Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-08-20
1999-11-23
Spivack, Phyllis G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514262, 514267, 544251, 544265, 544276, 544277, A61K 3152, C07D47334, C07D48714
Patent
active
059901187
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to novel purine compounds or triazolopurine compounds having xanthine oxidase inhibitory activity, as well as to pharmaceutical compositions containing the compounds as an active ingredient.
BACKGROUND ART
Xanthine oxidase is an enzyme which plays an important role in in vivo uricogenesis. Thus, xanthine oxidase inhibitors are useful as remedies for hyperuricemia, which is a causal disease of gouty attack, and as preventive agents against gouty attack. Presently, allopurinol is the sole drug clinically used as a xanthine oxidase inhibitor. Compounds other than allopurinol having xanthine oxidase inhibitory activity have been reported, and some of them are under investigation for the development of pharmaceuticals (Japanese Patent Application Laid-Open (kokai) Nos. 5-310742 and 6-316578, and Japanese Patent Publication (kokoku) No. 6-41466).
Recently, purines have been reported to have pharmacological activities such as bronchodialating action, and therefore, use of the compounds as pharmaceuticals is expected [Pharmaceutical Society of Japan, Lecture Summaries of the 112th Annual Conference, 233 (1992)]. However, xanthine oxidase inhibitory activities of those compounds have so far not been reported.
Accordingly, the primary object of the present invention is to provide novel purine compounds endowed with xanthine oxidase inhibitory activity.
DISCLOSURE OF THE INVENTION
The present inventors have conducted careful studies in an attempt to attain the above-mentioned object, and have found that purine compounds or triazolopurine compounds having a specific structure exhibit a xanthine oxidase inhibiting effect and are useful as pharmaceuticals. The present invention was accomplished based on this finding.
Accordingly, the present invention is directed to a purine compound of the following formula (I): ##STR2## (wherein R.sup.1 represents a hydrogen atom, a halogen atom, a hydroxyl group, a mercapto group, or an amino group; R.sup.2 represents an alkyl group or an aryl group; and R.sup.3 represents a hydrogen atom, an alkyl group, or an aryl group), as well as to pharmaceutical compositions containing the compound as an active ingredient, such as xanthine oxidase inhibitors, remedies for hyperuricemia, and preventive and therapeutic agents for gout.
The present invention is also directed to a triazolopurine compound of the following formula (II): ##STR3## (wherein R.sup.4 represents a hydrogen atom, a halogen atom, a hydroxyl group, a mercapto group, or an amino group; and R.sup.5 represents a hydrogen atom, an alkyl group, or an aryl group), as well as to pharmaceutical compositions containing the compound as an active ingredient, such as xanthine oxidase inhibitors, remedies for hyperuricemia, and preventive and therapeutic agents for gout.
The present invention is also directed to use of the above-described purine compound of formula (I) or triazolopurine compound of formula (II) as a xanthine oxidase inhibitor, a remedy for hyperuricemia, or as a preventive and therapeutic agent for gout.
The present invention is also directed to a method for preventing and treating hyperuricemia or gout, characterized by administering an effective amount of the aforementioned purine compound (I) or triazolopurine compound (II).
BEST MODES FOR CARRYING OUT THE INVENTION
The purine compounds of the present invention are represented by the above-described formula (I), and R.sup.1 to R.sup.3 in the formula are defined as above.
The halogen atoms represented by R.sup.1 include a chlorine atom, a bromine atom, an iodine atom, and a fluorine atom.
The alkyl groups represented by R.sup.2 and R.sup.3 include C1-C7 linear or branched lower alkyl groups such as methyl, ethyl, propyl, and butyl.
The aryl groups represented by R.sup.2 and R.sup.3 include a phenyl group having a substituent of the following formula (III): ##STR4## (wherein R.sup.6 represents a halogen atom, an alkyl group, an alkoxy group, an amino group, an alkylamino group, a methylenedioxy group, a hydroxyl gr
REFERENCES:
A. Griner-Sorolla et al., "Nitrosaminopurines and Nucleosides, Synthesis and Biological Activivty", Journal of Medicinal Chemistry, vol. 16, No. 4, pp. 365-369 (1973).
J. Goodfellow, "Cooperative Effects in Water-biomolecule Crystal Systems", Proc. Natl. Acad. Sci. USA, vol. 79, pp. 4977-4979 (Aug. 1982).
Brown et al., Aust. Chem35(6), 1263-7, 1982.
Endo Kazuki
Imaizumi Masahiro
Nagamatsu Tomohisa
Watanabe Yoko
Spivack Phyllis G.
Yamasa Corporation
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