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The Discovery of N‑[5-(4-Bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]‑N′‑propylsulfamide (Macitentan), an Orally Active, Potent Dual Endothelin Receptor Antagonist

Journal of medicinal chemistry, 2012-09, Vol.55 (17), p.7849-7861

2012

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Pharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonist

The Journal of pharmacology and experimental therapeutics, 2008-12, Vol.327 (3), p.736-745

2008

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From bosentan (Tracleer®) to macitentan (Opsumit®): The medicinal chemistry perspective

Bioorganic & medicinal chemistry letters, 2016-08, Vol.26 (15), p.3381-3394

2016

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Distinct ETA receptor binding mode of macitentan as determined by site directed mutagenesis

PloS one, 2014-09, Vol.9 (9), p.e107809

2014

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The selective sphingosine 1-phosphate receptor 1 agonist ponesimod protects against lymphocyte-mediated tissue inflammation

The Journal of pharmacology and experimental therapeutics, 2011-05, Vol.337 (2), p.547-556

2011

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The Discovery of Macitentan - A Standard Medicinal Chemistry Program?

Chimia, 2017-08, Vol.71 (7), p.420

Bolli, Martin H

2017

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Synthetic sphingosine 1-phosphate receptor modulators--opportunities and potential pitfalls

Current topics in medicinal chemistry, 2011-03, Vol.11 (6), p.726-757

2011

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Practical Synthesis of a S1P Receptor 1 Agonist via a Guareschi–Thorpe Reaction

Organic process research & development, 2016-09, Vol.20 (9), p.1637-1646

2016

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Reversible oxidation/reduction steps in the metabolic degradation of the glycerol side chain of the S1P1 modulator ponesimod

Xenobiotica, 2024-04, Vol.54 (4), p.182-194

2024

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Reversible oxidation/reduction steps in the metabolic degradation of the glycerol side chain of the S1P 1 modulator ponesimod

Xenobiotica, 2024-04, Vol.54 (4), p.182-194

2024

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Discovery of Nivasorexant (ACT-539313): The First Selective Orexin‑1 Receptor Antagonist (SO1RA) Investigated in Clinical Trials

Journal of medicinal chemistry, 2024-02, Vol.67 (4), p.2337-2348

2024

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Discovery of the Novel, Orally Active, and Selective LPA1 Receptor Antagonist ACT-1016-0707 as a Preclinical Candidate for the Treatment of Fibrotic Diseases

Journal of medicinal chemistry, 2024-02, Vol.67 (4), p.2397-2424

2024

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Discovery of a Novel Orally Active, Selective LPA Receptor Type 1 Antagonist, 4‑(4-(2-Isopropylphenyl)-4-((2-methoxy-4-methylphenyl)carbamoyl)piperidin-1-yl)-4-oxobutanoic Acid, with a Distinct Molecular Scaffold

Journal of medicinal chemistry, 2024-02, Vol.67 (4), p.2379-2396

2024

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Sphingosine 1-Phosphate (S1P) Receptor Agonists Mediate Pro-fibrotic Responses in Normal Human Lung Fibroblasts via S1P2 and S1P3 Receptors and Smad-independent Signaling

The Journal of biological chemistry, 2013-05, Vol.288 (21), p.14839-14851

2013

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Pyrazole derivatives as selective orexin-2 receptor antagonists (2-SORA): synthesis, structure-activity-relationship, and sleep-promoting properties in rats

RSC medicinal chemistry, 2024-01, Vol.15 (1), p.344-354

2024

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Oxadiazole Derivatives as Dual Orexin Receptor Antagonists: Synthesis, Structure–Activity Relationships, and Sleep‐Promoting Properties in Rats

ChemMedChem, 2019-07, Vol.14 (13), p.1257-1270

2019

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From Oxadiazole to Triazole Analogues: Optimization toward a Dual Orexin Receptor Antagonist with Improved in vivo Efficacy in Dogs

ChemMedChem, 2020-03, Vol.15 (5), p.430-448

2020

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Sphingosine-1-phosphate (S1P) displays sustained S1P1 receptor agonism and signaling through S1P lyase-dependent receptor recycling

Cellular signalling, 2014-07, Vol.26 (7), p.1576-1588

2014

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The metabolism of the dual endothelin receptor antagonist macitentan in rat and dog

Xenobiotica, 2016-03, Vol.46 (3), p.253-267

2016

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Discovery of Highly Potent Dual Orexin Receptor Antagonists via a Scaffold-Hopping Approach

