PMID

Data

Article Title

Organization

SAR Exploration Guided by LE and Fsp(3): Discovery of a Selective and Orally Efficacious ROR¿ Inhibitor.

Central Pharmaceutical Research Institute

Indole Glucocorticoid Receptor Antagonists Active in a Model of Dyslipidemia Act via a Unique Association with an Agonist Binding Site.

Eli Lilly

Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate.

Boehringer Ingelheim Pharmaceuticals

Synthesis and biological action of two glucocorticoid alkylating agents.

TBA

The discovery of potent and selective non-steroidal glucocorticoid receptor modulators, suitable for inhalation.

Astrazeneca

Discovery of liver selective non-steroidal glucocorticoid receptor antagonist as novel antidiabetic agents.

Zydus Research Centre

Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist.

Schering

Steroidal C-21 heteroaryl thioethers. Part 3: pregn-4-eno-[3,2-c]pyrazole fused A ring modified steroids as selective glucocorticoid receptor modulators (dissociated steroids).

Merck Research Laboratories

Bile acid conjugates of a nonsteroidal glucocorticoid receptor modulator.

Abbott Laboratories

Synthesis, activity, metabolic stability, and pharmacokinetics of glucocorticoid receptor modulator-statin hybrids.

Abbott Laboratories

Anti-inflammatory 17beta-thioalkyl-16alpha,17alpha-ketal and -acetal androstanes: a new class of airway selective steroids for the treatment of asthma.

Rh£Ne-Poulenc Rorer Central Research

Synthesis and evaluation of antiinflammatory activities of a series of corticosteroid 17 alpha-esters containing a functional group.

Mitsubishi Kasei

An evaluation of a C-glucuronide as a liver targeting group: conjugate of a glucocorticoid antagonist.

Abbott Laboratories

Steroidal C-21 heteroaryl thioethers (Part 2): discovery of orally bioavailable selective glucocorticoid receptor modulators (dissociated steroids).

Merck Research Laboratories

Steroidal C-21 mercapto derivatives as dissociated steroids: discovery of an inhaled dissociated steroid.

Merck Research Laboratories

Tetrahydroquinolines as a novel series of nonsteroidal selective androgen receptor modulators: structural requirements for better physicochemical and biological properties.

Kaken Pharmaceutical

Design and synthesis of tricyclic tetrahydroquinolines as a new series of nonsteroidal selective androgen receptor modulators (SARMs).

Kaken Pharmaceutical

Discovery of Apararenone (MT-3995) as a Highly Selective, Potent, and Novel Nonsteroidal Mineralocorticoid Receptor Antagonist.

Mitsubishi Tanabe Pharma

Stereoisomers of an Aryl Pyrazole Glucocorticoid Receptor Agonist Scaffold Elicit Differing Anti-inflammatory Responses.

University of Tennessee

Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacy.

Merck Research Laboratories

Design and evaluation of novel nonsteroidal dissociating glucocorticoid receptor ligands.

University of California San Francisco

Potent Anti-Inflammatory, Arylpyrazole-Based Glucocorticoid Receptor Agonists That Do Not Impair Insulin Secretion.

University of Tennessee

Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.

Abbott Laboratories

1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as potent GR antagonists with reduced hERG inhibition and an improved pharmacokinetic profile.

Corcept Therapeutics

Synthesis and radiopharmacological characterization of [11C]AL-438 as a nonsteroidal ligand for imaging brain glucocorticoid receptors.

Forschungszentrum Dresden-Rossendorf

Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.

Astrazeneca

Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).

Oric Pharmaceuticals

Identification of the Clinical Candidate (R)-(1-(4-Fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): A Selective Glucocorticoid Receptor (GR) Antagonist.

Corcept Therapeutics

Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases.

Astrazeneca

Beneficial effects of a new 20-hydroxyeicosatetraenoic acid synthesis inhibitor, TS-011 [N-(3-chloro-4-morpholin-4-yl) phenyl-N'-hydroxyimido formamide], on hemorrhagic and ischemic stroke.

Taisho Pharmaceutical

Hepatic glucocorticoid receptor antagonism is sufficient to reduce elevated hepatic glucose output and improve glucose control in animal models of type 2 diabetes.

Abbott Laboratories

Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.

Abbott Laboratories