Fused pyrazole compounds and pharmaceutical use thereof

Details Fused pyrazole compounds and pharmaceutical use thereof Fused pyrazole compounds and pharmaceutical use thereof

1989-06-13

1991-04-09

Bentz, Bernard I.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

514218, 5142285, 5142315, 514253, 514303, 540475, 540597, 544 586, 544 61, 544362, 546119, 548371, 548372, A61K 31435, C07D47104

Patent

active

050065203

DESCRIPTION:

BRIEF SUMMARY
TECHNICAL FIELD AND BACKGROUND ART

This invention relates to fused pyrazole compounds which are novel and useful as pharmaceuticals.
Heretofore, as fused pyrazole compounds, there have been described the indazole derivatives in Japanese Patent Application Laid-open (Kokai) No. 125281/1976 and pyrazolo[3,4-b]pyridine derivatives in U.S. Pat. No. 3,983,128 respectively.
Meanwhile, with the considerable developments of chemotherapeutic agents in the recent years, there has been seen remarkable progress in the therapy of infectious diseases. On the other hand, however, there have appeared new problems such as opportunistic infectious diseases on which the previous chemotherapeutic agents fail to effectively act and infectious diseases which result from leukopenia caused by the application of radiation-therapy or medicine-therapy to patients of cancers. For the purpose of the treatment of such infectious diseases, there have been desired not only the application of antibacterial agents but also the development of the medicines which are capable of recovering infection-phylactic action of feeble patients. However, success has not been attained.


DISCLOSURE OF THE INVENTION

For the purpose of developing infection-phylactic agents possessing as their main actions leukocytophagy-sthenic action and leukocyte multiplication action which seem to play the most important role at the initial stage of infection, the present inventors conducted intensive researches to find that the novel fused pyrazole compounds achieved the contemplated purpose, which resulted in the completion of this invention. That is, the present invention relates to the fused pyrazole compounds of the general formula ##STR2## and their pharmaceutically acceptable salts.
In the above formula, X is .dbd.N- or .dbd.CH-, R represents hydrogen, an alkyl group, an alkoxy group or a halogen; Y.sup.1 represents a group of the formula: ##STR3## phenyl group or a phenyl group substituted by one to three halogen(s), alkyl group(s) and/or alkoxy group(s), and Y.sup.2 represents a group of the formula: ##STR4## a group of the formula: --A.sup.2 --B.sup.2, hydrogen, an alkyl group, a phenylalkyl group, a phenylalkyl group in which the phenyl nucleus is substituted by one to three halogen(s), alkyl group(s) and/or alkoxy group(s), phenyl group or a phenyl group substituted by one to three halogen(s), alkyl group(s) and/or alkoxy group(s), an alkoxyalkyl group, a hydroxyalkyl group, an alkoxycarbonylalkyl group, a carboxyalkyl group or an acyloxyalkyl group, wherein either Y.sup.1 or Y.sup.2 represents or both of Y.sup.1 and Y.sup.2 represent a group of the formula: ##STR5## or of the formula ##STR6##
Herein, Z.sup.1 and Z.sup.2 are the same or different, and respectively represent --O--, --S-- or --NR.sup.3 (wherein R.sup.3 represents hydrogen or an alkyl group); A.sup.1 and A.sup.2 are the same or different, and respectively represent an alkylene group; B.sup.1 and B.sup.2 are the same or different, and respectively represent carboxyl group, an alkoxycarbonyl group, a phenylalkoxycarbonyl group (in which the phenyl necleus may be substituted by one to three halogen(s), alkyl group(s), and/or alkoxy group(s)), an acyl group, hydroxy group, an acyloxy group or a group of the formula: ##STR7## (wherein R.sup.1 and R.sup.2 are the same or different and respectively represent hydrogen, an alkyl group, a dialkylaminoalkyl group or a hydroxyalkyl group or represent a group which combinedly forms, together with the adjacent nitrogen atom, a heterocycle group) and L.sup.1 and L.sup.2 are the same or different and respectively represent hydrogen, a halogen, an alkyl group or an alkoxy group.
In this specification, the halogens include chlorine, bromine, fluorine and iodine and the alkyls mean straight- or branched-chain alkyls having 1-8 carbon atoms, which are exemplified by methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl, isopentyl, hexyl and the like. The alkoxys mean straight- or branched-chain alkoxys having 1-8 carbon atoms, which are exemplif

REFERENCES:
patent: 4612318 (1986-09-01), Winters
patent: 4808620 (1989-02-01), Oe et al.

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