KR880009021A - Pyrazolo [3,4-d] pyrimidine derivatives, compositions and uses thereof - Google Patents

Abstract

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Description

Pyrazolo [3,4-d] pyrimidine derivatives, compositions and uses thereof

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Claims (21)

A compound of formula (I) or a salt thereof pharmaceutically usable for use: [Wherein, R ¹ is an aryl or heteroaryl group which may be substituted: R ² is a lower alkyl group: R ³ and R ⁴ are each independently hydrogen or a lower alkyl group: R ⁵ is hydrogen, a lower alkyl group or a lower group As an acyl group, bonded at the 1- or 2-position of the pyrazole ring, X is a lower alkylene group which may contain a hetero atom, and the dashed line indicates that there are two double bonds in the pyrazole ring.] The compound of claim 1, wherein R ¹ is halogen, C _1-4 alkyl, C _1-4 alkoxy, nitro, amino, NC _1-4 alkylamino, C _1-4 alkylamino, hydroxy, trifluoromethyl , Aryl or heteroaryl, which may be substituted with 1-3 substituents selected from the group consisting of carbamoyl, NC _1-4 alkylcarbamoyl and N, N-diC _1-4 alkylcar N, N-dirbamoyl R ² is C _1-4 alkyl; R ³ and R ⁴ are each independently hydrogen or C ₁ ~ ₄ alkyl; R ⁵ is hydrogen, C _1-2 alkyl, C _1-5 alkanoyl or C _1-4 alkoxycarbonyl, which is bonded at the 1- or 2-position of the pyrazole ring; X is a group of C _1-7 alkylene or a general formula-(CH ₂ ) _m -Y- (CH ₂ ) _n- (wherein m is 2 or 3, n is an integer from 0 to 3, and Y is Oxygen, sulfur, imino or NC _1-4 alkylimino. And a compound of formula (I) or a salt thereof for pharmaceutical use, wherein the dotted line indicates that there are two double bonds in the pyrazole ring. The compound of claim 1 wherein R ¹ is phenyl, naphthyl, cinnaolinyl, furyl, isobenzofuranyl, isothiazolyl, isoxazolyl, naphthyridinyl, phthalazinyl, pyrazinyl, pyridazinyl, Pyridyl, pyrimidinyl, quinazolinyl, quinolyl, quinoxalinyl, thienyl, pyridinio, quinazolinio, quinolinio or quinoxalliniorose, each of the groups described above being halogen, C _1-4 Alkyl, C _1-4 alkoxy, nitro, amino, NC _1-4 alkylamino, N, N-diC _1-4 alkylamino, hydroxy, trifluoromethyl, carbamoyl, NC _1-4 alkylcarba Moles and N, N-diC _1-4 alkylcarbamoyl compounds of the general formula (I) which are substituted or unsubstituted with 1-3 substituents selected from the group consisting of: salt. The phenyl, pyridyl or thienyl of claim 1, wherein R ¹ may be substituted with 1 to 3 substituents selected from the group consisting of halogen, C _1-4 alkyl, C _1-4 alkoxy, nitro, and amino. A compound of formula (I) or a salt thereof for use in pharmaceutical use, characterized in that A compound of formula (I) or a salt thereof for use in pharmaceuticals according to claim 1, wherein R ¹ is phenyl which may be substituted with 1-3 substituents selected from the group consisting of halogen and nitro. A compound of formula (I) or a salt thereof for use in pharmaceutical use according to claim 1, wherein R ² is propyl or butyl. A compound of formula (I) or a salt thereof for use in pharmaceutical use according to claim 1, wherein R ³ is methyl or ethyl and R ⁴ is hydrogen. A compound of formula (I) or a salt thereof for use in pharmaceutical use according to claim 1, wherein R ⁵ is hydrogen or C _2-4 alkanoyl. A compound of formula (I) or a salt thereof for use in pharmaceutical use according to claim 1, wherein R ⁵ is hydrogen. A compound of formula (I) or a salt thereof for use in pharmaceutical use according to claim 1, wherein X is methylene or ethylene. A compound according to claim 1, wherein R ¹ is phenyl which may be substituted with 1-3 substituents selected from the group consisting of halogen and nitro; R ² is propyl or butyl; R ³ is methyl; R ₄ is hydrogen; R ⁵ is C _2-4 alkanoyl bonded to the 2-position of hydrogen or pyrazole ring; And a compound of formula (I) or a salt thereof for pharmaceutical use, wherein X is methylene or ethylene. The salt according to claim 1, which is an acid addition salt usable for pharmaceutical use, for the pharmaceutical use of the compound of general formula (I). The compound of formula (I) according to claim 1, wherein the compound is 7-benzyl-3-methylamino-5-propylpyrazolo [3,4-d] pyrimidine-4,6 (5H, 7H) -dione. Or a salt thereof for use in pharmaceutical use. The compound of claim 1, wherein the compound is 7- (3-chlorobenzyl) -3-methylamino-5-propylpyrazolo [3,4-d] pyrimidine-4,6 (5H, 7H) -dione A compound of formula (I) or a salt thereof usable for pharmaceutical use. The compound of claim 1, wherein the compound is 7- (4-chlorobenzyl) -3-methylamino-5-propylpyrazolo [3,4-d] pyrimidine-4,6 (5H, 7H) -dione A compound of formula (I) or a salt thereof usable for pharmaceutical use. The general formula of claim 1, wherein the compound is 3-methylamino-7-phenethyl-5-propylpyrazolo [3,4-d] pyrimidine-4,6- (5H, 7H) -dione. A compound of (I) or a salt thereof usable for pharmaceutical use. The compound of claim 1, wherein the compound is 2-butyryl-7- (3-chlorobenzyl) -3-methylamino-5-propyl-2H-pyrazolo [3,4-d] pyrimidine-4,6 (5H , 7H) -dione, a compound of formula (I) or a salt thereof usable for pharmaceutical use. The compound of claim 1, wherein the compound is 5-butyl-3-methylamino-7- (2-nitrobenzyl) pyrazolo [3,4-d] pyrimidine-4,6 (5H, 7H) -dione A compound of formula (I) or a salt thereof usable for pharmaceutical use. (a) an effective amount of a compound as claimed in any one of claims 1 to 18, or a salt thereof available for pharmaceutical use, as an active ingredient required for activating the action and metabolism of the brain; A pharmaceutical composition suitable for activating the action and metabolism of the brain characterized by having a carrier, excipient or diluent available for utility use. 19. A method of claim 1 wherein the compound claimed in any one of claims 1-18 or a salt thereof for use in pharmaceutical use, or a pharmaceutical composition claimed in claim 19, is administered to a mammal in an effective amount necessary to activate the function and metabolism of the brain. A method for activating the action and metabolism of the brain in a mammal. Use of the compound claimed in any one of claims 1 to 18 or a salt thereof for use in pharmaceutical use, or a pharmaceutical composition as claimed in claim 19 for the treatment of mammals. ※ Note: The disclosure is based on the initial application.