ChemMedChem, 2016-10, Vol.11 (19), p.2132-2146

2016

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Novel S1P1 receptor agonists – Part 5: From amino-to alkoxy-pyridines

European journal of medicinal chemistry, 2016-06, Vol.115, p.326-341

2016

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Novel S1P(1) receptor agonists--part 3: from thiophenes to pyridines

Journal of medicinal chemistry, 2014-01, Vol.57 (1), p.110-130

2014

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Novel S1P1 receptor agonists – Part 4: Alkylaminomethyl substituted aryl head groups

European journal of medicinal chemistry, 2016-06, Vol.116, p.222-238

2016

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Novel S1P(1) receptor agonists--part 2: from bicyclo[3.1.0]hexane-fused thiophenes to isobutyl substituted thiophenes

Journal of medicinal chemistry, 2014-01, Vol.57 (1), p.78-97

2014

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Novel S1P1 Receptor Agonists - Part 2: From Bicyclo[3.1.0]hexane-Fused Thiophenes to Isobutyl Substituted Thiophenes

Journal of medicinal chemistry, 2014-01, Vol.57 (1), p.78-97

2014

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The Discovery of N‑[5-(4-Bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]‑N′‑propylsulfamide (Macitentan), an Orally Active, Potent Dual Endothelin Receptor Antagonist

Pharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonist

From bosentan (Tracleer®) to macitentan (Opsumit®): The medicinal chemistry perspective

Distinct ETA receptor binding mode of macitentan as determined by site directed mutagenesis

The selective sphingosine 1-phosphate receptor 1 agonist ponesimod protects against lymphocyte-mediated tissue inflammation

The Discovery of Macitentan - A Standard Medicinal Chemistry Program?

Synthetic sphingosine 1-phosphate receptor modulators--opportunities and potential pitfalls

Practical Synthesis of a S1P Receptor 1 Agonist via a Guareschi–Thorpe Reaction

Reversible oxidation/reduction steps in the metabolic degradation of the glycerol side chain of the S1P1 modulator ponesimod

Reversible oxidation/reduction steps in the metabolic degradation of the glycerol side chain of the S1P 1 modulator ponesimod

Discovery of Nivasorexant (ACT-539313): The First Selective Orexin‑1 Receptor Antagonist (SO1RA) Investigated in Clinical Trials

Discovery of the Novel, Orally Active, and Selective LPA1 Receptor Antagonist ACT-1016-0707 as a Preclinical Candidate for the Treatment of Fibrotic Diseases

Discovery of a Novel Orally Active, Selective LPA Receptor Type 1 Antagonist, 4‑(4-(2-Isopropylphenyl)-4-((2-methoxy-4-methylphenyl)carbamoyl)piperidin-1-yl)-4-oxobutanoic Acid, with a Distinct Molecular Scaffold

Sphingosine 1-Phosphate (S1P) Receptor Agonists Mediate Pro-fibrotic Responses in Normal Human Lung Fibroblasts via S1P2 and S1P3 Receptors and Smad-independent Signaling

Pyrazole derivatives as selective orexin-2 receptor antagonists (2-SORA): synthesis, structure-activity-relationship, and sleep-promoting properties in rats

Oxadiazole Derivatives as Dual Orexin Receptor Antagonists: Synthesis, Structure–Activity Relationships, and Sleep‐Promoting Properties in Rats

From Oxadiazole to Triazole Analogues: Optimization toward a Dual Orexin Receptor Antagonist with Improved in vivo Efficacy in Dogs

Sphingosine-1-phosphate (S1P) displays sustained S1P1 receptor agonism and signaling through S1P lyase-dependent receptor recycling

The metabolism of the dual endothelin receptor antagonist macitentan in rat and dog

Discovery of Highly Potent Dual Orexin Receptor Antagonists via a Scaffold-Hopping Approach

Novel S1P1 receptor agonists – Part 5: From amino-to alkoxy-pyridines

Novel S1P(1) receptor agonists--part 3: from thiophenes to pyridines

Novel S1P1 receptor agonists – Part 4: Alkylaminomethyl substituted aryl head groups

Novel S1P(1) receptor agonists--part 2: from bicyclo[3.1.0]hexane-fused thiophenes to isobutyl substituted thiophenes

Novel S1P1 Receptor Agonists - Part 2: From Bicyclo[3.1.0]hexane-Fused Thiophenes to Isobutyl Substituted Thiophenes

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