166 articles for thisTarget
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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
Identification of potent and selective cathepsin S inhibitors containing different central cyclic scaffolds.
Pharma Research and Early
Pyrazole-based arylalkyne cathepsin S inhibitors. Part III: modification of P4 region.
Janssen Research and Development
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
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
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
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
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
Discovery of CMX990: A Potent SARS-CoV-2 3CL Protease Inhibitor Bearing a Novel Warhead.
Calibr At Scripps Research Institute
Dipeptide-Derived Alkynes as Potent and Selective Irreversible Inhibitors of Cysteine Cathepsins.
Helmholtz-Zentrum Dresden-Rossendorf
Bicyclic carbamates as inhibitors of papain-like cathepsin proteases.
The Genomics Institute of The Novartis Research Foundation
Synthesis and structure-activity relationship studies of cruzain and rhodesain inhibitors.
Universidade Federal Do Rio Grande Do Sul
Design and synthesis of dual cathepsin L and S inhibitors and antimetastatic activity evaluation in pancreatic cancer cells.
Shenyang Pharmaceutical University
Discovery of selective covalent cathepsin K inhibitors containing novel 4-cyanopyrimidine warhead based on quantum chemical calculations and binding mode analysis.
China Pharmaceutical University
Design and synthesis of tetracyclic nonpeptidic biaryl nitrile inhibitors of cathepsin K.
Celera Genomics
Non-peptidyl non-covalent cathepsin C inhibitoEEr bearing a unique thiophene-substituted pyridine: Design, structure-activity relationship and anti-inflammatory activity in vivo.
Anhui Medical University
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
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
The University of Sydney
The SAR of 4-substituted (6,6-bicyclic) piperidine cathepsin S inhibitors.
Johnson and Johnson Pharmaceutical Research and Development
The Alpha Keto Amide Moiety as a Privileged Motif in Medicinal Chemistry: Current Insights and Emerging Opportunities.
Niddk
Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.
Celera Genomics
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
Peptidomimetic nitrile warheads as SARS-CoV-2 3CL protease inhibitors.
University of Alberta Edmonton
A structural screening approach to ketoamide-based inhibitors of cathepsin K.
Glaxosmithkline
Discovery of Chlorofluoroacetamide-Based Covalent Inhibitors for Severe Acute Respiratory Syndrome Coronavirus 2 3CL Protease.
Kyushu University
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
N-Sulfonyl dipeptide nitriles as inhibitors of human cathepsin S: In silico design, synthesis and biochemical characterization.
University of Bonn
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
Structure-activity relationships of triazole-benzodioxine inhibitors of cathepsin X.
University of Ljubljana
Design, synthesis and stepwise optimization of nitrile-based inhibitors of cathepsins B and L.
University of S£O Paulo
Identification of dipeptidyl nitriles as potent and selective inhibitors of cathepsin B through structure-based drug design.
Novartis Pharmaceuticals
Highly Selective Sub-Nanomolar Cathepsin S Inhibitors by Merging Fragment Binders with Nitrile Inhibitors.
Grunenthal
Potent reversible inhibitors of the protein tyrosine phosphatase CD45.
Astrazeneca Pharmaceuticals
Identification and Optimization of Novel Cathepsin C Inhibitors Derived from EGFR Inhibitors.
National Institute of Biological Sciences (Nibs)
Design, synthesis and biological evaluation of inhibitors of cathepsin K on dedifferentiated chondrocytes.
Jilin University
Peptidomimetic Vinyl Heterocyclic Inhibitors of Cruzain Effect Antitrypanosomal Activity.
Texas A&M University
Development of a potent and selective cell penetrant Legumain inhibitor.
Queen'S University Belfast
Identification of new peptide amides as selective cathepsin L inhibitors: the first step towards selective irreversible inhibitors?
National Institute of Biology
Substrate-derived triazolo- and azapeptides as inhibitors of cathepsins K and S.
Cnrs Upr 4301
Selective inhibition of human cathepsin S by 2,4,6-trisubstituted 1,3,5-triazine analogs.
Orleans University
Peptidomimetic nitrile inhibitors of malarial protease falcipain-2 with high selectivity against human cathepsins.
Irbm Science Park
Repurposing a Library of Human Cathepsin L Ligands: Identification of Macrocyclic Lactams as Potent Rhodesain and Trypanosoma brucei Inhibitors.
Eth Zurich
Discovery of Novel and Highly Selective Inhibitors of Calpain for the Treatment of Alzheimer's Disease: 2-(3-Phenyl-1H-pyrazol-1-yl)-nicotinamides.
Abbvie Deutschland
Blockade of Asparagine Endopeptidase Inhibits Cancer Metastasis.
Emory Chemical Biology Discovery Center Emory University School of Medicine Atlanta
Pyranopyrazole and pyrazolopyridine immunomodulators for treatment of autoimmune diseases
Rockefeller University
Chiral N-acyl-5,6,7(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-A]pyrazines as selective NK-3 receptor antagonists, pharmaceutical composition, methods for use in NK-3 receptor mediated disorders and chiral synthesis thereof
Ogeda
Isoindoline or isoquinoline compounds, a process for their preparation and pharmaceutical compositions containing them
Les Laboratoires Servier
Inhibitors of BCR-ABL mutants and use thereof
The Regents of The University of Michigan
Use of small molecule inhibitors targeting EYA tyrosine phosphatase
Cincinnati Childrens Hospital Medical Center
Piperidine substituted tricyclic pyrazolo[1,5-a]pyrimidine derivatives with inhibitory activity on the replication of the respiratory syncytial virus (RSV)
Janssen Ireland
Bicyclic heteroaryl derivatives as CFTR potentiators
Cystic Fibrosis Foundation Therapeutics
Substituted benzothiophenyl derivatives as GPR40 agonists for the treatment of type II diabetes
Janssen Pharmaceutica
Substituted [1,2,4]triazolo[4,3-A]pyrazines that are BRD4 inhibitors
Boehringer Ingelheim International
[(3)H]MRE 3008F20: a novel antagonist radioligand for the pharmacological and biochemical characterization of human A(3) adenosine receptors.
University of Ferrara
Differential binding of inhibitors to active and inactive CDK2 provides insights for drug design.
Cyclacel
Oxindole-based inhibitors of cyclin-dependent kinase 2 (CDK2): design, synthesis, enzymatic activities, and X-ray crystallographic analysis.
Glaxosmithkline
Imidazo[1,2-b]pyridazines: a potent and selective class of cyclin-dependent kinase inhibitors.
Astrazeneca
Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 2: identification and optimisation of substituted 2,4-bis anilino pyrimidines.
Astrazeneca
Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 1: identification and optimisation of substituted 4,6-bis anilino pyrimidines.
Astrazeneca
Cyclin-dependent kinase inhibition by new C-2 alkynylated purine derivatives and molecular structure of a CDK2-inhibitor complex.
Institut Curie
Cinnamaldehydes inhibit cyclin dependent kinase 4/cyclin D1.
Korea Research Institute of Bioscience and Biotechnology