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PROTEASE INHIBITORS AND METHODS OF USE

US Patent US20240239772 (2024)

The Cleveland Clinic Foundation

10/30/24

2D 3D

PROTEASE INHIBITORS AND METHODS OF MAKING SAME

US Patent US20240228460 (2024)

Variational AI

10/22/24

2D 3D

SUBSTITUTED HYDANTOIN COMPOUNDS, METHODS FOR PREPARATION THEREOF AND USE THEREOF IN THE TREATMENT AND/OR PREVENTION OF A CORONA VIRUS DISEASE

US Patent US20240208970 (2024)

TBA

10/04/24

2D 3D

Saturated spirocyclics as antiviral agents

US Patent US11993600 (2024)

Enanta Pharmaceuticals, Inc.

08/29/24

2D 3D

NUCLEOSIDE ANALOG AND USE THEREOF

US Patent US20240166680 (2024)

SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

08/27/24

2D 3D

COMPOUNDS, COMPOSITIONS, AND METHODS OF USING THE SAME

US Patent US20240166598 (2024)

Arizona Board of Regents on Behalf of the University of Arizona; The Board of Trustees of the University of Illinois

08/26/24

2D 3D

Pyrrolidine Main Protease Inhibitors as Antiviral Agents

US Patent US20240158368 (2024)

Abbvie

08/19/24

2D 3D

INHIBITORS OF CYSTEINE PROTEASES

US Patent US20240150396 (2024)

Texas A&M University

08/09/24

2D 3D

ANTIVIRAL APPLICATION OF NUCLEOSIDE ANALOG OR COMBINATION FORMULATION CONTAINING NUCLEOSIDE ANALOG

US Patent US20240140975 (2024)

Shanghai Institute of Materia Medica, Chinese Academyof Sciences

07/25/24

2D 3D

COMPOSITIONS AND METHODS OF TREATING CONDITIONS

US Patent US20240131036 (2024)

The Uab Research Foundation

07/16/24

2D 3D

Inhibitors for coronavirus

US Patent US11963959 (2024)

Southwest Research Institute

07/12/24

2D 3D

SARS-COV2 MAIN PROTEASE INHIBITORS

US Patent US20240116946 (2024)

Gilead Sciences, Inc.

06/29/24

2D 3D

Non-Covalent Inhibitors of the Main Protease of SARS-CoV-2 and Methods of Use

US Patent US20240092759 (2024)

Yale University

06/04/24

2D 3D

COMPOSITIONS AND METHODS FOR INHIBITING M PRO PROTEASE ACTIVITY AND FOR PREVENTING AND TREATING SARS-COV-2 INFECTION

US Patent US20240083885 (2024)

Arizona Board Of Regents On Behalf Of The University Of Arizona

05/30/24

2D 3D

Spiropyrrolidine derived antiviral agents

US Patent US11912714 (2024)

Enanta Pharmaceuticals

05/03/24

2D 3D

Substituted phenyl ethynyl pyridine carboxamides as potent inhibitors of SARS virus

US Patent US11905306 (2024)

Southern Research Institute

04/24/24

2D 3D

Discovery of 3-phenyl-1,2,4-oxadiazole derivatives as a new class of SARS-CoV-2 main protease inhibitors.

Bioorg Med Chem Lett 86: (2023)

Sichuan University

04/22/24

2D 3D

Advances in research on 3C-like protease (3CL

RSC Med Chem 14: 9-21 (2023)

Huaqiao University

04/22/24

2D 3D

Insights into targeting SARS-CoV-2: design, synthesis,

RSC Med Chem 14: 899-920 (2023)

Egyptian Russian University

04/22/24

2D 3D

Design, synthesis and biological evaluation of covalent peptidomimetic 3CL protease inhibitors containing nitrile moiety.

Bioorg Med Chem 87: (2023)

An Hui University of Traditional Chinese Medicine

04/22/24

2D 3D

Design and synthesis of naturally-inspired SARS-CoV-2 inhibitors.

RSC Med Chem 14: 507-519 (2023)

Institut Pasteur

04/22/24

2D 3D

Easy access to ?-ketoamides as SARS-CoV-2 and MERS M

Eur J Med Chem 244: (2022)

University of Naples Federico Ii

04/21/24

2D 3D

Fight against novel coronavirus: A perspective of medicinal chemists.

Eur J Med Chem 201: (2020)

Jadavpur University

04/21/24

2D 3D

Rational design of the zonulin inhibitor AT1001 derivatives as potential anti SARS-CoV-2.

Eur J Med Chem 244: (2022)

European Biomedical Research Institute of Salerno (Ebris)

04/21/24

2D 3D

Potential treatment methods targeting 2019-nCoV infection.

Eur J Med Chem 205: (2020)

Southern Medical University

04/21/24

2D 3D

COVID-19 therapy: What weapons do we bring into battle?

Bioorg Med Chem 28: (2020)

Universidade De Pernambuco

04/19/24

2D 3D

Identification of Natural Products Inhibiting SARS-CoV-2 by Targeting Viral Proteases: A Combined in Silico and in Vitro Approach.

J Nat Prod 86: 264-275 (2023)

University of Vienna

04/19/24

2D 3D

Targeting SARS-CoV-2 Main Protease for Treatment of COVID-19: Covalent Inhibitors Structure-Activity Relationship Insights and Evolution Perspectives.

