IP Library Granted Patent US 9,795,597
Granted Patent B2
US 9,795,597 · App. 15/095,280 · Granted Oct 24, 2017

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 9,795,597
App. No.
15/095,280
Granted
Oct 24, 2017
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 (7)

1. A method of treating 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 cancer is selected from the group consisting of: brain cancer, glioblastomas, leukemias, lymphomas, Bannayan-Zonana syndrome Cowden disease, Lhermitte-Duclos disease, breast cancer, inflammatory breast cancer, Wilm's tumor, Ewing's sarcoma, Rhabdomyosarcoma, ependymoma, medulloblastoma, colon cancer, gastric cancer, bladder cancer, head and neck cancer, kidney cancer, lung cancer, liver cancer, melanoma, renal cancer, ovarian cancer, pancreatic cancer, prostate cancer, sarcoma, osteosarcoma, giant cell tumor of bone, and thyroid cancer.

2. The method of claim 1 wherein the compound is administered within a pharmaceutical composition comprising the compound and a pharmaceutically acceptable excipient.

3. The method of claim 1 , wherein said cancer is acute myeloid leukemia.

4. The method of claim 2 , wherein said cancer is acute myeloid leukemia.

5. The method of claim 1 , wherein said cancer is small cell lung cancer.

6. The method of claim 2 , wherein said cancer is small cell lung cancer.

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 Apr 25, 2016
From: JOHNSON, NEIL W.; KASPAREC, JIRI; MILLER, WILLIAM HENRY; ROUSE, MEAGAN B.; SUAREZ, DOMINIC; TIAN, XINRONG
To: GLAXOSMITHKLINE LLC
Reel/Frame 038365/0504 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 25, 2016
From: GLAXOSMITHKLINE LLC
To: GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED
Reel/Frame 038365/0565 →
Continuity (6)
Continuation 14475762 · Sep 3, 2014
Continuation 14007035
Provisional Application 61467524 · Mar 25, 2011
Provisional Application 61514140 · Aug 2, 2011
Provisional Application 61594012 · Feb 2, 2012
Related Publication 20160220547A1 · Aug 4, 2016