IP Library Granted Patent US 10,064,854
Granted Patent B2
US 10,064,854 · App. 15/708,270 · Granted Sep 4, 2018

Cyclopropylamines as LSD1 inhibitors

Inventors: Neil W. Johnson (Collegeville, PA); Jiri Kasparec (Collegeville, PA)
Assignee: GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED
A61K31/445C07C211/35C07C211/36C07C271/24C07D207/09C07D211/26C07D211/62C07D211/96C07D223/04C07D265/30C07D401/04C07D401/06C07D401/10C07D401/12C07D413/06C07F5/02C07F5/025C07F9/591C07C2601/02C07C2601/14
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Quick Facts
Patent No.
US 10,064,854
App. No.
15/708,270
Granted
Sep 4, 2018
Kind
B2
Abstract

This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.

Claims (15)

1. A method of treating a hematologic cancer which comprises administering to a human in need thereof an effective amount of a compound which is 4-((4-((((1R,2S)-2-phenylcyclopropyl)amino)methyl)piperidin-1-yl)methyl)benzoic acid, represented by the formula:

or a pharmaceutically acceptable salt thereof, wherein said hematologic cancer is selected from the group consisting of: acute myeloid leukemia, chronic myeloid leukemia, acute lymphoblastic leukemia, chronic lymphocytic leukemia, myeloproliferative diseases, multiple myeloma, myelodysplastic syndrome, Hodgkin's disease, and non-Hodgkin's lymphoma.

2. The method of claim 1 wherein said hematologic cancer is myelodysplastic syndrome.

3. The method of claim 1 , further comprising administering an additional therapeutic agent selected from the group consisting of tretinoin, azacitidine, and decitabine.

4. The method of claim 3 , wherein said additional therapeutic agent is tretinoin.

5. The method of claim 3 , wherein said additional therapeutic agent is azacitidine.

6. The method of claim 3 , wherein said additional therapeutic agent is decitabine.

7. The method of claim 3 , wherein said hematologic cancer is myelodysplastic syndrome.

8. The method of claim 4 , wherein said hematologic cancer is myelodysplastic syndrome.

9. The method of claim 5 , wherein said hematologic cancer is myelodysplastic syndrome.

10. The method of claim 6 , wherein said hematologic cancer is myelodysplastic syndrome.

11. The method of claim 3 , wherein said hematologic cancer is acute myeloid leukemia.

12. The method of claim 4 , wherein said hematologic cancer is acute myeloid leukemia.

13. The method of claim 5 , wherein said hematologic cancer is acute myeloid leukemia.

14. The method of claim 6 , wherein said hematologic cancer is acute myeloid leukemia.

Assignments (3)
CHANGE OF ADDRESS Recorded Apr 16, 2025
From: GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED
To: GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED
Reel/Frame 070854/0469 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 19, 2017
From: JOHNSON, NEIL W.; KASPAREC, JIRI; MILLER, WILLIAM HENRY; ROUSE, MEAGAN B.; SUAREZ, DOMINIC; TIAN, XINRONG
To: GLAXOSMITHKLINE LLC
Reel/Frame 043621/0204 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 19, 2017
From: GLAXOSMITHKLINE LLC
To: GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED
Reel/Frame 043621/0298 →
Continuity (7)
Continuation 15095280 · Apr 11, 2016
Continuation 14475762 · Sep 3, 2014
Continuation 14007035
Provisional Application 61594012 · Feb 2, 2012
Provisional Application 61514140 · Aug 2, 2011
Provisional Application 61467524 · Mar 25, 2011
Related Publication 20180000805A1 · Jan 4, 2018
Cited By (1)
US 12,479,845