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US 2006/0079554 A1Published application
Inhibitors of monomine uptake
OwnerPeter Barry, Manuel Cases-Thomas +6inventors
InventorsPeter Barry, Manuel Cases-Thomas, Peter Gallagher, Jeremy Gilmore, John Masters, Graham Timms, Maria Whatton, Virginia Wood
Life of this patent
Estimating the term…
Abstract
N,N-disubstituted 4-amino-piperidines of the general Formula (I) are inhibitors of the uptake of serotonin and/or norepinephrine and/or dopamine. As such, they may be useful for the treatment of disorders of the central and/or peripheral nervous system.
Claims24
A compound of formula I
- wherein
- n is 1, 2 or 3;
- R1 is C2-C10alkyl, C2-C10alkenyl, C3-C8cycloalkyl or C4-C10cycloalkylalkyl, wherein one C—C bond within any cycloalkyl moiety is optionally substituted by an O—C, S—C or C═C bond and wherein each group is optionally substituted with from 1 to 7 halogen substituents and/or with from 1 to 3 substituents each independently selected from hydroxy, cyano, C1-C4alkyl, C1-C4alkylthio (optionally substituted with from 1 to 3 halogen atoms) and C1-C4alkoxy (optionally substituted with from 1 to 3 halogen atoms);
- R2 is H, C1-C4alkyl (optionally substituted with from 1 to 7 halogen atoms), C1-C4alkyl-S(O)x— wherein x is 0, 1 or 2 (optionally substituted with from 1 to 7 halogen atoms), C1-C4alkoxy (optionally substituted with from 1 to 7 halogen atoms), cyano, halogen, phenyl (optionally substituted with from 1 to 3 substituents each independently selected from halogen, C1-C4alkyl and C1-C4alkoxy), phenoxy (optionally substituted with from 1 to 3 substituents each independently selected from halogen, C1-C4alkyl and C1-C4alkoxy) or —CO2(C1-C4alkyl), or together with R3 forms a further benzene ring (optionally substituted with from 1 to 3 substituents each independently selected from halogen, C1-C4alkyl and C1-C4alkoxy);
- R3 is H, C1-C4alkyl (optionally substituted with from 1 to 7 halogen atoms), C1-C4alkyl-S(O)x— wherein x is 0, 1 or 2 (optionally substituted with from 1 to 7 halogen atoms), C1-C4alkoxy (optionally substituted with from 1 to 7 halogen atoms), cyano, halogen, phenyl (optionally substituted with from 1 to 3 substituents each independently selected from halogen, C1-C4alkyl and C1-C4alkoxy), phenoxy (optionally substituted with from 1 to 3 substituents each independently selected from halogen, C1-C4alkyl and C1-C4alkoxy) or —CO2(C1-C4alkyl), or together with R2 or R4 forms a further benzene ring (optionally substituted with from 1 to 3 substituents each independently selected from halogen, C1-C4alkyl and C1-C4alkoxy);
- R4 is H, C1-C4alkyl (optionally substituted with from 1 to 7 halogen atoms), C1-C4alkyl-S(O)x— wherein x is 0, 1 or 2 (optionally substituted with from 1 to 7 halogen atoms), C1-C4alkoxy (optionally substituted with from 1 to 7 halogen atoms), cyano, halogen, phenyl (optionally substituted with from 1 to 3 substituents each independently selected from halogen, C1-C4alkyl and C1-C4alkoxy), phenoxy (optionally substituted with from 1 to 3 substituents each independently selected from halogen, C1-C4alkyl and C1-C4alkoxy) or —CO2(C1-C4alkyl), or together with R3 forms a further benzene ring (optionally substituted with from 1 to 3 substituents each independently selected from halogen, C1-C4alkyl and C1-C4alkoxy);
- R5 is H, C1-C4alkyl (optionally substituted with from 1 to 7 halogen atoms), C1-C4alkoxy (optionally substituted with from 1 to 7 halogen atoms) or halogen;
- R6 is H, C1-C4alkyl (optionally substituted with from 1 to 7 halogen atoms), C1-C4alkoxy (optionally substituted with from 1 to 7 halogen atoms) or halogen;
- R7 is H or C1-C4alkyl;
- R8 is H or C1-C4alkyl;
- R9 is H, halogen, hydroxy, cyano, C1-C4alkyl or C1-C4alkoxy;
- and
- R10 is H, halogen, hydroxy, cyano, C1-C4alkyl or C1-C4alkoxy;
- or a pharmaceutically acceptable salt thereof,
- with the proviso that the compound N-ethyl-N-benzyl-4-piperidinamine is excluded.
12 more elements
(canceled)
(canceled)
Dependencies are inferred from the claim text.