Piperazine derivatives as FASN inhibitors

Patent metadata

Field	Value
Publication number	US-9809552-B2
Application number	US-201414778253-A
Country	US
Kind code	B2
Filing date	Feb 24, 2014
Priority date	Mar 21, 2013
Publication date	Nov 7, 2017
Grant date	Nov 7, 2017

Abstract

Compounds of the formula I

in which R, X 1 , X 2 , X 3 , X 4 , R 1 , R 2 and q have the meanings indicated in Claim 1,

are inhibitors of fatty acid synthase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.

First claim

The invention claimed is:

1. A compound selected from the group consisting of

No.
Name

“A1”
1-[4-(4-isoquinolin-6-yl-benzoyl)-piperazin-1-yl]-propan-1-one

“A2”
1-[4-(4-isoquinolin-6-yl-benzoyl)-piperazin-1-yl]-ethanone

“A4”
1-{4-[4-(3-methoxy-isoquinolin-6-yl)-benzoyl]-piperazin-1-yl}-

butan-1-one

“A5”
1-[4-(4-isoquinolin-6-yl-benzoyl)-piperazin-1-yl]-pentan-1-one

“A6”
1-[4-(4-isoquinolin-6-yl-benzoyl)-piperazin-1-yl]-butan-1-one

“A7”
1-{4-[4-(2-oxy-isoquinolin-6-yl)-benzoyl]-piperazin-1-yl}-

propan-1-one

or a pharmaceutically acceptable salt, tautomer and/or stereoisomer thereof, and/or mixtures thereof in all ratios.

2. A pharmaceutical composition comprising at least one compound of claim 1 , and/or a pharmaceutically acceptable salt, tautomer and/or stereoisomer thereof in all ratios, and a pharmaceutically acceptable carrier, excipient or vehicle.

Assignees

• Merck Patent Gmbh

Inventors

• Staehle Wolfgang
• Tsaklakidis Christos
• Friese-Hamim Manja
• Leuthner Birgitta
• Wienke Dirk

Classifications

• A61P35/00

  Antineoplastic agents · CPC title

• A61P35/02

  specific for leukemia · CPC title

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61P25/28

  for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia · CPC title

• A61P29/00

  Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] · CPC title