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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

Design, synthesis, and evaluation of (2S,4R)-Ketoconazole sulfonamide analogs as potential treatments for Metabolic Syndrome.

Temple University School Of Pharmacy

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

University Of Bologna

Discovery of the Selective CYP17A1 Lyase Inhibitor BMS-351 for the Treatment of Prostate Cancer.

Bristol-Myers Squibb Research And Development

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.

Universit£

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

Design, synthesis, and structure-activity relationships of azolylmethylpyrroloquinolines as nonsteroidal aromatase inhibitors.

University Of Padova

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

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

Novel CYP17 inhibitors: synthesis, biological evaluation, structure-activity relationships and modelling of methoxy- and hydroxy-substituted methyleneimidazolyl biphenyls.

Saarland University

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

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

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

Selective inhibition of mammalian lanosterol 14 alpha-demethylase: a possible strategy for cholesterol lowering.

Syntex Discovery Research

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

UniversitäT Des Saarlandes

Accelerated skin wound healing by selective 11?-Hydroxylase (CYP11B1) inhibitors.

Saarland University

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

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

gamma-Aminobutyric acidA receptor heterogeneity in rat central nervous system: studies with clonazepam and other benzodiazepine ligands.

Georgetown University

Inhibition of a viral enzyme by a small-molecule dimer disruptor.

University Of California San Francisco

Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.

Vanderbilt University

Synthesis and SAR studies of indole-based MK2 inhibitors.

Boehringer Ingelheim Pharmaceuticals

The discovery of carboline analogs as potent MAPKAP-K2 inhibitors.

Boehringer Ingelheim Pharmaceuticals

Asymmetric synthesis of inhibitors of glycinamide ribonucleotide transformylase.

The Scripps Research Institute

Crystal structure of avian aminoimidazole-4-carboxamide ribonucleotide transformylase in complex with a novel non-folate inhibitor identified by virtual ligand screening.

The Scripps Research Institute

4-benzyl-1H-imidazoles with oxazoline termini as histamine H3 receptor agonists.

Vu University Amsterdam

2-Amino-1,3-thiazol-4(5H)-ones as Potent and Selective 11beta-Hydroxysteroid Dehydrogenase Type 1 Inhibitors: Enzyme-Ligand Co-Crystal Structure and Demonstration of Pharmacodynamic Effects in C57Bl/6 Mice.

Biovitrum

Indanylacetic acid derivatives carrying 4-thiazolyl-phenoxy tail groups, a new class of potent PPAR alpha/gamma/delta pan agonists: synthesis, structure-activity relationship, and in vivo efficacy.

Bayer Healthcare Pharmaceuticals

Synthesis and biological evaluation of 1-(2,4,5-trisubstituted phenyl)-3-(5-cyanopyrazin-2-yl)ureas as potent Chk1 kinase inhibitors.

Abbott Laboratories

Benzimidazolones and indoles as non-thiol farnesyltransferase inhibitors based on tipifarnib scaffold: synthesis and activity.

Abbott Laboratories

Structural basis for selectivity of a small molecule, S1-binding, submicromolar inhibitor of urokinase-type plasminogen activator.

Axys Pharmaceutical

SAR and inhibitor complex structure determination of a novel class of potent and specific Aurora kinase inhibitors.

Astrazeneca

Enthalpy versus entropy-driven binding of bisphosphonates to farnesyl diphosphate synthase.

University Of Illinois At Urbana-Champaign

 

Thermodynamics of Binding of 2-Methoxy-3-isopropylpyrazine and 2-Methoxy-3-isobutylpyrazine to the Major Urinary Protein

University Of Leeds