PATENT STATUS OF

MOLNUPIRAVIR
As of 6 August 2021

1. BRIEF SUMMARY

1.1. The patent application, which claims the molnupiravir compound, formulation
comprising such compound, including its use in treating viral infections such as
SARS, MERS, among others is pending at IPOPHL.

1.2. IPOPHL has not received patent applications directed to processes for
manufacturing the molnupiravir compound as well as to combinations of such
compound with other active ingredients.

1.3. Currently, there are no patent applications directed to inventions relating to the
use of molnupiravir for the treatment of COVID-19 disease.
2. DETAILED PATENT INFORMATION 1
2.1. Compound and Formulation Patent(s)
2.1.1. Pending patent application PH 1/2020/550607 claims the molnupiravir
molecule. Pharmaceutical compositions comprising the molnupiravir
compound with pharmaceutically acceptable excipients, including the
medical uses of the same compound are also recited in the claims.

FOREIGN
PH PATENT STATUS SCOPE OF CLAIMS APPLICATIONS
Patent No. : PH 1/2020/550607 Molnupiravir molecule, WO2019113462
Title : “N4-Hydroxycytidine and pharmaceutical compositions EP3706762 A1
Derivatives and Anti-Viral comprising the same including its (PUBLISHED);
Uses Related Thereto” indication against viral infections JP202142235 A
PENDING2 (Eastern, Western and Venezuelan (PUBLISHED);
Int’l. Filing Date : 07 December 2018 Equine Encephalitis, Chikungunya JP6804790 B1
fever, Ebola, Influenza, Respiratory (GRANTED);
National Phase 08 May 2020
Synctial Virus, Zika virus, and viral US2020276219 A1
Entry: infections such as SARS, MERS, (w/ NOTICE OF
Applicant : Emory University etc) ALLOWANCE)

2.2. Process Patents

2.2.1. There are no active patents, which relate to methods of synthesizing
molnupiravir.

2.2.2. The method of synthesizing the molnupiravir compound is described

in the same patent application PH1/2020/550607 but not clearly recited
in the claims.

2.3. Indication Patents

2.3.1. The medical indications of molnupiravir against viral infections such
as Eastern, Western and Venezuelan Equine Encephalitis, Chikungunya
fever, Ebola, Influenza, Respiratory Synctial Virus, Zika virus, and viral
infections such as SARS, MERS, etc., are claimed in the same pending
patent application, PH 1/2020/550607.

2.3.2. There are no active patents directed to inventions relating to subsequent

medical indications of molnupiravir.

2.4. Combination Patents

2.4.1. IPOPHL has not received a patent application directed to inventions
relating to combinations of molnupiravir and other active ingredients.

2.4.2. The molecule patent application PH 1/2020/550607 describes general

combination therapies comprising molnupiravir and other active agents
but were not recited in the claims.

Compound patent – primary patent covering the molnupiravir compound including its salts and polymorphs
Processes patent – processes of manufacturing the molnupiravir compound or to its methods of synthesis
Formulation patent – products comprising molnupiravir as the sole active ingredient
Medical Indication/Uses patent – subsequent medical uses of molnupiravir alone or in combination with another active ingredient
Combination patent – formulations/kits comprising the combination of molnupiravir with other active ingredients. Molnupiravir can be
administered sequentially or as a composition with another active ingredient.

with Substantive Examination Report

3. OTHER RELEVANT INFORMATION
• Molnupiravir (drug development code: EIDD-2801 or MK-4482) is an isopropyl ester
prodrug of N4-hydroxycytidine (EIDD-1931) being studied for its antiviral activity
against influenza, MERS-CoV, and SARS-CoV2.3 N4-hydroxycytidine (EIDD-1931)
was first described in literature in 1980 as a potent mutagen of bacteria and phage;
it has shown antiviral activity against Venezuelan equine encephalitis virus and the
human coronavirus HCoV-NL63 in vitro, as well as in SARS-CoV2 and other human
and bat coronaviruses in mice and human airway epithelial cells. 4,5

• Molnupiravir has improved bioavailability in non-human primates and becomes the

active 5’-triphosphate form when hydrolyzed in vivo.

• The drug was developed at Emory University by its drug innovation company
(Drug Innovation Ventures at Emory or DRIVE), and was acquired by (licensed to)
Ridgeback Biotherapeutics, which then partnered with Merck & Co. for further
development.

