Isoquinoline derivatives, methods of synthesis and uses thereof
Inventors
Paulvannan, Kumarapandian • Solas, Dennis • Kitaygorodskyy, Anatoliy • Lingappa, Vishwanath R.
Assignees
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Publication Number
US-12024521-B2
Publication Date
2024-07-02
Expiration Date
Abstract
Described herein are compounds, pharmaceutical compositions and methods of using these compounds and pharmaceutical compositions for treating and/or preventing conditions such as amyotrophic lateral sclerosis. These compounds and pharmaceutical compositions are also useful as antivirals and antimicrobial agents.
Core Innovation
The invention relates to structurally defined compounds, including isoquinoline-derivative compounds and other structure-defined compounds with extensive R-group definitions across multiple positions. The compounds include solvates, hydrates, and pharmaceutically acceptable salts, and the disclosure also states prodrugs and metabolites.
The disclosed structural embodiments include benzyloxy, dimethoxy, fluoro, benzodioxole, ether-linked biaryl or heterocycle systems, amino and amide functionalities, hydroxyl substituents, ester or acid groups such as -CO2H and -CO2Me, sulfonamide, and fused N-heterocycles. Specific compound examples are identified as labeled examples corresponding to structural embodiments within the disclosed scaffold.
The document further describes biological contexts including inhibition of HIV-1 replication, nematode movement assay outcomes, and treatment-related contexts for amyotrophic lateral sclerosis (ALS). It also mentions formulation and dosage considerations, including pharmaceutical compositions with a pharmaceutically acceptable vehicle and multiple delivery approaches.
Claims Coverage
The independent claims cover structurally defined compounds with multiple R-group substitution constraints, including solvate, hydrate, and pharmaceutically acceptable salt forms. Across the claim families, there are three inventive features, and dependent claims further specify pharmaceutical compositions and treatment of amyotrophic lateral sclerosis (ALS).
Isoquinoline-derivative compound with R-group limitations
A compound defined by structural formulas with extensive substituent limitations on R groups, provided as a solvate, hydrate, or pharmaceutically acceptable salt thereof.
Structurally defined compound with extensive R-group substitution scope
A compound of structural Formula, or a solvate, hydrate or pharmaceutically acceptable salt thereof, wherein multiple R positions are defined by enumerated allowed substituent types.
Compound having a specific structure with solvate, hydrate, or salt variants
A compound having the structure, or a solvate, hydrate or pharmaceutically acceptable salt thereof.
Overall, the independent claims primarily cover structure-defined compounds, including solvates, hydrates, and pharmaceutically acceptable salts, with defined structural characteristics and permitted substitutions. Dependent claims further specify pharmaceutical compositions and therapeutic treatment methods for amyotrophic lateral sclerosis (ALS).
Stated Advantages
Useful for treating or preventing amyotrophic lateral sclerosis (ALS).
Stated antiviral activity.
Stated antimicrobial activity.
Documented Applications
Treatment or prevention of amyotrophic lateral sclerosis (ALS) by administering the compound or a pharmaceutical composition.
Inhibition of HIV-1 replication.
Nematode movement assay context with assay outcomes reported for select compounds.
Antimicrobial application.
Alzheimer’s disease is mentioned among the conditions discussed.
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