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US 2024/0190841 A1Published application
Modulators of bcl6 proteolysis and associated methods of use
AssigneeArvinas Operations, Inc.
InventorDan SHERMAN
Life of this patent
Estimating the term…
Abstract
This disclosure pertains to bifunctional compounds, the preparation thereof, and the use of these bifunctional compounds in the treatment of diseases or disorders that result from aggregation or accumulation of B-cell lymphoma 6 protein, in subjects in need thereof.
Claims29
A bifunctional compound of Formula (I), Formula (II), or Formula (III):
- or a pharmaceutically acceptable salt thereof, wherein:
- R1 is H or C1-C6 alkyl;
- Q is
- X is N or CH;
- Y1, Y2, and Y3 are each, independently, N or CR3;
- Z1 and Z2 are each, independently, N or CH;
- R2 is H or C1-C6 alkyl;
- each R3 is, independently, H, halogen, C1-C6 alkyl, C1-C6 haloalkyl, —O—(C1-C6 alkyl), —O—(C1-C6 haloalkyl);
- of the Q indicates the point of attachment with the X or the glutarimide;
- R1a is H or halogen;
- R2a is H or C1-C3 alkyl;
- X3a is CHR3a or C(O);
- R3a is H or C1-C3 alkyl;
- X4a and X6a are each independently CH or N;
- R5a is H, C1-C3 alkyl or halogen;
- L is
- R6b is CHR6b or C(O);
- R6b is H or C1-C3 alkyl;
- R1b, R2b, R3b, and R4b are each independently H or halogen, wherein at least one of R1b, R2b, R3b, R4b is halogen;
- R5b is H or halogen;
- X1b and X2b are each independently CH or N, wherein at least one of X1b and X2b is N;
- and
- wherein each of L indicates a point of attachment.
20 more elements
A bifunctional compound of Formula (I), Formula (II), or Formula (III):
- wherein:
- R1 is H or C1-C6 alkyl;
- Q is
- X is N or CH;
- Y1, Y2, and Y3 are each, independently, N or CR3;
- Z1 and Z2 are each, independently, N or CH;
- R2 is H or C1-C6 alkyl;
- each R3 is, independently, H, halogen, C1-C6 alkyl, C1-C6 haloalkyl, —O—(C1-C6 alkyl), or —O—(C1-C6 haloalkyl);
- of the Q indicates the point of attachment with the X or the glutaramide;
- R1a is H or halogen;
- R2a is H or C1-C3 alkyl;
- X3a is CHR3a or C(O);
- R3a is H or C1-C3 alkyl;
- X4a and X6a are each independently CH or N;
- R5a is H, C1-C3 alkyl or halogen;
- L is
- X6b is CHR6b or C(O);
- R6b is H or C1-C3 alkyl;
- R1b, R2b, R3b, and R4b are each independently H or halogen, wherein at least one of R1b, R2b, R3b, R4b is halogen;
- R5b is H or halogen;
- X1b and X2b are each independently CH or N, wherein at least one of X1b and X2b is N;
- and
- wherein each of L indicates a point of attachment.
20 more elements
A bifunctional compound that is selected from any one of the compounds in Table 1, or a pharmaceutically acceptable salt thereof.
(canceled)
Dependencies are inferred from the claim text.