BICYCLIC gamma-AMINO ACID DERIVATIVE
AssigneeDaiichi Sankyo Company, Limited
InventorsKOUSEI SHIMADA, ASUKA KAWAMURA, NAOHISA ARAKAWA, YUKI DOMON
Life of this patent
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Abstract
It is intended to provide a bicyclic γ-amino acid derivative having excellent activity as an α2δ ligand. The present invention provides a compound represented by the general formula (I): wherein R1, R2, R2′, R4, R5, R6, R7, R8, and R8′ are a hydrogen atom or the like; and R3 is a hydrogen atom, a halogen atom, a C1-C6 alkyl group, or the like.
Claims23
-27. (canceled)
A compound according to formula (I) or a pharmacologically acceptable salt thereof, wherein formula (I) is selected from the group consisting of:
- wherein
- R1, R2, R2′, R4, R5, R6, R7, R8, and R8′ are a hydrogen atom;
- and
- R3 is a hydrogen atom, a C1-C6 alkyl group, a C2-C6 alkenyl group, a C1-C6 alkylsulfanyl-C1-C6 alkyl group, or a C3-C7 cycloalkyl group.
A compound according to formula (Ia) or a pharmacologically acceptable salt thereof:
- wherein
- R1, R2, R2′, R4, R5, R6, R7, R8, and R8′ are a hydrogen atom;
- and
- R3 is a hydrogen atom, a C1-C6 alkyl group, a C2-C6 alkenyl group, a C1-C6 alkylsulfanyl-C1-C6 alkyl group, or a C3-C7 cycloalkyl group.
A compound according to formula (Ib) or a pharmacologically acceptable salt thereof:
- wherein
- R1, R2, R2′, R4, R5, R6, R7, R8, and R8′ are a hydrogen atom;
- and
- R3 is a hydrogen atom, a C1-C6 alkyl group, a C2-C6 alkenyl group, a C1-C6 alkylsulfanyl-C1-C6 alkyl group, or a C3-C7 cycloalkyl group.
A compound selected from the group consisting of:
- (±)-[(1S,5R,6R)-6-(aminomethyl)bicyclo[3.2.0]hept-3-en-6-yl]acetic acid;
- (±)-[(1S,5R,6R)-6-aminomethyl-3-methylbicyclo[3.2.0]hept-3-en-6-yl]acetic acid;
- (±)-[(1S,5R,6R)-6-aminomethyl-3-ethylbicyclo[3.2.0]hept-3-en-6-yl]acetic acid;
- (±)-[(1S,5R,6R)-6-aminomethyl-3-propylbicyclo[3.2.0]hept-3-en-6-yl]acetic acid;
- (±)-[(1S,5R,6R)-6-aminomethyl-3-butylbicyclo[3.2.0]hept-3-en-6-yl]acetic acid;
- [(1R,5S,6S)-6-(aminomethyl)bicyclo[3.2.0]hept-3-en-6-yl]acetic acid;
- [(1S,5R,6R)-6-(aminomethyl)bicyclo[3.2.0]hept-3-en-6-yl]acetic acid;
- [(1S,5R,6R)-6-(aminomethyl)bicyclo[3.2.0]hept-3-en-6-yl]acetic acid hydrochloride;
- [(1S,5R,6R)-6-(aminomethyl)bicyclo[3.2.0]hept-3-en-6-yl]acetic acid benzenesulfonate;
- [(1R,5S,6S)-6-aminomethyl-3-ethylbicyclo[3.2.0]hept-3-en-6-yl]acetic acid;
- [(1R,5S,6S)-6-aminomethyl-3-ethylbicyclo[3.2.0]hept-3-en-6-yl]acetic acid p-toluenesulfonate;
- [(1R,5S,6S)-6-aminomethyl-3-ethylbicyclo[3.2.0]hept-3-en-6-yl]acetic acid benzenesulfonate;
- and
- [(1S,5R,6R)-6-aminomethyl-3-ethylbicyclo[3.2.0]hept-3-en-6-yl]acetic acid.
(±)-[(1S,5R,6R)-6-(aminomethyl)bicyclo[3.2.0]hept-3-en-6-yl]acetic acid.
(±)-[(1S,5R,6R)-6-aminomethyl-3-methylbicyclo[3.2.0]hept-3-en-6-yl]acetic acid.
(±)-[(1S,5R,6R)-6-aminomethyl-3-ethylbicyclo[3.2.0]hept-3-en-6-yl]acetic acid.
(±)-[(1S,5R,6R)-6-aminomethyl-3-propylbicyclo[3.2.0]hept-3-en-6-yl]acetic acid.
(±)-[(1S,5R,6R)-6-aminomethyl-3-butylbicyclo[3.2.0]hept-3-en-6-yl]acetic acid.
[(1R,5S,6S)-6-(aminomethyl)bicyclo[3.2.0]hept-3-en-6-yl]acetic acid.
[(1S,5R,6R)-6-(aminomethyl)bicyclo[3.2.0]hept-3-en-6-yl]acetic acid.
[(1S,5R,6R)-6-(aminomethyl)bicyclo[3.2.0]hept-3-en-6-yl]acetic acid hydrochloride.
[(1S,5R,6R)-6-(aminomethyl)bicyclo[3.2.0]hept-3-en-6-yl]acetic acid benzenesulfonate.
[(1R,5S,6S)-6-aminomethyl-3-ethylbicyclo[3.2.0]hept-3-en-6-yl]acetic acid.
[(1R,5S,6S)-6-aminomethyl-3-ethylbicyclo[3.2.0]hept-3-en-6-yl]acetic acid p-toluenesulfonate.
[(1R,5S,6S)-6-aminomethyl-3-ethylbicyclo[3.2.0]hept-3-en-6-yl]acetic acid benzenesulfonate.
[(1S,5R,6R)-6-aminomethyl-3-ethylbicyclo[3.2.0]hept-3-en-6-yl]acetic acid.
Dependencies are inferred from the claim text.