69 articles for thisTarget
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Article Title
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A benzo[b]thiophene-based selective type 4 S1P receptor agonist.
Harvard Medical School
Novel S1P1 receptor agonists - Part 4: Alkylaminomethyl substituted aryl head groups.
Actelion Pharmaceuticals
Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P3)-Sparing S1P1 Agonists Active at Low Oral Doses.
Glaxosmithkline
Discovery of novel S1P2 antagonists, part 3: Improving the oral bioavailability of a series of 1,3-bis(aryloxy)benzene derivatives.
Ono Pharmaceutical
Discovery of novel S1P2 antagonists. Part 2: Improving the profile of a series of 1,3-bis(aryloxy)benzene derivatives.
Ono Pharmaceutical
Discovery of novel S1P2 antagonists. Part 1: discovery of 1,3-bis(aryloxy)benzene derivatives.
Ono Pharmaceutical
Design and synthesis of new tricyclic indoles as potent modulators of the S1P1 receptor.
Arena Pharmaceuticals
(7-Benzyloxy-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic Acids as S1P1 Functional Antagonists.
Arena Pharmaceuticals
Discovery of APD334: Design of a Clinical Stage Functional Antagonist of the Sphingosine-1-phosphate-1 Receptor.
Arena Pharmaceuticals
An oral sphingosine 1-phosphate receptor 1 (S1P(1)) antagonist prodrug with efficacy in vivo: discovery, synthesis, and evaluation.
Novartis Pharma
Fused tricyclic indoles as S1P1 agonists with robust efficacy in animal models of autoimmune disease.
Arena Pharmaceuticals
Discovery of a novel class of potent and orally bioavailable sphingosine 1-phosphate receptor 1 antagonists.
Exelixis
4-Methoxy-N-[2-(trifluoromethyl)biphenyl-4-ylcarbamoyl]nicotinamide: A Potent and Selective Agonist of S1P1.
TBA
Synthesis of 4(5)-phenylimidazole-based analogues of sphingosine-1-phosphate and FTY720: discovery of potent S1P1 receptor agonists.
University of Virginia
Synthesis of benzimidazole based analogues of sphingosine-1-phosphate: discovery of potent, subtype-selective S1P4 receptor agonists.
University of Virginia
Design and synthesis of conformationally constrained 3-(N-alkylamino)propylphosphonic acids as potent agonists of sphingosine-1-phosphate (S1P) receptors.
Merck Research Laboratories
The discovery of 3-(N-alkyl)aminopropylphosphonic acids as potent S1P receptor agonists.
Merck Research Laboratories
Synthesis of para-alkyl aryl amide analogues of sphingosine-1-phosphate: discovery of potent S1P receptor agonists.
University of Virginia
Novel immunomodulators based on an oxazolin-2-one-4-carboxamide scaffold.
Institute of Pharmacology & Toxicology
Discovery and characterization of potent and selective 4-oxo-4-(5-(5-phenyl-1,2,4-oxadiazol-3-yl)indolin-1-yl)butanoic acids as S1P¿? agonists.
Arena Pharmaceuticals
Discovery, synthesis and SAR analysis of novel selective small molecule S1P4-R agonists based on a (2Z,5Z)-5-((pyrrol-3-yl)methylene)-3-alkyl-2-(alkylimino)thiazolidin-4-one chemotype.
The Scripps Research Institute
Discovery of a brain-penetrant S1P3-sparing direct agonist of the S1P¿? and S1P5 receptors efficacious at low oral dose.
Glaxosmithkline
SAR analysis of innovative selective small molecule antagonists of sphingosine-1-phosphate 4 (S1P4) receptor.
The Scripps Research Institute
Discovery, design and synthesis of the first reported potent and selective sphingosine-1-phosphate 4 (S1P4) receptor antagonists.
The Scripps Research Institute
Structure-activity relationship studies of sphingosine-1-phosphate receptor agonists with N-cinnamyl-ß-alanine moiety.
Ono Pharmaceutical
2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists.
Actelion Pharmaceuticals
Stereochemistry-activity relationship of orally active tetralin S1P agonist prodrugs.
Biogen Idec
S1P receptor mediated activity of FTY720 phosphate mimics.
Novartis Institutes For Biomedical Research
Synthesis and biological evaluation of gamma-aminophosphonates as potent, subtype-selective sphingosine 1-phosphate receptor agonists and antagonists.
