IP Library Granted Patent US 11,771,711
Granted Patent B2
US 11,771,711 · App. 17/966,504 · Granted Oct 3, 2023

Substituted pyridines as DNMT1 inhibitors

Inventors: Andrew B. Benowitz (Stevenage, GB); David T. Fosbenner (Collegeville, PA); Bryan Wayne King (Collegeville, PA); Stuart Paul Romeril (Collegeville, PA)
Assignee: GlaxoSmith Kline Intellectual Property Development Limited
A61K31/675A61K31/44A61P35/02C07D213/85C07F9/58C07B2200/13
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Quick Facts
Patent No.
US 11,771,711
App. No.
17/966,504
Granted
Oct 3, 2023
Kind
B2
Abstract

The invention relates to substituted pyridine derivatives that are inhibitors of the activity of DNA methyltransferase 1 (DNMT1). The invention also relates to pharmaceutical compositions comprising such compounds and methods of using such compounds in the treatment of cancer, pre-cancerous syndromes, beta haemoglobinopathy disorders, and other diseases associated with inappropriate DNMT1 activity.

Claims (21)

1. A compound of formula (I)

or a prodrug or a pharmaceutically acceptable salt thereof.

2. A compound of formula (II)

or a prodrug or a pharmaceutically acceptable salt thereof.

3. A compound of formula (IV)

or a pharmaceutically acceptable salt thereof.

4. A compound of formula (V)

or a pharmaceutically acceptable salt thereof.

5. The compound according to claim 4 , which is a glycine salt having a formula of

6. The glycine salt according to claim 5 , wherein the salt is crystalline.

7. The glycine salt according to claim 6 , wherein the salt is anhydrous.

8. A pharmaceutical composition comprising the compound according to claim 4 , or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable excipients.

9. A combination comprising the compound of claim 4 , or a pharmaceutically acceptable salt thereof, and one or more other active agents.

10. The glycine salt according to claim 6 , wherein the salt is hydrated.

11. The glycine salt according to claim 10 , wherein the salt is a monohydrate.

12. A pharmaceutical composition comprising the compound according to claim 5 and one or more pharmaceutically acceptable excipients.

13. A combination comprising the compound of claim 5 and one or more other active agents.

14. The compound according to claim 1 , having formula (I)

15. The compound according to claim 2 , having formula (II)

16. The compound according to claim 3 , having formula (IV)

17. The compound according to claim 4 , having formula (V)

Assignments (2)
CHANGE OF ADDRESS Recorded Oct 8, 2025
From: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
To: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
Reel/Frame 073032/0390 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 2, 2023
From: BENOWITZ, ANDREW B.; KING, BRYAN WAYNE; ROMERIL, STUART PAUL; FOSBENNER, DAVID T
To: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
Reel/Frame 063504/0658 →
Continuity (3)
Continuation PCTIB2022051637 · Feb 24, 2022
Provisional Application 63155325 · Mar 2, 2021
Related Publication 20230101987A1 · Mar 30, 2023