Lipoprotein lipase-activating compositions comprising benzene derivates
AssigneeOtsuka Pharmaceutical Factory, Inc.
InventorsIrina Neagu, Michael Ohlmeyer, Vidyadhar M. Paradkar, Kurt W. Saionz, Koushi Iwata, Takashi Okamura, Tadao Shibutani
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Abstract
The present invention provides pharmaceutical compositions containing benzene compound(s) represented by General Formula (1) below and, particularly, LPL-activating compositions for use in hyperlipidemia therapeutic and preventive agents, anti-obesity agents, and the like: wherein R1, R2, R3 and R4 are as defined in the specification.
Claims7
A method for activating LPL in a patient in need of LPL activation treatment, comprising administering an effective amount of a benzene compound into the patient, the benzene compound being represented by General Formula (1):
- wherein R1 is lower alkoxy;
- R2, R3 and Z are any one of the groups (1-1) to (1-3):
- (1-1) R2 is phenyl, phenyl having one or two halogen atoms as substituents on the benzene ring, phenyl lower alkyl group, phenyl lower alkyl group having on the benzene ring one or two substituents selected from the group consisting of halogen, and cyano, or R1 and R2 are jointed to form —CH═C(Ph)- (wherein Ph is phenyl);
- R3 is hydrogen or lower alkoxy;
- and Z is a group represented by the formula below:
- wherein R4 is hydrogen, lower alkyl, or halogen;
- R5 is hydrogen, lower alkyl, halogen, hydroxy, lower alkoxy, phenyl lower alkoxy;
- R6 is hydrogen, lower alkyl, carboxy, or halogenated lower alkyl;
- R7 is hydrogen, lower alkyl, halogen, halogenated lower alkyl, lower alkoxycarbonyl, carboxy, cyano, carbamoyl, or phenyl;
- and
- R8 is hydrogen or lower alkyl;
- (1-2) R2 is phenyl lower alkyl having one or two halogen atoms as substituents on the benzene ring:
- R3 is hydrogen or lower alkoxy;
- and Z is imidazo[2,1-b]thiazol-6-yl or imidazo[2,1-b]thiazol-6-yl having one lower alkyl substituent;
- and
- (1-3) R2 is phenyl lower alkyl, or phenyl lower alkyl having one or two halogen atoms as substituents on the benzene ring;
- R3 is hydrogen or lower alkoxy;
- and Z is imidazo[1,2-a]pyridin-3-yl.
A benzene compound represented by General Formula (1a)
- wherein
- R1a is lower alkoxy;
- and R2a and Z are any one of groups (2-1) to (2-3):
- (2-1) R2a is phenyl lower alkyl having one or two halogen atoms as substituents on the benzene ring;
- and Z is imidazo[2,1-b]thiazol-6-yl or imidazo[2,1-b]thiazol-6-yl having one lower alkyl substituent;
- (2-2) R2a is phenyl lower alkyl or phenyl lower alkyl having one or two halogen atoms as substituents on the benzene ring;
- and Z is imidazo[1,2-a]pyridin-3-yl;
- (2-3) R2a is phenyl, phenyl having one or two halogen atoms as substituents on the benzene ring, phenyl lower alkyl group having on the benzene ring one or two substituents selected from the group consisting of halogen, and cyano, or R1a and R2a are jointed to form —CH═C(Ph)- (wherein Ph is phenyl);
- and Z is a group represented by the formula below:
- wherein R4 is hydrogen, lower alkyl, or halogen;
- R5 is hydrogen, lower alkyl, halogen, hydroxy, lower alkoxy, phenyl lower alkoxy;
- R6 is hydrogen, lower alkyl, carboxy, or halogenated lower alkyl;
- R7 is hydrogen, lower alkyl, halogen, halogenated lower alkyl, lower alkoxycarbonyl, carboxy, cyano, carbamoyl, or phenyl;
- and
- R8 is hydrogen or lower alkyl.
Dependencies are inferred from the claim text.