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US 12,691,182 B2Granted
Maytansinoid derivatives, conjugates thereof, and methods of use
AssigneeRegeneron Pharmaceuticals, Inc.
InventorsThomas Nittoli, Thomas P. Markotan
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Abstract
Provided herein are maytansinoid compounds, derivatives thereof, conjugates thereof, and methods of treating or preventing proliferative diseases with the same.
Claims18
A compound of Formula I
- or a pharmaceutically acceptable salt or stereoisomer thereof, wherein:
- A is arylene or heteroarylene;
- L is a linker;
- BA is a binding agent;
- and
- k is an integer from one to ten.
3 more elements
A compound of Formula II
- or a pharmaceutically acceptable salt or stereoisomer thereof,
- in A is a divalent radical of benzene, pyridine, naphthalene, or quinolone.
A compound of Formula P1
- wherein A is a divalent radical of benzene, pyridine, naphthalene, or quinolone;
- and RL is a reactive linker.
A compound of Formula PPII
- wherein A is a divalent radical of benzene, naphthalene, or quinolone.
A method of preparing a compound of Formula I
- comprising contacting a compound of P1
- with a binding agent under conjugation conditions, wherein
- A is a divalent radical of benzene, pyridine, naphthalene, or quinolone;
- L is a linker;
- BA is a binding agent;
- k is an integer from one to ten;
- and
- RL is a reactive linker.
5 more elements
A method of making a compound of Formula II
- wherein
- A is a divalent radical of benzene, pyridine, naphthalene, or quinolone comprising:
- (a) contacting a compound of Formula P2
- with a compound of Formula PP6
- under Lewis acid synthesis conditions to form a compound of Formula PPII
- and
- (b) reducing the compound of Formula PPII by contacting the compound of Formula PPII with a reducing agent to form the compound of Formula II.
4 more elements
A method of making a compound of Formula PPII, comprising contacting a compound of Formula P2 with a compound of Formula PP6 under Lewis acid synthesis conditions
- wherein A is a divalent radical of benzene, naphthalene, or quinolone.
Dependencies are inferred from the claim text.