Non-hormonal steroid modulators of NF-κβ for treatment of disease
Inventors
McCall, John M. • Hoffman, Eric • Kanneboyina, Nagaraju (Raju) • Damsker, Jesse
Assignees
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Publication Number
US-10464967-B2
Publication Date
2019-11-05
Expiration Date
Abstract
The present invention relates to compounds and methods which may be useful as treatments of diseases.
Core Innovation
The disclosed subject matter concerns cyclopenta[a]phenanthrene-derived steroid-like compounds, including stereoisomers and substituent variants. The invention relates to non-hormonal steroid modulators of NF-baB, including compounds that modulate NF-baB/IbaB/IKK signaling, and is presented as a method to provide disease treatment by administering the disclosed compounds.
The compounds are represented by a structural Formula I having variable substituents (R1R9), and the disclosure provides pharmaceutically acceptable compositions and carriers. Structural depictions are provided for related compounds such as cyclopenta[a]phenanthren-3-one derivatives incorporating hydroxyacetyl and hydroxy groups, and the document indicates that therapeutically effective amounts of the compounds can be administered.
The disclosure is organized around substituent variables R1/R2/R3/R4/R5/R6 and includes transformation endpoints described as ester formation, hydrolysis, and derivatization. The document frames the problem as addressing NF-baB-mediated disorders and cancers by modulating NF-baB/IbaB/IKK signaling using non-hormonal steroid compounds, with reported disease-related contexts including edema, rheumatoid arthritis, allergic asthma endpoints, and cancer types including astrocytoma and glioblastoma.
Claims Coverage
The provided claim set includes one independent claim with three dependent refinements, covering administration of a compound having a structural formula to reduce astrocytoma symptoms.
Reducing astrocytoma symptoms by administering a compound of structural formula
A method of reducing the symptoms of astrocytoma in a patient in need thereof, comprising the administration, to the patient, of a therapeutically effective amount of a compound having the structural formula.
Reducing inflammation as the astrocytoma symptom
The method is characterized by the symptom being inflammation.
Reducing edema as the astrocytoma symptom
The method is further defined such that the symptom being addressed is edema.
Reducing glioblastoma symptoms within astrocytoma treatment
The method is carried out using an astrocytoma that is specifically a glioblastoma.
The inventive concept is administering therapeutically effective amounts of a compound with the specified structural formula to reduce astrocytoma symptoms, with refinements to inflammation and edema and to astrocytoma specifically being glioblastoma.
Stated Advantages
Reducing the symptoms of astrocytoma in a patient in need thereof.
Documented Applications
Reducing the symptoms of astrocytoma (including glioblastoma) in a patient in need thereof.
Treatment of NF-baB-mediated disorders including edema, rheumatoid arthritis, and allergic asthma, with described inflammatory endpoints such as eosinophil counts and CD4+ infiltration.
Treatment of cancers including astrocytoma and glioblastoma.
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