Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1985-07-22
1988-03-01
Rizzo, Nicholas S.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514227, 514254, 514261, 544 61, 544118, 544276, 544277, C07D47304, A61K 3152
Patent
active
047286440
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
The present invention relates to novel and pharmaceutically useful purine derivatives.
BACKGROUND OF THE INVENTION
Anti-tumor active 8-(2-, 3-, and 4-pyridyl)purine compounds are disclosed in British Pat. No. 1201997, 8-phenyladenine compounds exhibiting xanthineoxydase inhibitory activity are disclosed in Journal of Medicinal Chemistry, vol. 11, p. 656, 1968, and 9-purinyl hydroxy alkanoic acid derivatives useful as hypocholesterolaemic agents are disclosed in Belgium Pat. No. 737949.
However, there are no disclosures on purine derivatives having antiinflammatory, analgesic, antipyretic or antiallergic activity, or inhibitory activity on platelet aggregation, in the prior art, including the above documents.
Therefore, the purpose of the present invention is to provide novel purine derivatives having antiinflammatory, analgesic, antiseptic and antiallergic activity, and inhibitory activity on platelet aggregation.
As a result of intensive investigations, the present inventors have completed the present invention.
The present invention relates to purine derivatives of the formula: ##STR2## or pharmaceutically acceptable acid addition salts thereof and/or hydrates thereof.
In the above formula (I), R is a hydrogen atom, an alkyl group or a phenyl group which may be optionally substituted by at least one substituent selected from a halogen atom, a lower alkyl group and a lower alkoxy group; each of R.sup.1 and R.sup.2 is a hydrogen atom, an alkyl group, a cycloalkyl group, a hydroxyalkyl group, a dialkylaminoalkyl group, a cyclic amino alkyl group, an alkenyl group or an aralkyl group, or R.sup.1 and R.sup.2 together with the adjacent nitrogen atom form a heterocycle; and each of R.sup.3 and R.sup.4 is a hydrogen atom or a lower alkyl group.
In this specification, the alkyl group means a straight or branched alkyl group having 1 to 8 carbon atoms and includes, for example, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl, hexyl and octyl; the halogen atom means fluorine, chlorine, bromine and iodine. The lower alkyl group means a straight or branched alkyl group having 1 to 4 carbon atoms and includes, for example, methyl, ethyl, propyl, isopropyl, butyl, isobutyl and tert-butyl. The lower alkoxy group means a straight or branched alkoxy group having 1 to 4 carbon atoms and includes, for example, methoxy, ethoxy, propoxy, isopropoxy, butoxy and tert-butoxy. The cycloalkyl group means a cyclic saturated hydrocarbon group having 3 to 7 carbon atoms and includes cyclopropyl, cyclobutyl, cylopentyl,cyclohexyl and cycloheptyl. The hydroxyalkyl group has 1 to 8 carbon atoms in the alkyl moiety and includes, for example, 2-hydroxyethyl, 2-hydroxypropyl, 3-hydroxypropyl and 4-hydroxybutyl. The dialkylaminoalkyl group has 1 to 8 carbon atoms in each alkyl moiety and includes, for example, 2-dimethylaminoethyl, 2-diethylaminoethyl, 3-dimethylaminopropyl and 4-dimethylaminobutyl. The cyclic aminoalkyl group may have at least one nitrogen atom, which may be substituted by a lower alkyl group or a hydroxyalkyl group, oxygen atom or sulfur atom as other heteroatom in the cyclic amino moiety and has 1 to 8 carbon atoms in the alkyl moiety, and includes, for example, 1-pyrrolidinylmethyl, 2-(1-pyrrolidinyl)ethyl, 2-piperidinoethyl, 2-morpholinoethyl, 3-thiomorpholinopropyl, 2 -(1-piperazinyl)ethyl, 2-(4-methyl-1-piperazinyl)ethyl, 2-[4-(2-hydroxyethyl)-1-piperazinyl]ethyl and 2-(4-methyl-1-homopiperazinyl)ethyl. The alkenyl group means a straight or branched alkenyl group having 2 to 8 carbon atoms and includes, for example, vinyl, allyl, isopropenyl, butenyl, pentenyl, 1-methyl-3-butenyl and hexenyl. The aralkyl group means an arylalkyl group and includes, for example, benzyl, 2-phenylethyl and 3-phenylpropyl. The heterocyle formed by R.sup.1 and R.sup.2 together with the adjacent nitrogen atom may have at least one nitrogen atom, which may be substituted by a lower alkyl group or a hydroxyalkyl group, oxygen atom or sulfur atom as other heteroatom, and includes, for example,
REFERENCES:
patent: 4473571 (1984-09-01), Lesher et al.
Imayoshi Tomonori
Sueoka Hiroyuki
Terasawa Michio
Yasumoto Mitsuyoshi
Yuki Hiroshi
Rizzo Nicholas S.
Yoshitomi Pharmaceutical Industries Ltd.
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