J Med Chem 65: 12500-12534 (2022)

University of Palermo

04/18/24

2D 3D

A review of the latest research on M

RSC Med Chem 12: 1026-1036 (2021)

Nantong University

04/18/24

2D 3D

The race to treat COVID-19: Potential therapeutic agents for the prevention and treatment of SARS-CoV-2.

Eur J Med Chem 213: (2021)

American University of Ras Al Khaimah

04/18/24

2D 3D

Design, synthesis, docking, and biochemical characterization of non-nucleoside SARS-CoV-2 RdRp inhibitors.

Bioorg Med Chem 80: (2023)

Istituto Italiano Di Tecnologia

04/18/24

2D 3D

COMPOUNDS FOR THE TREATMENT OF SARS

US Patent US20240043417 (2024)

Purdue Research Foundation

04/12/24

2D 3D

INHIBITORS OF POSITIVE STRAND RNA VIRUSES

US Patent US20240033256 (2024)

National Health Research Institutes

04/04/24

2D 3D

PYRAZOLO DERIVATIVES AS HUMAN DIHYDROOROTATE DEHYDROGENASE (HDHODH) INHIBITORS FOR USE AS ANTIVIRALS

US Patent US20240034730 (2024)

Drug Discovery and Clinic

04/04/24

2D 3D

COMPOUNDS AND METHODS FOR TREATING VIRAL INFECTIONS

US Patent US20240016777 (2024)

Beth Israel Deaconess Medical Center

03/12/24

2D 3D

Alkyne-containing antiviral agents

US Patent US11858945 (2024)

Enanta Pharmaceuticals

02/22/24

2D 3D

RNA VIRUS INHIBITOR COMPOUNDS WITH IMPROVED METABOLIC STABILITY AND USES THEREOF

US Patent US20230399296 (2023)

The Governors of The University of Alberta

02/03/24

2D 3D

3-TETRAZOLYLMETHYL-1,3,5-TRIAZIN-2,4-DIONE COMPOUND INHIBITING CORONAVIRUS 3CL PROTEASE ACTIVITY AND PREPARATION METHOD AND USE THEREOF

US Patent US20230391736 (2023)

Shaanxi Panlong Pharmaceutical Co.

01/28/24

2D 3D

Compounds for the treatment of SARS

US Patent US11795159 (2023)

Purdue Research Foundation

12/05/23

2D 3D

Compounds and pharmaceutical uses thereof

US Patent US11793823 (2023)

SyneuRx International (Taiwan)

12/05/23

2D 3D

NOVEL SPIROPYRROLIDINE DERIVED ANTIVIRAL AGENTS

US Patent US20230331734 (2023)

Enanta Pharmaceuticals

12/01/23

2D 3D

Open science discovery of potent noncovalent SARS-CoV-2 main protease inhibitors.

Science 382: (2023)

Cornell University

11/27/23

2D 3D

RING-MODIFIED PROLINE SHORT PEPTIDE COMPOUND AND USE THEREOF

US Patent US20230312571 (2023)

Fujian Akeylink Biotechnology

11/13/23

2D 3D

Protease inhibitors as antivirals

US Patent US11753373 (2023)

Acea Therapeutics

10/20/23

2D 3D

SARS-CoV-2 inhibitors for treating coronavirus infections

US Patent US11731944 (2023)

Insilico Medicine Ip

09/26/23

2D 3D

Enzyme inhibition as a potential therapeutic strategy to treat COVID-19 infection.

Bioorg Med Chem 48: (2021)

Kingston University

06/26/23

2D 3D

Penicillin Derivatives Inhibit the SARS-CoV-2 Main Protease by Reaction with Its Nucleophilic Cysteine.

J Med Chem 65: 7682-7696 (2022)

University of Oxford

06/25/23

2D 3D

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

J Med Chem 65: 6499-6512 (2022)

Shionogi

06/25/23

2D 3D

Structure-Guided Design of Potent Spirocyclic Inhibitors of Severe Acute Respiratory Syndrome Coronavirus-2 3C-like Protease.

J Med Chem 65: 7818-7832 (2022)

Wichita State University

06/25/23

2D 3D

The Alpha Keto Amide Moiety as a Privileged Motif in Medicinal Chemistry: Current Insights and Emerging Opportunities.

J Med Chem 64: 3508-3545 (2021)

Niddk

06/24/23

2D 3D

Bisubstrate Inhibitors of Severe Acute Respiratory Syndrome Coronavirus-2 Nsp14 Methyltransferase.

ACS Med Chem Lett 13: 1477-1484 (2022)

University of Minnesota

06/24/23

2D 3D

Expedited Approach toward the Rational Design of Noncovalent SARS-CoV-2 Main Protease Inhibitors.

J Med Chem 65: 2848-2865 (2022)

The University of Arizona

06/24/23

2D 3D

Discovery and Crystallographic Studies of Nonpeptidic Piperazine Derivatives as Covalent SARS-CoV-2 Main Protease Inhibitors.

J Med Chem 65: 16902-16917 (2022)

Shandong University

06/24/23

2D 3D

Novel Coronavirus Main Protease Di- and Tripeptide Inhibitors for Treating COVID-19.

