IP Library Granted Patent US 12,668,571
Granted Patent B2
US 12,668,571 · App. 18/020,492 · Granted Jun 30, 2026

Substituted 3-amino-4-methylbenzenesulfonamides as small molecule inhibitors of ubiquitin-specific protease 28

Inventors: Sara Buhrlage (Somerville, MA); Anthony Varca (Brookline, MA); Bin Hu (Natick, MA)
Assignee: Dana-Farber Cancer Institute, Inc.
C07C311/46C07C233/65C07C317/40C07D233/61C07D295/108C07D295/135C07D295/26
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Quick Facts
Patent No.
US 12,668,571
App. No.
18/020,492
Granted
Jun 30, 2026
Kind
B2
Abstract

The present disclosure relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof and pharmaceutical composition comprising the compound of formula (I). The present composition also relates to methods treating a disease or disorder associated with ubiquitin-specific protease 28 (USP28), methods of treating cancer, and methods of inhibiting USP28.

Claims (38)

1 . A compound of formula (I)

or a pharmaceutically acceptable salt thereof, wherein, independently for each occurrence,

X 1 is —S(O) 2 R 1 or —C(═O)NR 8 (C 1-3 alkyl), wherein C 1-3 alkyl is optionally substituted with one or more C 6-10 aryl;

R 1 is C 1-2 alkyl or —NR 4 R 5 ;

R 4 is H or C 1-3 alkyl;

R 5 is C 1-3 alkyl or C 6-10 aryl, or

R 4 and R 5 , together with the nitrogen atom to which they are attached, optionally form a C 5-8 heterocyclyl;

R 2 is C 1-3 alkyl, —OR 6 , or halogen;

R 6 is H, C 1-3 alkyl, or —C(halogen) 3 ;

Z 1 is —C(═O)— or —NR 8 —;

each R 8 is independently H or C 1-3 alkyl;

Z 2 is —C(═O)— or —NR 8 —, or

R 2 , Z 2 , and Z 1 , taken together with the atoms to which they are attached, form a C 5-6 heteroaryl,

Z 3 is absent or C 1-3 alkylene; and

R 3 is C 6-10 aryl, C 5-6 heteroaryl, or C 5-8 heterocyclyl, wherein R 3 is substituted with one or more groups independently selected from C 1-3 alkyl, C 5-8 heterocyclyl, —OH, halogen, —NHC(═O)(C 1-3 alkyl), and —NH(C 1-3 alkyl); and wherein

each C 1-3 alkyl, C 6-10 aryl, C 5-6 heteroaryl, and C 5-8 heterocyclyl is independently optionally substituted with one or more groups independently selected from C 1-3 alkyl, C 6-10 aryl, C 5-8 heterocyclyl, halogen, —C(halogen) 3 , —OH, —NO 2 , —NHC(═O) (C 1-3 alkyl), and —NH(C 1-3 alkyl);

provided the compound is not

2 . The compound of claim 1 , wherein the compound is a compound of formula (II)

3 . The compound of claim 1 , wherein R 4 is H.

4 . The compound of claim 1 , wherein R 4 is C 1-3 alkyl.

5 . The compound of claim 1 , wherein R 5 is C 1-3 alkyl.

6 . The compound of claim 1 , wherein R 4 and R 5 , together with the nitrogen atom to which they are attached, form a C 5-8 heterocyclyl.

7 . The compound of claim 1 , wherein R 5 is C 1-3 alkyl substituted with one or more C 6-10 aryl.

8 . The compound of claim 1 , wherein R 5 is C 6-10 aryl optionally substituted with one or more groups independently selected from C 1-3 alkyl, C 6-10 aryl, C 5-8 heterocyclyl, halogen, —C(halogen) 3 , —OH, —NO 2 , —NHC(═O)(C 1-3 alkyl), and —NH(C 1-3 alkyl).

9 . The compound of claim 1 , wherein R 2 is C 1-3 alkyl.

10 . The compound of claim 1 , wherein R 2 is halogen.

11 . The compound of claim 1 , wherein Z 3 is C 1-2 alkylene.

12 . The compound of claim 1 , wherein R 3 is C 6-10 aryl, substituted with one or more groups independently selected from C 1-3 alkyl, C 5-8 heterocyclyl, —OH, halogen, —NHC(═O)(C 1-3 alkyl), and —NH(C 1-3 alkyl).

13 . The compound of claim 12 , wherein R 3 is substituted with one or more halogen.

14 . The compound of claim 1 , wherein R 3 is

15 . The compound of claim 1 , wherein the compound is selected from

or a pharmaceutically acceptable salt thereof.

16 . A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier.

17 . A method of treating a disease or disorder associated with ubiquitin-specific protease 28 (USP28), comprising administering to a subject in need thereof a compound of claim 1 , or a pharmaceutically acceptable salt thereof.

18 . The method of claim 17 , wherein the disease or disorder associated with USP28 is cancer.

19 . A compound, or a pharmaceutically acceptable salt thereof, selected from:

20 . A method of treating a disease or disorder associated with ubiquitin-specific protease 15 (USP28), comprising administering to a subject in need thereof a compound, or a pharmaceutically acceptable salt thereof, selected from:

21 . The method of claim 20 , wherein the disease or disorder associated with USP28 is cancer.