PMID

Data

Article Title

Organization

4-Anilino-pyrimidine, novel aldosterone synthase (CYP11B2) inhibitors bearing pyrimidine structures.

Daiichi Sankyo

Imidazopyridyl compounds as aldosterone synthase inhibitors.

Merck Usa

Discovery of Spirocyclic Aldosterone Synthase Inhibitors as Potential Treatments for Resistant Hypertension.

Merck Research Laboratories

Exploiting the Chromone Scaffold for the Development of Inhibitors of Corticosteroid Biosynthesis.

University of Bologna

Discovery of 4-Aryl-5,6,7,8-tetrahydroisoquinolines as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors: In Vivo Evaluation in Rodents and Cynomolgus Monkeys.

Roche Pharma Research and Early Development (Pred)

Discovery of Triazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.

Merck Research Laboratories

Discovery of Benzimidazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.

Merck Research Laboratories

Identification of 4-(4-nitro-2-phenethoxyphenyl)pyridine as a promising new lead for discovering inhibitors of both human and rat 11ß-Hydroxylase.

Saarland University

Novel pyridyl substituted 4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolines as potent and selective aldosterone synthase inhibitors with improved in vitro metabolic stability.

Saarland University and Helmholtz Institute For Pharmaceutical Research Saarland (Hips)

Heteroatom insertion into 3,4-dihydro-1H-quinolin-2-ones leads to potent and selective inhibitors of human and rat aldosterone synthase.

Saarland University

Aldosterone synthase inhibitors as promising treatments for mineralocorticoid dependent cardiovascular and renal diseases.

Saarland University and Helmholtz Institute For Pharmaceutical Research Saarland (Hips)

1-Phenylsulfinyl-3-(pyridin-3-yl)naphthalen-2-ols: a new class of potent and selective aldosterone synthase inhibitors.

Saarland University and Helmholtz Institute For Pharmaceutical Research Saarland (Hips)

Discovery of new 7-substituted-4-imidazolylmethyl coumarins and 4'-substituted-2-imidazolyl acetophenones open analogues as potent and selective inhibitors of steroid-11ß-hydroxylase.

University of Bari Aldo Moro

Potent 11ß-hydroxylase inhibitors with inverse metabolic stability in human plasma and hepatic S9 fractions to promote wound healing.

Saarland University and Helmholtz Institute For Pharmaceutical Research Saarland (Hips)

Novel pyridyl- or isoquinolinyl-substituted indolines and indoles as potent and selective aldosterone synthase inhibitors.

Saarland University

Discovery and in Vivo Evaluation of Potent Dual CYP11B2 (Aldosterone Synthase) and CYP11B1 Inhibitors.

Novartis Institutes For Biomedical Research

Emerging technologies for metabolite generation and structural diversification.

Abbvie Bioresearch Center

Cushing's syndrome: development of highly potent and selective CYP11B1 inhibitors of the (pyridylmethyl)pyridine type.

Saarland University

Highly potent and selective nonsteroidal dual inhibitors of CYP17/CYP11B2 for the treatment of prostate cancer to reduce risks of cardiovascular diseases.

Saarland University & Helmholtz Institute For Pharmaceutical Research Saarland (Hips)

Modulation of cytochromes P450 with xanthone-based molecules: from aromatase to aldosterone synthase and steroid 11ß-hydroxylase inhibition.

University of Bologna

Selective Cyp11B1 Inhibitors for the Treatment of Cortisol Dependent Diseases.

Temple University

Aldosterone synthase inhibitors.

Temple University

Aldosterone synthase inhibitors: targeting chronic kidney disease and diabetic nephropathy.

Therachem Research Medilab (India)

Tetrahydropyrroloquinolinone type dual inhibitors of aromatase/aldosterone synthase as a novel strategy for breast cancer patients with elevated cardiovascular risks.

Saarland University & Helmholtz Institute For Pharmaceutical Research Saarland (Hips)

Selective dual inhibitors of CYP19 and CYP11B2: targeting cardiovascular diseases hiding in the shadow of breast cancer.

