IP Library › Granted Patent US 12,583,838
Granted Patent B2
US 12,583,838 · App. 17/817,853 · Granted Mar 24, 2026

Analogs for the treatment of disease

Inventors: Aleksandrs Zavoronkovs (Hong Kong, CN); Aleksandr Aliper (Ramenskoye, RU); Vladimir Aladinskiy (Kaliningrad, RU); Andrey Kukharenko (Moscow, RU)
Assignee: INSILICO MEDICINE HONG KONG LIMITED
C07D403/04A61P11/00A61P13/12C07D233/90C07D401/04C07D403/14C07D405/04C07D487/08
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Quick Facts
Patent No.
US 12,583,838
App. No.
17/817,853
Granted
Mar 24, 2026
Kind
B2
Abstract

The disclosure provides TNIK and/or MAP4K4 kinases inhibitors for the treatment of disease. In one aspect, disclosed herein are kinase inhibitors having a structure of Formula (A), (A*), (I), (IIA), or (IIB). Further described herein are pharmaceutical composition comprising these compounds and methods of using these compounds. In one aspect, disclosed herein are methods of treating a disease or condition by administering the kinases inhibitors described herein.

Claims (18)

1 . A compound represented by Formula (IIA),

or a pharmaceutically acceptable salt thereof, wherein:

R 1 is selected from

substituted C 1 -C 6 alkyl, wherein the C 1 -C 6 alkyl is substituted with one or more substituents selected from halogen, —OH, —CN, —NO 2 , —NH 2 , oxo, ═S, —C 1-10 haloalkyl, —O—C 1-10 alkyl, —O—C 1-6 alkyl-O—C(O)(O—C 1-10 alkyl), C 2-10 alkenyl, C 2-10 alkynyl, C 3-12 carbocycle, and 3- to 12-membered heterocycle; and

3 to 8-membered heterocycle, wherein the 3 to 8-membered heterocycle is optionally substituted with one or more substituents selected from halogen, —OH, —CN, —NO 2 , —NH 2 , oxo, ═S, —S(O 2 )NH 2 , —C 1-10 haloalkyl, —O—C 1-10 alkyl, C 2-10 alkenyl, C 2-10 alkynyl, C 3-12 carbocycle, 3- to 12-membered heterocycle, and optionally substituted C 1-10 alkyl, wherein the C 1-10 alkyl is optionally substituted with one or more substituents selected from hydroxy, halogen, oxo, —C 1-10 haloalkyl, —NH 2 , —CN, and —NO 2 ;

R 3 is phenyl, which is optionally substituted with one or more substituents selected from halogen, —OH, —CN, —NO 2 , —NH 2 , exe, —S, C 1-6 alkyl, and —C 1-10 haloalkyl; and

R 4 is non-halogenated C 1 -C 6 alkyl.

2 . The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 4 is selected from

3 . The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 3 is substituted phenyl, and wherein the phenyl is substituted with one or more substituents selected from halogen and —C 1-10 haloalkyl.

4 . The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 1 is substituted C 1 -C 6 alkyl, wherein the C 1 -C 6 alkyl is substituted with one or more substituents selected from halogen, —OH, —CN, —NO 2 , —NH 2 , oxo, ═S, —C 1-10 haloalkyl, —O—C 1-10 alkyl, —O—C 1-6 alkyl-O—C(O)(O—C 1-10 alkyl), C 2-10 alkenyl, C 2-10 alkynyl, C 3-12 carbocycle, and 3- to 12-membered heterocycle.

5 . The compound of claim 4 , or a pharmaceutically acceptable salt thereof, wherein R 1 is substituted with one or more substituents selected from oxo, halogen, —O—C 1-10 alkyl, —C 1-10 haloalkyl, and —OH.

6 . The compound of claim 4 , or a pharmaceutically acceptable salt thereof, wherein R 1 is substituted with one or more substituents selected from —OH, oxo, and —O—C 1-10 alkyl.

7 . The compound of claim 4 , or a pharmaceutically acceptable salt thereof, wherein R 1 is

8 . The compound of claim 4 , or a pharmaceutically acceptable salt thereof, wherein R 1 is

9 . The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R1 is an optionally substituted bicyclic heterocycle.

10 . The compound of claim 9 , or a pharmaceutically acceptable salt thereof, wherein R 1 is an optionally substituted bridged bicyclic heterocycle.

11 . The compound of claim 9 , or a pharmaceutically acceptable salt thereof, wherein R 1 is

12 . A pharmaceutical composition comprising (i) a compound of claim 1 or a pharmaceutically acceptable salt thereof; and (ii) a pharmaceutically acceptable excipient.

Assignments (4)
CORRECTIVE ASSIGNMENT TO CORRECT THE ASSIGNEE ADDRESS PREVIOUSLY RECORDED ON REEL 62647 FRAME 187. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT OF ASSIGNORS INTEREST. Recorded Oct 22, 2025
From: INSILICO MEDICINE HONG KONG LIMITED
To: INSILICO MEDICINE IP LIMITED
Reel/Frame 073154/0989 →
CORRECTIVE ASSIGNMENT TO CORRECT THE ASSIGNEE COUNTRY PREVIOUSLY RECORDED ON REEL 62633 FRAME 126. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT OF ASSIGNORS INTEREST. Recorded Oct 22, 2025
From: ZAVORONKOVS, ALEKSANDRS; ALIPER, ALEKSANDR; ALADINSKIY, VLADIMIR; KUKHARENKO, ANDREY
To: INSILICO MEDICINE HONG KONG LIMITED
Reel/Frame 073155/0115 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 9, 2023
From: INSILICO MEDICINE HONG KONG LIMITED
To: INSILICO MEDICINE IP LIMITED
Reel/Frame 062647/0187 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 8, 2023
From: ZAVORONKOVS, ALEKSANDRS; ALIPER, ALEKSANDR; ALADINSKIY, VLADIMIR; KUKHARENKO, ANDREY
To: INSILICO MEDICINE HONG KONG LIMITED
Reel/Frame 062633/0126 →
Priority Claims (2)
WO PCT/CN2021/077706 · Feb 24, 2021 · international
WO PCT/CN2021/142622 · Dec 29, 2021 · international
Continuity (2)
Continuation 17678301 · Feb 23, 2022
Related Publication 20230116632A1 · Apr 13, 2023
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