PMID

Data

Article Title

Organization

Straightforward synthesis of 2,4,6-trisubstituted 1,3,5-triazine compounds targeting cysteine cathepsins K and S.

Cnrs

Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986).

Charles River Discovery Research Services

Cathepsin B Inhibitors: Combining Dipeptide Nitriles with an Occluding Loop Recognition Element by Click Chemistry.

University Of Bonn

Development of N-(Functionalized benzoyl)-homocycloleucyl-glycinonitriles as Potent Cathepsin K Inhibitors.

National Institute Of Chemistry

Structure-based design and optimization of potent inhibitors of the adenoviral protease.

Novartis Institute For Biomedical Research

Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm.

Eli Lilly

3-Cyano-3-aza-ß-amino Acid Derivatives as Inhibitors of Human Cysteine Cathepsins.

University Of Bonn

Cathepsin C inhibitors: property optimization and identification of a clinical candidate.

Astrazeneca

Pyrazole-based arylalkyne cathepsin S inhibitors. Part III: modification of P4 region.

Janssen Research And Development

Discovery of novel cyanamide-based inhibitors of cathepsin C.

TBA

Design of selective Cathepsin inhibitors.

Astrazeneca

Keto-1,3,4-oxadiazoles as cathepsin K inhibitors.

Celera Genomics

Fluorescent nitrile-based inhibitors of cysteine cathepsins.

University Of Bonn

Exploration of cathepsin S inhibitors characterized by a triazole P1-P2 amide replacement.

Boehringer Ingelheim Pharmaceuticals

Synopsis of some recent tactical application of bioisosteres in drug design.

Bristol-Myers Squibb Pharmaceutical Research And Development

Structural investigation of anti-Trypanosoma cruzi 2-iminothiazolidin-4-ones allows the identification of agents with efficacy in infected mice.

Universidade Federal De Pernambuco

Pharmacokinetic benefits of 3,4-dimethoxy substitution of a phenyl ring and design of isosteres yielding orally available cathepsin K inhibitors.

Astrazeneca

(1R,2R)-N-(1-cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): a potent and highly selective cathepsin K inhibitor for the treatment of osteoarthritis.

Astrazeneca

Selective nitrile inhibitors to modulate the proteolytic synergism of cathepsins S and F.

University Of Bonn

Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition.

Astrazeneca

Structural optimization of azadipeptide nitriles strongly increases association rates and allows the development of selective cathepsin inhibitors.

University Of Bonn

Diazinones as P2 replacements for pyrazole-based cathepsin S inhibitors.

Johnson & Johnson Pharmaceutical Research & Development

Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.

University Of Florida

Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing.

Merck Research Laboratories

New chemotypes for cathepsin K inhibitors.

Novartis Institutes For Biomedical Research

Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.

Johnson & Johnson Pharmaceutical Research & Development

The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.

Merck Frosst Centre For Therapeutic Research

cis-6-oxo-hexahydro-2-oxa-1,4-diazapentalene and cis-6-oxo-hexahydropyrrolo[3,2-c]pyrazole based scaffolds: design rationale, synthesis and cysteinyl proteinase inhibition.

Amura Therapeutics

Simple, intuitive calculations of free energy of binding for protein-ligand complexes. 1. Models without explicit constrained water.

University Of Parma

Azepanone-based inhibitors of human cathepsin S: optimization of selectivity via the P2 substituent.

Glaxosmithkline

In vitro activity and preclinical profile of TMC435350, a potent hepatitis C virus protease inhibitor.

Tibotec

1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors: separation of desired cellular activity from undesired tissue accumulation through optimization of basic nitrogen pka.

Merck Research Laboratories

Identification of potent and reversible cruzipain inhibitors for the treatment of Chagas disease.

Merck Research Laboratories

Trifluoromethylphenyl as P2 for ketoamide-based cathepsin S inhibitors.

Merck Research Laboratories

Optimisation of 2-cyano-pyrimidine inhibitors of cathepsin K: improving selectivity over hERG.

Merck Research Laboratories

Nitrile-containing pharmaceuticals: efficacious roles of the nitrile pharmacophore.

