Pyrazolo[1,5-a]pyrimidine derivatives

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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544253, 544256, 544255, 544280, C07D48704, C07D48700, A61K 31505

Patent

active

059858826

DESCRIPTION:

BRIEF SUMMARY
TECHNICAL FIELD

The present invention relates to novel pyrazolo[1,5-a]pyrimidine derivatives.


PRIOR ART

The pyrazolo[1,5-a]pyrimidine derivatives of the invention are novel compounds which have never been published in the literature.


DISCLOSURE OF THE INVENTION

An object of this invention is to provide compounds useful as medicine. The use of the compounds as medicine will be described hereinafter.
The present invention provides novel pyrazolo[1,5-a]pyrimidine derivatives represented by the following formula (1) ##STR2## wherein R.sup.1 is lower alkyl, lower alkenyl, hydroxy(lower)alkyl, (lower)alkanoyloxy(lower)alkyl, (lower)alkoxy(lower)alkyl, (lower)alkylthio(lower)alkyl, furyl or thienyl, R.sup.2 is pyridyl, 1-oxide-pyridyl, lower alkyl-substituted pyrazinyl, lower alkyl-substituted pyrimidinyl, or phenyl which may have 1 to 3 substituents selected from the group consisting of lower alkyl, lower alkoxy and halogen, R.sup.3 is hydrogen or halogen, and A is a single bond or lower alkylene; with the proviso that when R.sup.1 is lower alkyl, R.sup.2 is lower alkyl-substituted pyrazinyl or lower alkyl-substituted pyrimidinyl.
Examples of the groups in the compounds represented by the formula (1) are as follows.
The lower alkyl group includes straight- or branched-chain lower alkyl groups such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl, hexyl and the like.
The lower alkenyl group includes vinyl, allyl, isopropenyl, 1-butenyl, 2-butenyl, 3-butenyl, 1-pentenyl, 2-pentenyl, 3-pentenyl, 4-pentenyl, 1-hexenyl, 2-hexenyl, 3-hexenyl, 4-hexenyl, 5-hexenyl and the like.
The hydroxy(lower)alkyl group includes hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl,3-hydroxy-propyl, 3-hydroxybutyl, 4-hydroxybutyl, 5-hydroxypentyl, 6-hydroxyhexyl and the like.
The (lower)alkanoyloxy(lower)alkyl group includes acetoxymethyl, propionyloxymethyl, butyryloxymethyl, valeryloxymethyl, pivaloyloxymethyl, hexanoyloxymethyl, heptanoyloxymethyl, 2-acetoxyethyl, 3-acetoxypropyl, 3-acetoxybutyl, 4-acetoxybutyl, 5-acetoxypentyl, 6-acetoxyhexyl and the like.
The (lower)alkoxy(lower)alkyl group includes methoxymethyl, ethoxymethyl, propoxymethyl, isopropoxymethyl, butoxymethyl, pentyloxymethyl, hexyloxymethyl, 2-methoxyethyl, 2-ethoxyethyl, 3-methoxypropyl, 3-methoxybutyl, 4-methoxybutyl, 5-methoxypentyl, 6-methoxyhexyl and the like.
The furyl group includes 2-furyl and 3-furyl.
The thienyl group includes 2-thienyl and 3-thienyl.
The pyridyl group includes 2-pyridyl, 3-pyridyl and 4-pyridyl.
The 1-oxide-pyridyl group includes 1-oxide-2-pyridyl, 1-oxide-3-pyridyl and 1-oxide-4-pyridyl.
The halogen atom includes fluorine, chlorine, bromine and iodine.
The lower alkoxy group includes methoxy, ethoxy, propoxy, isopropoxy, butoxy, pentyloxy, hexyloxy and the like.
The (lower)alkylthio(lower)alkyl group includes methylthiomethyl, ethylthiomethyl, propylthiomethyl, butylthiomethyl, pentylthiomethyl, hexylthiomethyl, 2-methylthioethyl, 2-ethylthioethyl, 3-methylthiopropyl, 3-methylthiobutyl, 4-methylthiobutyl, 5-methylthiopentyl, 6-methylthiohexyl and the like.
The lower alkyl-substituted pyrimidinyl group includes 4-methyl-2-pyrimidinyl, 5-methyl-2-pyrimidinyl, 4,6-dimethyl-2-pyrimidinyl, 4-ethyl-2-pyrimidinyl, 5-ethyl-2-pyrimidinyl, 4,6-diethyl-2-pyrimidinyl, 4-propyl-2-pyrimidinyl, 5-propyl-2-pyrimidinyl, 4,6-dipropyl-2-pyrimidinyl, 4-butyl-2-pyrimidinyl, 5-butyl-2-pyrimidinyl, 4,6-dibutyl-2-pyrimidinyl, 4-pentyl-2-pyrimidinyl, 5-pentyl-2-pyrimidinyl, 4,6-dipentyl-2-pyrimidinyl, 4-hexyl-2-pyrimidinyl, 5-hexyl-2-pyrimidinyl, 4,6-dihexyl-2-pyrimidinyl and the like.
The lower alkyl-substituted pyrazinyl group includes 2-methyl-5-pyrazinyl, 2-methyl-3-pyrazinyl, 2-methyl-6-pyrazinyl, 2-ethyl-5-pyrazinyl, 2-propyl-5-pyrazinyl, 2-butyl-5-pyrazinyl, 2-pentyl-5-pyrazinyl, 2-hexyl-5-pyrazinyl and the like.
The lower alkylene group includes methylene, ethylene, trimethylene, tetramethylene, pentamethylene, hexamethylene and the like.
The phenyl group which may have 1 to 3 substituents selected from the group consisting of

REFERENCES:
Robins et al., (J. Heterocycl. Chem. (1985), 22 (3), pp. 601-364).
English Abstract of JP 61-57587, 1986.

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