IP Library › Granted Patent US 12,358,887
Granted Patent B2
US 12,358,887 · App. 18/184,335 · Granted Jul 15, 2025

IKAROS Zinc Finger Family degraders and uses thereof

Inventors: Gayatri Balan (Bellevue, WA); Peter A. Blomgren (Issaquah, WA); Chen Chen (Newark, CA); Julian A. Codelli (Mountlake Terrace, WA); Zhimin Du (Belmont, CA); Musong Kim (Bellevue, WA); Dorothée Saddier Axe (San Carlos, CA); Gregg M. Schwarzwalder (Redwood City, CA); Rhiannon Thomas-Tran (San Jose, CA); Michael T. Tudesco (Chapel Hill, NC); Chandrasekar Venkataramani (San Carlos, CA); William J. Watkins (Saratoga, CA); Brian M. Weist (Dublin, CA); Suet C. Yeung (Redmond, WA); Helen Yu (Mountain View, CA)
Assignee: Gilead Sciences, Inc.
C07D401/04C07B2200/05
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Quick Facts
Patent No.
US 12,358,887
App. No.
18/184,335
Granted
Jul 15, 2025
Kind
B2
Abstract

The present disclosure relates generally to compounds that bind to and act as degraders of an IKAROS Family Zinc Finger (IKZF) protein, such as IKZF2 (Helios) and/or IKZF4 (Eos). The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding and degradation of an IKZF protein, such as IKZF2 and/or IKZF4, including cancer.

Claims (16)

1. A compound of Formula (V):

or a pharmaceutically acceptable salt thereof,

wherein

R 2 is —H or —F;

R 21 is —H or —F;

R 3 is —H or —F;

R 7 is C 1-8 alkyl or C 3-12 cycloalkyl,

wherein each C 1-8 alkyl or C 3-12 cycloalkyl of R 7 is optionally substituted with one to four Z 2 ,

which may be the same or different; and

each Z 2 is independently deuterium, halogen, C 1-3 alkyl, C 1-3 haloalkyl, or C 6-10 aryl.

2. The compound or pharmaceutically acceptable salt thereof of claim 1 , wherein the compound of Formula (V) is a compound of Formula (Va):

3. The compound or pharmaceutically acceptable salt thereof of claim 1 , wherein R 2 is —H; R 21 is —H; and R 3 is —H or —F.

4. The compound or pharmaceutically acceptable salt thereof of claim 1 , wherein R 7 is C 1-8 alkyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, spiro [2.3]hexyl, bicyclo[3.1.1]heptyl, spiro [3.3]heptyl, spiro [2.5]octyl, bicyclo[3.2.1]octyl, (1R,5S) bicyclo[3.1.0]hexyl, (1R,5S) bicyclo[3.2.0]heptyl, or spiro [2.4]heptyl, each optionally substituted with 1 to 3 Z 2 , which may be the same or different, wherein each Z 2 is independently deuterium, —CH 3 , —C 2 F, —CHF 2 , —CF 3 , —F, or phenyl.

5. The compound or pharmaceutically acceptable salt thereof of claim 1 , wherein R 7 is C 1-3 alkyl or cyclohexyl, each optionally substituted with 1 to 2 Z 2 , which may be the same or different, wherein each Z 2 is independently —F or phenyl.

6. The compound or pharmaceutically acceptable salt thereof of claim 1 , wherein R 7 is

7. A pharmaceutical composition comprising a therapeutically effective amount of the compound of claim 1 , or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 12, 2023
From: BALAN, GAYATRI; BLOMGREN, PETER A.; CHEN, CHEN; CODELLI, JULIAN A.; DU, ZHIMIN; KIM, MUSONG; SADDIER AXE, DOROTHÉE; SCHWARZWALDER, GREGG M.; THOMAS-TRAN, RHIANNON; TUDESCO, MICHAEL T.; VENKATARAMANI, CHANDRASEKAR; WATKINS, WILLIAM J.; WEIST, BRIAN M.; YEUNG, SUET C.; YU, HELEN
To: GILEAD SCIENCES, INC.
Reel/Frame 063926/0657 →
Continuity (3)
Provisional Application 63386605 · Dec 8, 2022
Provisional Application 63321030 · Mar 17, 2022
Related Publication 20230373950A1 · Nov 23, 2023
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