Human papilloma virus inhibitors and pharmaceutical compositions containing same
Inventors
Blumenfeld, Marta • Compere, Delphine • Gauthier, Jean-Michel
Assignees
Publication Number
US-8440833-B2
Publication Date
2013-05-14
Expiration Date
2028-11-20
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Abstract
HPV inhibitors of formula (I) in which G1 is —NHCO(CH2)n-, where n is an integer between 1 and 4, R3 is —CW(CH2)m—NR4R5 or —CW(CH2)mCH3 or —CN, where W is O, S or NH and m is an integer between 0 and 5, or R3 is one of the following groups: and A is an optionally substituted aryl group and B is an aryl group, preferably a phenyl which is substituted.
Core Innovation
The invention relates to novel antiviral compounds of formula (I) that act as inhibitors of human papilloma virus (HPV). These compounds notably interfere with the formation of the complex between the viral proteins E1 and E2, which is essential for the replication of HPVs. The invention also encompasses pharmaceutical compositions containing these compounds, methods for their preparation, and their use in treating or preventing infections caused by the papilloma virus.
Human papilloma viruses are widespread and responsible for a range of epithelial lesions in humans and animals, including conditions associated with both high and low risk HPVs such as verrucas, condylomas, papillomas, and various neoplasias and carcinomas. Current treatments for HPV-related lesions are based on physical destruction or cytotoxic and immunomodulatory agents, none of which fully remove viral particles and are often associated with high recurrence rates and adverse side effects. Importantly, there is a lack of antiviral treatments that specifically target the papilloma virus.
The core innovation presented in the patent is the development of small molecule inhibitors that specifically suppress the replication of HPVs by disrupting the critical E1/E2 protein interaction, thereby directly preventing viral DNA replication. These compounds provide a new means to address the existing gap in targeted antiviral therapy for HPV infections, especially in treating or preventing lesions and diseases resulting from replication of the papilloma virus.
Claims Coverage
The patent includes several independent claims that define the inventive features of the new HPV inhibitors, their pharmaceutical compositions, and therapeutic uses. There are multiple directions of claim focus, covering both the compounds, compositions, and methods.
Novel HPV inhibitor compounds of formula (I)
The invention covers compounds of formula (I), wherein: - G1 is —NHCO(CH2)n-, where n is an integer between 1 and 4. - R3 is —CW(CH2)m—NR4R5 or —CW(CH2)mCH3 or —CN, with W as O, S, or NH and m between 0 and 5, or R3 is specified structural groups. - A is an optionally substituted aryl group and B is an aryl group, preferably a substituted phenyl. - All stereoisomers are included. - The patent also covers pharmaceutically acceptable salts of these compounds.
Pharmaceutical compositions comprising compounds of formula (I)
A pharmaceutical composition comprising at least one compound of formula (I) or a pharmaceutically acceptable salt thereof, in association with a pharmaceutically acceptable excipient.
Method of treating or inhibiting papilloma virus replication
A method of treating infection by the papilloma virus or inhibiting papilloma virus replication by administering an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof to a person in need thereof.
Method for treating a pathology related to papilloma virus
A method for treating a pathology related to the papilloma virus comprising administering a compound of formula (I) or a pharmaceutically acceptable salt thereof to a person in need thereof.
In sum, the inventive features protect the structure and specific substitution patterns of the HPV inhibitor compounds, cover pharmaceutical compositions containing them, and broadly claim their use in inhibiting HPV replication and treating HPV-related diseases.
Stated Advantages
The compounds specifically inhibit the interaction between HPV E1 and E2 proteins, which is necessary for HPV replication.
These compounds are active against papilloma viruses and can inhibit their replication, addressing the lack of targeted antiviral treatments for HPV.
The invention provides pharmaceutical compositions that can be formulated for various routes of administration, including topical, oral, and others.
Documented Applications
Treating or preventing infection by the papilloma virus in humans.
Treating or preventing infections by low risk papilloma viruses, such as HPV6 and HPV11.
Treating or preventing ano-genital verrucas such as acuminated condylomas and planar condylomas.
Treating or preventing laryngeal, conjunctival, or buccal papillomas and other epithelial lesions, including recurrent respiratory papillomatoses, low grade and high grade intra-epithelial neoplasias, bowenoid papuloses, verrucas (vulgar, plantar, myrmecias, superficial, flat), verruciform epidermodysplasias, and carcinomas such as ano-genital carcinomas.
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