ACS Med Chem Lett 13: 1388-1389 (2022)

Experimental Drug Development Centre

06/24/23

2D 3D

Structure-Based Design of a Dual-Targeted Covalent Inhibitor Against Papain-like and Main Proteases of SARS-CoV-2.

J Med Chem 65: 16252-16267 (2022)

China Pharmaceutical University

06/24/23

2D 3D

In silico screening-based discovery of novel covalent inhibitors of the SARS-CoV-2 3CL protease.

Eur J Med Chem 231: (2022)

Shanghai Institute of Materia Medica

06/24/23

2D 3D

Discovery of 9,10-dihydrophenanthrene derivatives as SARS-CoV-2 3CL

Eur J Med Chem 228: (2022)

Shanghai University of Traditional Chinese Medicine

06/24/23

2D 3D

Identification of Aloe-derived natural products as prospective lead scaffolds for SARS-CoV-2 main protease (M

Bioorg Med Chem Lett 66: (2022)

University of Colorado

06/23/23

2D 3D

Discovery of 2-(furan-2-ylmethylene)hydrazine-1-carbothioamide derivatives as novel inhibitors of SARS-CoV-2 main protease.

Eur J Med Chem 238: (2022)

Peking University

06/23/23

2D 3D

The Natural Products Withaferin A and Withanone from the Medicinal Herb

J Nat Prod 85: 2340-2350 (2022)

Shiv Nadar University

06/23/23

2D 3D

Main protease mutants of SARS-CoV-2 variants remain susceptible to nirmatrelvir.

Bioorg Med Chem Lett 62: (2022)

Australian National University

06/23/23

2D 3D

Discovery of highly potent SARS-CoV-2 M

Bioorg Med Chem Lett 58: (2022)

Nanjing University of Chinese Medicine

06/23/23

2D 3D

Evolutionary and Structural Insights about Potential SARS-CoV-2 Evasion of Nirmatrelvir.

J Med Chem 65: 8686-8698 (2022)

Texas A&M University

06/23/23

2D 3D

A Warhead Substitution Study on the Coronavirus Main Protease Inhibitor Nirmatrelvir.

ACS Med Chem Lett 13: 1345-1350 (2022)

Experimental Drug Development Centre

06/23/23

2D 3D

Targeting SARS-CoV-2 Proteases and Polymerase for COVID-19 Treatment: State of the Art and Future Opportunities.

J Med Chem 65: 2716-2746 (2022)

University of Naples "Federico Ii

06/22/23

2D 3D

Novel Halomethylketone Azadipeptides for Treating COVID-19.

ACS Med Chem Lett 13: 875-876 (2022)

A*Star

06/22/23

2D 3D

Small-Molecule Thioesters as SARS-CoV-2 Main Protease Inhibitors: Enzyme Inhibition, Structure-Activity Relationships, Antiviral Activity, and X-ray Structure Determination.

J Med Chem 65: 9376-9395 (2022)

Eberhard Karls University T£Bingen

06/22/23

2D 3D

Kinases as Potential Therapeutic Targets for Anti-coronaviral Therapy.

J Med Chem 65: 955-982 (2022)

Eberhard Karls University T£Bingen

06/22/23

2D 3D

Target-Based Virtual Screening and LC/MS-Guided Isolation Procedure for Identifying Phloroglucinol-Terpenoid Inhibitors of SARS-CoV-2.

J Nat Prod 85: 327-336 (2022)

Kunming Institute of Botany

06/22/23

2D 3D

Progress and Challenges in Targeting the SARS-CoV-2 Papain-like Protease.

J Med Chem 65: 7561-7580 (2022)

The State University of New Jersey

06/22/23

2D 3D

Discovery of 2-Phenylquinolines with Broad-Spectrum Anti-coronavirus Activity.

ACS Med Chem Lett 13: 855-864 (2022)

University of Perugia

06/22/23

2D 3D

The structure-based design of peptidomimetic inhibitors against SARS-CoV-2 3C like protease as Potent anti-viral drug candidate.

Eur J Med Chem 238: (2022)

Nankai University

06/22/23

2D 3D

Tuaimenal A, a Meroterpene from the Irish Deep-Sea Soft Coral

J Nat Prod 85: 1315-1323 (2022)

University of South Florida

06/21/23

2D 3D

Oral Nonpeptidic, Noncovalent Triazine Coronavirus Main Protease Inhibitors for Treating COVID-19.

ACS Med Chem Lett 13: 1394-1396 (2022)

Experimental Drug Development Centre

06/21/23

2D 3D

Peptidomimetic nitrile warheads as SARS-CoV-2 3CL protease inhibitors.

RSC Med Chem 12: 1722-1730 (2021)

University of Alberta Edmonton

06/21/23

2D 3D

Chemo- and Site-Selective Lysine Modification of Peptides and Proteins under Native Conditions Using the Water-Soluble Zolinium.

J Med Chem 65: 11840-11853 (2022)

Chinese Academy of Sciences

06/21/23

2D 3D

Aspulvins A-H, Aspulvinone Analogues with SARS-CoV-2 M

J Nat Prod 85: 878-887 (2022)

Yunnan University

06/21/23

2D 3D

Discovery of potent benzoxaborole inhibitors against SARS-CoV-2 main and dengue virus proteases.

