1-azaindolizine derivatives, synthetic intermediates thereof and

Details 1-azaindolizine derivatives, synthetic intermediates thereof and 1-azaindolizine derivatives, synthetic intermediates thereof and

1991-06-26

1992-05-12

Dentz, Bernard

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

546121, A61K 31435, C07D47104

Patent

active

051128330

DESCRIPTION:

BRIEF SUMMARY
TECHNICAL FIELD

The present invention relates to novel 1-azaindolizine (i.e., imidazo[1,2-a]pyridine) derivatives or pharmaceutically acceptable salts thereof, synthetic intermediates thereof and antiallergic agents containing 1-azaindolizine derivatives.


BACKGROUND ART

Several 1-azaindolizine derivatives have been already reported, but the derivatives having oxy and vinyl groups at positions 2 and 3, respectively, are disclosed only in Yakugaku Zasshi, 101, 11, pp. 980-990 (1981), Kurata et al, which has no pharmaceutical data. In recently increasing allergic diseases, rhinitis, bronchial asthma and others, patients are mainly treated with agents, such as disodium chromoglycate (DSCG) or tranilast, which inhibit the release of chemical mediators.
However, these agents do not exhibit sufficient effects against these disease and it is desired to develop a new antiallergic agent having more excellent activity.
Under these circumstances, we, the inventors carried out studies to find that the below-mentioned 1-azaindolizine derivatives of formula (I) exhibits remarkably excellent antiallergic activity, thus completing the present invention.
More specifically, 1-azaindolizine derivatives according to the present invention (hereinafter referred to as compounds of the present invention) are compounds or pharmaceutically acceptable salts thereof represented by formula (I) ##STR1## wherein R.sub.1 and R.sub.2 represent independently hydrogen atom, halogen atom, C.sub.1-4 alkyl group or C.sub.1-4 alkoxy group; and R.sub.3 represents C.sub.1-6 alkyl group, substituted C.sub.1-4 alkyl group (substituent is C.sub.3-5 cycloalkyl group, hydroxyl group, acetylamino group, C.sub.1-4 alkoxy group or cyano group) or C.sub.2-4 alkenyl group. invention (hereinafter referred to as synthetic intermediates of the present invention) are represented by formula (II) ##STR2## wherein R.sub.1, R.sub.2 and R.sub.3 are as defined above and R.sub.4 represents C.sub.1-10 alkyl group or benzyl group.
Antiallergic agents of the present invention are agents containing the compound of the present invention as effective component.
The terms used for definition of letters in the formulas (I) and (II) by which the compounds of the present invention and synthetic intermediates thereof are respectively represented are defined and exemplified in the following.
The "halogen atom" may be chlorine, bromine or iodine atom.
The "C.sub.1-4 alkyl group" refers to a straight- or branched-chain alkyl group having 1 to 4 carbon atoms such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl or the like.
The "C.sub.1-6 alkyl group" refers to a straight- or branched-chain alkyl group having 1 to 6 carbon atoms such as those referred to in the above-mentioned C.sub.1-4 alkyl group, pentyl, hexyl or the like.
The "C.sub.1-10 alkyl group" refers to a straight- or branched-chain alkyl group having 1 to 10 carbon atoms such as those referred to in the above-mentioned C.sub.1-6 alkyl group, octyl, decyl or the like.
The "C.sub.3-5 cycloalkyl group" refers to a cycloalkyl group having 3 to 5 carbon atoms such as cyclopropyl, cyclobutyl, cyclopentyl or the like.
The "C.sub.1-4 alkoxy group" refers to a straight- or branched-chain alkoxy group having 1 to 4 carbon atoms such as methoxy, ethoxy, propoxy, isopropoxy, butoxy, isobutoxy, sec-butoxy, tert-butoxy or the like.
The "C.sub.2-4 alkenyl group" refers to an alkenyl group having 2 to 4 carbon atoms such as vinyl, 1-propenyl, 2-propenyl, 2-butenyl, 3-butenyl or the like.
The compounds of the present invention are for example as follows: salt sodium salt sodium salt sodium salt sodium salt its sodium salt its sodium salt sodium salt its sodium salt sodium salt its sodium salt sodium salt its sodium salt its sodium salt its sodium salt and its sodium salt and its sodium salt its sodium salt sodium salt sodium salt its sodium salt its sodium salt its sodium salt its sodium salt its sodium salt its sodium salt and its sodium salt its sodium salt its sodium salt and its sodium salt its sodium s

REFERENCES:
Kurata et al., Yakugaku Zasshi, 101 (11), pp. 980-990 (1981).

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