Fused-polycyclic compounds
AssigneeTanabe Seiyaku Co., Ltd.
InventorsTatsuzo Ukita, Yoshihiro Terakawa, Kazuteru Wada, Aya Nakata, Atsuko Sakai, Koji Ogawa
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Abstract
The present invention provides a novel a condensed polycyclic compound useful as a phosphodiesterase 4 inhibitor, which is shown by the formula [I]: 1 or a pharmaceutically acceptable salt thereof and a pharmaceutical composition containing the same.
Claims31
A condensed polycyclic compound of the formula [I]:
- 31
- wherein,
- r1 and r2 are the same or different and each a group selected from a hydroxy group and a lower alkoxy group;
- ring A0 is a group of the formula:
- 32
- ring A is:
- (1) a substituted or unsubstituted benzene ring or a substituted or unsubstituted aromatic heterocyclic ring, when ring A0 is a group of the formula:
- 33
- or
- (2) a group of the formula:
- 34
- wherein n is an integer of 1 to 6, when ring A0 is a group of the formula:
- 35
- R3 is:
- (1) a hydrogen atom, a group of the formula:
- —(CH2)m—R31 or a group of the formula:
- —CO—R32, when ring A is a substituted benzene ring or a substituted or unsubstituted aromatic heterocyclic group;
- or
- (2) a group of the formula:
- —(CH2)m—R31 or a group of the formula:
- —CO—R32, when ring A is an unsubstituted benzene ring;
- R31 is a hydrogen atom, an aryl group, a hydroxy group, an amino group, a carboxyl group, a lower alkoxycarbonyl group or a lower alkylthio group;
- R32 is an aryl group, a lower alkyl group, a hydroxy-lower alkyl group or an amino-lower alkyl group;
- m is an integer of 1 to 6;
- Q is a single bond linked to ring A;
- and
- Ra and Rb are the same or different and each a group selected from a hydrogen atom and an acyl group,
- or a pharmaceutically acceptable salt thereof.
6-[4-(Isopropyloxy)phenyl]-8,9-dimethoxy-1,3,4,6,11,11a-hexahydro-2H-pyrazino[1,2-b]isoquinoline, or a pharmaceutically acceptable salt thereof.
6-(4-Fluorophenyl)-8,9-dimethoxy-1,3,4,6,11,11a-hexahydro-2H-pyrazino[1,2-b]isoquinoline, or a pharmaceutically acceptable salt thereof.
6,7-Dimethoxy-1-[2-(1,3-dioxocyclohexan-2-yl)pyridin-4-yl]-2,3-bis(hydroxymethyl)naphthalene, or a pharmaceutically acceptable salt thereof.
A PDE4 inhibitor, which comprises as an active ingredient a pyrazinoisoquinoline derivative of the formula [I-C]:
- 38
- wherein R1 and R2 are the same or different and each a group selected from a hydroxy group and a lower alkoxy group, or a pharmaceutically acceptable salt thereof.
A PDE4 inhibitor, which comprises as an active ingredient 8,9-dimethoxy-6-phenyl-1,3,4,6,11,11a-hexahydro-2H-pyrazino[1,2-b]isoquinoline, or a pharmaceutically acceptable salt thereof.
A method for treatment or prophylaxis of PDE4-associated diseases, which comprises administering an effective amount of a pyrazinoisoquinoline compound of the formula [I-C]:
- 39
- wherein R1 and R2 are the same or different and each a group selected from a hydroxy group and a lower alkoxy group, or a pharmaceutically acceptable salt thereof or an effective amount of a PDE4 inhibitor comprising as an active ingredient the said compound or a pharmaceutically acceptable salt thereof, to a patient in need thereof.
A pharmaceutically acceptable salt of pyrazinoisoquinoline compound of the formula [I-C]:
- 40
- wherein R1 and R2 are the same or different and each a group selected from a hydroxy group and a lower alkoxy group.
A pharmaceutically acceptable salt of 8,9-dimethoxy-6-phenyl-1,3,4,6,11,11a-hexahydro-2H-pyrazino[1,2-b]isoquinoline.
A pharmaceutically acceptable salt of 8,9-dimethoxy-6-phenyl-1,3,4,6,11,11a-hexahydro-2H-pyrazino[1,2-b]isoquinoline dihydrochloride.
Dependencies are inferred from the claim text.