Duquesne University

MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.

Merck Research Laboratories

6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors.

Merck Research Laboratories

2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors.

Merck Research Laboratories

4-(3-Trifluoromethylphenyl)-pyrimidine-2-carbonitrile as cathepsin S inhibitors: N3, not N1 is critically important.

Merck Research Laboratories

Design and synthesis of alpha-ketoamides as cathepsin S inhibitors with potential applications against tumor invasion and angiogenesis.

National Tsing Hua University

Thioether acetamides as P3 binding elements for tetrahydropyrido-pyrazole cathepsin S inhibitors.

Johnson & Johnson Pharmaceutical Research & Development

Discovery and SAR of novel pyrazole-based thioethers as cathepsin S inhibitors. Part 2: Modification of P3, P4, and P5 regions.

Johnson & Johnson Pharmaceutical Research & Development

Discovery and SAR of novel pyrazole-based thioethers as cathepsin S inhibitors: part 1.

Johnson & Johnson Pharmaceutical Research & Development

Dioxo-triazines as a novel series of cathepsin K inhibitors.

Schering-Plough

Design and optimization of a series of novel 2-cyano-pyrimidines as cathepsin K inhibitors.

Schering-Plough

Synthesis and preclinical evaluations of 2-(2-fluorophenyl)-6,7-methylenedioxyquinolin-4-one monosodium phosphate (CHM-1-P-Na) as a potent antitumor agent.

China Medical University

Design and synthesis of dipeptidyl nitriles as potent, selective, and reversible inhibitors of cathepsin C.

Merck Frosst Canada

Pyrazole-based arylalkyne cathepsin S inhibitors. Part II: optimization of cellular potency.

Johnson & Johnson Pharmaceutical Research And Development

 

MDL 74147, a novel selective and soluble inhibitor of human renin. Synthesis, structure-activity relationship, species and protease selectivities.

TBA

5-Aminopyrimidin-2-ylnitriles as cathepsin K inhibitors.

Astrazeneca

Solid-phase parallel synthesis and SAR of 4-amidofuran-3-one inhibitors of cathepsin S: effect of sulfonamides P3 substituents on potency and selectivity.

Medivir

Overcoming hERG issues for brain-penetrating cathepsin S inhibitors: 2-cyanopyrimidines. Part 2.

Novartis Institutes For Biomedical Research

Effect of cathepsin K inhibitors on bone resorption.

Novartis Institutes For Biomedical Research

4-Amino-2-cyanopyrimidines: novel scaffold for nonpeptidic cathepsin S inhibitors.

Novartis Institutes For Biomedical Research

Discovery of selective and nonpeptidic cathepsin S inhibitors.

Novartis Institutes For Biomedical Research

Substrate optimization for monitoring cathepsin C activity in live cells.

Genomics Institute Of The Novartis Research Foundation

Novel scaffold for cathepsin K inhibitors.

Novartis Institutes For Biomedical Research

Pyrazole-based cathepsin S inhibitors with improved cellular potency.

Johnson & Johnson Pharmaceutical Research & Development

Primary amides as selective inhibitors of cathepsin K.

Merck Frosst Centre For Therapeutic Research

Identification of a novel class of succinyl-nitrile-based Cathepsin S inhibitors.

Boehringer Ingelheim Pharmaceuticals

Bicyclic carbamates as inhibitors of papain-like cathepsin proteases.

The Genomics Institute Of The Novartis Research Foundation

Design and synthesis of tetracyclic nonpeptidic biaryl nitrile inhibitors of cathepsin K.

Celera Genomics

Optimization of subsite binding to the beta5 subunit of the human 20S proteasome using vinyl sulfones and 2-keto-1,3,4-oxadiazoles: syntheses and cellular properties of potent, selective proteasome inhibitors.

Celera

The SAR of 4-substituted (6,6-bicyclic) piperidine cathepsin S inhibitors.

Johnson And Johnson Pharmaceutical Research And Development

Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.

Celera Genomics

Azepanone-based inhibitors of human cathepsin L.

