PMID

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Article Title

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

Charles River Discovery Research Services

Tasiamide F, a potent inhibitor of cathepsins D and E from a marine cyanobacterium.

University of Florida

trans-(3S,4S)-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part I: prime site exploration using an amino linker.

Novartis Pharma

trans-3,4-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part II: prime site exploration using an oxygen linker.

Novartis Pharma

Iminopyrimidinones: a novel pharmacophore for the development of orally active renin inhibitors.

Merck Research Laboratories

Structure-based optimization of non-peptidic Cathepsin D inhibitors.

Merck

Structure-based design of substituted piperidines as a new class of highly efficacious oral direct Renin inhibitors.

Novartis Institutes For Biomedical Research

Inhibitors of฿-site amyloid precursor protein cleaving enzyme (BACE1): identification of (S)-7-(2-fluoropyridin-3-yl)-3-((3-methyloxetan-3-yl)ethynyl)-5'H-spiro[chromeno[2,3-b]pyridine-5,4'-oxazol]-2'-amine (AMG-8718).

Amgen

ß-Secretase (BACE1) inhibitors with high in vivo efficacy suitable for clinical evaluation in Alzheimer's disease.

F. Hoffmann-La Roche

The discovery of novel potent trans-3,4-disubstituted pyrrolidine inhibitors of the human aspartic protease renin from in silico three-dimensional (3D) pharmacophore searches.

Novartis Pharma

A novel class of oral direct renin inhibitors: highly potent 3,5-disubstituted piperidines bearing a tricyclic p3-p1 pharmacophore.

Novartis Pharma

Cyanobacterial peptides as a prototype for the design of potentß-secretase inhibitors and the development of selective chemical probes for other aspartic proteases.

University of Florida

Discovery of DS-8108b, a Novel Orally Bioavailable Renin Inhibitor.

TBA

Total synthesis of grassystatin A, a probe for cathepsin E function.

Fudan University

Symplocin A, a linear peptide from the Bahamian cyanobacterium Symploca sp. Configurational analysis of N,N-dimethylamino acids by chiral-phase HPLC of naphthacyl esters.

University of California

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

University of Florida

Discovery of an orally efficaceous 4-phenoxypyrrolidine-based BACE-1 inhibitor.

Schering-Plough Research Institute

Potent pyrrolidine- and piperidine-based BACE-1 inhibitors.

Schering-Plough Research Institute

Renin inhibitors containing conformationally restricted P1-P1' dipeptide mimetics.

Merck Sharp and Dohme Research Laboratories

 

Peptidomimetic inhibitors of human immunodeficiency virus protease (HIV-PR): Design, enzyme binding and selectivity, antiviral efficacy, and cell permeability properties

TBA

Direct renin inhibitors as a new therapy for hypertension.

Novartis Pharmaceuticals

Piperazine sulfonamide BACE1 inhibitors: design, synthesis, and in vivo characterization.

Merck Research Laboratories

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

Macrocyclic BACE-1 inhibitors acutely reduce Abeta in brain after po application.

Novartis Institutes For Biomedical Research

 

Novel pseudosymmetric inhibitors of HIV-1 protease

TBA

Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors.

Schering-Plough Research Institute

Cathepsin D inhibitors based on tasiamide B derivatives with cell membrane permeability.

Fudan University

Design and discovery of C2-fluoroalkyl iminothiazine dioxides as BACE inhibitors.

Merck

Synthesis of the Potent, Selective, and Efficacious ?-Secretase (BACE1) Inhibitor NB-360.

TBA

Discovery of Umibecestat (CNP520): A Potent, Selective, and Efficacious ?-Secretase (BACE1) Inhibitor for the Prevention of Alzheimer's Disease.

Novartis Pharma

Re-emerging Aspartic Protease Targets: Examining

Institute of Organic Chemistry and Biochemistry of The Czech Academy of Sciences

Discovery of Atabecestat (JNJ-54861911): A Thiazine-Based ?-Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor Advanced to the Phase 2b/3 EARLY Clinical Trial.

Janssen Research & Development

The development of a structurally distinct series of BACE1 inhibitors via the (Z)-fluoro-olefin amide bioisosteric replacement.

Amgen

Discovery of Orally Active Hydroxyethylamine Based SPPL2a Inhibitors.

Novartis Institutes For Biomedical Research

Plasmepsin Inhibitors in Antimalarial Drug Discovery: Medicinal Chemistry and Target Validation (2000 to Present).

University of Zambia

Discovery of AM-6494: A Potent and Orally Efficacious ?-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor with in Vivo Selectivity over BACE2.

TBA

Renin inhibitors containing a pyridyl amino diol derived C-terminus.

Hoechst

Specificity in the binding of inhibitors to the active site of human/primate aspartic proteinases: analysis of P2-P1-P1'-P2' variation.

University of Florida

Grassystatins D-F, Potent Aspartic Protease Inhibitors from Marine Cyanobacteria as Potential Antimetastatic Agents Targeting Invasive Breast Cancer.

University of Florida