Eur J Med Chem 240: (2022)

Heidelberg University

06/20/23

2D 3D

Discovery of Chlorofluoroacetamide-Based Covalent Inhibitors for Severe Acute Respiratory Syndrome Coronavirus 2 3CL Protease.

J Med Chem 65: 13852-13865 (2022)

Kyushu University

06/20/23

2D 3D

Diastereomeric Resolution Yields Highly Potent Inhibitor of SARS-CoV-2 Main Protease.

J Med Chem 65: 13328-13342 (2022)

Bio-Techne (Tocris)

06/20/23

2D 3D

Discovery of 2-thiobenzimidazoles as noncovalent inhibitors of SARS-CoV-2 main protease.

Bioorg Med Chem Lett 72: (2022)

New York University Abu Dhabi

06/20/23

2D 3D

A multi-pronged evaluation of aldehyde-based tripeptidyl main protease inhibitors as SARS-CoV-2 antivirals.

Eur J Med Chem 240: (2022)

Texas A&M University

06/20/23

2D 3D

A systematic exploration of boceprevir-based main protease inhibitors as SARS-CoV-2 antivirals.

Eur J Med Chem 240: (2022)

Texas A&M University

06/20/23

2D 3D

Advanced approaches of developing targeted covalent drugs.

RSC Med Chem 13: 1460-1475 (2022)

College of Pharmacy

06/19/23

2D 3D

Chalcone-amide, a privileged backbone for the design and development of selective SARS-CoV/SARS-CoV-2 papain-like protease inhibitors.

Eur J Med Chem 240: (2022)

Mazandaran University of Medical Sciences

06/19/23

2D 3D

Protease targeted COVID-19 drug discovery and its challenges: Insight into viral main protease (Mpro) and papain-like protease (PLpro) inhibitors.

Bioorg Med Chem 29: (2021)

Jadavpur University

06/18/23

2D 3D

Discovery and Crystallographic Studies of Trisubstituted Piperazine Derivatives as Non-Covalent SARS-CoV-2 Main Protease Inhibitors with High Target Specificity and Low Toxicity.

J Med Chem 65: 13343-13364 (2022)

Shandong University

06/18/23

2D 3D

Two Binding Sites of SARS-CoV-2 Macrodomain 3 Probed by Oxaprozin and Meclomen.

J Med Chem 65: 15227-15237 (2022)

University of Science and Technology of China

06/18/23

2D 3D

Natural Products with Potential to Treat RNA Virus Pathogens Including SARS-CoV-2.

J Nat Prod 84: 161-182 (2021)

University of California San Diego

06/18/23

2D 3D

Anti-SARS-CoV-2 Activity of

J Nat Prod 84: 1261-1270 (2021)

Mahidol University

06/18/23

2D 3D

3-triazolyl methyl-1,3,5-triazine-2,4-dione compounds and preparation method and application thereof

US Patent US11612603 (2023)

Shaanxi Panlong Pharmaceutical

05/09/23

2D 3D

Protacs targeting coronavirus 3CL protease and preparation method and application thereof

US Patent US11530195 (2022)

Shaanxi Panlong Pharmaceutical

02/16/23

2D 3D

Inhibitors of cysteine proteases and methods of use thereof

US Patent US11524940 (2022)

Pardes Biosciences

02/12/23

2D 3D

Protacs based on VHL ligand targeting coronavirus 3CL protease and preparation method and application thereof

US Patent US11518759 (2022)

Shaanxi Panlong Pharmaceutical

02/05/23

2D 3D

ETHER-LINKED ANTIVIRAL COMPOUNDS

WIPO WO2022208262 (2022)

Pfizer

01/31/23

2D 3D

COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF CORONAVIRAL RELATED DISEASES

WIPO WO2022224223 (2022)

Novartis

01/31/23

2D 3D

CORONAVIRUS MAIN PROTEASE INHIBITORS AND METHODS USING SAME

WIPO WO2023004291 (2023)

Baylor College of Medicine

01/31/23

2D 3D

Inhibitors of cysteine proteases and methods of use thereof

US Patent US11472793 (2022)

Pardes Biosciences

12/24/22

2D 3D

Spiropyrrolidine derived antiviral agents

US Patent US11384090 (2022)

Enanta Pharmaceuticals

10/09/22

2D 3D

SARS-COV-2 MPRO INHIBITOR COMPOUNDS

WIPO WO2022129953 (2022)

Heptares Therapeutics

10/05/22

2D 3D

Functionalized peptides as antiviral agents

US Patent US11358953 (2022)

Enanta Pharmaceuticals

09/19/22

2D 3D

Spiropyrrolidine derived antiviral agents

US Patent US11352363 (2022)

Enanta Pharmaceuticals

09/11/22

2D 3D

Nitrile-containing antiviral compounds

US Patent US11351149 (2022)

Pfizer

09/10/22

2D 3D

Spiropyrrolidine derived antiviral agents

US Patent US11339170 (2022)

Enanta Pharmaceuticals

08/29/22

2D 3D

Discovery and optimization of 2-((1H-indol-3-yl)thio)-N-benzyl-acetamides as novel SARS-CoV-2 RdRp inhibitors.

