IP Library › Granted Patent US 12,616,682
Granted Patent B2
US 12,616,682 · App. 19/038,137 · Granted May 5, 2026

1-H-pyrrolo[2,3-c]pyridine compounds

Inventors: Stephen Atkinson (Saffron Walden, GB); Gerjan De Bruin (Oss, NL); Flavia Izzo (Oss, NL); Chimed Jansen (Oss, NL); Olaf Kinzel (Oss, NL); Martin Packer (Macclesfield, GB); Saskia Verkaik (Oss, NL); Robin Voets (Oss, NL)
Assignee: ACERTA PHARMA B.V.
A61K31/437A61K31/439A61K31/4545A61K31/506A61K31/5377A61K31/55C07D471/04
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Quick Facts
Patent No.
US 12,616,682
App. No.
19/038,137
Granted
May 5, 2026
Kind
B2
Abstract

Compounds having the structure of Formula (I): and pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 , R 4 , and A are as defined in the specification; pharmaceutical compositions comprising such compounds and salts; use of such compounds and salts to treat or prevent Menin-mediated conditions; kits comprising such compounds and salts; and methods for manufacturing such compounds and salts.

Claims (25)

1 . A compound that is(S)-2-(3-(1-(5,5-dimethylpyrrolidine-2-carbonyl) piperidine-4-carbonyl)-2-methyl-1H-pyrrolo[2,3-c]pyridin-1-yl)-5-fluoro-N,N-diisopropylbenzamide having the structure:

or a pharmaceutically acceptable salt thereof.

2 . A compound that is (S)-2-(3-(1-(5,5-dimethylpyrrolidine-2-carbonyl) piperidine-4-carbonyl)-2-methyl-1H-pyrrolo[2,3-c]pyridin-1-yl)-5-fluoro-N,N-diisopropylbenzamide having the structure:

or a pharmaceutically acceptable salt thereof.

3 . The compound of claim 2 that is (S)-2-(3-(1-(5,5-dimethylpyrrolidine-2-carbonyl)piperidine-4-carbonyl)-2-methyl-1H-pyrrolo[2,3-c]pyridin-1-yl)-5-fluoro-N,N-diisopropylbenzamide having the structure:

4 . The salt of claim 2 that is the pharmaceutically acceptable salt of the compound that is (S)-2-(3-(1-(5,5-dimethylpyrrolidine-2-carbonyl)piperidine-4-carbonyl)-2-methyl-1H-pyrrolo[2,3-c]pyridin-1-yl)-5-fluoro-N,N-diisopropylbenzamide having the structure:

5 . A pharmaceutical composition comprising a compound that is (S)-2-(3-(1-(5,5-dimethylpyrrolidine-2-carbonyl)piperidine-4-carbonyl)-2-methyl-1H-pyrrolo[2,3-c]pyridin-1-yl)-5-fluoro-N,N-diisopropylbenzamide having the structure:

or a pharmaceutically acceptable salt thereof; and one or more pharmaceutically acceptable excipients.

6 . The pharmaceutical composition of claim 5 comprising the compound that is (S)-2-(3-(1-(5,5-dimethylpyrrolidine-2-carbonyl)piperidine-4-carbonyl)-2-methyl-1H-pyrrolo[2,3-c]pyridin-1-yl)-5-fluoro-N,N-diisopropylbenzamide having the structure:

and one or more pharmaceutically acceptable excipients.

7 . The pharmaceutical composition of claim 5 comprising the pharmaceutically acceptable salt of the compound that is (S)-2-(3-(1-(5,5-dimethylpyrrolidine-2-carbonyl)piperidine-4-carbonyl)-2-methyl-1H-pyrrolo[2,3-c]pyridin-1-yl)-5-fluoro-N,N-diisopropylbenzamide having the structure:

and one or more pharmaceutically acceptable excipients.

8 . A method of treating leukemia in a subject suffering from or susceptible to the leukemia, wherein the method comprises administering to the subject a therapeutically effective amount of a compound that is (S)-2-(3-(1-(5,5-dimethylpyrrolidine-2-carbonyl)piperidine-4-carbonyl)-2-methyl-1H-pyrrolo[2,3-c]pyridin-1-yl)-5-fluoro-N,N-diisopropylbenzamide having the structure:

or a pharmaceutically acceptable salt thereof.

9 . The method of claim 8 , wherein the method comprises administering to the subject a therapeutically effective amount of a compound that is ((S)-2-(3-(1-(5,5-dimethylpyrrolidine-2-carbonyl)piperidine-4-carbonyl)-2-methyl-1H-pyrrolo[2,3-c]pyridin-1-yl)-5-fluoro-N,N-diisopropylbenzamide having the structure:

10 . The method of claim 8 , wherein the method comprises administering to the subject a therapeutically effective amount of the pharmaceutically acceptable salt of the compound that is(S)-2-(3-(1-(5,5-dimethylpyrrolidine-2-carbonyl)piperidine-4-carbonyl)-2-methyl-1H-pyrrolo[2,3-c]pyridin-1-yl)-5-fluoro-N,N-diisopropylbenzamide having the structure:

11 . The method of claim 8 , wherein the leukemia is selected from the group consisting of acute myeloid leukemia and acute lymphoid leukemia.

12 . The method of claim 8 , wherein the leukemia is acute myeloid leukemia.

13 . The method of claim 8 , wherein the leukemia is selected from the group consisting of mixed-lineage leukemia (MLL)-rearranged leukemia and NPM1-mutant acute myeloid leukemia.

14 . The method of claim 9 , wherein the leukemia is selected from the group consisting of acute myeloid leukemia and acute lymphoid leukemia.

15 . The method of claim 9 , wherein the leukemia is acute myeloid leukemia.

16 . The method of claim 9 , wherein the leukemia is selected from the group consisting of mixed-lineage leukemia (MLL)-rearranged leukemia and NPM1-mutant acute myeloid leukemia.

17 . The method of claim 10 , wherein the leukemia is selected from the group consisting of acute myeloid leukemia and acute lymphoid leukemia.

18 . The method of claim 10 , wherein the leukemia is acute myeloid leukemia.

19 . The method of claim 10 , wherein the leukemia is selected from the group consisting of mixed-lineage leukemia (MLL)-rearranged leukemia and NPM1-mutant acute myeloid leukemia.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 21, 2025
From: ATKINSON, STEPHEN; PACKER, MARTIN
To: ASTRAZENECA UK LIMITED
Reel/Frame 071771/0661 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 21, 2025
From: DE BRUIN, GERJAN; JANSEN, CHIMED; VERKAIK, SASKIA; VOETS, ROBIN; IZZO, FLAVIA; KINZEL, OLAF
To: ACERTA PHARMA B.V.
Reel/Frame 071771/0916 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 21, 2025
From: ASTRAZENECA UK LIMITED
To: ACERTA PHARMA B.V.
Reel/Frame 071772/0247 →
Continuity (3)
Continuation 18613180 · Mar 22, 2024
Provisional Application 63491978 · Mar 24, 2023
Related Publication 20250360112A1 · Nov 27, 2025
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