Cannabinoid receptor type 2 (CB2) modulators and uses thereof
Inventors
Assignees
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Publication Number
US-11564928-B1
Publication Date
2023-01-31
Expiration Date
Abstract
Disclosed herein are compounds, compositions, and methods for modulating the Cannabinoid receptor 2 (CB2) with the compounds and compositions disclosed herein. Also described are methods of treating diseases or conditions that are mediated by the action of Cannabinoid receptor 2 (CB2) or that we benefit from modulating the Cannabinoid receptor 2 (CB2).
Core Innovation
The disclosure presents substituted 1,8-naphthyridine-3-carboxamide and 1,2-dihydro-1,8-naphthyridine-3-carboxamide compounds and related heteroaromatic/cyclized scaffolds defined by Formula (I) and related structural formulas. The compounds vary by aryl and heteroaryl substituents, morpholinoethyl or morpholine-like side chains, spiro and bridged motifs, cycloalkyl amide substituents, and functional groups such as hydroxy, fluoro, difluoromethoxy, cyano, and trifluoromethyl. The structures include pharmaceutically acceptable salts, solvates, stereoisomers, prodrugs, and active metabolites.
The disclosure also provides specific compound series, numbered members, intermediates, and characterization data, including compounds represented by Formula (A), Formula (X), and related examples. Additional described variants include chiral (R)/(S) stereoisomers, bicyclic and heterocyclic substituents, and recurring 4-hydroxy and 2-oxo motifs with carboxamide-linked substituents. The examples further describe synthetic intermediates and reported LCMS and 1H NMR characterization.
The disclosed compounds are framed as cannabinoid 2 receptor (CB2R) modulators. The text states therapeutic use in CB2R-mediated disease/disorder and cancer, including restoration of anti-tumor immune function, treatment of solid tumors, and combination with immune checkpoint inhibitors such as PD-1, PD-L1, nivolumab, pembrolizumab, atezolizumab, and durvalumab.
Claims Coverage
The consolidated claim coverage centers on selected compounds defined by specified lists or structural definitions, together with pharmaceutically acceptable salt and/or stereoisomer forms. Across the provided claim families, the inventive features repeatedly include compound selection, pharmaceutical composition embodiments with pharmaceutically acceptable excipients, and a method directed to modulating cannabinoid 2 receptor (CB2R) activity in a mammal by administration. In total, the consolidated claim set reflects 3 core inventive feature types.
Selected compound with pharmaceutically acceptable salt or stereoisomer
A compound selected from a specified list or defined by the patent scope, including a pharmaceutically acceptable salt or stereoisomer thereof.
Pharmaceutical composition with pharmaceutically acceptable excipients
A pharmaceutical composition comprising the selected compound, or a pharmaceutically acceptable salt or stereoisomer thereof, together with at least one pharmaceutically acceptable excipient.
Modulating cannabinoid 2 receptor activity in a mammal
A method of modulating cannabinoid 2 receptor (CB2R) activity in a mammal by administering the selected compound, or a pharmaceutically acceptable salt or stereoisomer thereof.
The claim coverage is concentrated on selected substituted naphthyridine-based compounds and related scaffold compounds, extended to pharmaceutically acceptable salts and stereoisomers, with dependent coverage for pharmaceutical compositions containing pharmaceutically acceptable excipients and a CB2R modulation method in a mammal.
Stated Advantages
Restoring anti-tumor immune function in cancer treatment via CB2R modulation.
Documented Applications
Modulating cannabinoid 2 receptor (CB2R) activity in a mammal by administering the selected compound or a pharmaceutically acceptable salt or stereoisomer thereof.
Treating CB2-mediated disease/disorder.
Treating cancer, including solid tumors.
Treating cancer in combination with immune checkpoint inhibitors.
Pharmaceutical compositions comprising the claimed compound, or its pharmaceutically acceptable salt or stereoisomer, with pharmaceutically acceptable excipients.
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