PMID
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Article Title
Organization
Discovery of TAK-272: A Novel, Potent, and Orally Active Renin Inhibitor.

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

Charles River Discovery Research Services
Structure-based design of a new series of N-(piperidin-3-yl)pyrimidine-5-carboxamides as renin inhibitors.

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

University of Florida
Fragment-Linking Approach Using (19)F NMR Spectroscopy To Obtain Highly Potent and Selective Inhibitors ofß-Secretase.

Amgen
Fragment-Based Discovery of 2-Aminoquinazolin-4(3H)-ones As Novel Class Nonpeptidomimetic Inhibitors of the Plasmepsins I, II, and IV.

Latvian Institute of Organic Synthesis
Synthesis of (3S,4S)-4-aminopyrrolidine-3-ol derivatives and biological evaluation for their BACE1 inhibitory activities.

Korea University of Science and Technology
Transition state mimetics of the Plasmodium export element are potent inhibitors of Plasmepsin V from P. falciparum and P. vivax.

The Walter and Eliza Hall Institute of Medical Research
Preparation and biological evaluation of conformationally constrained BACE1 inhibitors.

Eli Lilly
Utilizing structures of CYP2D6 and BACE1 complexes to reduce risk of drug-drug interactions with a novel series of centrally efficacious BACE1 inhibitors.

The Scripps Research Institute
Discovery of a series of efficient, centrally efficacious BACE1 inhibitors through structure-based drug design.

Eurofarma Laboratorios
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
Development of 2-aminooxazoline 3-azaxanthenes as orally efficaciousß-secretase inhibitors for the potential treatment of Alzheimer's disease.

Amgen
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
Structure-based design, synthesis and biological evaluation of novelß-secretase inhibitors containing a pyrazole or thiazole moiety as the P3 ligand.

Purdue University
Discovery of potent iminoheterocycle BACE1 inhibitors.

Merck Research Laboratories
Inhibitors ofß-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
3-Cyano-3-aza-ß-amino Acid Derivatives as Inhibitors of Human Cysteine Cathepsins.

University of Bonn
Dose-dependent inhibition of BACE-1 by the monoterpenoid 2,3,4,4-tetramethyl-5-methylenecyclopent-2-enone in cellular and mouse models of Alzheimer's disease.

University of Coimbra
Plasmepsin inhibitory activity and structure-guided optimization of a potent hydroxyethylamine-based antimalarial hit.

Latvian Institute of Organic Synthesis
Discovery of 7-tetrahydropyran-2-yl chromans:ß-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors that reduce amyloidß-protein (Aß) in the central nervous system.

Array Biopharma
Novel BACE1 inhibitors with a non-acidic heterocycle at the P1' position.

Kyoto Pharmaceutical University
The thermodynamic basis for the use of lipophilic efficiency (LipE) in enthalpic optimizations.

Novartis Institutes For Biomedical Research
Discovery of cyclic sulfoxide hydroxyethylamines as potent and selectiveß-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure based design and in vivo reduction of amyloidß-peptides.

Novartis Pharma
Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: prime side chromane-containing inhibitors.

Elan Pharmaceuticals
Hydroxyethylamine-based inhibitors of BACE1: P1-P3 macrocyclization can improve potency, selectivity, and cell activity.

Amgen
Design and synthesis of thiophene dihydroisoquinolines as novel BACE1 inhibitors.

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

F. Hoffmann-La Roche
Spirocyclicß-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors: from hit to lowering of cerebrospinal fluid (CSF) amyloidß in a higher species.

Array Biopharma
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
Structure-based design of highly selectiveß-secretase inhibitors: synthesis, biological evaluation, and protein-ligand X-ray crystal structure.

Purdue University
Structure- and property-based design of aminooxazoline xanthenes as selective, orally efficacious, and CNS penetrable BACE inhibitors for the treatment of Alzheimer's disease.

Amgen
Design and synthesis of potent hydroxyethylamine (HEA) BACE-1 inhibitors carrying prime side 4,5,6,7-tetrahydrobenzazole and 4,5,6,7-tetrahydropyridinoazole templates.

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

TBA
Antiplasmodial activities of 4-aminoquinoline-statine compounds.

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

Fudan University
Synthesis and structure-activity relationship studies of 1,3-disubstituted 2-propanols as BACE-1 inhibitors.

University of South Florida
Discovery of cyclic sulfone hydroxyethylamines as potent and selectiveß-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure-based design and in vivo reduction of amyloidß-peptides.

Novartis Pharma
Structure guided P1' modifications of HEA derivedß-secretase inhibitors for the treatment of Alzheimer's disease.

