2-Hydroxy-1- {4 - [(4-phenyl) phenyl] carbonyl} piperazin-1-yl} ethane-1-one derivatives and related compounds as fatty acid synthase inhibitors (FASN) for the treatment of cancer
BAIR, Kenneth,LANCIA, David R.,LI, Hongbin,LOCH, James,LU, Wei,MARTIN, Matthew,MILLAN, David,SCHILLER, Shawn,TEBBE, Mark
申请号：
ES14779048
公开号：
ES2753386T3
申请日:
2014.03.11
申请国别(地区):
ES
年份:
2020
代理人:
摘要：
A compound of formula I: ** Formula ** wherein: R1 is ** Formula ** L is a 5-10 membered monocyclic ring or bicyclic alkyl or heteroalkyl wherein (i) the heteroatom ring members of the monocyclic heteroalkyl or 5-10 membered bicyclic are independently selected from O, S, or N, and (ii) each of the 5-10 membered monocyclic or bicyclic alkyl or heteroalkyl is either unsubstituted or optionally substituted by substituents selected from the group that it consists of deuterium and -Rb； A and B are independently O or S； An is aryl, heteroaryl, or 4-10 membered monocyclic or bicyclic heterocycloalkyl, wherein (i) said 4-10 membered monocyclic or bicyclic heteroaryl or heterocycloalkyl have 1, 2, 3, or 4 heteroatoms that are independently selected from N, S or O, and (ii) each of said 4-10 membered monocyclic or bicyclic aryl, heteroaryl, or heterocycloalkyl is either unsubstituted or optionally independently substituted with 1 or more substituents that may be the same or different and are selected independently of the group consisting of deuterium, halo, alkyl, -CHzF3-z, cyano, hydroxyl, hydroxyalkyl, amino, aminoalkyl, (amino) alkoxy, -CONH2, -C (O) NH (alkyl), -C (O) N (alkyl) 2, - C (O) NH (aryl), -C (O) N (aryl) 2, -OCHzF3-z, -alkyl, -alkenyl, alkynyl, alkoxy or (alkoxyalkyl) amino -, - N (Rc) - (O) -alkyl, -N (Rc) -C (O) aryl, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl, provided that there are not two adjacent heteroatoms in the ring are both S or both O； R2 is H or a 4-15 membered monocyclic, bicyclic or tricyclic aryl, heteroaryl, cycloalkyl, or heterocycloalkyl ring (i) the 4-15 membered monocyclic, bicyclic or tricyclic heteroaryl or heterocycloalkyl has 1, 2, 3, 4 , 5, 6, 7, or 8 heteroatoms that are independently selected from N, S, or O, and (ii) wherein each of said aryl, heteroaryl, cycloalkyl, and heterocycloalkyl is either unsubstituted or optionally substituted with 1 or more substituents which may be the same or different and are independently sel
