Novel biphenyl derivative and preparation and use thereof

Details Novel biphenyl derivative and preparation and use thereof Novel biphenyl derivative and preparation and use thereof

1988-01-19

1989-07-18

Chan, Nicky

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

549436, A61K 3136, C07D31706

Patent

active

048494488

DESCRIPTION:

BRIEF SUMMARY
TECHNICAL FIELD

The present invention relates to a novel biphenyl derivative having an action of moderating liver ailments, which is effective for remedy of actute hepatitis and chronic hepatitis, a process for the preparation thereof and a liver ailment-moderating agent comprising this derivative as an effective ingredient.


BACKGROUND ART

There are about two million patients suffering from acute hepatitis and chronic hepatitis in Japan, and the development of medicines to remedy these diseases is constantly underway. It is known that a dibenzocyclooctadiene type lignan contained in the fruit of Schisandra chinesis BAILL belonging to the genus Schisandraceae is valuable as a remedy for these liver diseases (see Japanese Patent Application No. 60-122560), and the development of a chemical having a higher liver ailment-moderating action is now desired.


DISCLOSURE OF THE INVENTION

The present inventors carried out research with a view to developing a substance having a more effective action of moderating liver ailments and have already found and proposed several compounds (see Japanese Patent Application No. 60-136261). This research was continued, and a novel compound represented by the following formula (I) was found. The present invention was completed on this basis.
More specifically, in accordance with the present invention, there is provided a novel biphenyl derivative represented by the following formula (I): ##STR2## wherein R.sub.0 and R.sub.1 independently stand for a lower alkyl group or R.sub.0 and R.sub.1 together represent a group O=C<, R.sub.2 stands for an alkyl group having 1 to 3 carbon atoms, and R.sub.3 and R.sub.4 independently stand for a hydrogen atom or a lower alkyl group.


BEST MODE FOR CARRYING OUT THE INVENTION

Of compounds of the formula (I) where R.sub.0 and R.sub.1 together form O=C< and R.sub.3 is a hydrogen atom, a compound in which R.sub.4 is an alkyl group having 1 to 3 carbon atoms is preferred.
Of compounds of the formula (I) where R.sub.0 and R.sub.1 together for O=C< and R.sub.3 is a lower alkyl group, a compound in which R.sub.2 is a methyl group and each of R.sub.3 and R.sub.4 is a methyl group is preferred.
Of compounds of the formula (I) where R.sub.0 and R.sub.1 stand for a lower alkyl group, a compound in which R.sub.2 is a methyl group is preferred, and a compound in which R.sub.2 is a methyl group and each of R.sub.3 and R.sub.4 is an ethyl group is especially preferred.
According to the present invention, the compound of the formula (I) is prepared according to the following procedures.
A compound of the formula (I) in which R.sub.0 and R.sub.1 together form O=C<, R.sub.3 is a hydrogen atom and R.sub.4 is a lower alkyl group is obtained by reacting a compound represented by the following formula (II): ##STR3## wherein R.sub.2 and R.sup.4 are as defined above and R.sub.5 stands for an alkyl group, with acetic acid. The compound of the formula (II) is prepared by reacting a compound represented by the following formula (III): ##STR4## wherein R.sub.2, R.sub.4 and R.sub.5 are as defined above, with lead tetra-acetate.
A compound of the formula (I) in which R.sub.0 and R.sub.1 stand for a lower alkyl group or R.sub.0 and R.sub.1 together form O=C< and R.sub.3 is a lower alkyl group is obtained by alkylating a compound represented by the following formula (IV): ##STR5## wherein R.sub.2 is as defined above, that is, a compound of the formula (I) in which R.sub.0 and R.sub.1 together form O=C<, R.sub.3 is a hydrogen atom and R.sub.4 is a methyl group.
A compound of the formula (I) in which Ro and R.sub.1 stand for a lower alkyl group is obtained by alkylating a compound of the following formula (V): ##STR6## that is, a compound of the formula (I) in which R.sub.0 and R.sub.1 together form O=C< and R.sub.3 and R.sub.4 stand for a methyl group.
Furthermore, a compound of the formula (I) in which R.sub.0 and R.sub.1 stand for a lower alkyl group and R.sub.3 and R.sub.4 stand for a hydrogen atom is obtained by subjecting a compound of the form

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