Glaxosmithkline

Trifluoroethylamines as amide isosteres in inhibitors of cathepsin K.

Merck Frosst Centre For Therapeutic Research

P2-P3 conformationally constrained ketoamide-based inhibitors of cathepsin K.

Glaxosmithkline

A structural screening approach to ketoamide-based inhibitors of cathepsin K.

Glaxosmithkline

Discovery and SAR studies of a novel series of noncovalent cathepsin S inhibitors.

Johnson And Johnson Pharmaceutical Research And Development

Novel purine nitrile derived inhibitors of the cysteine protease cathepsin K.

Novartis Institutes For Biomedical Research

Nonpeptidic, noncovalent inhibitors of the cysteine protease cathepsin S.

Johnson & Johnson Pharmaceutical Research And Development

Potent and selective P2-P3 ketoamide inhibitors of cathepsin K with good pharmacokinetic properties via favorable P1', P1, and/or P3 substitutions.

Glaxosmithkline

Rational design of potent and selective NH-linked aryl/heteroaryl cathepsin K inhibitors.

Merck Frosst Centre For Therapeutic Research

N-arylaminonitriles as bioavailable peptidomimetic inhibitors of cathepsin B.

Novartis Institute Of Biomedical Research

3,4-disubstituted azetidinones as selective inhibitors of the cysteine protease cathepsin K. Exploring P2 elements for selectivity.

Ligand Pharmaceuticals

Arylaminoethyl amides as inhibitors of the cysteine protease cathepsin K-investigating P1' substituents.

Novartis Pharma

3-Acylamino-azetidin-2-one as a novel class of cysteine proteases inhibitors.

Currently Naeja Pharmaceutical

Design and synthesis of dipeptide nitriles as reversible and potent Cathepsin S inhibitors.

Boehringer Ingelheim Pharmaceuticals

6-Acylamino-penam derivatives: synthesis and inhibition of cathepsins B, L, K, and S.

Currently Naeja Pharmaceutical

Design and synthesis of 6-substituted amino-4-oxa-1-azabicyclo[3,2,0]heptan-7-one derivatives as cysteine proteases inhibitors.

Currently Naeja Pharmaceutical

Novel route to the synthesis of peptides containing 2-amino-1'-hydroxymethyl ketones and their application as cathepsin K inhibitors.

Celera

Arylaminoethyl amides as novel non-covalent cathepsin K inhibitors.

TBA

Identification of dipeptidyl nitriles as potent and selective inhibitors of cathepsin B through structure-based drug design.

Novartis Pharmaceuticals

Potent reversible inhibitors of the protein tyrosine phosphatase CD45.

Astrazeneca Pharmaceuticals

Azepanone-based inhibitors of human and rat cathepsin K.

Glaxosmithkline

Vinyl sulfones as mechanism-based cysteine protease inhibitors.

Khepri Pharmaceuticals

Blockade of Asparagine Endopeptidase Inhibits Cancer Metastasis.

Emory Chemical Biology Discovery Center Emory University School Of Medicine Atlanta

Synthesis of a-oxycarbanilinophosphonates and their anticholinesterase activities: the most potent derivative is bound to the peripheral site of acetylcholinesterase.

Institute For Advanced Studies In Basic Sciences (Iasbs)

In vitro effects of some anabolic compounds on erythrocyte carbonic anhydrase I and II.

Balikesir University

In vitro and in vivo pharmacological characterization of JTE-907, a novel selective ligand for cannabinoid CB2 receptor.

Japan Tobacco

RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist.

Roche Bioscience

NNC-112, NNC-687 and NNC-756, new selective and highly potent dopamine D1 receptor antagonists.

Novo Nordisk

A neoceptor approach to unraveling microscopic interactions between the human A2A adenosine receptor and its agonists.

National Institutes Of Health

Rational design, synthesis and characterization of potent, non-peptidic Smac mimics/XIAP inhibitors as proapoptotic agents for cancer therapy.

Universita Degli Studi Di Milano

Triazine Compounds as Antagonists at Bv8-Prokineticin Receptors.

University Of Ferrara