Oxaborole analogs and uses thereof
Inventors
Jacobs, Robert Toms • Liu, Yang • Sciotti, Richard J. • Speake, Jason D. • Whitlock, Gavin Alistair • Glossop, Paul Alan • Mowbray, Charles Eric • Launay, Delphine Françoise Monique • Robinson, Stephen John
Assignees
DRUGS FOR NEGLECTED DISEASES INITIATIVE • Government Of United States Represented By Secretaryof Army AS • Anacor Pharmaceuticals LLC • United States Department of the Army
Publication Number
US-10961261-B2
Publication Date
2021-03-30
Expiration Date
2038-03-01
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Abstract
This application describes compounds, compositions, and methods which are useful in treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a parasite.
Core Innovation
This patent discloses compounds, compositions, and methods useful in treating, preventing, inhibiting, ameliorating, or eradicating diseases caused by parasites. The compounds are described by chemical formulae involving oxaborole analogs, including various substitutions on elements such as R1a, R1b, and Ring A, with detailed definitions for their chemical structures. Pharmaceutically acceptable salts of these compounds are also included. The compounds are effective against parasitic infections, particularly those caused by organisms belonging to Leishmania and Trypanosoma species.
The background identifies the significant global health burden posed by parasitic diseases such as leishmaniasis and Chagas disease. Existing treatments for these diseases face challenges such as limited efficacy, resistance, side effects, high costs, and lack of effective vaccines or chemoprophylactic options. The patent addresses the pressing need for novel chemical entities with new mechanisms of action to combat such diseases, aiming to provide compounds with improved therapeutic profiles to treat infections caused by Leishmania, Trypanosoma cruzi, and related parasites.
Claims Coverage
The patent discloses one independent claim directed to a compound of formula III and associated compositions and medical methods, featuring a series of inventive features related to the compound's structure, formulation, and medical applications.
Compound of formula III
The claim covers compounds characterized by the chemical structure of formula III, comprising a benzo[c][1,2]oxaborol core linked to a 1,2,3-triazole substituted with a 5-methyl and a pyridin-2-yl group, as well as pharmaceutically acceptable salts thereof.
Selected compounds with specific structural characteristics
Specific compounds within formula III are claimed, including compounds represented by structures I-1 through I-103, particular stereochemical forms, and pharmaceutically acceptable salts, such as the arginine monohydrate salt.
Pharmaceutical compositions comprising the compounds
Pharmaceutical compositions containing the compounds of formula III or their specified examples, with at least one pharmaceutically acceptable excipient, are claimed.
Methods of treating cutaneous leishmaniasis
Methods involving administration of compounds of formula III or their selected examples or pharmaceutically acceptable salts to subjects for the treatment of cutaneous leishmaniasis are claimed.
Methods of treating visceral leishmaniasis
Methods involving administration of compounds of formula III or their selected examples or pharmaceutically acceptable salts to subjects for the treatment of visceral leishmaniasis are claimed.
The claims center on the novel oxaborole-based compounds of formula III with specific substitution patterns, their pharmaceutical compositions, and their medical use in treating parasitic diseases, particularly cutaneous and visceral leishmaniasis.
Stated Advantages
The invention provides novel chemical entities with new mechanisms of action to combat parasitic diseases such as leishmaniasis and Chagas disease, addressing existing limitations of treatment options.
Documented Applications
Use of the compounds in the treatment, prevention, inhibition, amelioration, or eradication of diseases caused by parasites, including diseases caused by Leishmania species such as cutaneous, mucocutaneous, and visceral leishmaniasis.
Treatment of parasitic infections associated with Trypanosoma species, including T. cruzi (Chagas disease), T. congolense, T. brucei, and T. b. gambiense, and related conditions such as African Animal Trypanosomosis (AAT).
Pharmaceutical compositions for medical use comprising the compounds and pharmaceutically acceptable excipients.
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