The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28051871 |
100 |
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) |
27810243 |
87 |
Discovery of indazole ethers as novel, potent, non-steroidal glucocorticoid receptor modulators. |
Astrazeneca |
26990539 |
79 |
Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR)ß Agonist. |
Vitae Pharmaceuticals |
26683992 |
25 |
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 |
26218343 |
76 |
Indole Glucocorticoid Receptor Antagonists Active in a Model of Dyslipidemia Act via a Unique Association with an Agonist Binding Site. |
Eli Lilly |
25978072 |
53 |
Synthesis and Biological Evaluation of Cyclopentaquinoline Derivatives as Nonsteroidal Glucocorticoid Receptor Antagonists. |
TBA |
25879485 |
60 |
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 |
25941555 |
75 |
Discovery of benzimidazole oxazolidinediones as novel and selective nonsteroidal mineralocorticoid receptor antagonists. |
Merck Research Laboratories |
24980053 |
153 |
Discovery of acylurea isosteres of 2-acylaminothiadiazole in the azaxanthene series of glucocorticoid receptor agonists. |
Bristol-Myers Squibb |
25516791 |
177 |
Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. |
Boehringer Ingelheim Pharmaceuticals |
25305688 |
41 |
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORß and ROR¿t. |
Phenex Pharmaceuticals |
25187277 |
136 |
Discovery of 6-[5-(4-fluorophenyl)-3-methyl-pyrazol-4-yl]-benzoxazin-3-one derivatives as novel selective nonsteroidal mineralocorticoid receptor antagonists. |
Takeda Pharmaceutical |
24755427 |
107 |
The discovery of potent and selective non-steroidal glucocorticoid receptor modulators, suitable for inhalation. |
Astrazeneca |
24738581 |
81 |
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 |
24630411 |
38 |
Mineralocorticoid receptor antagonists: identification of heterocyclic amide replacements in the oxazolidinedione series. |
Merck Research Laboratories |
24656565 |
73 |
Discovery of a potent and dissociated non-steroidal glucocorticoid receptor agonist containing an alkyl carbinol pharmacophore. |
Boehringer Ingelheim Pharmaceuticals |
24506830 |
91 |
Identification of highly efficacious glucocorticoid receptor agonists with a potential for reduced clinical bone side effects. |
Boehringer Ingelheim Pharmaceuticals |
24446728 |
30 |
Glucocorticoid receptor modulators informed by crystallography lead to a new rationale for receptor selectivity, function, and implications for structure-based design. |
Eli Lilly |
24239189 |
85 |
Substituted phenyl as a steroid A-ring mimetic: providing agonist activity to a class of arylsulfonamide nonsteroidal glucocorticoid ligands. |
Boehringer Ingelheim Pharmaceuticals |
24215891 |
107 |
Function-regulating pharmacophores in a sulfonamide class of glucocorticoid receptor agonists. |
Boehringer Ingelheim Pharmaceuticals |
24157365 |
23 |
Design and synthesis of aryl sulfonamide-based nonsteroidal mineralocorticoid receptor antagonists. |
Pfizer |
24074876 |
17 |
Synthesis of sterically encumbered 11ß-aminoprogesterone derivatives and evaluation as 11ß-hydroxysteroid dehydrogenase inhibitors and mineralocorticoid receptor antagonists. |
University of Alberta |
23953070 |
146 |
Discovery of potent and selective nonsteroidal indazolyl amide glucocorticoid receptor agonists. |
Ironwood Pharmaceuticals |
23916594 |
92 |
Synthesis and structure-activity relationships of novel indazolyl glucocorticoid receptor partial agonists. |
Bristol-Myers Squibb |
23958516 |
61 |
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 |
23777778 |
101 |
Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists. |
Merck Research Laboratories |
23279862 |
1 |
Microwave-assisted synthesis of pyrimido[4,5-b][1,6]naphthyridin-4(3H)-ones with potential antitumor activity. |
Universidad Del Valle |
21129964 |
28 |
Discovery and optimisation of a selective non-steroidal glucocorticoid receptor antagonist. |
Merck Research Laboratories |
20812681 |
24 |
Synthesis and biochemical characterization of a series of 17a-perfluoroalkylated estradiols as selective ligands for estrogen receptora. |
Charles University In Prague |
20727743 |
64 |
Discovery of quinolines as selective glucocorticoid receptor agonists. |