Envoy Therapeutics
BACE-1 hydroxyethylamine inhibitors using novel edge-to-face interaction with Arg-296.

Glaxosmithkline
Di-substituted pyridinyl aminohydantoins as potent and highly selective human beta-secretase (BACE1) inhibitors.

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

University of Florida
Design and synthesis of cell potent BACE-1 inhibitors: structure-activity relationship of P1' substituents.

Elan Pharmaceuticals
Identification of 3-acetyl-2-aminoquinolin-4-one as a novel, nonpeptidic scaffold for specific calpain inhibitory activity.

Ewha Womans University
Synthesis, SAR, and X-ray structure of human BACE-1 inhibitors with cyclic urea derivatives.

Lg Life Sciences
Identification of acridinyl hydrazides as potent aspartic protease inhibitors.

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

Schering-Plough Research Institute
BACE-1 inhibitors part 1: identification of novel hydroxy ethylamines (HEAs).

Glaxosmithkline
Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1' substrate binding pocket.

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

Schering-Plough Research Institute
Synthesis of gallic acid based naphthophenone fatty acid amides as cathepsin D inhibitors.

Institute of Medicinal and Aromatic Plants
Incorporating molecular shape into the alignment-free Grid-Independent Descriptors.

Universitat Pompeu Fabra
Protease inhibitors: current status and future prospects.

University of Queensland
Non-peptide renin inhibitors containing 2-(((3-phenylpropyl)phosphoryl)oxy)alkanoic acid moieties as P2-P3 replacements.

E. Merck Darmstadt
Potent and selective inhibitors of an aspartyl protease-like endothelin converting enzyme identified in rat lung.

Abbott Laboratories
Specific inhibition of HIV-1 protease by boronated porphyrins.

University of California
Structure-activity relationships of a series of 2-amino-4-thiazole-containing renin inhibitors.

Parke-Davis Pharmaceutical Research Division of Warner-Lambert
Design and synthesis of potent, selective, and orally active fluorine-containing renin inhibitors.

Warner-Lambert
Renin inhibitors containing esters at the P2-position. Oral activity in a derivative of methyl aminomalonate.

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

Merck Sharp and Dohme Research Laboratories
Substrate analogue renin inhibitors containing replacements of histidine in P2 or isosteres of the amide bond between P3 and P2 sites.

E. Merck Darmstadt
Orally potent human renin inhibitors derived from angiotensinogen transition state: design, synthesis, and mode of interaction.

Kissei Pharmaceutical
Inhibition of cathepsin D by substrate analogues containing statine and by analogues of pepstatin.

TBA
Design and synthesis of a potent and specific renin inhibitor with a prolonged duration of action in vivo.

TBA
Design and synthesis of potent and specific renin inhibitors containing difluorostatine, difluorostatone, and related analogues.

TBA
Renin inhibitors. Syntheses of subnanomolar, competitive, transition-state analogue inhibitors containing a novel analogue of statine.

TBA
Difluorostatine- and difluorostatone-containing peptides as potent and specific renin inhibitors.

TBA
Synthesis and structure activity relationships of novel small molecule cathepsin D inhibitors.

Bayer
Identification of potent inhibitors of Plasmodium falciparum plasmepsin II from an encoded statine combinatorial library.

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

TBA
New benzimidazole derivatives as antiplasmodial agents and plasmepsin inhibitors: synthesis and analysis of structure-activity relationships.

University of Karachi
Discovery of pyrrolidine-basedß-secretase inhibitors: lead advancement through conformational design for maintenance of ligand binding efficiency.

Merck Research Laboratories
New pyrazolyl and thienyl aminohydantoins as potent BACE1 inhibitors: exploring the S2' region.

Pfizer
Structure based design, synthesis and SAR of cyclic hydroxyethylamine (HEA) BACE-1 inhibitors.

Novartis Institutes For Biomedical Research
Design and synthesis of potent macrocyclic renin inhibitors.

Medivir
Direct renin inhibitors as a new therapy for hypertension.

Novartis Pharmaceuticals
Triazolyl tryptoline derivatives asß-secretase inhibitors.

Mahidol University
Design and synthesis of aminohydantoins as potent and selective humanß-secretase (BACE1) inhibitors with enhanced brain permeability.

Pfizer
Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model.

Elan Pharmaceuticals
Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: structure-activity relationship of the aryl region.

Elan Pharmaceuticals
Fragment-based discovery and optimization of BACE1 inhibitors.

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

Merck Research Laboratories
Mechanism-based inhibitors of the aspartyl protease plasmepsin II as potential antimalarial agents.

