IP Library › Granted Patent US 12,624,030
Granted Patent B2
US 12,624,030 · App. 18/268,577 · Granted May 12, 2026

4-amino-3-(4-phenoxyphenyl)-1,3-dihydro-2H-imidazo[4,5-c]pyridin-2-one derivatives and salts thereof

Inventors: Catherine Arabeyre (Prades le Lez, FR); Patricia Moliner (Perols, FR); Sabine Boisnard (Boulogne, FR); Damien Sallaberry (Le Plessis Robinson, FR); Serge Perard (Palaiseau, FR); Sebastien Roy (Sermaise, FR)
Assignee: Principia Biopharma Inc.
C07D471/04
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Quick Facts
Patent No.
US 12,624,030
App. No.
18/268,577
Granted
May 12, 2026
Kind
B2
Abstract

The present disclosure relates to 4-amino-3-(4-phenoxyphenyl)-1,3-dihydro-2H-imidazo[4,5-c]pyridin-2-one variants or derivatives, and salts thereof, for use as agonists and antagonists. The disclosure further relates to compositions, methods of preparing, and methods of treatment.

Claims (43)

1 . A compound of Formula Ia:

or a salt thereof, wherein the compound or salt thereof is about 90% pure.

2 . The compound of claim 1 , wherein the compound or salt thereof is about 95% pure.

3 . The compound of claim 1 , wherein the compound or salt thereof is about 98% pure.

4 . A compound of Formula Ib:

or a salt thereof, wherein the compound or salt thereof is about 90% pure.

5 . The compound of claim 4 , wherein the compound or salt thereof is about 95% pure.

6 . The compound of claim 4 , wherein the compound or salt thereof is about 98% pure.

7 . The compound of claim 4 , the compound or salt thereof is about 99% pure.

8 . A compound of Formula II

or salt thereof, wherein the compound or salt thereof is about 99.6% pure.

9 . The compound of claim 8 , wherein the compound is

or salt thereof, wherein the compound or salt thereof is about 90% pure.

10 . The compound of claim 9 , wherein the compound of Formula IIa or salt thereof is about 95% pure.

11 . The compound of claim 9 , wherein the compound of Formula IIa or salt thereof is about 98% pure.

12 . The compound of claim 8 , wherein the compound is

or salt thereof, wherein the compound or salt thereof is about 90% pure.

13 . The compound of claim 12 , wherein the compound of Formula IIb or salt thereof is about 95% pure.

14 . The compound of claim 12 , wherein the compound of Formula IIb or salt thereof is about 98% pure.

15 . A composition comprising a pharmaceutically acceptable excipient and at least one compound chosen from:

or salts thereof.

16 . The composition of claim 15 , wherein at least one compound is a compound of Formula Ia or a salt thereof, and wherein the compound of Formula Ia or a salt thereof is at least about 98% pure.

17 . The composition of claim 15 , wherein at least one compound is a compound of Formula Ib or a salt thereof, and wherein the compound of Formula Ib or salt thereof is at least about 99% pure.

18 . The composition of claim 15 , wherein the composition is in the form of a capsule, tablet, or pill.

19 . A method of preparing the compound of Formula Ia of claim 1 or salt thereof,

the method comprising reacting a compound of Formula VIa

with acryloyl chloride.

20 . The method of claim 19 , wherein the method further comprises preparing a compound of Formula VIa from a compound of Formula IX

by acid-based deprotection.

21 . A method of preparing the compound of Formula Ib of claim 4 or salt thereof,

the method comprising reacting a compound of Formula VIb

with acryloyl chloride.

22 . The method of claim 21 , wherein the method further comprises preparing a compound of Formula VIb from a compound of Formula VII

by acid-based deprotection.

23 . The method of claim 22 , wherein the method further comprises preparing a compound of Formula VII from a compound of Formula VIII

by deprotection using a base.

24 . The method of claim 23 , wherein the method further comprises preparing a compound of Formula VIII from a compound of Formula IX

with triphenylphosphine and an azodicarboxylate.

25 . The method of claim 24 , wherein the azodicarboxylate is chosen from diethyl azodicarboxylate and diisopropyl azodicarboxylate.

26 . The composition of claim 15 , wherein at least one compound is a compound of Formula Ia or a salt thereof.

27 . The composition of claim 15 , wherein at least one compound is a compound of Formula Ib or a salt thereof.

28 . The composition of claim 15 , wherein at least one compound is a compound of Formula II or a salt thereof.

29 . The composition of claim 15 , wherein at least one compound is a compound of Formula III or a salt thereof.

Assignments (4)
ASSIGNEE CHANGE OF ADDRESS Recorded Sep 16, 2025
From: PRINCIPIA BIOPHARMA INC.
To: PRINCIPIA BIOPHARMA INC.
Reel/Frame 072881/0270 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 11, 2024
From: ARABEYRE-FABRE, CATHERINE; MOLINER, PATRICIA; BOISNARD, SABINE; SALLABERRY, DAMIEN; PERARD, SERGE; ROY, SEBASTIEN
To: SANOFI-AVENTIS RECHERCHE & DEVELOPPEMENT
Reel/Frame 067695/0216 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 11, 2024
From: SANOFI-AVENTIS RECHERCHE & DEVELOPPEMENT
To: GENZYME CORPORATION
Reel/Frame 067695/0245 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 11, 2024
From: GENZYME CORPORATION
To: PRINCIPIA BIOPHARMA INC.
Reel/Frame 067694/0242 →
Continuity (3)
Provisional Application 63245288 · Sep 17, 2021
Provisional Application 63130010 · Dec 23, 2020
Related Publication 20240051955A1 · Feb 15, 2024
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