Conjugates and methods of using the same
Inventors
PECK, Spencer Cory • Taylor, Steven John • BOGART, Elijah Lane • DOUD, Devin Forest Reed • IM, Joo Hyun • ISAAC, Dervla Tamara • Liu, Jenny • MASSARI, Ferdinand Edward • MYERS, Robert Walter • Proudfoot, John Robert • Ross, Cheri • CASEY, JR., John Patrick • Berry, David Arthur
Assignees
Flagship Pioneering Innovations V Inc • Flagship Pioneering Inc • Senda Biosciences Inc
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Publication Number
US-11998610-B2
Publication Date
2024-06-04
Expiration Date
Abstract
Disclosed are conjugates including a recognition element covalently bonded to or linked through a linker to a payload. The payload is a pharmaceutical agent (e.g., an antineoplastic agent, anti-infective agent, or anti-inflammatory agent) or a diagnostic agent. Also disclosed are methods of using the conjugates.
Core Innovation
The invention relates to a conjugate or pharmaceutically acceptable salt thereof comprising a specified structure. The conjugate comprises a recognition element covalently linked to a payload pharmaceutical agent or diagnostic agent by a linker, including ester bond, amide bond, thioester bond, glycosidic bond, carbonate linker, carbamate linker, and urea linker, including traceless linker concepts and in vivo cleavage concepts.
The recognition element is microorganism/protein-recognizable and includes a broad fatty-acyl/amide group of formula R1-L-, including D-amino acid residues and listed specific recognition groups. The payload pharmaceutical agent or diagnostic agent includes anti-infective agents such as aminoglycosides, beta-lactams, vancomycin-class agents, macrolides, fluoroquinolones, and additional antibacterial, antifungal, and antiprotozoal agents.
The disclosure further includes multiple specific conjugate examples and characterization data, including LCMS with M+H+ and 1H NMR, as well as in vitro stability evaluations in simulated gastric fluid, simulated intestinal fluid, and colonic material. It also describes enzyme-related conversion associated with bacterial enzymes, including clbP, and cell-based and fecal-matter cleavage or efficacy evaluations.
Claims Coverage
The provided material identifies one independent claim covering a conjugate or pharmaceutically acceptable salt thereof with a specified structure, and dependent claim coverage adding a pharmaceutical composition comprising the conjugate or salt and a pharmaceutically acceptable excipient. The inventive features described in the available content focus on the defined conjugate structure and the pharmaceutical composition format.
Conjugate with covalently linked recognition element, linker, and payload or diagnostic agent
A conjugate or pharmaceutically acceptable salt thereof comprising a recognition element covalently linked via a specified linker to a payload or diagnostic agent, including linker chemistries selected from ester bond, amide bond, thioester bond, glycosidic bond, carbonate linker, carbamate linker, and urea linker, including traceless linker concepts and in vivo cleavage concepts.
Pharmaceutical composition including the conjugate or salt
A pharmaceutical composition comprising the conjugate or pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipient.
Conjugate structure with specified chemical composition
A conjugate or pharmaceutically acceptable salt thereof comprising the following structure.
Across the available claim set, the scope is centered on a conjugate or pharmaceutically acceptable salt thereof defined by a specified structure, with additional coverage for formulation as a pharmaceutical composition containing a pharmaceutically acceptable excipient.
Stated Advantages
Documented Applications
Delivering payloads including an antineoplastic agent, an anti-infective agent, and an anti-inflammatory agent using the disclosed conjugates.
Modulating disease-associated markers for cancer and infection, including modulating cancer markers and infection markers and/or the microbiome.
Reducing E. coli or Klebsiella pneumoniae as a microbiome-related outcome.
Diagnostic approaches for patient selection by detecting neoplastic cells and bacteria capable of cleaving the conjugate using stool and oral cavity samples and the detection modalities explicitly listed in the document.
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