PMID

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Article Title

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Discovery of a Cyclic Boronic Acidß-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.

Rempex Pharmaceuticals

Discovery of novel series of 6-benzyl substituted 4-aminocarbonyl-1,4-diazepane-2,5-diones as human chymase inhibitors using structure-based drug design.

Asubio Pharma

Discovery of potent, selective chymase inhibitors via fragment linking strategies.

Boehringer Ingelheim Pharmaceuticals

Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors.

Celera Genomics

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

University Of Florida

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

Johnson & Johnson Pharmaceutical Research & Development

Discovery of a potent, selective, and orally active proteasome inhibitor for the treatment of cancer.

Cephalon

Synthesis, structure-activity relationships, and pharmacokinetic profiles of nonpeptidic difluoromethylene ketones as novel inhibitors of human chymase.

Welfide

Synthesis, structure-activity relationships, and pharmacokinetic profiles of nonpeptidic alpha-keto heterocycles as novel inhibitors of human chymase.

Welfide

Structure-based library design and the discovery of a potent and selective mast cellß-tryptase inhibitor as an oral therapeutic agent.

Sanofi Pharmaceuticals

Benzimidazolone as potent chymase inhibitor: modulation of reactive metabolite formation in the hydrophobic (P1) region.

Boehringer Ingelheim Pharmaceuticals

2-Azetidinone--a new profile of various pharmacological activities.

Barkatullah University

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

Merck Research Laboratories

Discovery and clinical evaluation of 1-{N-[2-(amidinoaminooxy)ethyl]amino}carbonylmethyl-6-methyl-3-[2,2-difluoro-2-phenylethylamino]pyrazinone (RWJ-671818), a thrombin inhibitor with an oxyguanidine P1 motif.

Johnson & Johnson Pharmaceutical Research And Development

Identification and optimization of inhibitors of Trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB.

National Human Genome Research Institute

Development of 6-benzyl substituted 4-aminocarbonyl-1,4-diazepane-2,5-diones as orally active human chymase inhibitors.

Daiichi Asubio Pharma

Identification of 6-substituted 4-arylsulfonyl-1,4-diazepane-2,5-diones as a novel scaffold for human chymase inhibitors.

Daiichi Asubio Pharma

Discovery of potent, selective, orally active, nonpeptide inhibitors of human mast cell chymase.

Johnson & Johnson Pharmaceutical Research And Development

Novel, potent, selective, and orally bioavailable human betaII-tryptase inhibitors.

Celera Genomics

Structure-activity relationship of benzo[b]thiophene-2-sulfonamide derivatives as novel human chymase inhibitors.

Toa Eiyo

Identification of a stable chymase inhibitor using a pharmacophore-Based database search.

Toa Eiyo

Total synthesis of human chymase inhibitor methyllinderone and structure--activity relationships of its derivatives.

Shionogi

Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones.

Shionogi

1-Oxacephem-based human chymase inhibitors: discovery of stable inhibitors in human plasma.

Shionogi

Synthesis and structure-activity relationships of a new class of 1-oxacephem-based human chymase inhibitors.

Shionogi

Structure-activity relationship studies of chloromethyl ketone derivatives for selective human chymase inhibitors.

Kyoto Pharmaceutical University

Symmetrical anhydride-type serine protease inhibitors: structure-activity relationship studies of human chymase inhibitors.

Nippon Steel

N-[2,2-dimethyl-3-(N-(4-cyanobenzoyl)amino)nonanoyl]-L-phenylalanine ethyl ester as a stable ester-type inhibitor of chymotrypsin-like serine proteases: structural requirements for potent inhibition of alpha-chymotrypsin.

Nippon Steel

Peptidyl human heart chymase inhibitors. 2. Discovery of highly selective difluoromethylene ketone derivatives with Glu at P3 site.

Green Cross Research Laboratories

Peptidyl human heart chymase inhibitors. 1. Synthesis and inhibitory activity of difluoromethylene ketone derivatives bearing P' binding subsites.

Green Cross Research Laboratories

Substituted 3-(phenylsulfonyl)-1-phenylimidazolidine-2,4-dione derivatives as novel nonpeptide inhibitors of human heart chymase.

Suntory

Design, synthesis and evaluation of new thiazole-piperazines as acetylcholinesterase inhibitors.

Anadolu University

Potent reversible inhibition of myeloperoxidase by aromatic hydroxamates.

University Of Otago Christchurch

Design, synthesis and biological screening of new 4-thiazolidinone derivatives with promising COX-2 selectivity, anti-inflammatory activity and gastric safety profile.

Beni-Suef University

Engineering novel specificities for ligand-activated transcription in the nuclear hormone receptor RXR.

University Of Texas Southwestern Medical Center