Piperidine and piperazine derivatives as inhibitors of the abeta fibril formation
OwnerRainer M. Luond, Markus Banziger +1inventors
InventorsRainer M. Luond, Markus Banziger, Peter Frey
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Abstract
The invention provides a compound of formula I 1 wherein R, X, Y1 and Y2 are as defined in the description, and a process for preparing them. The compounds of formula I are useful as pharmaceuticals.
Claims11
A compound of formula I
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- wherein
- X is
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- wherein R′ is a group (a)
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- and either R″ is H or OH and R′″ is a group (b), (c) or (d)
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- or R″ and R′″ each are a group (c),
- wherein Z is H, halogen, trifluoromethyl, (C1-4)alkyl or (C1-4)alkoxy, Q° is —O—, —NH—CO— or a single bond and R° is hydrogen or hydroxy,
- Y1 and Y2 are H or, when X is
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- wherein R″ is H and R′″ is a group (d), Y1 and Y2 can also form together a —CH2—CH2— bridge, and
- R is a group (e) or (f)
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- wherein
- n is 0 to 3
- R1 is H, (C1-4)alkyl or —SO2—CH3
- R2 is H, halogen, (C1-4)alkyl, (C1-4)alkoxy, (C1-4)alkylthio or phenyl,
- R3 is H, (C1-4)alkyl or a group (g)
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- wherein Z is as defined above,
- R4 and R5 each are H or together form a bond, or R4 is H and R5 is (C1-4)alkoxy,
- R6 is (C1-4) alkyl or a group (g) and
- R7 is (C1-4) alkoxy,
- provided that when X is
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- R is of formula (f) and n is 1, then Z is different from fluor in free base or acid addition salt form.
[3S,4aR,10aR]-3-(endo-3-Benzhydryloxy-8-aza-bicyclo[3.2.1]oct-8-ylmethyl)-6-methoxy-1-methyl-1,2,3,4,4a,5,10,10a-octahydro-benzo[g]quinoline in free base or acid addition salt form.
[3R,4aR,10aR]-3-(endo-3-Benzhydryloxy-8-aza-bicyclo[3.2.1]oct-8-ylmethyl)-6-methoxy-1-methyl-1,2,3,4,4a,5,10,10a-octahydro-benzo[g]quinoline in free base or acid addition salt form.
[6aR,9R]-9-[2-(endo-3-Benzhydryloxy-8-aza-bicyclo[3.2.1]oct-8-yl)-ethyl]-7-methyl-4,6,6a,7,8,9-hexahydro-indolo[4,3-fg]quinoline in free base or acid addition salt form.
Dependencies are inferred from the claim text.