, their pharmaceutically acceptable acid-additive salts where: Q - piperidinyl, morpholine group, piperazine group that can be substituted if necessary with C1-4-alkyl, or group of the formula S-(O)-p-R3 where p = 0, 1 or 2; R3 - direct or branched C1-8-alkyl, C2-6-alkenyl or phenyl-(C1-4-alkyl) being the latter has one or more halogen- or nitro-substituents; or group of the formula NR4R5 where each R4 and R5 means hydrogen, direct or branched C1-10-alkyl, C2-6-alkenyl, phenyl-(C1-4-alkyl) or di-(C1-4-alkyl)-amino-(C1-6-alkyl); each R1 and R2 means hydrogen or direct or branched C1-4-alkyl, or R1 and R2 form together group of the formula (CH2)n-Y-(CH2)m, where Y - CH2-group, sulfur atom or group of the formula NR6, where R6 means phenyl-(C1-4-alkyl); n and m are whole numbers: 0, 1, 2, 3, 4 or 5; Z - group of the formula NR7R8 where each R7 and R8 means hydrogen, C2-6-alkenyl, C3-8-cycloalkyl, adamantyl or phenyl-(C1-4-alkyl) being the latter has possibly one or more substituents taken from the group including halogen, hydroxy, C1-4-alkyl, C1-4-alkoxy, amino and nitro, (C1-4-alkyl)-amino-(C1-6-alkyl), di-(C1-4-alkyl)-amino-(C1-6-alkyl) or C1-6-alkyl being the latter can be substituted with hydroxy, amino, carboxy, morpholine-carbonyl, 4-(2-hydroxyethyl)-piperazine-1-yl-carbonyl, (C1-4-alkoxy)-carbonyl or 5- or 6-membered saturated or unsaturated heterocyclic group containing one or more nitrogen and/or oxygen atoms and, possibly, fused to benzene ring; or R7 and R8 form together group of the formula (CH2)J-W-(CH2)K where each j and K means 1, 2 or 3 and W - oxygen, CH2, CHOH or group of the formula NR10 where: R10 - hydrogen, C1-4-alkoxycarbonyl or C1-4-alkyl being the latter has, possibly, substituent taken from the group including hydroxy and phenyl; or group of the formula SR9 where R9 - C1-4-alkyl substituted with (C1-4-alkoxy)-carbonyl at condition that if Q - hydrogen or group of the formula S-(O)-p-R3 then R1 and R2 are not hydrogen and not C1-4-alkyl. The synthesized compounds show valuable biological properties (antiinflammatory, spasmolytic, analgetic, they inhibit bile and stomach acid secretion). Invention relates to pharmaceutical composition, method of cardiotonic and/or coronary dilating effect on heart also. EFFECT: improved method of synthesis, enhanced effectiveness. 14 cl"/>
DERIVATIVES OF 5-(AMINO-SUBSTITUTED)-1,2,4-TRIAZOLO-1,5-A-PYRIMIDINE, THEIR PHARMACEUTICALLY ACCEPTABLE ACID-ADDITIVE SALTS, PHARMACEUTICAL COMPOSITION SHOWING CARDIOTONIC AND CORONARY-DILATING ACTION AND A METHOD OF CARDIOTONIC AND/OR CORONARY-DILATING EFFECT ON HEART
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DERIVATIVES OF 5-(AMINO-SUBSTITUTED)-1,2,4-TRIAZOLO-1,5-A-PYRIMIDINE, THEIR PHARMACEUTICALLY ACCEPTABLE ACID-ADDITIVE SALTS, PHARMACEUTICAL COMPOSITION SHOWING CARDIOTONIC AND CORONARY-DILATING ACTION AND A METHOD OF CARDIOTONIC AND/OR CORONARY-DILATING EFFECT ON HEART
DERIVATIVES OF 5-(AMINO-SUBSTITUTED)-1,2,4-TRIAZOLO-1,5-A-PYRIMIDINE, THEIR PHARMACEUTICALLY ACCEPTABLE ACID-ADDITIVE SALTS, PHARMACEUTICAL COMPOSITION SHOWING CARDIOTONIC AND CORONARY-DILATING ACTION AND A METHOD OF CARDIOTONIC AND/OR CORONARY-DILATING EFFECT ON HEART
FIELD: organic chemistry, heterocyclic compounds. SUBSTANCE: invention relates to derivatives of 5-(amino-substituted)-1,2,4-triazolo-[1,5-a]-pyrimidine of the general formula (I): , their pharmaceutically acceptable acid-additive salts where: Q - piperidinyl, morpholine group, piperazine group that can be substituted if necessary with C1-4-alkyl, or group of the formula S-(O)-p-R3 where p = 0, 1 or 2; R3 - direct or branched C1-8-alkyl, C2-6-alkenyl or phenyl-(C1-4-alkyl) being the latter has one or more halogen- or nitro-substituents; or group of the formula NR4R5 where each R4 and R5 means hydrogen, direct or branched C1-10-alkyl, C2-6-alkenyl, phenyl-(C1-4-alkyl) or di-(C1-4-alkyl)-amino-(C1-6-alkyl); each R1 and R2 means hydrogen or direct or branched C1-4-alkyl, or R1 and R2 form together group of the formula (CH2)n-Y-(CH2)m, where Y - CH2-group, sulfur atom or group of the formula NR6, where R6 means phenyl-(C1-4-alkyl); n and m are whole numbers: 0, 1, 2, 3, 4 or 5; Z - group of the formula NR7R8 where each R7 and R8 means hydrogen, C2-6-alkenyl, C3-8-cycloalkyl, adamantyl or phenyl-(C1-4-alkyl) being the latter has possibly one or more substituents taken from the group including halogen, hydroxy, C1-4-alkyl, C1-4-alkoxy, amino and nitro, (C1-4-alkyl)-amino-(C1-6-alkyl), di-(C1-4-alkyl)-amino-(C1-6-alkyl) or C1-6-alkyl being the latter can be substituted with hydroxy, amino, carboxy, morpholine-carbonyl, 4-(2-hydroxyethyl)-piperazine-1-yl-carbonyl, (C1-4-alkoxy)-carbonyl or 5- or 6-membered saturated or unsaturated heterocyclic group containing one or more nitrogen and/or oxygen atoms and, possibly, fused to benzene ring; or R7 and R8 form together group of the formula (CH2)J-W-(CH2)K where each j and K means 1, 2 or 3 and W - oxygen, CH2, CHOH or group of the formula NR10 where: R10 - hydrogen, C1-4-alkoxycarbonyl or C1-4-alkyl being the latter has, possibly, substituent taken from the group including hydroxy and phenyl; or group of the formula SR9 where R9 - C1-4-alkyl substituted with (C1-4-alkoxy)-carbonyl at condition that if Q - hydrogen or group of the formula S-(O)-p-R3 then R1 and R2 are not hydrogen and not C1-4-alkyl. The synthesized compounds show valuable biological properties (antiinflammatory, spasmolytic, analgetic, they inhibit bile and stomach acid secretion). Invention relates to pharmaceutical composition, method of cardiotonic and/or coronary dilating effect on heart also. EFFECT: improved method of synthesis, enhanced effectiveness. 14 cl
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