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US 2025/0049937 A1Published application
Novel auristatin analogs and immunoconjugates thereof
AssigneeAdcentrx Therapeutics Inc.
InventorsRichard Hui Li, Dong Jun Lee
Life of this patent
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Abstract
The invention provides novel auristatin analogs and immunoconjugates thereof, as well as pharmaceutical compositions and methods of preparation and use for treating various diseases and disorders (e.g., cancer).
Claims32
A compound having the structural formula (I):
- or a pharmaceutically acceptable salt thereof,
- wherein
- R1 is
- wherein R2 is a unsubstituted or substituted C1-C6 alkyl, heteroalkyl, cycloalkyl or cycloheteroalkyl;
- each of Ra, Rb and Rc is selected from H and NRxRy, provided that only one of Ra, Rb and Rc is NRxRy and each of the others is H;
- each of Rx and Ry is independently selected from R, Rr and L-Rz, provided that when one of Rx and Ry is L-Rz or Rr, the other is R;
- R5 is H or CR′3, wherein each R′ is independently H or F;
- L is a linker;
- Rr is (C═O)—O—(CH2)p—Rv or (C═O)—(CH2)q—Rv;
- Rv is R, OR, NHR, NR2, an aryl group or an amino acid;
- p is 0, 1, 2, 3, 4, 5 or 6;
- q is 0, 1, 2, 3, 4, 5 or 6;
- Rz comprises a functional or reactive group;
- and
- R is H or a C1-C3 alkyl.
12 more elements
(canceled)
7-11. (canceled)
22-41. (canceled)
44-47. (canceled)
51-56. (canceled)
A compound selected from the table below:
- 1
- 2
- 3
- 4
- 5
- 6
- 7
- 8
- 9
- 10
- 11
- 12, 13
- 14, 15
- 16, 17
- 18, 19
- 20
- 21
- 22
- 23
- 24
- 25
- 26
- 27
- 28
- 29
- 30
23 more elements
An immunoconjugate having the structural formula (VI):
- or a pharmaceutically acceptable salt thereof,
- wherein
- Ab represents an antigen binding moiety;
- R1 is
- wherein R2 is a unsubstituted or substituted C1-C6 alkyl, heteroalkyl, cycloalkyl or cycloheteroalkyl;
- each of Rx and Ry is independently selected from R and L-Rz, provided that when one of Rx and Ry is NRz, the other is R;
- R5 is H or CR′3, wherein each R′ is independently H or F;
- L is a linker;
- and
- R is H or a C1-C3 alkyl;
- i is an integer in the range of 1 to about 20.
8 more elements
61-82. (canceled)
84-89. (canceled)
Dependencies are inferred from the claim text.