agents on prostaglandin and leukotriene synthesis in mouse peritoneal macrophages

Biochemical pharmacology, 1983-08, Vol.32 (15), p.2319-2322

1983

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Determination of the amino acid residues in substance P conferring selectivity and specificity for the rat neurokinin receptors

Molecular pharmacology, 1992-06, Vol.41 (6), p.1096-1099

1992

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N-Acyl-L-tryptophan benzyl esters: potent substance P receptor antagonists

Journal of medicinal chemistry, 1993-07, Vol.36 (14), p.2044-2045

1993

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L-tryptophan urea amides as NK1/ nk2 dual antagonists

Bioorganic & medicinal chemistry letters, 1998-08, Vol.8 (16), p.2259-2262

1998

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4,4-Disubstituted Piperidine High-Affinity NK1 Antagonists: Structure−Activity Relationships and in Vivo Activity

Journal of medicinal chemistry, 1998-11, Vol.41 (23), p.4623-4635

1998

Volltextzugriff (PDF)

Spirocyclic NK(1) antagonists I: [4.5] and [5.5]-spiroketals

Bioorganic & medicinal chemistry letters, 2002-09, Vol.12 (18), p.2515-2518

2002

Volltextzugriff (PDF)

Identification of L-Tryptophan Derivatives with Potent and Selective Antagonist Activity at the NK1 Receptor

Journal of medicinal chemistry, 1994-04, Vol.37 (9), p.1269-1274

1994

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Spirocyclic NK 1 antagonists I: [4.5] and [5.5]-Spiroketals

Bioorganic & medicinal chemistry letters, 2002, Vol.12 (18), p.2515-2518

2002

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L-tryptophan urea amides as [formula omitted] dual antagonists

Bioorganic & medicinal chemistry letters, 1998-08, Vol.8 (16), p.2259-2262

1998

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4,4-Disubstituted piperidines : a new class of NK1 antagonist

Journal of medicinal chemistry, 1995-04, Vol.38 (8), p.1264-1266

1995

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Characterization of the interaction of diacylpiperazine antagonists with the human neurokinin-1 receptor: identification of a common binding site for structurally dissimilar antagonists

Molecular pharmacology, 1995-04, Vol.47 (4), p.660-665

1995

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Structural Optimization Affording 2-(R)-(1-(R)-3,5-Bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a Potent, Orally Active, Long-Acting Morpholine Acetal Human NK-1 Receptor Antagonist

Cyclopentane-based human NK1 antagonists. Part 2: Development of potent, orally active, water-soluble derivatives

Combinatorial synthesis of 3-(Amidoalkyl) and 3-(Aminoalkyl)-2-arylindole derivatives: discovery of potent ligands for a variety of G-protein coupled receptors

In vitro and in vivo predictors of the anti-emetic activity of tachykinin NK1 receptor antagonists

Characterization of a Novel, Non-peptidyl Antagonist of the Human Glucagon Receptor

Spirocyclic NK1 antagonists I:[4.5] and [5.5]-spiroketals

Identification and isolation of a membrane protein necessary for leukotriene production

Tryptophan-Derived NK1 Antagonists: Conformationally Constrained Heterocyclic Bioisosteres of the Ester Linkage

Distinct Mechanism for Antidepressant Activity by Blockade of Central Substance P Receptors

Cyclopentane-based human NK1 antagonists. Part 1: Discovery and initial SAR

An Orally Active, Water-Soluble Neurokinin-1 Receptor Antagonist Suitable for Both Intravenous and Oral Clinical Administration

Phosphorylated Morpholine Acetal Human Neurokinin-1 Receptor Antagonists as Water-Soluble Prodrugs

Characterization of the binding of a potent, selective, radioiodinated antagonist to the human neurokinin-1 receptor

Characterization of the interaction of N-acyl-L-tryptophan benzyl ester neurokinin antagonists with the human neurokinin-1 receptor

Pharmacological effects of non-steroidal antiinflammatory agents on prostaglandin and leukotriene synthesis in mouse peritoneal macrophages

Determination of the amino acid residues in substance P conferring selectivity and specificity for the rat neurokinin receptors

N-Acyl-L-tryptophan benzyl esters: potent substance P receptor antagonists

L-tryptophan urea amides as NK1/ nk2 dual antagonists

4,4-Disubstituted Piperidine High-Affinity NK1 Antagonists: Structure−Activity Relationships and in Vivo Activity

Spirocyclic NK(1) antagonists I: [4.5] and [5.5]-spiroketals

Identification of L-Tryptophan Derivatives with Potent and Selective Antagonist Activity at the NK1 Receptor

Spirocyclic NK 1 antagonists I: [4.5] and [5.5]-Spiroketals

L-tryptophan urea amides as [formula omitted] dual antagonists

4,4-Disubstituted piperidines : a new class of NK1 antagonist

Characterization of the interaction of diacylpiperazine antagonists with the human neurokinin-1 receptor: identification of a common binding site for structurally dissimilar antagonists

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