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Publication Number
US-12319680-B2
Publication Date
2025-06-03
Expiration Date
Abstract
Compounds of formula (I) and related aspects.
Core Innovation
The disclosure relates to compound families defined by specified chemical formulas, including benzamide compounds, amide-linked heteroaryl-containing compounds, and related derivatives, together with pharmaceutically acceptable salts, solvates, isotopic forms, N-oxides, and other derivatives. The formula descriptions use variable substituent definitions for Ar1, Ar2, R1, R3, R4, R5, R6, R10, R11, and R12, and include named example compounds, stereoisomers, geometric, tautomeric, optical, and racemic forms.
The compounds are associated with CTPS1 inhibition and with potency and selectivity relative to CTPS2, including selectivity of CTPS1 over CTPS2 based on IC50 thresholds and fold selectivity. The disclosure also states that CTPS1 inhibition relates to reduced T-cell and B-cell proliferation and frames the compounds in therapeutic use cases spanning immune disorders, cancer, and vascular injury-related indications such as neointima and restenosis.
The document further provides synthetic schemes, intermediate compounds, and analytical characterization for multiple compound series and intermediates. It describes preparation routes for compounds of formula (I) and related formulas, with examples of intermediates, carboxylic acids, ester deprotection, salt formation, and reported NMR and chromatographic observations for specific compounds.
Claims Coverage
The claim coverage is centered on compounds defined by specified chemical formulas and includes pharmaceutically acceptable salts. Across the provided items, the independent claims consistently define the core scope as a formula-defined compound, with no additional independent-claim refinements available in the excerpts. The consolidated set reflects 1 inventive feature across the repeated claim summaries.
Formula-defined compound and pharmaceutically acceptable salts
A compound of the following formula, or salts thereof, including the formula-defined benzamide or related compound scope described in the patent text.
The consolidated claim scope is limited to formula-defined compounds and their pharmaceutically acceptable salts. No further independent-claim inventive features are explicitly provided in the supplied material.
Stated Advantages
Selectivity of CTPS1 over CTPS2 is stated using IC50 thresholds, selectivity ranges, and fold selectivity.
Inhibition of CTPS1 is stated, including human CTPS1 inhibition.
Reduction of T-cell proliferation is stated.
Reduction of B-cell proliferation is stated.
Treatment and prophylaxis of cancers, including hematological and non-haematological cancers, is stated.
Treatment and prophylaxis of inflammatory, autoimmune, and immune-related conditions is stated.
Documented Applications
Diseases involving T-cell and/or B-cell activation, including transplant rejection, GVHD, and HVGD.
Autoimmune diseases and inflammatory diseases.
Neoplasms, including cancer.
Pharmaceutical composition use as a CTPS1 inhibitor medicament.
Use in a medical device context, including device-coating and stent-related applications such as drug-eluting stent contexts, and immunosuppressant, antiplatelet, and anticoagulant context as described.
Treatment and prophylaxis of cancers, including hematological and non-haematological cancers.
Treatment and prophylaxis of inflammatory, autoimmune, and immune-related conditions.
Use in CTPS1 inhibition context, including human CTPS1 inhibition.
Use in CTPS1 versus CTPS2 selectivity assessment (fold selectivity).
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