US 9,809,552 B2
Piperazine derivatives as FASN inhibitors
Wolfgang Staehle, Ingelheim (DE); Christos Tsaklakidis, Weinheim (DE); Manja Friese-Hamim, Moerfelden-Walldorf (DE); Birgitta Leuthner, Darmstadt (DE); and Dirk Wienke, Darmstadt (DE)
Assigned to MERCK PATENT GMBH, Darmstadt (DE)
Appl. No. 14/778,253
Filed by Merck Patent GmbH, Darmstadt (DE)
PCT Filed Feb. 24, 2014, PCT No. PCT/EP2014/000478
§ 371(c)(1), (2) Date Sep. 18, 2015,
PCT Pub. No. WO2014/146747, PCT Pub. Date Sep. 25, 2014.
Claims priority of application No. 13001462 (EP), filed on Mar. 21, 2013.
Prior Publication US 2016/0280655 A1, Sep. 29, 2016
Int. Cl. C07D 217/02 (2006.01); C07D 217/08 (2006.01); A61K 31/496 (2006.01); C07D 217/24 (2006.01); A61K 9/00 (2006.01); A61K 9/02 (2006.01)
CPC C07D 217/02 (2013.01) [A61K 9/0014 (2013.01); A61K 9/0019 (2013.01); A61K 9/02 (2013.01); A61K 31/496 (2013.01); C07D 217/08 (2013.01); C07D 217/24 (2013.01)] 2 Claims
 
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.