Wayne State University
Novel pyrrolyl 2-aminopyridines as potent and selective human beta-secretase (BACE1) inhibitors.

Wyeth
Pyridinyl aminohydantoins as small molecule BACE1 inhibitors.

Wyeth Research
Structure-based design and synthesis of novel P2/P3 modified, non-peptidic beta-secretase (BACE-1) inhibitors.

University of Montreal
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
Synthesis of potent BACE-1 inhibitors incorporating a hydroxyethylene isostere as central core.

Link£Ping University
Design and synthesis of potent and selective BACE-1 inhibitors.

Stockholm University
Discovery of potent BACE-1 inhibitors containing a new hydroxyethylene (HE) scaffold: exploration of P1' alkoxy residues and an aminoethylene (AE) central core.

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

Novartis Institutes For Biomedical Research
Discovery and initial optimization of 5,5'-disubstituted aminohydantoins as potent beta-secretase (BACE1) inhibitors.

Wyeth Research
Design and synthesis of 5,5'-disubstituted aminohydantoins as potent and selective human beta-secretase (BACE1) inhibitors.

Wyeth Research
Aminoimidazoles as potent and selective human beta-secretase (BACE1) inhibitors.

Wyeth Research
Discovery of cyclic acylguanidines as highly potent and selective beta-site amyloid cleaving enzyme (BACE) inhibitors: Part I--inhibitor design and validation.

Schering-Plough Research Institute
alpha-Substituted norstatines as the transition-state mimic in inhibitors of multiple digestive vacuole malaria aspartic proteases.

Uppsala University
The P1N-isopropyl motif bearing hydroxyethylene dipeptide isostere analogues of aliskiren are in vitro potent inhibitors of the human aspartyl protease renin.

Nagasaki International University
Design and synthesis of BACE-1 inhibitors utilizing a tertiary hydroxyl motif as the transition state mimic.

Uppsala University
Macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors with activity in vivo.

Novartis Institutes For Biomedical Research
Synthesis of irreversible HIV-1 protease inhibitors containing sulfonamide and sulfone as amide bond isosteres

TBA
Novel low molecular renin inhibitors which show good oral blood pressure lowering effects in marmosets

TBA
Design, synthesis, and characterization of dipeptide isostere containing
cis-epoxide for the irreversible inactivation of HIV protease

TBA
Synthesis and structure-activity relationships of benzophenones as inhibitors of cathepsin D

TBA
Novel pseudosymmetric inhibitors of HIV-1 protease

TBA
2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects.

Abbott Laboratories
Harnessing nature's insight: design of aspartyl protease inhibitors from treatment of drug-resistant HIV to Alzheimer's disease.

Purdue University
Design, synthesis and SAR of potent statine-based BACE-1 inhibitors: exploration of P1 phenoxy and benzyloxy residues.

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

Schering-Plough Research Institute
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.

Ambrilia Biopharma
BACE-1 inhibitors part 2: identification of hydroxy ethylamines (HEAs) with reduced peptidic character.

Glaxosmithkline
Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1 and S3 substrate binding pockets.

Wyeth Research
Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors.

Merck Research Laboratories
Macrocyclic Peptidomimetic Plasmepsin X Inhibitors with Potent

Latvian Institute of Organic Synthesis
Potent and selective isophthalamide S2 hydroxyethylamine inhibitors of BACE1.

Pfizer
Synthesis and biological evaluation of phosphino dipeptide isostere inhibitor of human beta-secretase (BACE1).

Technische UniversitäT MüNchen
Discovery of quinazolin-4-one-based non-covalent inhibitors targeting the severe acute respiratory syndrome coronavirus 2 main protease (SARS-CoV-2 M

China Pharmaceutical University
Structure-guided design of direct-acting antivirals that exploit the gem-dimethyl effect and potently inhibit 3CL proteases of severe acute respiratory syndrome Coronavirus-2 (SARS-CoV-2) and middle east respiratory syndrome coronavirus (MERS-CoV).

Wichita State University
Design of potent inhibitors of human beta-secretase. Part 1.

Pfizer
Discovery of S-217622, a Noncovalent Oral SARS-CoV-2 3CL Protease Inhibitor Clinical Candidate for Treating COVID-19.

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

Fudan University
Synthesis of malarial plasmepsin inhibitors and prediction of binding modes by molecular dynamics simulations.

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

Merck
Design and synthesis of potent inhibitors of plasmepsin I and II: X-ray crystal structure of inhibitor in complex with plasmepsin II.

LinköPing University
Small molecules targeting γ-secretase and their potential biological applications.

