Cyclopropylamines as LSD1 inhibitors

Patent metadata

Field	Value
Publication number	US-9670210-B2
Application number	US-201514620903-A
Country	US
Kind code	B2
Filing date	Feb 12, 2015
Priority date	Feb 13, 2014
Publication date	Jun 6, 2017
Grant date	Jun 6, 2017

Abstract

The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

First claim

What is claimed is:

1. A compound which is 1-{[4-(methoxymethyl)-4-({[(1R,2S)-2-phenylcyclopropyl]amino}methyl)piperidin-1-yl]methyl}cyclopentanecarboxylic acid, or a pharmaceutically acceptable salt thereof.

2. A compound which is 1-{[4-(methoxymethyl)-4-({[(1R,2S)-2-phenylcyclopropyl]amino}methyl)piperidin-1-yl]methyl}cyclopentanecarboxylic acid.

3. A compound which is 1-{[4-(methoxymethyl)-4-({[(1R, 2S)-2-phenylcyclopropyl]amino}methyl)piperidin-1-yl]methyl}cyclobutanecarboxylic acid, or a pharmaceutically acceptable salt thereof.

4. A compound which is 1-{[4-(methoxymethyl)-4-({[(1R, 2S)-2-phenylcyclopropyl]amino}methyl)piperidin-1-yl]methyl}cyclobutanecarboxylic acid.

5. A compound which is 1-{[4-({[(1R, 2S)-2-(4-fluorophenyl)cyclopropyl]amino}methyl)-4-(methoxymethyl)piperidin-1-yl]methyl}cyclobutanecarboxylic acid, or a pharmaceutically acceptable salt thereof.

6. A compound which is 1-{[4-({[(1R, 2S)-2-(4-fluorophenyl)cyclopropyl]amino}methyl)-4-(methoxymethyl)piperidin-1-yl]methyl}cyclobutanecarboxylic acid.

7. A compound which is 1-{[4-(ethoxymethyl)-4-({[(1R, 2S)-2-phenylcyclopropyl]amino}methyl)piperidin-1-yl]methyl}cyclobutanecarboxylic acid, or a pharmaceutically acceptable salt thereof.

8. A compound of claim 1 , which is 1-{[4-(ethoxymethyl)-4-({[(1R, 2S)-2-phenylcyclopropyl]amino }methyl)piperidin-1-yl]methyl}cyclobutanecarboxylic acid.

9. A pharmaceutical composition comprising the compound of claim 1 , or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier or excipient.

10. A pharmaceutical composition comprising the compound of claim 2 and at least one pharmaceutically acceptable carrier or excipient.

11. A pharmaceutical composition comprising the compound of claim 3 , or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier or excipient.

12. A pharmaceutical composition comprising the compound of claim 4 and at least one pharmaceutically acceptable carrier or excipient.

13. A pharmaceutical composition comprising the compound of claim 5 , or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier or excipient.

14. A pharmaceutical composition comprising the compound of claim 6 and at least one pharmaceutically acceptable carrier or excipient.

15. A pharmaceutical composition comprising the compound of claim 7 , or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier or excipient.

16. A pharmaceutical composition comprising the compound of claim 8 and at least one pharmaceutically acceptable carrier or excipient.

Assignees

• Incyte Corp

Inventors

• Wu Liangxing
• He Chunhong
• Yao Wenqing
• Zhang Fenglei

Classifications

• A61P31/12

  Antivirals · CPC title

• A61P35/02

  specific for leukemia · CPC title

• A61P7/00

  Drugs for disorders of the blood or the extracellular fluid · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61P7/06

  Antianaemics · CPC title