• It was recently reported that molnupiravir, as a treatment for mild and moderate
COVID-19 cases is now on Phase 3 clinical trial at the Lung Center of the Philippines.
The drug was seen to prevent the progression of COVID-19.6

• Molnupiravir has a similar mechanism of action with Remdesivir in that both drugs
attack the same viral enzyme RNA polymerase in the treatment of SARS-CoV2;
however, unlike Remdesivir, which has to be administered intravenously, molnupiravir
can be taken orally as a pill.

• Chemical Structure for molnupiravir (isopropyl ester prodrug of N4-hydroxycytidine)

3
https://go.drugbank.com/drugs/DB15661
4
PubChem [Internet]. Bethesda (MD): National Library of Medicine (US), National Center for Biotechnology Information; 2004-. PubChem
Compound Summary for CID 197020, N(4)-Hydroxycytidine; [cited 2021 Aug. 6]. Available from: https://pubchem.ncbi.nlm.nih.gov/
compound/N_4_-Hydroxycytidine
5
Painter WP, Holman W, Bush JA, Almazedi F, Malik H, Eraut NCJE, Morin MJ, Szewczyk LJ, Painter GR. Human Safety, Tolerability, and
Pharmacokinetics of Molnupiravir, a Novel Broad-Spectrum Oral Antiviral Agent with Activity Against SARS-CoV-2. Antimicrob Agents
Chemother. 2021 Mar 1;65(5):e02428-20. doi: 10.1128/AAC.02428-20. Epub ahead of print. PMID: 33649113; PMCID: PMC8092915.
6
https://mb.com.ph/2021/08/06/promising-oral-antiviral-drug-vs-covid-19-now-on-phase-3-clinical-trial-at-lung-center/
4. SCOPE AND LIMITATION
• This report was generated using widely-used public and proprietary patent databases and
defined search strings.

Example Search Keywords: » molnupiravir, MK4482; EIDD2801; N4-hydroxycytidine-5’-isopropyl

ester; uridine-5’-(2-methylpropanoate)-4-oxime; applicant’s name
(e.g. Emory University, Merck, Ridgeback); N4-hydroxycytidine;
EIDD1931; anti-viral; virus; coronavirus

Example International Patent » A61K31/00 (Medicinal preparations containing organic active

Classification (IPC): ingredients)
• A61K31/70 (Carbohydrates; Sugars; Derivatives thereof)
° A61K31/7042 (Compounds having saccharide radicals and
heterocyclic rings)
– A61K31/7052 (having nitrogen as a ring hetero atom)
• A61K31/706 (containing six-membered rings with
nitrogen as a ring hetero atom)
° A61K31/7064 (containing condensed or non-
condensed pyrimidines)
– A61K31/7068 (having oxo groups directly
attached to the pyrimidine ring, e.g. cytidine)

» C07H19/00 (Compounds containing a hetero ring sharing

one ring hetero atom with a saccharide radical; Nucleosides;
Mononucleotides; Anhydro-derivatives thereof)
• C07H19/02 (sharing nitrogen)
° C07H19/04 (Heterocyclic radicals containing only nitrogen
atoms as ring hetero atom)
– C07H19/06 (Pyrimidine radicals)
• C07H19/067 (with ribosyl as the saccharide
radical)

» IPOPHL Patent Search, IPOPHL IP Administration System (IPAS),

Example of Patent Databases Espacenet, USPTO, WIPO Patentscope (WIPO COVID-19 Search
Facility), Google Patents
» EPOQUENET, CAS STN, Web of Science
» SureChEMBL
» US Food and Drug Administration Orange Book, Canada’s Drug
Patent Register, Medicine Patent Pool’s MedsPal, WIPO Pat-
INFORMED

» innovator’s website, press releases, annual reports, and journals

Other sources of information: » PubChem, ChemSpider
» World Health Organization, clinical trials databases, PublicCitizen,
DrugBank, and Patent blogs such as Patently O, Patent Progress, IP
Watchdog, PharmaPatents, etc.

• Due to the temporally dynamic nature of the legal status of patents, users should undertake
additional search and legal analysis before making any decision based on this report, particularly
those for commercial purposes.

• This report only provides a snapshot of the patent information at a point in time, based on the
information available to the search team when the patent search was conducted.
PATENT STATUS OF
MOLNUPIRAVIR
As of 6 August 2021