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Publication Number

US-12180211-B2

Patent

Publication Date

2024-12-31

Expiration Date


Abstract

The present disclosure relates generally to methods and compositions for preventing or arresting cell death and/or inflammation.

Core Innovation

The invention relates to administering an effective amount of a compound of Formula I, or a pharmaceutically acceptable salt, stereoisomer, or mixture of stereoisomers thereof, to a subject in need thereof. Formula I is defined with a fused bicyclic ring system and variable substituents including Y, n, m, p, A, R1, R2, R3, R4, R5, R6, R14, and Z groups. The disclosure includes stereochemically defined small-molecule structures and representative compounds within the Formula I chemical space.

The biological utility tied to these Formula I compounds is described as methods for treating necrotic cell disease and inflammatory disorders. The dependent content further narrows inflammatory disorder applications to inflammatory bowel disease, Crohn’s disease, and ulcerative colitis. The disclosure also includes explicit exclusions of certain listed compounds from the claimed set.

Claims Coverage

Two independent claims are present. The claims share the same Formula I structural framework and differ in the therapeutic condition category, with one claim directed to necrotic cell disease and the other to inflammatory disorder, for a total of 2 inventive features.

Treatment of necrotic cell disease with Formula I compounds

A method for treating a necrotic cell disease by administering an effective amount of a compound of Formula I, or a pharmaceutically acceptable salt, stereoisomer, or mixture of stereoisomers thereof, to a subject in need thereof, with Formula I defined by Y, n, m, p, A, R1, R2, R3, R4, R5, R6, R14, and Z group substitution rules, and excluding specified compounds.

Treatment of inflammatory disorder with Formula I compounds

A method for treating an inflammatory disorder by administering an effective amount of a compound of Formula I, or a pharmaceutically acceptable salt, stereoisomer, or mixture of stereoisomers thereof, to a subject in need thereof, with the same Formula I structural framework, substitution rules, and exclusions.

Across both independent claims, the core coverage is the therapeutic administration of Formula I compounds with extensive substituent and ring definitions, permitted salt and stereoisomer forms, and explicit exclusions. The principal distinction is the treated condition: necrotic cell disease versus inflammatory disorder.

Stated Advantages

Not explicitly described in patent.

Documented Applications

Treating a necrotic cell disease.

Treating an inflammatory disorder.

Treating inflammatory bowel disease.

Treating Crohn’s disease or ulcerative colitis.

Treating RIPK1-mediated disease areas, including necroptosis-associated inflammatory and immune disorders.

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