107 articles for thisTarget
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Article Title
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Modulating Mineralocorticoid Receptor with Non-steroidal Antagonists. New Opportunities for the Development of Potent and Selective Ligands without Off-Target Side Effects.
Instituto De Qu£Mica M£Dica (Iqm-Csic)
Discovery of indazole ethers as novel, potent, non-steroidal glucocorticoid receptor modulators.
Astrazeneca
Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR)ß Agonist.
Vitae Pharmaceuticals
2-Chloro-4-[[(1R,2R)-2-hydroxy-2-methyl-cyclopentyl]amino]-3-methyl-benzonitrile: A Transdermal Selective Androgen Receptor Modulator (SARM) for Muscle Atrophy.
Eli Lilly
Indole Glucocorticoid Receptor Antagonists Active in a Model of Dyslipidemia Act via a Unique Association with an Agonist Binding Site.
Eli Lilly
Synthesis and Biological Evaluation of Cyclopentaquinoline Derivatives as Nonsteroidal Glucocorticoid Receptor Antagonists.
TBA
Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts.
Seragon Pharmaceuticals
Discovery of benzimidazole oxazolidinediones as novel and selective nonsteroidal mineralocorticoid receptor antagonists.
Merck Research Laboratories
Discovery of acylurea isosteres of 2-acylaminothiadiazole in the azaxanthene series of glucocorticoid receptor agonists.
Bristol-Myers Squibb
Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate.
Boehringer Ingelheim Pharmaceuticals
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORß and ROR¿t.
Phenex Pharmaceuticals
Discovery of 6-[5-(4-fluorophenyl)-3-methyl-pyrazol-4-yl]-benzoxazin-3-one derivatives as novel selective nonsteroidal mineralocorticoid receptor antagonists.
Takeda Pharmaceutical
The discovery of potent and selective non-steroidal glucocorticoid receptor modulators, suitable for inhalation.
Astrazeneca
Identification of (R)-6-(1-(4-cyano-3-methylphenyl)-5-cyclopentyl-4,5-dihydro-1H-pyrazol-3-yl)-2-methoxynicotinic acid, a highly potent and selective nonsteroidal mineralocorticoid receptor antagonist.
Pfizer
Mineralocorticoid receptor antagonists: identification of heterocyclic amide replacements in the oxazolidinedione series.
Merck Research Laboratories
Discovery of a potent and dissociated non-steroidal glucocorticoid receptor agonist containing an alkyl carbinol pharmacophore.
Boehringer Ingelheim Pharmaceuticals
Identification of highly efficacious glucocorticoid receptor agonists with a potential for reduced clinical bone side effects.
Boehringer Ingelheim Pharmaceuticals
Glucocorticoid receptor modulators informed by crystallography lead to a new rationale for receptor selectivity, function, and implications for structure-based design.
Eli Lilly
Substituted phenyl as a steroid A-ring mimetic: providing agonist activity to a class of arylsulfonamide nonsteroidal glucocorticoid ligands.
Boehringer Ingelheim Pharmaceuticals
Function-regulating pharmacophores in a sulfonamide class of glucocorticoid receptor agonists.
Boehringer Ingelheim Pharmaceuticals
Design and synthesis of aryl sulfonamide-based nonsteroidal mineralocorticoid receptor antagonists.
Pfizer
Synthesis of sterically encumbered 11ß-aminoprogesterone derivatives and evaluation as 11ß-hydroxysteroid dehydrogenase inhibitors and mineralocorticoid receptor antagonists.
University of Alberta
Discovery of potent and selective nonsteroidal indazolyl amide glucocorticoid receptor agonists.
Ironwood Pharmaceuticals
Synthesis and structure-activity relationships of novel indazolyl glucocorticoid receptor partial agonists.
Bristol-Myers Squibb
Design, synthesis, and structure-activity relationships of dihydrofuran-2-one and dihydropyrrol-2-one derivatives as novel benzoxazin-3-one-based mineralocorticoid receptor antagonists.
Takeda Pharmaceutical
Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists.
Merck Research Laboratories
Microwave-assisted synthesis of pyrimido[4,5-b][1,6]naphthyridin-4(3H)-ones with potential antitumor activity.
Universidad Del Valle
Discovery and optimisation of a selective non-steroidal glucocorticoid receptor antagonist.
Merck Research Laboratories
Synthesis and biochemical characterization of a series of 17a-perfluoroalkylated estradiols as selective ligands for estrogen receptora.
Charles University In Prague
Discovery of quinolines as selective glucocorticoid receptor agonists.
