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Positive allosteric modulators of nicotinic acetylcholine receptor
专利权人:
H. LUNDBECK A/S
发明人:
ESKILDSEN JØRGEN,SAMS ANETTE GRAVEN,PÜSCHL ASK
申请号:
NZ61736712
公开号:
NZ617367A
申请日:
2012.07.06
申请国别(地区):
NZ
年份:
2015
代理人:
摘要:
Disclosed are compounds of formula (I) wherein R1, R2, R3, R4 and R5 are H; R6 is methoxymethyl; A7 is C-R7, A8 is N and A9 is C-R9; R7, R9, R10 and R11 are selected independently of each other from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6alkoxy and OR12; wherein R12 represents a monocyclic saturated ring moiety having 4-6 ring atoms wherein one of said ring atoms is O and the rest is C; and pharmaceutically acceptable salts thereof, which are positive allosteric modulators (PAMs) of the nicotinic acetylcholine α7 receptor and are therefore useful in the treatment of conditions including schizophrenia, psychosis and other cognitive disorders. Compounds of formula I include (1S,2S)-2-phenyl-cyclopropanecarboxylic acid[(R)-1-(6-ethoxy-pyridin-3-yl)-2-methoxyethyl]-amide; (1S,2S)-N-[(1R)-2-methoxy-1-[6-[(3R)-tetrahydrofuran-3-yl]oxy-3-pyridyl]ethyl]-2-phenylcyclopropanecarboxamide; (1S,2S)-N-[(1R)-2-methoxy-1-[6-[(3S)-tetrahydrofuran-3-yl]oxy-3-pyridyl]ethyl]-2-phenylcyclopropanecarboxamide; and (1S,2S)-2-phenyl-cyclopropanecarboxylic acid { (R)-2-methoxy-1-[6-(tetrahydro-pyran-4-yloxy)-pyridin-3-yl]-ethyl} -amide.
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