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US 12,338,199 B2Granted
Bis-octahydrophenanthrene carboxamides and protein conjugates thereof
AssigneeRegeneron Pharmaceuticals, Inc.
InventorsAmy Han, Andrew J. Murphy, William Olson
Life of this patent
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Abstract
Provided herein are compounds, compositions and methods for the treatment of diseases and disorders associated with the liver X receptor, including bis-octahydrophenanthrene carboxamides and protein (e.g., antibody) drug conjugates thereof.
Claims23
A compound of Formula A
- or a pharmaceutically acceptable salt, or stereoisomeric form thereof, wherein
- L is a linker or X—Y—Z, wherein
- X is —NH— or —O—;
- Y is an enzymatically cleavable moiety;
- a self-immolative group;
- an acid-labile moiety comprising an alkoxamine, ketoxamine, carbonate, or phosphonate;
- PEGn;
- a sugar moiety comprising a glucuronide;
- and/or an enhancement group comprising a cyclodextrin and/or an alkyl, heteroalkyl, alkylenyl, or heteroalkylenyl sulfonic acid;
- and
- Z is a binding agent linker (BL) wherein Z is covalently bound to BA;
- BA is an antibody or antigen binding fragment thereof;
- k ranges from about one to about eight, representing an average number of units of a payload conjugated to BA;
- each of Q1 and Q2 is independently —CH2, C(O)—, —C(H)(OH)—, or —C(OH)2—;
- W is —CH2—, —N(H)—, or —O—;
- R is independently hydrogen, —OH, C1-6 alkyl, or —OP (O)(OR6)(OH);
- and
- each R6 is, independently in each instance, hydrogen, an amino acid residue, a peptide, or alkyl;
- and
- each R7 is independently halo, C1-6 alkyl, C1-6 alkoxy, —CN, O-glucose, O-amino acid residue, or O-PEGn, wherein each n is an integer from zero to three.
17 more elements
Dependencies are inferred from the claim text.