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Synthesis and structure–activity relationship of N-(3-azabicyclo[3.1.0]hex-6-ylmethyl)-5-(2-pyridinyl)-1,3-thiazol-2-amines derivatives as NPY Y5 antagonists

Bioorganic & medicinal chemistry letters, 2010-08, Vol.20 (16), p.4741-4744

2010

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Novel morpholine scaffolds as selective dopamine (DA) D3 receptor antagonists

Bioorganic & medicinal chemistry letters, 2016-02, Vol.26 (4), p.1329-1332

2016

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1,2,4-Triazolyl 5‑Azaspiro[2.4]heptanes: Lead Identification and Early Lead Optimization of a New Series of Potent and Selective Dopamine D3 Receptor Antagonists

Journal of medicinal chemistry, 2016-09, Vol.59 (18), p.8549-8576

2016

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1,2,4-Triazolyl octahydropyrrolo[2,3-b]pyrroles: A new series of potent and selective dopamine D3 receptor antagonists

Bioorganic & medicinal chemistry, 2016-04, Vol.24 (8), p.1619-1636

2016

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The NK 1 receptor antagonist aprepitant attenuates NK 1 agonist‐induced scratching behaviour in the gerbil after intra‐dermal, topical or oral administration

Experimental dermatology, 2015-04, Vol.24 (4), p.312-314

2015

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The NK1 receptor antagonist aprepitant attenuates NK1 agonist-induced scratching behaviour in the gerbil after intra-dermal, topical or oral administration

Experimental dermatology, 2015-04, Vol.24 (4), p.312-314

2015

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In vitro and in vivo characterization of the novel GABA B receptor positive allosteric modulator, 2-{1-[2-(4-chlorophenyl)-5-methylpyrazolo[1,5-a]pyrimidin-7-yl]-2-piperidinyl}ethanol (CMPPE)

Neuropharmacology, 2011-10, Vol.61 (5), p.957-966

2011

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In vivo rat PK profiling in drug discovery: new challenges

Expert opinion on drug discovery, 2010-11, Vol.5 (11), p.1031-1037

2010

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Design, synthesis and SAR of a novel series of benzimidazoles as potent NPY Y5 antagonists

Bioorganic & medicinal chemistry letters, 2010-12, Vol.20 (23), p.7120-7123

2010

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1-Heteroaryl-6-(3,4-dichlorophenyl)-3-azabicyclo[4.1.0]heptane: Further insights into a class of triple re-uptake inhibitors

Bioorganic & medicinal chemistry, 2011-06, Vol.19 (11), p.3451-3461

2011

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Synthesis and pharmacological characterization of 5-phenyl-2-[2-(1-piperidinylcarbonyl)phenyl]-2,3-dihydro-1H-pyrrolo[1,2-c]imidazol-1-ones: A new class of Neuropeptide S antagonists

Bioorganic & medicinal chemistry letters, 2010-12, Vol.20 (24), p.7308-7311

2010

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Discovery of 1-(3-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}phenyl)-2-imidazolidinone (GSK163090), a Potent, Selective, and Orally Active 5-HT 1A/B/D Receptor Antagonist

Journal of medicinal chemistry, 2010-12, Vol.53 (23), p.8228-8240

2010

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Discovery of 1-(3-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}phenyl)-2-imidazolidinone (GSK163090), a Potent, Selective, and Orally Active 5-HT1A/B/D Receptor Antagonist

Journal of medicinal chemistry, 2010-12, Vol.53 (23), p.8228-8240

2010

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8-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors--part II

Bioorganic & medicinal chemistry letters, 2009-04, Vol.19 (8), p.2338-2342

2009

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Discovery and structure–activity relationship of a novel spirocarbamate series of NPY Y5 antagonists

Bioorganic & medicinal chemistry letters, 2010-10, Vol.20 (20), p.6103-6107

2010

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In vitro and in vivo characterization of the novel GABA sub(B receptor positive allosteric modulator, 2-{1-[2-(4-chlorophenyl)-5-methylpyrazolo[1,5-a]pyrimidin-7-yl]-2- p iperidinyl}ethanol (CMPPE))

Neuropharmacology, 2011-11, Vol.61 (5-6), p.957-966

2011

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In vitro and in vivo characterization of the novel GABAB receptor positive allosteric modulator, 2-{1-[2-(4-chlorophenyl)-5-methylpyrazolo[1,5-a]pyrimidin-7-yl]-2-piperidinyl}ethanol (CMPPE)

Neuropharmacology, 2011-10, Vol.61 (5-6), p.957-966

2011

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Synthesis and structure-activity relationship of N-(3-azabicyclo[3.1.0]hex-6-ylmethyl)-5-(2-pyridinyl)-1,3-thiaz ol-2-amines derivatives as NPY Y5 antagonists