Bayer Schering Pharma
The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist.
Medicines Research Centre
The first X-ray crystal structure of the glucocorticoid receptor bound to a non-steroidal agonist.
Glaxosmithkline
Mineralocorticoid receptor antagonists for the treatment of hypertension and diabetic nephropathy.
Pfizer
Dimethyl-diphenyl-propanamide Derivatives As Nonsteroidal Dissociated Glucocorticoid Receptor Agonists.
Bristol-Myers Squibb
Nonsteroidal dissociated glucocorticoid agonists containing azaindoles as steroid A-ring mimetics.
Boehringer Ingelheim Pharmaceuticals
Discovery of (3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid (PF-3882845), an orally efficacious mineralocorticoid receptor (MR) antagonist for hypertension and nephropathy.
Pfizer
Discovery of novel cyanodihydropyridines as potent mineralocorticoid receptor antagonists.
Pfizer
1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists.
Pfizer
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.
Chinese Academy of Sciences
The lecanindoles, nonsteroidal progestins from the terrestrial fungus Verticillium lecanii 6144.
Wyeth Research
1,5-Dihydro-benzo[e][1,4]oxazepin-2(1H)-ones containing a 7-(5'-cyanopyrrol-2-yl) group as nonsteroidal progesterone receptor modulators.
Wyeth Research
7-aryl 1,5-dihydro-benzo[e][1,4]oxazepin-2-ones and analogs as non-steroidal progesterone receptor antagonists.
Wyeth Research
Discovery of nonsteroidal glucocorticoid receptor ligands based on 6-indole-1,2,3,4-tetrahydroquinolines.
Ligand Pharmaceuticals
Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein-protein interaction profile.
Ligand Pharmaceuticals
Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
Wyeth Research
Identification of dissociated non-steroidal glucocorticoid receptor agonists.
Boehringer Ingelheim Pharmaceuticals
Alpha-methyltryptamine sulfonamide derivatives as novel glucocorticoid receptor ligands.
Boehringer Ingelheim Pharmaceuticals
Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists.
Boehringer Ingelheim Pharmaceuticals
Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study.
University of Perugia
Trifluoromethyl group as a pharmacophore: effect of replacing a CF3 group on binding and agonist activity of a glucocorticoid receptor ligand.
Boehringer Ingelheim Pharmaceuticals
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.
Abbott Laboratories
6-Aryl-1,4-dihydro-benzo[d][1,3]oxazin- 2-ones: a novel class of potent, selective, and orally active nonsteroidal progesterone receptor antagonists.
Women'S Health Research Institute
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.
Ligand Pharmaceuticals
Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists.
Abbott Laboratories
Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.
Ligand Pharmaceuticals
Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators.
Ligand Pharmaceuticals
Nonsteroidal progesterone receptor antagonists based on 6-thiophenehydroquinolines.
Ligand Pharmaceuticals
Identification of benzoxazin-3-one derivatives as novel, potent, and selective nonsteroidal mineralocorticoid receptor antagonists.
Takeda Pharmaceutical
Non-steroidal dissociated glucocorticoid agonists: indoles as A-ring mimetics and function-regulating pharmacophores.
Boehringer Ingelheim Pharmaceuticals
Azaxanthene based selective glucocorticoid receptor modulators: design, synthesis, and pharmacological evaluation of (S)-4-(5-(1-((1,3,4-thiadiazol-2-yl)amino)-2-methyl-1-oxopropan-2-yl)-5H-chromeno[2,3-b]pyridin-2-yl)-2-fluoro-N,N-dimethylbenzamide (BMS-776532) and its methylene homologue (BMS-791
Bristol-Myers Squibb
Structure-based design and synthesis of 1,3-oxazinan-2-one inhibitors of 11ß-hydroxysteroid dehydrogenase type 1.
Vitae Pharmaceuticals
Nonsteroidal 2,3-dihydroquinoline glucocorticoid receptor agonists with reduced PEPCK activation.
Ligand Pharmaceuticals
Tetrahydroquinolin-3-yl carbamate glucocorticoid receptor agonists with reduced PEPCK activation.
Ligand Pharmaceuticals
Discovery of orally available tetrahydroquinoline-based glucocorticoid receptor agonists.
Ligand Pharmaceuticals
Tetrahydroquinoline glucocorticoid receptor agonists: discovery of a 3-hydroxyl for improving receptor selectivity.
Ligand Pharmaceuticals
Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists.
Phenex Pharmaceuticals
Stereochemical requirements for the mineralocorticoid receptor antagonist activity of dihydropyridines.
