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
Anacor Pharmaceuticals LLC • United States Department of the Army
Publication Number
US-11691992-B2
Publication Date
2023-07-04
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
The invention provides compounds, compositions, and methods useful for treating, preventing, inhibiting, ameliorating, or eradicating diseases caused by parasites. Specifically, compounds of formula I and their pharmaceutically acceptable salts are disclosed, featuring variable substituents such as R1a, R1b which can be hydrogen or C1-6 aliphatic groups, and Ring A which is a triazolyl substituted with groups R2 and R3. These compounds encompass a wide range of substituted triazole analogs with specific structural features including optionally substituted carbocyclic and heteroaryl groups, as detailed extensively in the description.
The compounds are designed to address diseases caused by kinetoplastid parasites such as Leishmania species and Trypanosoma species. The background discloses that leishmaniasis is a widespread and increasing disease with limited treatment options having issues of resistance, toxicity, and cost. Similarly, Chagas disease caused by Trypanosoma cruzi presents a significant public health challenge with limited approved treatments. The need for novel chemical entities with new mechanisms of action to effectively combat these parasite-caused diseases is emphasized.
Claims Coverage
The patent contains one independent claim defining a class of compounds and methods of treatment related to these compounds. The inventive features focus on the chemical structure of the compounds and their therapeutic uses.
Compound structure with specific substituents
A compound of formula I comprising R1a and R1b independently selected as hydrogen or C1-6 aliphatic groups, optionally forming a substituted 3- to 6-membered carbocyclic ring together; Ring A as a triazolyl substituted with R2 and R3; R2 as hydrogen or optionally substituted C1-6 aliphatic or 3-6 membered carbocyclyl groups; and R3 as optionally substituted phenyl, C1-6 aliphatic, 3-8 membered carbocyclyl, or 5-6 membered heteroaryl containing 1-3 heteroatoms (nitrogen, oxygen, sulfur).
Pharmaceutical compositions including the compound
Pharmaceutical compositions comprising a compound of formula I or pharmaceutically acceptable salts thereof, together with at least one pharmaceutically acceptable excipient.
Methods of treating parasitic diseases using the compounds
Methods of treating cutaneous leishmaniasis, visceral leishmaniasis, and parasitic infections caused by specific Leishmania species or Trypanosoma species by administering the compound of formula I or its pharmaceutically acceptable salt to a subject in need thereof.
The claims primarily cover compounds of formula I with detailed structural definitions, pharmaceutical compositions containing these compounds, and methods of treating parasitic infections, specifically leishmaniasis and diseases caused by Trypanosoma, highlighting their utility as antiparasitic agents.
Stated Advantages
Compounds provide novel chemical entities with potentially improved mechanisms of action to combat parasitic diseases such as leishmaniasis and Chagas disease.
The compounds are designed to overcome limitations of existing therapies, including resistance, toxicity, and expense associated with current drugs.
The pharmaceutical compositions and methods provide options for treatment, prevention, inhibition, amelioration, or eradication of diseases caused by parasites.
Documented Applications
Treatment, prevention, inhibition, amelioration, or eradication of parasitic infections caused by organisms belonging to Leishmania species including cutaneous, mucocutaneous, and visceral leishmaniasis.
Treatment of parasitic infections caused by Trypanosoma species such as T. cruzi (Chagas disease), T. congolense, T. brucei, and T. b. gambiense.
Use in veterinary medicine for treating animals such as dogs and cattle infected with relevant parasites.
Pharmaceutical compositions can be administered via various routes to humans or animals for treatment of parasitic diseases.
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