Bioorganic & medicinal chemistry letters, 2010-08, Vol.20 (16), p.4741-4744

2010

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6-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones : Dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors

Bioorganic & medicinal chemistry letters, 2008-10, Vol.18 (20), p.5653-5656

2008

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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

Synthesis and structure–activity relationship of N-(3-azabicyclo[3.1.0]hex-6-ylmethyl)-5-(2-pyridinyl)-1,3-thiazol-2-amines derivatives as NPY Y5 antagonists

Novel morpholine scaffolds as selective dopamine (DA) D3 receptor antagonists

1,2,4-Triazolyl 5‑Azaspiro[2.4]heptanes: Lead Identification and Early Lead Optimization of a New Series of Potent and Selective Dopamine D3 Receptor Antagonists

1,2,4-Triazolyl octahydropyrrolo[2,3-b]pyrroles: A new series of potent and selective dopamine D3 receptor antagonists

The NK 1 receptor antagonist aprepitant attenuates NK 1 agonist‐induced scratching behaviour in the gerbil after intra‐dermal, topical or oral administration

6-(3,4-Dichlorophenyl)-1-[(Methyloxy)methyl]-3-azabicyclo[4.1.0]heptane: A New Potent and Selective Triple Reuptake Inhibitor

The NK1 receptor antagonist aprepitant attenuates NK1 agonist-induced scratching behaviour in the gerbil after intra-dermal, topical or oral administration

1-(Aryl)-6-[alkoxyalkyl]-3-azabicyclo[3.1.0]hexanes and 6-(Aryl)-6-[alkoxyalkyl]-3-azabicyclo[3.1.0]hexanes: A New Series of Potent and Selective Triple Reuptake Inhibitors

Design and Synthesis of Novel Tricyclic Benzoxazines as Potent 5-HT1A/B/D Receptor Antagonists Leading to the Discovery of 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4H-imidazo[5,1-c][1,4]benzoxazine-3-carboxamide (GSK588045)

In vitro and in vivo characterization of the novel GABA B receptor positive allosteric modulator, 2-{1-[2-(4-chlorophenyl)-5-methylpyrazolo[1,5-a]pyrimidin-7-yl]-2-piperidinyl}ethanol (CMPPE)

Design and Synthesis of Novel Tricyclic Benzoxazines as Potent 5-HT 1A/B/D Receptor Antagonists Leading to the Discovery of 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4 H -imidazo[5,1- c ][1,4]benzoxazine-3-carboxamide (GSK588045)

Discovery and Biological Characterization of (2R,4S)-1′-Acetyl-N-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl}-2-(4-fluoro-2-methylphenyl)-N-methyl-4,4′-bipiperidine-1-carboxamide as a New Potent and Selective Neurokinin 1 (NK1) Receptor Antagonist Clinical Candidate

In vivo rat PK profiling in drug discovery: new challenges

Design, synthesis and SAR of a novel series of benzimidazoles as potent NPY Y5 antagonists

1-Heteroaryl-6-(3,4-dichlorophenyl)-3-azabicyclo[4.1.0]heptane: Further insights into a class of triple re-uptake inhibitors

Synthesis and pharmacological characterization of 5-phenyl-2-[2-(1-piperidinylcarbonyl)phenyl]-2,3-dihydro-1H-pyrrolo[1,2-c]imidazol-1-ones: A new class of Neuropeptide S antagonists

Discovery of 1-(3-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}phenyl)-2-imidazolidinone (GSK163090), a Potent, Selective, and Orally Active 5-HT 1A/B/D Receptor Antagonist

Discovery of 1-(3-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}phenyl)-2-imidazolidinone (GSK163090), a Potent, Selective, and Orally Active 5-HT1A/B/D Receptor Antagonist

8-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors--part II

Discovery and structure–activity relationship of a novel spirocarbamate series of NPY Y5 antagonists

In vitro and in vivo characterization of the novel GABA sub(B receptor positive allosteric modulator, 2-{1-[2-(4-chlorophenyl)-5-methylpyrazolo[1,5-a]pyrimidin-7-yl]-2- p iperidinyl}ethanol (CMPPE))

In vitro and in vivo characterization of the novel GABAB receptor positive allosteric modulator, 2-{1-[2-(4-chlorophenyl)-5-methylpyrazolo[1,5-a]pyrimidin-7-yl]-2-piperidinyl}ethanol (CMPPE)

Synthesis and structure-activity relationship of N-(3-azabicyclo[3.1.0]hex-6-ylmethyl)-5-(2-pyridinyl)-1,3-thiaz ol-2-amines derivatives as NPY Y5 antagonists

6-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones : Dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors

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