Bayer Schering Pharma |
20202837 |
51 |
The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist. |
Medicines Research Centre |
18952422 |
5 |
The first X-ray crystal structure of the glucocorticoid receptor bound to a non-steroidal agonist. |
Glaxosmithkline |
23079530 |
27 |
Novel progesterone receptor modulators: 4-aryl-phenylsulfonamides. |
Pfizer |
22866979 |
19 |
Mineralocorticoid receptor antagonists for the treatment of hypertension and diabetic nephropathy. |
Pfizer |
21073190 |
135 |
Dimethyl-diphenyl-propanamide Derivatives As Nonsteroidal Dissociated Glucocorticoid Receptor Agonists. |
Bristol-Myers Squibb |
20735001 |
145 |
Nonsteroidal dissociated glucocorticoid agonists containing azaindoles as steroid A-ring mimetics. |
Boehringer Ingelheim Pharmaceuticals |
20672822 |
108 |
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 |
20672820 |
92 |
Discovery of novel cyanodihydropyridines as potent mineralocorticoid receptor antagonists. |
Pfizer |
20638844 |
25 |
1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists. |
Pfizer |
20510622 |
142 |
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists. |
Chinese Academy of Sciences |
19863083 |
25 |
The lecanindoles, nonsteroidal progestins from the terrestrial fungus Verticillium lecanii 6144. |
Wyeth Research |
18722119 |
55 |
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 |
18504132 |
51 |
7-aryl 1,5-dihydro-benzo[e][1,4]oxazepin-2-ones and analogs as non-steroidal progesterone receptor antagonists. |
Wyeth Research |
18513967 |
103 |
Discovery of nonsteroidal glucocorticoid receptor ligands based on 6-indole-1,2,3,4-tetrahydroquinolines. |
Ligand Pharmaceuticals |
18032610 |
4 |
Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein-protein interaction profile. |
Ligand Pharmaceuticals |
18318463 |
53 |
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 |
17692519 |
108 |
Identification of dissociated non-steroidal glucocorticoid receptor agonists. |
Boehringer Ingelheim Pharmaceuticals |
17118655 |
73 |
Alpha-methyltryptamine sulfonamide derivatives as novel glucocorticoid receptor ligands. |
Boehringer Ingelheim Pharmaceuticals |
17181172 |
94 |
Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists. |
Boehringer Ingelheim Pharmaceuticals |
16250653 |
22 |
Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study. |
Universit£ |
16112571 |
93 |
Trifluoromethyl group as a pharmacophore: effect of replacing a CF3 group on binding and agonist activity of a glucocorticoid receptor ligand. |
Boehringer Ingelheim Pharmaceuticals |
15293993 |
172 |
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes. |
Abbott Laboratories |
12238914 |
48 |
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 |
8627601 |
169 |
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether. |
Ligand Pharmaceuticals |
15080982 |
122 |
Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists. |
Abbott Laboratories |
12781198 |
108 |
Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore. |
Ligand Pharmaceuticals |
12781197 |
59 |
Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators. |
Ligand Pharmaceuticals |
10743938 |
103 |
Nonsteroidal progesterone receptor antagonists based on 6-thiophenehydroquinolines. |
Ligand Pharmaceuticals |
22074142 |
89 |
Identification of benzoxazin-3-one derivatives as novel, potent, and selective nonsteroidal mineralocorticoid receptor antagonists. |
Takeda Pharmaceutical |
21963986 |
162 |
Non-steroidal dissociated glucocorticoid agonists: indoles as A-ring mimetics and function-regulating pharmacophores. |
Boehringer Ingelheim Pharmaceuticals |
21899328 |
244 |
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 |
21786805 |
130 |
Structure-based design and synthesis of 1,3-oxazinan-2-one inhibitors of 11ß-hydroxysteroid dehydrogenase type 1. |
Vitae Pharmaceuticals |
21324689 |
74 |
Nonsteroidal 2,3-dihydroquinoline glucocorticoid receptor agonists with reduced PEPCK activation. |
Ligand Pharmaceuticals |
21349714 |
118 |
Tetrahydroquinolin-3-yl carbamate glucocorticoid receptor agonists with reduced PEPCK activation. |
Ligand Pharmaceuticals |
21316964 |
108 |
Discovery of orally available tetrahydroquinoline-based glucocorticoid receptor agonists. |
Ligand Pharmaceuticals |
24900294 |
