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Breakthrough Inhibitors for Equine Encephalitis

Introduction

This covalent inhibitor technology presents a significant advancement in combating equine encephalitis viruses, which pose a serious threat to both equine populations and humans. By inhibiting key viral proteins necessary for the replication and spread of the virus, these inhibitors offer a novel and powerful approach to treating infections. For pharmaceutical companies, veterinary medicine providers, and biotechnology firms, this technology provides an opportunity to lead in the development of therapies that target these dangerous viruses, protecting both animal and human health.

The Challenge: Managing Viral Infections in Animals and Humans

Equine encephalitis viruses, including Eastern, Western, and Venezuelan variants, are mosquito-borne pathogens that can cause severe neurological diseases in horses and humans. Current treatment options are limited and mostly preventative, with vaccines being the primary form of control. However, once infection occurs, there are few effective treatments available, leading to high mortality rates in horses and significant risk to human populations. As zoonotic diseases continue to rise in prominence, the need for effective, post-infection therapeutic options has become more urgent.

Covalent Inhibitors for Powerful Viral Control

This covalent inhibitor technology targets and neutralizes key enzymes involved in the replication of equine encephalitis viruses. By forming a covalent bond with viral proteins, the inhibitors effectively block the virus’s ability to reproduce and spread within the host, offering a direct and powerful intervention to halt disease progression. The inhibitors can be used as part of a therapeutic regimen to treat infected animals, and potentially humans, following exposure. This innovative approach provides a much-needed solution for managing outbreaks and reducing the risk of widespread infection.

Key Benefits for Pharmaceutical and Veterinary Sectors

For pharmaceutical companies, this technology represents a promising new class of antiviral treatments that could be developed into life-saving medications. Veterinary care providers can use these inhibitors to treat infected horses, providing a viable treatment option where currently none exists. Biotechnology firms can explore the potential of these inhibitors in broader antiviral applications, including use in human medicine for emerging zoonotic threats. This technology offers a significant advantage in controlling viral outbreaks in equine populations and preventing potential spillover into human populations.

Invest in Antiviral Innovation

Licensing this inhibitor technology for equine encephalitis positions your company as a leader in the fight against infectious diseases. By offering an innovative solution for treating viral infections in both animals and humans, your business can meet the rising demand for antiviral therapies that protect against zoonotic diseases. This technology provides a strategic investment for companies focused on improving public health, advancing veterinary medicine, and delivering cutting-edge antiviral solutions.

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Embodiments and methods for a new class of potent non-peptidic covalent inhibitors of nsP2 cysteine protease that inhibit Venezuelan equine encephalitis virus’s (VEEV) replication in neuroblasts are disclosed. More particularly, an acrylate and vinyl sulfone-based chemical series were investigated as promising starting scaffolds against VEEV and as inhibitors of the cysteine protease domain of VEEV’s non-structural protein 2 (nsP2). The invention discloses compounds of Formula I and analogues for treatment of VEEV.
1. A compound of Formula (I):
Figure US20220235007A1-20220728-C00108
or a stereoisomer, solvate and/or pharmaceutical acceptable salt thereof; wherein
A is C(O)OR3 or S(O2)R3;
R3 is (C1-6)alkyl, (C3-7) cycloalkyl, (C3-7)cycloalkyl(C1-5)alkyl, optionally substituted aryl, or optionally substituted (C6-12)aralkyl;
R1 and R2 are independently selected from H, (C1-6)alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-5)alkyl, optionally substituted aryl, or optionally substituted (C6-12)aralkyl;
R is a group selected from
Figure US20220235007A1-20220728-C00109
Figure US20220235007A1-20220728-P00003

is a single bond or double bond.

2. The compound of claim 1 wherein said compound has the Formula II:
Figure US20220235007A1-20220728-C00110
or a stereoisomer, solvate and/or pharmaceutical acceptable salt thereof; wherein
A, R1, R2, R3 and R, are as defined in claim 1.
3. The compound of claim 2, wherein R1 is H, methyl or benzyl and R2 is H or methyl.
4. The compound of formula (I) of claim 1 wherein substituents on optionally substituted aryl or optionally substituted (C6-12)aralkyl in R3, R1 and R2 are selected from (C1-6)alkyl, (C1-6)alkoxy, halogen, halogen substituted (C1-6)alkyl, hydroxyl or amino.
5. A composition comprising compound of formula (I) as inhibitors of the cysteine protease domain of Venezuelan equine encephalitis virus (VEEV’s) non-structural protein 2 (nsp2).
6. A method of treating infectious disease caused by Venezuelan equine encephalitis virus (VEEV) comprising administering a compound of Formula (I) to the patient.
7. A compound of Formula (III):
Figure US20220235007A1-20220728-C00111
or a stereoisomer, solvate and/or pharmaceutical acceptable salt thereof; wherein
R4 is (C1-6)alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-5)alkyl, optionally substituted aryl, or optionally substituted (C6-12)aralkyl;
R5 and R6 are independently selected from H, (C1-6)alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-5)alkyl, optionally substituted aryl, or optionally substituted (C6-12)aralkyl;
R7 is a group selected from
Figure US20220235007A1-20220728-C00112
8. The compound of claim 7, wherein R5 is H.
9. The compound of claim 7, wherein R5 is CH3.
10. The compound of claim 7, wherein R5 is benzyl.
11. The compound of claim 7, wherein R6 is H.
12. The compound of claim 7, wherein R6 is CH3.
13. The compound of formula (III) of claim 7 wherein substituents on optionally substituted aryl or optionally substituted (C6-12)aralkyl in R4, R5 and R6 are selected from (C1-6)alkyl, (C1-6)alkoxy, halogen, halogen substituted (C1-6)alkyl, hydroxyl or amino.
14. The compound of claim 11, selected from:
Figure US20220235007A1-20220728-C00113
15. A composition comprising compound of formula (III) as inhibitors of the cysteine protease domain of Venezuelan equine encephalitis virus (VEEV’s) non-structural protein 2 (nsp2).
16. A method of treating infectious disease caused by Venezuelan equine encephalitis virus (VEEV) comprising administering a compound of Formula (III) to the patient.
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Title

Covalent inhibitors of equine encephalitis virus

Inventor(s)

Ifedayo Victor Ogungbe, Huaisheng ZHANG

Assignee(s)

Jackson State University

Patent #

20220235007

Patent Date

July 28, 2020

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