Back to results
US 2023/0227418 A1Published application
Usp9x inhibitors
AssigneeProDeg, LLC
InventorsRichard Martinelli, Julian F. Bond
Life of this patent
Estimating the term…
Abstract
The invention relates to compounds that inhibit DUBs, particularly USP9X. The invention also includes methods of inhibiting DUBs, including USP9X, and methods of treating cancers.
Claims37
A compound represented by Formula (I):
- or optionally by a formula with a linear backbone structure obtained by breaking a carbon-carbon or carbon-nitrogen single bond on the cyclic backbone of Formula (I) at any site, and pharmaceutically acceptable salts thereof,
- wherein R1 and R10 are each independently selected from H, 2H, and substituted or unsubstituted alkyl;
- R2, R3, R4, R6, and R7 are each independently selected from H, 2H, halogen, substituted or unsubstituted alkyl, and substituted or unsubstituted alkoxy;
- and optionally, R3 and R4 together form a substituted or unsubstituted 5- or 6-membered heterocyclic ring;
- R5 and R9 are each independently selected from H, 2H, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, and one or more aryl substituents, such as halogen;
- R8 is absent, or substituted or unsubstituted 1- to 4-carbon alkylene;
- R11 is a hydrophobic alkyl selected from substituted or unsubstituted alkyl, and substituted or unsubstituted cycloalkyl;
- Z1, Z2, and Z3 are each independently selected from CH and N;
- X1 is selected from —O—, —S—, —NH—, —CH2—;
- X2 is absent, or selected from -L-NRA—, -L-NRAC(O)—, -L-C(O)—, -L-OC(O)—, -L-C(O)O—, -L-CH(COORA)—, -L-C(O)NRA-L-, -L-C(O)NRAC(O)—, wherein RA is selected from H, 2H, substituted or unsubstituted alkyl;
- and optionally, RA, R8, and X2 together with the aryl to which R8 is attached to form a substituted or unsubstituted 5- or 6-membered heterocyclic ring;
- L is a linker group —(CH2)nCRBRC(CH2)n—, wherein RB and RC are each independently selected from H, 2H, substituted or unsubstituted alkyl;
- or RB and RC together with the carbon to which they are attached form a substituted or unsubstituted C3-C6 cycloalkyl, or a substituted or unsubstituted 3- to 6-membered heterocyclic ring;
- and wherein each n is independently 0, 1, or 2;
- and m=0, 1, 2, 3, or 4.
12 more elements
A compound represented by Formula (II) or (III):
- and pharmaceutically acceptable salts thereof,
- wherein R1, R2, R3, R4, R5, R6, R7, and R8 are independently hydrogen or a substituted or unsubstituted alkyl,
- R9, and R10 are independently hydrogen, substituted or unsubstituted alkyl, or substituted or unsubstituted acyl,
- L is a linker group, such as a substituted or unsubstituted, saturated or unsaturated 1 to 10 carbon alkyl,
- Z1, Z2, and Z3 are independently selected from N or CH,
- X1, X2, X3 are independently H or one or more aryl substituents, such as a halogen, e.g., fluorine,
- n and m are independently 0 or an integer, such as 1, 2, 3, 4, or 5.
4 more elements
(canceled)
(canceled)
(canceled)
(canceled)
37-38. (canceled)
Dependencies are inferred from the claim text.