Saarland University & Helmholtz Institute For Pharmaceutical Research Saarland (Hips)

Novel imidazol-1-ylmethyl substituted 1,2,5,6-tetrahydropyrrolo[3,2,1-ij]quinolin-4-ones as potent and selective CYP11B1 inhibitors for the treatment of Cushing's syndrome.

Saarland University and Helmholtz Institute For Pharmaceutical Research Saarland (Hips)

Optimization of the First Selective Steroid-11ß-hydroxylase (CYP11B1) Inhibitors for the Treatment of Cortisol Dependent Diseases.

TBA

Isopropylidene substitution increases activity and selectivity of biphenylmethylene 4-pyridine type CYP17 inhibitors.

Saarland University

Fine-tuning the selectivity of aldosterone synthase inhibitors: structure-activity and structure-selectivity insights from studies of heteroaryl substituted 1,2,5,6-tetrahydropyrrolo[3,2,1-ij]quinolin-4-one derivatives.

Saarland University

Design, synthesis, and biological evaluation of imidazolyl derivatives of 4,7-disubstituted coumarins as aromatase inhibitors selective over 17-a-hydroxylase/C17-20 lyase.

Universita` Degli Studi Di Bari Aldo Moro

First Selective CYP11B1 Inhibitors for the Treatment of Cortisol-Dependent Diseases

TBA

N-(Pyridin-3-yl)benzamides as selective inhibitors of human aldosterone synthase (CYP11B2).

Saarland University & Helmholtz Institute For Pharmaceutical Research Saarland

Replacement of imidazolyl by pyridyl in biphenylmethylenes results in selective CYP17 and dual CYP17/CYP11B1 inhibitors for the treatment of prostate cancer.

Saarland University

The discovery of potent inhibitors of aldosterone synthase that exhibit selectivity over 11-beta-hydroxylase.

Novartis Institutes For Biomedical Research

Synthesis, biological evaluation, and molecular modeling of 1-benzyl-1H-imidazoles as selective inhibitors of aldosterone synthase (CYP11B2).

Eindhoven University of Technology

In vivo active aldosterone synthase inhibitors with improved selectivity: lead optimization providing a series of pyridine substituted 3,4-dihydro-1H-quinolin-2-one derivatives.

Saarland University

Novel aldosterone synthase inhibitors with extended carbocyclic skeleton by a combined ligand-based and structure-based drug design approach.

Saarland University

Overcoming undesirable CYP1A2 inhibition of pyridylnaphthalene-type aldosterone synthase inhibitors: influence of heteroaryl derivatization on potency and selectivity.

Saarland University

A decade of approved first-in-class small molecule orphan drugs: Achievements, challenges and perspectives.

China Pharmaceutical University

Fluorinated aldosterone synthase (CYP11B2)-inhibitors for differential diagnosis between bilateral and unilateral conditions of primary aldosteronism.

University Hospital of Wuerzburg

Design, Synthesis, and Biological Evaluations of Pyridyl 4,5,6,7-Tetrahydro-4,7-Methanobenzo[

Guangzhou University of Chinese Medicine

Discovery of 3-Pyridyl Isoindolin-1-one Derivatives as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors.

TBA

Strategies for the development of highly selective cytochrome P450 inhibitors: Several CYP targets in current research.

Shenyang Pharmaceutical University

Development of Highly Selective Pyrimidine-Based Aldosterone Synthase (CYP11B2) Inhibitors.

Selenity Therapeutics

Tetrahydronaphthalenes: influence of heterocyclic substituents on inhibition of steroid enzymes P450 arom and P450 17.

UniversitäT De Saarlandes

Discovery of N-[5-(6-Chloro-3-cyano-1-methyl-1H-indol-2-yl)-pyridin-3-ylmethyl]-ethanesulfonamide, a Cortisol-Sparing CYP11B2 Inhibitor that Lowers Aldosterone in Human Subjects.

Novartis Institutes For Biomedical Research

Pyridyl-substituted tetrahydrocyclopropa[a]naphthalenes: highly active and selective inhibitors of P450 arom.

UniversitäT Des Saarlandes

Drifting of heme-coordinating group in imidazolylmethylxanthones leading to improved selective inhibition of CYP11B1.

