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Efficient synthesis of bicyclic oxazolino- and thiazolino[3,2- c]pyrimidine-5,7-diones and its application to the synthesis of GnRH antagonists

Bioorganic & medicinal chemistry letters, 2005-03, Vol.15 (5), p.1407-1411

2005

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Synthesis of aryl-1,2,4-triazine-3,5-diones as antagonists of the gonadotropin-releasing hormone receptor

Bioorganic & medicinal chemistry letters, 2005-10, Vol.15 (19), p.4363-4366

2005

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Potent and orally active non-peptide antagonists of the human melanocortin-4 receptor based on a series of trans-2-disubstituted cyclohexylpiperazines

Bioorganic & medicinal chemistry letters, 2005-10, Vol.15 (19), p.4389-4395

2005

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A potent and selective nonpeptide antagonist of the melanocortin-4 receptor induces food intake in satiated mice

Bioorganic & medicinal chemistry letters, 2005-05, Vol.15 (10), p.2541-2546

2005

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Facile Preparation of Allenic Hydroxyketones via Rearrangement of Propargylic Alcohols

Organic letters, 1999-08, Vol.1 (3), p.367-370

1999

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Discovery of Sodium R-(+)-4-{2-[5-(2-Fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (Elagolix), a Potent and Orally Available Nonpeptide Antagonist of the Human Gonadotropin-Releasing Hormone Receptor

Journal of medicinal chemistry, 2008-12, Vol.51 (23), p.7478-7485

2008

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LBSAT142 Discovery And Characterization Of A Potent And Orally Bioavailable Parathyroid Hormone Receptor Type-1 (PTHR1) Antagonist For The Treatment Of Hypercalcemia

Journal of the Endocrine Society, 2022-11, Vol.6 (Supplement_1), p.A151-A152

2022

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4-{( 2R )-[3-Aminopropionylamido]-3-(2,4-dichlorophenyl)propionyl}-1-{2-[(2-thienyl)ethylaminomethyl]phenyl}piperazine as a Potent and Selective Melanocortin-4 Receptor AntagonistDesign, Synthesis, and Characterization

Journal of medicinal chemistry, 2004-12, Vol.47 (27), p.6821-6830

2004

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Studies on the structure-activity relationship of the basic amine of phenylpiperazines as melanocortin-4 receptor antagonists

Medicinal chemistry (Shp-sariqah, United Arab Emirates), 2008-01, Vol.4 (1), p.67-74

2008

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Synthesis of Piperazinephen-1-ylethylamines as Potent and Selective Antagonists of the Human Melanocortin-4 Receptor

Letters in drug design & discovery, 2006-07, Vol.3 (5), p.311-315

2006

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Discovery of a potent, selective, and less flexible selective norepinephrine reuptake inhibitor (sNRI)

Bioorganic & medicinal chemistry, 2008-07, Vol.18 (14), p.4224-4227

2008

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Synthetic approach to potential precursors of sclerophytin A

Tetrahedron, 2003-04, Vol.59 (15), p.2729-2736

2003

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4-{(2R)-[3-Aminopropionylamido]-3-(2,4-dichlorophenyl)propionyl}-1-{2-[(2-thienyl)ethylaminomethyl]phenyl}piperazine as a Potent and Selective Melanocortin-4 Receptor AntagonistDesign, Synthesis, and Characterization

Journal of medicinal chemistry, 2004-12, Vol.47 (27), p.6821-6830

2004

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Synthetic Approach to Analogues of the Original Structure of Sclerophytin A

Journal of organic chemistry, 2002-09, Vol.67 (19), p.6848-6851

2002

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Piperazinebenzylamines as potent and selective antagonists of the human melanocortin-4 receptor

Bioorganic & medicinal chemistry letters, 2004-11, Vol.14 (22), p.5605-5609

2004

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Potent and orally bioavailable zwitterion GnRH antagonists with low CYP3A4 inhibitory activity

Bioorganic & medicinal chemistry, 2008-06, Vol.18 (11), p.3301-3305

2008

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Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with improved pharmaceutical characteristics

Bioorganic & medicinal chemistry, 2008-12, Vol.18 (23), p.6151-6155

2008

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Structure–activity relationships of piperazinebenzylamines as potent and selective agonists of the human melanocortin-4 receptor

Bioorganic & medicinal chemistry letters, 2004-09, Vol.14 (17), p.4417-4423

2004

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Substituted chromones and quinolones as potent melanin-concentrating hormone receptor 1 antagonists

Bioorganic & medicinal chemistry letters, 2006-08, Vol.16 (16), p.4237-4242

2006

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Arylpropionylpiperazines as antagonists of the human melanocortin-4 receptor