Eur J Med Chem 223: (2021)

Chinese Academy of Medical Science and Peking Union Medical College

08/23/22

2D 3D

Promising anti-SARS-CoV-2 drugs by effective dual targeting against the viral and host proteases.

Bioorg Med Chem Lett 43: (2021)

Bristol University

08/20/22

2D 3D

Discovery and structural optimization of 3-O-?-chacotriosyl oleanane-type triterpenoids as potent entry inhibitors of SARS-CoV-2 virus infections.

Eur J Med Chem 215: (2021)

South China Agricultural University

08/19/22

2D 3D

Challenges of short substrate analogues as SARS-CoV-2 main protease inhibitors.

Bioorg Med Chem Lett 50: (2021)

Australian National University

08/19/22

2D 3D

Spiropyrrolidine derived antiviral agents

US Patent US11325916 (2022)

Enanta Pharmaceuticals

08/15/22

2D 3D

Inhibitors of cysteine proteases and methods of use thereof

US Patent US11312704 (2022)

Pardes Biosciences

08/06/22

2D 3D

ANTIVIRAL HETEROARYL KETONE DERIVATIVES

WIPO WO2022013684 (2022)

Pfizer

06/09/22

2D 3D

NOVEL CORONAVIRUS MAIN PROTEASE INHIBITOR, AND PREPARATION METHOD THEREFOR AND USE THEREOF

WIPO WO2022021841 (2022)

Sichuan University

06/09/22

2D 3D

PHOSPHOLIPID COMPOUNDS AND USES THEREOF

WIPO WO2022081973 (2022)

Gilead Sciences

05/24/22

2D 3D

Potent Inhibition of SARS-CoV-2 nsp14

J Med Chem 65: 6231-6249 (2022)

University of Montpellier

05/17/22

2D 3D

A TMPRSS2 inhibitor acts as a pan-SARS-CoV-2 prophylactic and therapeutic.

Nature (2022)

University of British Columbia

03/30/22

2D 3D

Aminocarbamoyl compounds for the treatment of viral infections

WIPO WO2022043374 (2022)

F. Hoffmann-La Roche

03/30/22

2D 3D

Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2).

J Med Chem 63: 13205-13227 (2020)

South China Agricultural University

03/27/22

2D 3D

Druggable targets from coronaviruses for designing new antiviral drugs.

Bioorg Med Chem 28: (2020)

Federal University of Alagoas

03/27/22

2D 3D

Substituted nucleosides, nucleotides and analogs thereof

US Patent US11149049 (2021)

Janssen Biopharma

03/13/22

2D 3D

 

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

bioRxiv 2022: (2022)

Shionogi

02/02/22

2D 3D

Perspectives on SARS-CoV-2 Main Protease Inhibitors.

J Med Chem 64: 16922-16955 (2021)

Michigan State University

01/27/22

2D 3D

Sars-cov-2 inhibitors having covalent modifications for treating coronavirus infections

WIPO WO2021219089 (2021)

Insilico Medicine Ip

01/27/22

2D 3D

Inhibitors of cysteine proteases and methods of use thereof

US Patent US11124497 (2021)

Pardes Biosciences

01/13/22

2D 3D

Nitrile-containing antiviral compounds

WIPO WO2021250648 (2021)

Pfizer

01/13/22

2D 3D

Compounds and method of treating covid-19

WIPO WO2021205290 (2021)

Pfizer

01/13/22

2D 3D

Compounds and methods for the treatment of covid-19

WIPO WO2021205298 (2021)

Pfizer

01/13/22

2D 3D

Discovery of Di- and Trihaloacetamides as Covalent SARS-CoV-2 Main Protease Inhibitors with High Target Specificity.

J Am Chem Soc 143: 20697-20709 (2021)

The University of Arizona

01/13/22

2D 3D

Design of SARS-CoV-2 PLpro Inhibitors for COVID-19 Antiviral Therapy Leveraging Binding Cooperativity.

J Med Chem (2021)

University of Illinois At Chicago

11/05/21

2D 3D

Indole Chloropyridinyl Ester-Derived SARS-CoV-2 3CLpro Inhibitors: Enzyme Inhibition, Antiviral Efficacy, Structure-Activity Relationship, and X-ray Structural Studies.

J Med Chem 64: 14702-14714 (2021)

Purdue University

11/05/21

2D 3D

 

An oral SARS-CoV-2 Mpro inhibitor clinical candidate for the treatment of COVID-19

Science 374: 1-13 (2021)

Pfizer

11/05/21

2D 3D

A patent review on SARS coronavirus main protease (3CLpro) inhibitors.

ChemMedChem (2021)

Experimental Drug Development Centre

11/05/21

2D 3D

 

Open Science Discovery of Oral Non-Covalent SARS-CoV-2 Main Protease Inhibitor Therapeutics

bioRxiv 2021: (2021)

Israel Institution of Biological Research

11/05/21

2D 3D

DNA-encoded chemistry technology yields expedient access to SARS-CoV-2 M

Proc Natl Acad Sci U S A 118: (2021)

Baylor College of Medicine

09/11/21

2D 3D

Optimization of Triarylpyridinone Inhibitors of the Main Protease of SARS-CoV-2 to Low-Nanomolar Antiviral Potency.