Alma Mater Studiorum-University of Bologna

Discovery of Novel Pyrazole-Based Selective Aldosterone Synthase (CYP11B2) Inhibitors: A New Template to Coordinate the Heme-Iron Motif of CYP11B2.

Mitsubishi Tanabe Pharma

Design and optimization of highly-selective, broad spectrum fungal CYP51 inhibitors.

Viamet Pharmaceuticals

Synthesis and aromatase inhibitory activity of novel 1-(4-aminophenyl)-3-azabicyclo[3.1.0]hexane- and -[3.1.1]heptane-2,4- diones.

Ciba-Geigy

Discovery of indazole aldosterone synthase (CYP11B2) inhibitors as potential treatments for hypertension.

Merck Research Laboratories

Lead Optimization Generates CYP11B1 Inhibitors of Pyridylmethyl Isoxazole Type with Improved Pharmacological Profile for the Treatment of Cushing's Disease.

Saarland University

4,6-substituted-pyrazolo[1,5-a]pyrazines as janus kinase inhibitors

Array Biopharma

5-HT2C receptor agonists and compositions and methods of use

Arena Pharmaceuticals

Benzodiazepines as bromodomain inhibitors

Catalyst Therapeutics

ASK1 inhibitor compounds and uses thereof

Seal Rock Therapeutics

Imidazo[1,2-α]pyridine derivatives as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto

Arena Pharmaceuticals

Triazine derivative and pharmaceutical composition having an analgesic activity comprising the same

Shionogi

Pharmaceutical compositions and their use for treatment of cancer and autoimmune diseases

Zhejiang Dtrm Biopharma

Inhibitors of c-fms kinase

Janssen Pharmaceutica

Opioid receptor function is regulated by post-endocytic peptide processing.

Icahn School of Medicine At Mount Sinai

An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED.

Novartis Institutes For Biomedical Research

1,2,5-oxadiazoles as inhibitors of indoleamine 2,3-dioxygenase

Incyte

Substituted imidazo[1,2-a]pyrazines as MPS-1 inhibitors

Bayer Intellectual Property

Pyrazolyl-pyrimidine derivatives as kinase inhibitors

Nerviano Medical Sciences

Inhibition of the Flavin-Dependent Monooxygenase Siderophore A (SidA) Blocks Siderophore Biosynthesis and Aspergillus fumigatus Growth.

Virginia Tech

Design and characterization of bivalent BET inhibitors.

Dana-Farber Cancer Institute

Use of rosuvastatin lactols as medicaments

Redx Pharma

2-Arylquinazolin-4(3H)-ones: A novel class of thymidine phosphorylase inhibitors.

University of Karachi

Antimalarial agents that are inhibitors of dihydroorotate dehydrogenase

Board of Regents, The University of Texas System

Sulfamide derivative having an adamantyl group and its pharmaceutically acceptable salt

Korea Research Institute of Chemical Technology

Alicyclic carboxylic acid derivatives of benzomorphans and related scaffolds, medicaments containing such compounds and their use

Boehringer Ingelheim International

Fused bicyclic heterocycles useful as dipeptidyl peptidase-IV inhibitors

Merck Sharp & Dohme

Spiropiperidine prolylcarboxypeptidase inhibitors

Merck Sharp & Dohme

Glucagon receptor antagonists, preparation and therapeutic uses

Eli Lilly

Primary amines and derivatives thereof as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto

Arena Pharmaceuticals

Azabiphenylaminobenzoic acid derivatives as DHODH inhibitors

Almirall

Heterocyclic compounds, processes for their preparation, medicaments comprising these compounds, and the use thereof

Sanofi

Pharmacological characterization of (E)-N-(4-fluorobut-2-enyl)-2beta-carbomethoxy-3beta-(4'-tolyl)nortropane (LBT-999) as a highly promising fluorinated ligand for the dopamine transporter.

University of Tours

Development of molecular probes for the identification of extra interaction sites in the mid-gorge and peripheral sites of butyrylcholinesterase (BuChE). Rational design of novel, selective, and highly potent BuChE inhibitors.

Universita Di Siena

Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.

Eli Lilly

4-hydroxy-5,6-dihydropyrones. 2. Potent non-peptide inhibitors of HIV protease.

Parke-Davis Pharmaceutical Research