Bioorganic & medicinal chemistry letters, 2006-09, Vol.16 (17), p.4674-4678

2006

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Pyrrolidinones as orally bioavailable antagonists of the human melanocortin-4 receptor with anti-cachectic activity

Bioorganic & medicinal chemistry, 2007-08, Vol.15 (15), p.5166-5176

2007

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Uracils as potent antagonists of the human gonadotropin-releasing hormone receptor without atropisomers

Bioorganic & medicinal chemistry letters, 2005-05, Vol.15 (10), p.2519-2522

2005

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Optimization of piperazinebenzylamines with a N-(1-methoxy-2-propyl) side chain as potent and selective antagonists of the human melanocortin-4 receptor

Bioorganic & medicinal chemistry letters, 2005-10, Vol.15 (20), p.4615-4618

2005

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Synthesis and structure–activity relationships of retro bis-aminopyrrolidine urea (rAPU) derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1). Part 2

Bioorganic & medicinal chemistry letters, 2006-09, Vol.16 (18), p.4922-4930

2006

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Structure–activity relationship of a series of cyclohexylpiperidines bearing an amide side chain as antagonists of the human melanocortin-4 receptor

Bioorganic & medicinal chemistry letters, 2005-07, Vol.15 (14), p.3434-3438

2005

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Efficient synthesis of bicyclic oxazolino- and thiazolino[3,2- c]pyrimidine-5,7-diones and its application to the synthesis of GnRH antagonists

Synthesis of aryl-1,2,4-triazine-3,5-diones as antagonists of the gonadotropin-releasing hormone receptor

Potent and orally active non-peptide antagonists of the human melanocortin-4 receptor based on a series of trans-2-disubstituted cyclohexylpiperazines

A potent and selective nonpeptide antagonist of the melanocortin-4 receptor induces food intake in satiated mice

Facile Preparation of Allenic Hydroxyketones via Rearrangement of Propargylic Alcohols

Discovery of Sodium R-(+)-4-{2-[5-(2-Fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (Elagolix), a Potent and Orally Available Nonpeptide Antagonist of the Human Gonadotropin-Releasing Hormone Receptor

LBSAT142 Discovery And Characterization Of A Potent And Orally Bioavailable Parathyroid Hormone Receptor Type-1 (PTHR1) Antagonist For The Treatment Of Hypercalcemia

4-{( 2R )-[3-Aminopropionylamido]-3-(2,4-dichlorophenyl)propionyl}-1-{2-[(2-thienyl)ethylaminomethyl]phenyl}piperazine as a Potent and Selective Melanocortin-4 Receptor AntagonistDesign, Synthesis, and Characterization

Studies on the structure-activity relationship of the basic amine of phenylpiperazines as melanocortin-4 receptor antagonists

Synthesis of Piperazinephen-1-ylethylamines as Potent and Selective Antagonists of the Human Melanocortin-4 Receptor

Discovery of a potent, selective, and less flexible selective norepinephrine reuptake inhibitor (sNRI)

Synthetic approach to potential precursors of sclerophytin A

4-{(2R)-[3-Aminopropionylamido]-3-(2,4-dichlorophenyl)propionyl}-1-{2-[(2-thienyl)ethylaminomethyl]phenyl}piperazine as a Potent and Selective Melanocortin-4 Receptor AntagonistDesign, Synthesis, and Characterization

Synthetic Approach to Analogues of the Original Structure of Sclerophytin A

Piperazinebenzylamines as potent and selective antagonists of the human melanocortin-4 receptor

Potent and orally bioavailable zwitterion GnRH antagonists with low CYP3A4 inhibitory activity

Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with improved pharmaceutical characteristics

Structure–activity relationships of piperazinebenzylamines as potent and selective agonists of the human melanocortin-4 receptor

Substituted chromones and quinolones as potent melanin-concentrating hormone receptor 1 antagonists

Arylpropionylpiperazines as antagonists of the human melanocortin-4 receptor

Pyrrolidinones as orally bioavailable antagonists of the human melanocortin-4 receptor with anti-cachectic activity

Uracils as potent antagonists of the human gonadotropin-releasing hormone receptor without atropisomers

Optimization of piperazinebenzylamines with a N-(1-methoxy-2-propyl) side chain as potent and selective antagonists of the human melanocortin-4 receptor

Synthesis and structure–activity relationships of retro bis-aminopyrrolidine urea (rAPU) derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1). Part 2

Structure–activity relationship of a series of cyclohexylpiperidines bearing an amide side chain as antagonists of the human melanocortin-4 receptor

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