Shenyang Pharmaceutical University
Sebetralstat (KVD900): A Potent and Selective Small Molecule Plasma Kallikrein Inhibitor Featuring a Novel P1 Group as a Potential Oral On-Demand Treatment for Hereditary Angioedema.

Kalvista Pharmaceuticals
Discovery and Characterization of Potent, Efficacious, Orally Available Antimalarial Plasmepsin X Inhibitors and Preclinical Safety Assessment of

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

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

Novartis Pharma
A Brain-Penetrant and Bioavailable Pyrazolopiperazine BACE1 Inhibitor Elicits Sustained Reduction of Amyloid β In Vivo.

Janssen Research & Development
Re-emerging Aspartic Protease Targets: Examining

Institute of Organic Chemistry and Biochemistry of The Czech Academy of Sciences
Discovery and Early Clinical Development of LY3202626, a Low-Dose, CNS-Penetrant BACE Inhibitor.

Lilly Research Laboratories
JNJ-67569762, A 2-Aminotetrahydropyridine-Based Selective BACE1 Inhibitor Targeting the S3 Pocket: From Discovery to Clinical Candidate.

Janssen Research & Development
Discovery of GLPG1972/S201086, a Potent, Selective, and Orally Bioavailable ADAMTS-5 Inhibitor for the Treatment of Osteoarthritis.

Galapagos
Rational design and synthesis of selective BACE-1 inhibitors.

Merck Research Laboratories
Discovery of Atabecestat (JNJ-54861911): A Thiazine-Based β-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
Identification and structure-activity relationship studies of small molecule inhibitors of the human cathepsin D.

Aten Porus Lifesciences
Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19.

Pfizer
Molecular dynamics and free energy analyses of cathepsin D-inhibitor interactions: insight into structure-based ligand design.

University of California
Discovery of Orally Active Hydroxyethylamine Based SPPL2a Inhibitors.

Novartis Institutes For Biomedical Research
Preparation and biological evaluation of BACE1 inhibitors: Leveraging trans-cyclopropyl moieties as ligand efficient conformational constraints.

Eli Lilly
Discovery of Fluoromethylketone-Based Peptidomimetics as Covalent ATG4B (Autophagin-1) Inhibitors.

Roche Pharma Research and Early Development
Potent, low-molecular-weight non-peptide inhibitors of malarial aspartyl protease plasmepsin II.

University of California
Evaluation of a structure-based statine cyclic diamino amide encoded combinatorial library against plasmepsin II and cathepsin D.

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

University of Zambia
Exploiting Structural Dynamics To Design Open-Flap Inhibitors of Malarial Aspartic Proteases.

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

TBA
New evolutions in the BACE1 inhibitor field from 2014 to 2018.

Janssen Research & Development
Peptidomimetic plasmepsin inhibitors with potent anti-malarial activity and selectivity against cathepsin D.

Latvian Institute of Organic Synthesis
Biomimetic Macrocyclic Inhibitors of Human Cathepsin D: Structure-Activity Relationship and Binding Mode Analysis.

Czech Academy of Sciences
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
SMall Molecule Growth 2001 (SMoG2001): an improved knowledge-based scoring function for protein-ligand interactions.

Harvard University
Discovery of Potent and Centrally Active 6-Substituted 5-Fluoro-1,3-dihydro-oxazine β-Secretase (BACE1) Inhibitors via Active Conformation Stabilization.

TBA
2-Aminoquinazolin-4(3H)-one based plasmepsin inhibitors with improved hydrophilicity and selectivity.

Latvian Institute of Organic Synthesis
Renin inhibitors. Dipeptide analogues of angiotensinogen incorporating transition-state, nonpeptidic replacements at the scissile bond.

Abbott Laboratories
Renin inhibitors. Design and synthesis of a new class of conformationally restricted analogues of angiotensinogen.

Abbott Laboratories
Synthesis and biological activity of some transition-state inhibitors of human renin.

Ciba-Geigy
Inhibition of porcine pepsin by two substrate analogues containing statine. The effect of histidine at the P2 subsite on the inhibition of aspartic proteinases.

University of Wisconsin
Rational Design of Novel 1,3-Oxazine Based β-Secretase (BACE1) Inhibitors: Incorporation of a Double Bond To Reduce P-gp Efflux Leading to Robust Aβ Reduction in the Brain.

TBA
Design and Synthesis of Clinical Candidate PF-06751979: A Potent, Brain Penetrant, β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor Lacking Hypopigmentation.

Pfizer
Izenamides A and B, Statine-Containing Depsipeptides, and an Analogue from a Marine Cyanobacterium.