ACS Med Chem Lett 12: 1325-1332 (2021)

Yale University

09/10/21

2D 3D

Rational Design of Hybrid SARS-CoV-2 Main Protease Inhibitors Guided by the Superimposed Cocrystal Structures with the Peptidomimetic Inhibitors GC-376, Telaprevir, and Boceprevir.

ACS Pharmacol Transl Sci 4: 1408-1421 (2021)

The University of Arizona

09/10/21

2D 3D

Structure-Based Optimization of ML300-Derived, Noncovalent Inhibitors Targeting the Severe Acute Respiratory Syndrome Coronavirus 3CL Protease (SARS-CoV-2 3CL

J Med Chem 65: 2880-2904 (2021)

Cleveland Clinic

08/14/21

2D 3D

Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-?-lactamases.

J Med Chem 63: 7491-7507 (2020)

Qpex Biopharma

08/13/21

2D 3D

A head-to-head comparison of the inhibitory activities of 15 peptidomimetic SARS-CoV-2 3CLpro inhibitors.

Bioorg Med Chem Lett 48: 128263 (2021)

A*Star

07/29/21

2D 3D

Structure-Guided Design of Conformationally Constrained Cyclohexane Inhibitors of Severe Acute Respiratory Syndrome Coronavirus-2 3CL Protease.

J Med Chem 64: 10047-10058 (2021)

Wichita State University

07/29/21

2D 3D

Peptidomimetic ?-Acyloxymethylketone Warheads with Six-Membered Lactam P1 Glutamine Mimic: SARS-CoV-2 3CL Protease Inhibition, Coronavirus Antiviral Activity, and

J Med Chem (2021)

University of Alberta

07/29/21

2D 3D

Highly active compounds against COVID-19

US Patent US10874687 (2020)

Atea Pharmaceuticals

07/25/21

2D 3D

N4-hydroxycytidine and derivatives and anti-viral uses related thereto

US Patent US10874683 (2020)

Emory University

07/25/21

2D 3D

SARS-CoV-2 Mpro inhibitors with antiviral activity in a transgenic mouse model

Science (2021)

Sichuan University

02/28/21

2D 3D

 

Potent Noncovalent Inhibitors of the Main Protease of SARS-CoV-2 from Molecular Sculpting of the Drug Perampanel Guided by Free Energy Perturbation Calculations

ACS Cent Sci (2021)

Yale University

02/28/21

2D 3D

Identification and design of novel small molecule inhibitors against MERS-CoV papain-like protease via high-throughput screening and molecular modeling.

Bioorg Med Chem 27: 1981-1989 (2019)

University of Illinois At Chicago

02/24/21

2D 3D

The Other Angiotensin II Receptor: AT

J Med Chem 63: 1978-1995 (2020)

Centre Hospitalier Universitaire Vaudois (Chuv) and University of Lausanne (Unil

02/21/21

2D 3D

 

Identification of inhibitors of SARS-CoV-2 3CL-Pro enzymatic activity using a small molecule in-vitro repurposing screen

bioRxiv 2020: (2020)

Fraunhofer Institute For Translational Medicine and Pharmacology (Itmp) and Fraunhofer Cluster of Excellence For Immune Mediated Diseases (Cimd

01/31/21

2D 3D

A Quick Route to Multiple Highly Potent SARS-CoV-2 Main Protease Inhibitors

ChemMedChem (2020)

Texas A&M University

01/31/21

2D 3D

Anticoronaviral compounds and compositions, their pharmaceutical uses and materials for their synthesis

WIPO WO2006061714 (2006)

Pfizer

01/31/21

2D 3D

 

Inhibition of SARS-CoV-2 main protease by allosteric drug-binding

bioRxiv 2020: (2020)

Center For Free-Electron Laser Science

01/31/21

2D 3D

An orally bioavailable broad-spectrum antiviral inhibits SARS-CoV-2 in human airway epithelial cell cultures and multiple coronaviruses in mice.

Sci Transl Med 12: 1-15 (2020)

University of North Carolina At Chapel Hill

11/13/20

2D 3D

Identification of Antiviral Drug Candidates against SARS-CoV-2 from FDA-Approved Drugs.

Antimicrob Agents Chemother 64: (2020)

Institut Pasteur Korea

11/13/20

2D 3D

The recent outbreaks of human coronaviruses: A medicinal chemistry perspective.

Med Res Rev (2020)

University of Bonn

11/07/20

2D 3D

An Overview of Severe Acute Respiratory Syndrome-Coronavirus (SARS-CoV) 3CL Protease Inhibitors: Peptidomimetics and Small Molecule Chemotherapy.

J Med Chem 59: 6595-628 (2016)

University of Bonn

11/07/20

2D 3D

Anticoronviral compounds and compositions, their pharmaceutical uses and materials for their synthesis

WIPO WO2005113580 (2005)

Pfizer

10/17/20

2D 3D

Broad-spectrum non-covalent coronavirus protease inhibitors

US Patent US9975885 (2018)

Purdue Research Foundation

09/25/20

2D 3D

Identification of SARS-CoV-2 3CL Protease Inhibitors by a Quantitative High-throughput Screening.

bioRxiv (2020)

National Institutes of Health

09/21/20

2D 3D

Discovery of a Novel Inhibitor of Coronavirus 3CL Protease as a Clinical Candidate for the Potential Treatment of COVID-19.

bioRxiv (2020)

Pfizer

09/21/20

2D 3D

 

Discovery of potent inhibitors of PLproCoV2 by screening a library of selenium-containing compounds

bioRxiv 1-12 (2020)

University Ofamsterdam

09/21/20

2D 3D

Crystal structure of SARS-CoV-2 main protease provides a basis for design of improved ?-ketoamide inhibitors.

