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US 7,030,267 B2Granted
Cycloproply β-amino acid derivatives
AssigneeWarner-Lambert Company
InventorsJacob Bradley Schwarz, David Juergen Wustrow
Life of this patent
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Abstract
This invention relates to novel cyclopropyl β-amino acids derivatives of the formula wherein R1 through R4 are defined as in the specification, pharmaceutical compositions containing them and their use for the treatment of various central nervous system and other disorders. The cyclopropyl β-amino acids derivatives of this invention exhibit activity as alpha2delta ligands (α2δ ligands). Such compounds have affinity for the α2δ subunit of a calcium channel.
Claims3
A compound of the formula I
- wherein R1 and R2 are selected, independently, from hydrogen, (C1–C10)straight or branched alkyl, (C1–C10)straight or branched alkoxyalkyl, phenyl-(C1–C3)straight or branched alkyl and phenyl-(C1–C3)straight or branched alkoxyalkyl, wherein said phenyl moieties can optionally be substituted with one or two substituents selected, independently, from halo or (C1–C3)alkyl;
- or R1 and R2, together with the carbon to which they are attached, form a cyclopentyl, cyclohexyl or cycloheptyl ring which can optionally be substituted with one or two substituents selected, independently, from the group of substituents named in the definition of R1 and R2 above;
- and
- R3 and R4 are selected, independently, from hydrogen and methyl;
- with the proviso that at least one of R1, R2, R3 and R4 is other than hydrogen;
- or a pharmaceutically acceptable salt thereof.
3 more elements
A pharmaceutical composition comprising a therapeutically effective amount of a compound of the formula I
- wherein R1 and R2 are selected, independently, from hydrogen, (C1–C10) straight or branched alkyl, (C1–C10) straight or branched alkoxyalkyl, phenyl-(C1–C3) straight or branched alkyl and phenyl-(C1–C3) straight or branched alkoxyalkyl, wherein said phenyl moieties can optionally be substituted with one or two substituents selected, independently, from halo or (C1–C3)alkyl;
- or R1 and R2, together with the carbon to which they are attached, form a cyclopentyl, cyclohexyl or cycloheptyl ring which can optionally be substituted with one or two substituents selected, independently, from the group of substituents named in the definition of R1 and R2 above;
- and
- R3 and R4 are selected, independently, from hydrogen and methyl;
- with the proviso that at least one of R1, R2, R3 and R4 is other than hydrogen;
- or a pharmaceutically acceptable salt thereof.
3 more elements
Dependencies are inferred from the claim text.