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

University of Florida
New inhibitors of human renin that contain novel replacements at the P2 site.

Warner-Lambert
Aminomethyl-Derived Beta Secretase (BACE1) Inhibitors: Engaging Gly230 without an Anilide Functionality.

The Scripps Research Institute
Renin inhibitory pentols showing improved enteral bioavailability.

Hoechst
Renin inhibitors containing alpha-heteroatom amino acids as P2 residues.

Warner-Lambert
Causes and Significance of Increased Compound Potency in Cellular or Physiological Contexts.

Merck
Renin inhibitors containing new P1-P1' dipeptide mimetics with heterocycles in P1'.

E. Merck Darmstadt
Design, synthesis, and X-ray structural studies of BACE-1 inhibitors containing substituted 2-oxopiperazines as P1'-P2' ligands.

Purdue University
IRAK4 PROTACS

Astrazeneca
Phenothiazine derivatives and uses thereof

Camp4 Therapeutics
Pyridazinones as PARP7 inhibitors

Ribon Therapeutics
Compounds that interact with the Ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease

Shy Therapeutics
KDM1A inhibitors for the treatment of disease

Imago Biosciences
Phenylate derivative, preparation method therefor, and pharmaceutical composition and uses thereof

Institute of Materia Medica, Chinese Academy of Medical Sciences
Substituted pyrrolizine compounds and uses thereof

Gilead Sciences
Inhibiting agents for Bruton's tyrosine kinase

Biogen Ma
Factor IXa inhibitors

Merck Sharp & Dohme
Substituted pyridines as inhibitors of human immunodeficiency virus replication

Viiv Healthcare UK (NO.5)
N-substituted pyrazolo [3,4-D] pyrimidine ketone compound, and preparation process and use thereof

Sun Yat-Sen University
Rho kinase inhibitors and methods of use

H. Lee Moffitt Cancer Center and Research Institute
Inhibitors of lysine specific demethylase-1

Celgene Quanticel Research
Substituted benzene compounds

Epizyme
Inhibitors of lysine specific demethylase-1

Celgene Quanticel Research
Substituted piperazine compounds and methods of use thereof

Sunshine Lake Pharma
Heterocyclic compounds and methods of their use

Novartis
Quinazoline derivatives as kinases inhibitors and methods of use thereof

Teligene
Synthesis and preliminary biological assay of uridine glycoconjugate derivatives containing amide and/or 1,2,3-triazole linkers.

Silesian University of Technology
Key mutations alter the cytochrome P450 BM3 conformational landscape and remove inherent substrate bias.

University of Manchester
Serine/threonine kinase inhibitors

Array Biopharma
Heterocyclic derivative and pharmaceutical composition comprising the same

Shionogi
Triazolopyridine compounds

Novartis
Synthesis of Novel Hybrids Inspired from Bromopyrrole Alkaloids Inhibiting MMP-2 and -12 as Antineoplastic Agents.

University of Kwazulu-Nata
Cycloalkylnitrile pyrazole carboxamides as janus kinase inhibitors

Merck Sharp & Dohme
Hybrid cholinesterase inhibitors

Uniwersytet Warszawski
Galactoside inhibitors of galectins

Galecto Biotech
Dioxa-bicyclo[3.2.1]octane-2,3,4-triol derivatives

Pfizer
2,3,4,5-tetrahydro-benzo{B}{1,4}diazepine-comprising compounds of formula(III) for treating pain

Purde Pharma
3-substituted-2-(arlyalkyl)-1-azabicycloalkanes and methods of use thereof

Targacept
Interactive binding between the substrate and allosteric sites of carbamoyl-phosphate synthetase.

Pennsylvania State University
Indolequinone inhibitors of NRH:quinone oxidoreductase 2. Characterization of the mechanism of inhibition in both cell-free and cellular systems.

University of Colorado Denver
Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro.

Eli Lilly
Discovery of novel heterocyclic factor VIIa inhibitors.

Celera
Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and aromatase inhibitory activity of novel pyridine-containing isoflavones.

Ohio State University
1,7-annulated indolocarbazoles as cyclin-dependent kinase inhibitors.

Eli Lilly
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. Part 4: Heterocycles at C3.

Bristol-Myers Squibb
Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors.

Glaxosmithkline
Cyclic HIV-1 protease inhibitors derived from mannitol: synthesis, inhibitory potencies, and computational predictions of binding affinities.

Uppsala University
Stereospecific synthesis, structure-activity relationship, and oral bioavailability of tetrahydropyrimidin-2-one HIV protease inhibitors.

Dupont Pharmaceuticals