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US 10,159,745 B2Granted
Tubulysin derivatives
AssigneeMedImmune, LLC
InventorsLakshmaiah Gingipalli, Dorin Toader, Fengjiang Wang
Life of this patent
Estimating the term…
Abstract
Novel tubulysin derivatives which may be useful as cytotoxic agents to provide therapeutic benefits in the treatment of various types of cancers, alone, as drug conjugates or in combination with other chemotherapies are provided.
Claims18
A method of making an antibody-drug conjugate comprising:
- contacting an antibody with a compound of Formula (II):
- or a pharmaceutically acceptable salt thereof, wherein:
- R1 is CH3 or CH2CH3;
- R2 is H or CH3;
- R4 is CH3, (CH2)4NH2, or (CH2)3NHC(═O)NH2;
- R5 is H or CH(CH3)(CH3);
- R6 is NHC(═O) or CH2;
- n is 1 or 2;
- and
- m is 0, 1, 2, or 3;
- under conditions sufficient to covalently conjugate the compound of Formula (II) to the antibody.
8 more elements
A method of making an antibody-drug conjugate comprising:
- contacting an antibody with a compound of Formula (IIiv):
- or a pharmaceutically acceptable salt thereof,
- under conditions sufficient to covalently conjugate the compound of Formula (IIiv) to the antibody.
A method of treating cancer by administering to a subject suffering from cancer, an effective amount of an antibody-drug conjugate which is a conjugate of a compound of the Formula (IIi):
- of the Formula (IIii):
- of the Formula (IIiii):
- or of the Formula (IIiv):
Dependencies are inferred from the claim text.