Science 368: 409-412 (2020)

University of Lubeck

09/21/20

2D 3D

Structure-based design of antiviral drug candidates targeting the SARS-CoV-2 main protease.

Science 368: 1331-1335 (2020)

Shanghai Institute of Materia Medica

09/21/20

2D 3D

Characterization and Noncovalent Inhibition of the Deubiquitinase and deISGylase Activity of SARS-CoV-2 Papain-Like Protease.

ACS Infect Dis 6: 2099-2109 (2020)

University of Georgia

09/21/20

2D 3D

The androgen-regulated protease TMPRSS2 activates a proteolytic cascade involving components of the tumor microenvironment and promotes prostate cancer metastasis.

Cancer Discov 4: 1310-25 (2014)

Fred Hutchinson Cancer Research Center

09/21/20

2D 3D

Screening of drugs by FRET analysis identifies inhibitors of SARS-CoV 3CL protease.

Biochem Biophys Res Commun 333: 194-9 (2005)

National Taiwan University

09/21/20

2D 3D

3C-like protease inhibitors block coronavirus replication in vitro and improve survival in MERS-CoV-infected mice.

Sci Transl Med 12: (2020)

Wichita State University

09/06/20

2D 3D

Structure of Mpro from SARS-CoV-2 and discovery of its inhibitors

Nature 582: 289-293 (2020)

Shanghaitech University

09/06/20

2D 3D

Synthesis, modification and docking studies of 5-sulfonyl isatin derivatives as SARS-CoV 3C-like protease inhibitors.

Bioorg Med Chem 22: 292-302 (2014)

Tianjin University of Science and Technology

09/02/20

2D 3D

Identification of novel drug scaffolds for inhibition of SARS-CoV 3-Chymotrypsin-like protease using virtual and high-throughput screenings.

Bioorg Med Chem 22: 167-77 (2014)

University of Illinois At Chicago

09/02/20

2D 3D

Dieckol, a SARS-CoV 3CL(pro) inhibitor, isolated from the edible brown algae Ecklonia cava.

Bioorg Med Chem 21: 3730-7 (2013)

Korea Research Institute of Bioscience and Biotechnology

09/01/20

2D 3D

Design, synthesis, and bioevaluation of viral 3C and 3C-like protease inhibitors.

Bioorg Med Chem Lett 23: 6317-20 (2013)

Kansas State University

09/01/20

2D 3D

Design, synthesis and crystallographic analysis of nitrile-based broad-spectrum peptidomimetic inhibitors for coronavirus 3C-like proteases.

Eur J Med Chem 59: 1-6 (2013)

The Chinese University of Hong Kong

08/31/20

2D 3D

Synthesis and evaluation of pyrazolone compounds as SARS-coronavirus 3C-like protease inhibitors.

Bioorg Med Chem 18: 7849-54 (2010)

Academia Sinica

08/28/20

2D 3D

Biflavonoids from Torreya nucifera displaying SARS-CoV 3CL(pro) inhibition.

Bioorg Med Chem 18: 7940-7 (2010)

Korea Research Institute of Bioscience and Biotechnology

08/28/20

2D 3D

SARS-CoV 3CLpro inhibitory effects of quinone-methide triterpenes from Tripterygium regelii.

Bioorg Med Chem Lett 20: 1873-6 (2010)

Korea Research Institute of Bioscience and Biotechnology

08/27/20

2D 3D

Quantitative high-throughput screening identifies inhibitors of anthrax-induced cell death.

Bioorg Med Chem 17: 5139-45 (2009)

National Human Genome Research Institute

08/27/20

2D 3D

New developments for the design, synthesis and biological evaluation of potent SARS-CoV 3CL(pro) inhibitors.

Bioorg Med Chem Lett 19: 2722-7 (2009)

Kyoto Pharmaceutical University

08/27/20

2D 3D

Novel small-molecule inhibitors of transmissible gastroenteritis virus.

Antimicrob Agents Chemother 51: 3924-31 (2007)

National Health Research Institute

08/27/20

2D 3D

Structure-based design, synthesis, and biological evaluation of peptidomimetic SARS-CoV 3CLpro inhibitors.

Bioorg Med Chem Lett 17: 5876-80 (2007)

Purdue University

08/24/20

2D 3D

Structure-guided design of potent and permeable inhibitors of MERS coronavirus 3CL protease that utilize a piperidine moiety as a novel design element.

Eur J Med Chem 150: 334-346 (2018)

Wichita State University

08/16/20

2D 3D

Identification, synthesis and evaluation of SARS-CoV and MERS-CoV 3C-like protease inhibitors.

Bioorg Med Chem 24: 3035-3042 (2016)

Academia Sinica

09/14/17

2D 3D

Phenolic phytochemical displaying SARS-CoV papain-like protease inhibition from the seeds of Psoralea corylifolia.