University of Virginia
Discovery of 3-arylpropionic acids as potent agonists of sphingosine-1-phosphate receptor-1 (S1P1) with high selectivity against all other known S1P receptor subtypes.
Merck Research Laboratories
2-Aryl(pyrrolidin-4-yl)acetic acids are potent agonists of sphingosine-1-phosphate (S1P) receptors.
Merck Research Laboratories
2,5-Disubstituted pyrrolidine carboxylates as potent, orally active sphingosine-1-phosphate (S1P) receptor agonists.
Merck Research Laboratories
The Repertoire of Small-Molecule PET Probes for Neuroinflammation Imaging: Challenges and Opportunities beyond TSPO.
Massachusetts General Hospital
Novel immunomodulator FTY720 is phosphorylated in rats and humans to form a single stereoisomer. Identification, chemical proof, and biological characterization of the biologically active species and its enantiomer.
Novartis Institutes For Biomedical Research
Novel 5-fluorouracil sensitizers for colorectal cancer therapy: Design and synthesis of S1P receptor 2 (S1PR2) antagonists.
Ocean University of China
Synthesis and evaluation of highly selective quinazoline-2,4-dione ligands for sphingosine-1-phosphate receptor 2.
Washington University
Rational Design, Synthesis, and Biological Evaluation of Novel S1PR2 Antagonists for Reversing 5-FU-Resistance in Colorectal Cancer.
Ocean University of China
A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists.
Merck Research Laboratories
Discovery and Optimization of Orally Bioavailable Phthalazone and Cinnolone Carboxylic Acid Derivatives as S1P2 Antagonists against Fibrotic Diseases.
Galapagos
Selecting against S1P3 enhances the acute cardiovascular tolerability of 3-(N-benzyl)aminopropylphosphonic acid S1P receptor agonists.
Merck Research Laboratories
Potent S1P receptor agonists replicate the pharmacologic actions of the novel immune modulator FTY720.
Merck Research Laboratories
Design, synthesis and biological evaluation of sphingosine-1-phosphate receptor 2 antagonists as potent 5-FU-resistance reversal agents for the treatment of colorectal cancer.
Laboratory For Marine Drugs and Bioproducts of Qingdao National Laboratory For Marine Science and Technology
Discovery of the S1P2 Antagonist GLPG2938 (1-[2-Ethoxy-6-(trifluoromethyl)-4-pyridyl]-3-[[5-methyl-6-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]pyridazin-3-yl]methyl]urea), a Preclinical Candidate for the Treatment of Idiopathic Pulmonary Fibrosis.
Galapagos
Discovery of Soft-Drug Topical Tool Modulators of Sphingosine-1-phosphate Receptor 1 (S1PR1).
University of Dundee
Design, synthesis, and in vitro bioactivity evaluation of fluorine-containing analogues for sphingosine-1-phosphate 2 receptor.
Washington University
Discovery of Clinical Candidate GSK1842799 As a Selective S1P1 Receptor Agonist (Prodrug) for Multiple Sclerosis.
Praecis Pharmaceuticals
Discovery, design and synthesis of a selective S1P(3) receptor allosteric agonist.
The Scripps Research Institute
Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction.
Universitaire Vaudois
Discovery of a 1-Methyl-3,4-dihydronaphthalene-Based Sphingosine-1-Phosphate (S1P) Receptor Agonist Ceralifimod (ONO-4641). A S1P
Ono Pharmaceutical
DENDRIMER COMPOSITIONS AND METHODS FOR DRUG DELIVERY TO THE EYE
Ashvattha Therapeutics
Substituted benzimidazoles, their preparation and their use as pharmaceuticals
Neomed Institute
Pyrazolyl substituted carbonic acid derivatives as modulators of the prostacyclin (PGI2) receptor useful for the treatment of disorders related thereto
Arena Pharmaceuticals
Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as CETP inhibitors
Chong Kun Dang Pharmaceutical
Two members of a distinct subfamily of 5-hydroxytryptamine receptors differentially expressed in rat brain.
The Scripps Research Institute
Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors.
Pfizer
Structure-based drug design: the discovery of novel nonpeptide orally active inhibitors of human renin.
Novartis Pharmaceuticals
Discovery of a potent CDK2 inhibitor with a novel binding mode, using virtual screening and initial, structure-guided lead scoping.
Vernalis (R&D)