Pfizer
Rational design of orally-active, pyrrolidine-based progesterone receptor partial agonists.
Glaxosmithkline
Design, synthesis, and biological evaluation of 16-substituted 4-azasteroids as tissue-selective androgen receptor modulators (SARMs).
Merck Research Laboratories
A tissue-selective nonsteroidal progesterone receptor modulator: 7,9-difluoro-5-(3-methylcyclohex-2-enyl)-2,2,4-trimethyl-1,2-dihydrochromeno[3,4-f]quinoline.
Ligand Pharmaceuticals
(S)-N-{3-[1-cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulfonamide: a potent, nonsteroidal, functional antagonist of the mineralocorticoid receptor.
Eli Lilly
Discovery and optimization of novel, non-steroidal glucocorticoid receptor modulators.
Argenta Discovery
5(Z)-benzylidene-1,2-dihydro-9-hydroxy-10-methoxy-2,2,4-trimethyl-5H-1-aza-6-oxa-chrysenes as non-steroidal glucocorticoid receptor modulators.
Ligand Pharmaceuticals
The discovery of new 11beta-hydroxysteroid dehydrogenase type 1 inhibitors by common feature pharmacophore modeling and virtual screening.
University of Innsbruck
Discovery of Apararenone (MT-3995) as a Highly Selective, Potent, and Novel Nonsteroidal Mineralocorticoid Receptor Antagonist.
Mitsubishi Tanabe Pharma
5-benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as selective progesterone receptor modulators.
Ligand Pharmaceuticals
Discovery of novel non-steroidal reverse indole mineralocorticoid receptor antagonists.
Merck And
Discovery of 2-((R)-4-(2-Fluoro-4-(methylsulfonyl)phenyl)-2-methylpiperazin-1-yl)-N-((1R,2s,3S,5S,7S)-5-hydroxyadamantan-2-yl)pyrimidine-4-carboxamide (SKI2852): A Highly Potent, Selective, and Orally Bioavailable Inhibitor of 11?-Hydroxysteroid Dehydrogenase Type 1 (11?-HSD1).
Sk Chemicals
Synthesis and characterization of non-steroidal ligands for the glucocorticoid receptor: selective quinoline derivatives with prednisolone-equivalent functional activity.
Abbott Laboratories
Identification of Mineralocorticoid Receptor Modulators with Low Impact on Electrolyte Homeostasis but Maintained Organ Protection.
Pharmaron-Beijing
Nonsteroidal androgen receptor agonists based on 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one.
Ligand Pharmaceuticals
New nonsteroidal androgen receptor modulators based on 4-(trifluoromethyl)-2(1H)-pyrrolidino[3,2-g] quinolinone.
Ligand Pharmaceuticals
5-Benzylidene 1,2-dihydrochromeno[3,4-f]quinolines, a novel class of nonsteroidal human progesterone receptor agonists.
Ligand Pharmaceuticals
Development of indazole mineralocorticoid receptor antagonists and investigation into their selective late-stage functionalization.
Merck
5-Aryl-1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal human progesterone receptor agonists.
Ligand Pharmaceuticals
New steroidal diazo ketones as potential photoaffinity labeling reagents for the mineralocorticoid receptor: synthesis and biological activities.
Université
Discovery of 6-(4-{[5-Cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl]methoxy}piperidin-1-yl)-1-methyl-1H-indole-3-carboxylic Acid: A Novel FXR Agonist for the Treatment of Dyslipidemia.
Eli Lilly
Synthesis and evaluation of 4-cycloheptylphenols as selective Estrogen receptor-? agonists (SERBAs).
Marquette University
Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.
Astrazeneca
Novel Pyrrolidine Derivatives of Budesonide as Long Acting Inhaled Corticosteroids for the Treatment of Pulmonary Inflammatory Diseases.
TBA
Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases.
Astrazeneca
Identification of Morpholino-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-ones as Nonsteroidal Mineralocorticoid Antagonists.
Pfizer
Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs) Part III: Discovery of 4-(5-oxopyrrolidine-1-yl)benzonitrile derivative 2f as a clinical candidate.
Takeda Pharmaceutical
Pharmaceutical compositions and methods of use of 4-pregenen-11β-17-21-triol-3,20-dione derivatives
Allergan
17-(1′propenyl)-17-3′-oxidoestra-4-en-3-one derivative, use thereof, and medicament containing said derivative
Bayer Intellectual Property
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
Abbott Laboratories
Discovery and SAR study of novel dihydroquinoline-containing glucocorticoid receptor agonists.
Boehringer Ingelheim Pharmaceuticals