Antibody drug conjugates
AssigneeTakeda Pharmaceutical Company Limited
InventorsHe XU, Hong Myung LEE, Christopher ARENDT
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Abstract
The present disclosure provides antibody drug conjugates comprising STING modulators. Also provided are compositions comprising the antibody drug conjugates. The compounds and compositions are useful for stimulating an immune response in a subject in need thereof.
Claims35
A method of treating cancer in a subject in need thereof, the method comprising administering to the subject a pharmaceutically acceptable amount of a compound of the formula:
- or a pharmaceutically acceptable salt thereof, wherein:
- a is an integer from 1 to 8;
- Ab is an anti-CCR2 antibody or an anti-CCR2 antigen-binding fragment;
- R2′ is C1-C4alkyl;
- W is selected from:
- wherein
- is the point of attachment to the carbonyl group;
- and
- is the point of attachment to Z;
- Z is Ala-Val or Val-Ala;
- U is
- wherein
- p is an integer from 1 to 6;
- q is an integer from 1 to 20;
- is the point of attachment to Z;
- is the point of attachment to Q;
- Q is selected from
- wherein
- is the point of attachment to U;
- is the point of attachment to Ab;
- and
- D is
- wherein:
- R1 and R2 are each independently a hydroxy group or a halogen atom;
- B1 is:
- wherein
- R18 is hydrogen or C1-6 alkyl;
- R19 is a halogen atom;
- and
- is the point of attachment to D;
- and
- B2 is:
- wherein
- is the point of attachment to D;
- and
- is the point of attachment to the parent molecular moiety;
- and
- Q2 and Q4 are each independently an oxygen atom or a sulfur atom.
A method for stimulating an immune response in a subject in need thereof, the method comprising administering to the subject a pharmaceutically acceptable amount of a compound of the formula:
- or a pharmaceutically acceptable salt thereof, wherein:
- a is an integer from 1 to 8;
- Ab is an anti-CCR2 antibody or an anti-CCR2 antigen-binding fragment;
- R2′ is C1-C4alkyl;
- W is selected from:
- wherein
- is the point of attachment to the carbonyl group;
- and
- is the point of attachment to Z;
- Z is Ala-Val or Val-Ala;
- U is
- wherein
- p is an integer from 1 to 6;
- q is an integer from 1 to 20;
- is the point of attachment to Z;
- is the point of attachment to Q;
- Q is selected from
- wherein
- is the point of attachment to U;
- is the point of attachment to Ab;
- and
- D is
- wherein:
- R1 and R2 are each independently a hydroxy group or a halogen atom;
- B1 is:
- wherein
- R18 is hydrogen or C1-6 alkyl;
- R19 is a halogen atom;
- and
- is the point of attachment to D;
- and
- B2 is:
- wherein
- is the point of attachment to D;
- and
- is the point of attachment to the parent molecular moiety;
- and
- Q2 and Q4 are each independently an oxygen atom or a sulfur atom.
Dependencies are inferred from the claim text.