STAT3 inhibitors
Inventors
De Achaval, Sofia • Tweardy, David John
Assignees
Tvardi Operating Company Inc • Tvardi Therapeutics • Baylor College of Medicine
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Publication Number
US-11826315-B2
Publication Date
2023-11-28
Expiration Date
Abstract
Compounds as STAT3 inhibitors are described. A pharmaceutical composition comprising the same, methods of making the same, and a method for treating or preventing conditions such as cancer, chronic inflammation, and fibrosis using the same, are described.
Core Innovation
The invention relates to a pharmaceutical composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, together with a pharmaceutically acceptable excipient. The compounds are defined by a detailed set of substituent variables R1, R2, R3, R4, R5, R6, and R7, with each occurrence independently selected from specified structural groups and with n1, n2, and n3 limited to discrete values.
The substituent framework further constrains R3 and R4 to defined selections of hydrogen, halogen, cyano, nitro, CF3, OCF3, ORa, SRa, OC(O)Ra, and related options, and constrains R5, R6, and R7 to independently selected groups including halo, cyano, nitro, CF3, OCF3, ORa, SRa, carbonyl-containing substituent forms, and alkyl, aryl, or heterocycle options. The disclosure also includes Formula II and Formula III with defined substituent meanings and exemplified compound selections in tables for Formula I and Formula II.
The therapeutic context described in the document is directed to STAT3 inhibition. The disclosed subject matter is also linked to STAT3 phosphorylation and STAT3 nuclear translocation, with downstream cellular outcomes including apoptosis, angiogenesis, and anti-tumor immune-mediated cytotoxicity.
Claims Coverage
The independent claim coverage centers on one pharmaceutical composition claim with one core inventive structure definition, Formula I, and a broad set of defined substituent options across multiple positions, plus the inclusion of a pharmaceutically acceptable excipient. Dependent claims further refine the allowed structural parameters and, in some cases, specify narrower substituent lists or define the compound as Formula II.
Pharmaceutical composition with a compound of Formula I or pharmaceutically acceptable salt
A pharmaceutical composition comprising a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, and R7 and indices n1, n2, and n3 are defined by specified independent selections and discrete index values, and a pharmaceutically acceptable excipient.
The claim coverage centers on a pharmaceutical composition where the active is a compound of Formula I or a pharmaceutically acceptable salt, constrained by the specified substituent and index definitions, combined with a pharmaceutically acceptable excipient.
Stated Advantages
Treating or preventing STAT3-linked disorders including cancer, chronic inflammation, fibrosis, anaphylaxis, asthma, and inflammatory bowel disease.
Inhibiting STAT3 in a cell, including effects on STAT3 phosphorylation and STAT3 nuclear translocation.
Inducing outcomes associated with STAT3 inhibition, including apoptosis, angiogenesis, and anti-tumor immune-mediated cytotoxicity.
Documented Applications
Treating or preventing cancer.
Treating or preventing chronic inflammation.
Treating or preventing fibrosis.
Treating or preventing anaphylaxis.
Treating or preventing asthma.
Treating or preventing inflammatory bowel disease, including ulcerative colitis and Crohn’s disease.
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