J Enzyme Inhib Med Chem 29: 59-63 (2014)

Gyeongsang National University

08/28/17

2D 3D

Inhibitor recognition specificity of MERS-CoV papain-like protease may differ from that of SARS-CoV.

ACS Chem Biol 10: 1456-65 (2015)

University of Illinois At Chicago

10/15/15

2D 3D

Imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, substrate-dependent modulators of insulin-degrading enzyme in amyloid-ß hydrolysis.

Eur J Med Chem 79: 184-93 (2014)

University of Lille

02/07/15

2D 3D

Thiol-based angiotensin-converting enzyme 2 inhibitors: P1 modifications for the exploration of the S1 subsite.

Bioorg Med Chem Lett 18: 732-7 (2008)

Glaxosmithkline

05/21/13

2D 3D

Tanshinones as selective and slow-binding inhibitors for SARS-CoV cysteine proteases.

Bioorg Med Chem 20: 5928-35 (2012)

Korea Research Institute of Bioscience and Biotechnology

05/17/13

2D 3D

Structural basis of inhibition specificities of 3C and 3C-like proteases by zinc-coordinating and peptidomimetic compounds.

J Biol Chem 284: 7646-55 (2009)

National Yang-Ming University

10/29/12

2D 3D

Development of substrate analogue inhibitors for the human airway trypsin-like protease HAT.

Bioorg Med Chem Lett 21: 4860-4 (2011)

Philipps University Marburg

03/23/12

2D 3D

Virtual screening identification of novel severe acute respiratory syndrome 3C-like protease inhibitors and in vitro confirmation.

Bioorg Med Chem Lett 21: 3088-91 (2011)

Chonnam National University

12/04/11

2D 3D

Stable benzotriazole esters as mechanism-based inactivators of the severe acute respiratory syndrome 3CL protease.

Chem Biol 13: 261-8 (2006)

Academia Sinica

07/07/11

2D 3D

Phage-encoded combinatorial chemical libraries based on bicyclic peptides.

Nat Chem Biol 5: 502-7 (2009)

Laboratory of Molecular Biology, Medical Research Council

06/10/11

2D 3D

Investigation of the pharmacophore space of Severe Acute Respiratory Syndrome coronavirus (SARS-CoV) NTPase/helicase by dihydroxychromone derivatives.

Bioorg Med Chem Lett 19: 4538-41 (2009)

Konkuk University

08/27/10

2D 3D

Aryl diketoacids (ADK) selectively inhibit duplex DNA-unwinding activity of SARS coronavirus NTPase/helicase.

Bioorg Med Chem Lett 19: 1636-8 (2009)

Konkuk University

01/11/10

2D 3D

Thiol-based angiotensin-converting enzyme 2 inhibitors: P1' modifications for the exploration of the S1' subsite.

Bioorg Med Chem Lett 18: 1681-7 (2008)

Glaxosmithkline

11/11/09

2D 3D

Design and synthesis of peptidomimetic severe acute respiratory syndrome chymotrypsin-like protease inhibitors.

J Med Chem 48: 6767-71 (2005)

Purdue University

11/10/09

2D 3D

Design, synthesis, and evaluation of inhibitors for severe acute respiratory syndrome 3C-like protease based on phthalhydrazide ketones or heteroaromatic esters.

J Med Chem 50: 1850-64 (2007)

University of Alberta

11/10/09

2D 3D

Isatin compounds as noncovalent SARS coronavirus 3C-like protease inhibitors.

J Med Chem 49: 3440-3 (2006)

Peking University

11/10/09

2D 3D

Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors.

Bioorg Med Chem Lett 15: 3058-62 (2005)

Development Center For Biotechnology

11/10/09

2D 3D

Structure-Based Design, Synthesis, and Biological Evaluation of a Series of Novel and Reversible Inhibitors for the Severe Acute Respiratory Syndrome-Coronavirus Papain-Like Protease.

J Med Chem 52: 5228-40 (2009)

Purdue University

09/14/09

2D 3D

Structure-based virtual screening against SARS-3CL(pro) to identify novel non-peptidic hits.

Bioorg Med Chem 16: 4138-49 (2008)

University of Mississippi

07/08/08

2D 3D

Discovery of a novel family of SARS-CoV protease inhibitors by virtual screening and 3D-QSAR studies.

J Med Chem 49: 3485-95 (2006)

National Tsing Hua University

09/26/06

2D 3D

Inhibition of the severe acute respiratory syndrome 3CL protease by peptidomimetic alpha,beta-unsaturated esters.

Bioorg Med Chem 13: 5240-52 (2005)

National Taiwan University

09/26/06

2D 3D

Structure-based drug design and structural biology study of novel nonpeptide inhibitors of severe acute respiratory syndrome coronavirus main protease.

J Med Chem 49: 5154-61 (2006)

National Defense Medical Center

09/26/06

2D 3D

Discovery of potent anilide inhibitors against the severe acute respiratory syndrome 3CL protease.

J Med Chem 48: 4469-73 (2005)

National Taiwan University

09/26/06

2D 3D

Synthesis, crystal structure, structure-activity relationships, and antiviral activity of a potent SARS coronavirus 3CL protease inhibitor.

J Med Chem 49: 4971-80 (2006)

Taigen Biotechnology

09/23/06

2D 3D