72 |
Novel 3-Aryl Indoles as Progesterone Receptor Antagonists for Uterine Fibroids |
TBA |
21115247 |
64 |
Tetrahydroquinoline glucocorticoid receptor agonists: discovery of a 3-hydroxyl for improving receptor selectivity. |
Ligand Pharmaceuticals |
20638278 |
145 |
Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists. |
Phenex Pharmaceuticals |
20430618 |
21 |
Optimisation of a pyrazole series of progesterone antagonists; Part 1. |
Pfizer |
20408553 |
27 |
Stereochemical requirements for the mineralocorticoid receptor antagonist activity of dihydropyridines. |
Pfizer |
19595590 |
49 |
Rational design of orally-active, pyrrolidine-based progesterone receptor partial agonists. |
Glaxosmithkline |
19606870 |
53 |
Design, synthesis, and biological evaluation of 16-substituted 4-azasteroids as tissue-selective androgen receptor modulators (SARMs). |
Merck Research Laboratories |
18553958 |
28 |
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 |
18038968 |
26 |
(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 |
17587578 |
45 |
Discovery and optimization of novel, non-steroidal glucocorticoid receptor modulators. |
Argenta Discovery |
17553679 |
148 |
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 |
16759088 |
38 |
The discovery of new 11beta-hydroxysteroid dehydrogenase type 1 inhibitors by common feature pharmacophore modeling and virtual screening. |
University of Innsbruck |
15081010 |
66 |
Discovery of novel nonsteroidal glucocorticoid receptor modulators. |
Abbott Laboratories |
12954062 |
140 |
5-benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as selective progesterone receptor modulators. |
Ligand Pharmaceuticals |
11520196 |
81 |
Synthesis and characterization of non-steroidal ligands for the glucocorticoid receptor: selective quinoline derivatives with prednisolone-equivalent functional activity. |
Abbott Laboratories |
30596500 |
182 |
Identification of Mineralocorticoid Receptor Modulators with Low Impact on Electrolyte Homeostasis but Maintained Organ Protection. |
Pharmaron-Beijing |
10230628 |
95 |
Nonsteroidal androgen receptor agonists based on 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one. |
Ligand Pharmaceuticals |
9871534 |
95 |
New nonsteroidal androgen receptor modulators based on 4-(trifluoromethyl)-2(1H)-pyrrolidino[3,2-g] quinolinone. |
Ligand Pharmaceuticals |
9784110 |
81 |
5-Benzylidene 1,2-dihydrochromeno[3,4-f]quinolines, a novel class of nonsteroidal human progesterone receptor agonists. |
Ligand Pharmaceuticals |
31104995 |
22 |
Development of indazole mineralocorticoid receptor antagonists and investigation into their selective late-stage functionalization. |
Merck |
9464360 |
145 |
5-Aryl-1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal human progesterone receptor agonists. |
Ligand Pharmaceuticals |
8709117 |
7 |
New steroidal diazo ketones as potential photoaffinity labeling reagents for the mineralocorticoid receptor: synthesis and biological activities. |
Université |
26568144 |
8 |
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 |
30144697 |
66 |
Synthesis and evaluation of 4-cycloheptylphenols as selective Estrogen receptor-? agonists (SERBAs). |
Marquette University |
29424542 |
138 |
Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile. |
Astrazeneca |
29741897 |
62 |
Novel Pyrrolidine Derivatives of Budesonide as Long Acting Inhaled Corticosteroids for the Treatment of Pulmonary Inflammatory Diseases. |
TBA |
28043796 |
84 |
Discovery of new selective glucocorticoid receptor agonist leads. |
Bayer Pharma |
28479196 |
2 |
Conformational control in structure-based drug design. |
Allergan |
28937774 |
107 |
Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases. |
Astrazeneca |
29300474 |
45 |
Identification of Morpholino-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-ones as Nonsteroidal Mineralocorticoid Antagonists. |
Pfizer |
28454849 |
48 |
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 |
21250822 |
16 |
Synthesis and biological evaluation of novel N,N'-bis-methylenedioxybenzyl-alkylenediamines as bivalent anti-Alzheimer disease ligands. |
Sun Yat-Sen University |
19237285 |
44 |
Benzimidazolone-based serotonin 5-HT1A or 5-HT7R ligands: synthesis and biological evaluation. |
Cnrs |