Methods of treatment using BCN057 and BCN512
Inventors
NORRIS, ANDREW J. • Chakrabortty, Sudip
Assignees
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Publication Number
US-12435081-B2
Publication Date
2025-10-07
Expiration Date
Abstract
The present disclosure is directed to methods of treating or ameliorating various conditions by the administration of a BCN057, BCN512 or analogs of these compounds. The compounds can be used to reduce tumor burden in cancers, including pancreatic cancer and gastrointestinal (GI) cancer. The compounds can also be used to protect against chemotherapy induced toxicity to the GI tract. Further, they can be used to treat fibrosis and various inflammatory conditions. Analogs of BCN057 and BCN512 are also described.
Core Innovation
The patent describes a class of compounds defined by Formula C, where substituent groups R1, R2, R3, and R4 are selected from specified options including halogens, hydrogen, amino, hydroxy, methyl, and alkyl-aryl chains with defined ranges, or substituted or unsubstituted aryl. The structures include further combinatorial flexibility for the substituent groups, supporting preparation of multiple related compounds within the Formula C framework.
The patent connects the Formula C compounds and analogs to modulation of Wnt/beta-catenin signaling. The compounds and analogs are described as being believed to modulate Wnt/beta-catenin signaling and are related to therapeutic contexts involving Wnt pathway biology, including RSPO1/LGR5, DKK1, and LRP6/Frizzled leading to beta-catenin/TCF4 signaling.
The patent further expands on related structures by describing analogs of a compound of Formula XXI selected from Formula XXII, Formula XXIII, Formula XXIV, Formula XXV, Formula XXVI, and Formula XXVII. The therapeutic application coverage includes inflammation, including inflammatory conditions affecting the central nervous system, and ailments associated with Wnt activity modulation, as well as a fibrosis-focused subset that enumerates many specific fibrosis conditions.
Claims Coverage
The partial content includes two independent claims. Across both, the coverage centers on a defined Formula C compound class with variable substituents and analogs selected from specified formula groups, with dependent claim coverage linking these compounds and analogs to therapeutic treatment of inflammation and to modulation of Wnt activity for selected ailments including fibrosis and cancer.
Formula C compound class with variable substituents R1-R4
A compound of Formula C where R1, R2, R3, and R4 are defined as specified substituent sets including halogens, hydrogen, NH2, OH, CH3, and (CH2)n-CH3 chains with specified n ranges, or substituted or unsubstituted aryl.
Analog selection from specified formula groups of Formula XXI
An analog of the compound of Formula XXI where the analog is selected from Formula XXII, Formula XXIII, Formula XXIV, Formula XXV, Formula XXVI, and Formula XXVII.
Claim coverage is directed to structurally defined compounds and analogs, and through dependent claims to using those compounds to treat inflammation, including central nervous system inflammatory conditions, and to modulate Wnt activity to treat a broad set of ailments, including a fibrosis subset that names multiple specific fibrotic conditions.
Stated Advantages
Compounds and analogs are described as being believed to modulate Wnt/beta-catenin signaling.
The described methods provide therapeutic treatment for inflammation, including inflammatory conditions affecting the central nervous system.
The described methods provide therapeutic treatment of ailments addressed by modulating Wnt activity, including fibrosis and cancer-related conditions.
Documented Applications
Treating inflammation in a subject, including inflammation affecting the central nervous system.
Modulating Wnt activity in a subject to treat an ailment selected from radiation exposure, fibrosis, insulin sensitivity-related conditions, cancer, osteoporosis, alopecia/hair growth, wound healing, low bone density, and obesity.
Treating fibrosis of one or more specified fibrosis-related conditions, including pulmonary fibrosis, idiopathic pulmonary fibrosis, acute respiratory distress syndrome, cystic fibrosis, non-cystic fibrosis bronchiectasis, cirrhosis, liver fibrosis, endomyocardial fibrosis, old myocardial infarction, atrial fibrosis, mediastinal fibrosis, myelofibrosis, retroperitoneal fibrosis, progressive massive fibrosis, nephrogenic systemic fibrosis, Crohn's disease, gastrointestinal fibrosis, keloid conditions, scleroderma/systemic sclerosis, arthofibrosis, peyronie's disease, dupuytren's contracture, oral submucous fibrosis, renal fibrosis from kidney dialysis, and adhesive capsulitis.
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