1,2,3,4-TETRAHYDROPYRAZOLO-[5,1-C]-(1,2,4)-TRIAZINE OR ITS PHARMACEUTICALLY ACCEPTABLE SALT, METHOD OF ITS SYNTHESIS, PHARMACEUTICAL COMPOSITION INHIBITING PRODUCING AN INTERLEUKIN-1 AND TUMOR NECROSIS FACTOR, METHOD OF PROPHYLACTIC OR THERAPEUTIC TREATMENT OF PATIENTS WITH DISEASES MEDIATED BY INTERLEUKIN AND TUMOR NECROSIS FACTOR Russian patent published in 1999 - IPC

Abstract RU 2124517 C1

FIELD: organic chemistry. SUBSTANCE: invention relates to new derivatives of pyrazole of the formula (I) where R1 and R2 - phenyl possibly substituted with halide or pyridinyl possibly substituted with halide or lower alkoxy-group; R3 - hydrogen or lower alkanoyl; R4 - H, lower alkyl, cyclo-(lower)-alkyl, cyclo-(lower)-alkyl-(lower)-alkyl, lower alkoxycarbonylalkyl, phenylalkyl; adamantyl, phenylalkenyl, tetrahydropyrnyl, piperidyl or dioxapyroundecanyl, indanyl, lower alkanoyl, lower alkoxycarbonyl, lower alkoxyglyoxyloyl, lower alkylsulfonyl, cyclo-(lower)-alkylcarbonyl, benzoyl, phenyl-(lower)-alkenoyl, phenylthio-(lower)-alkanoyl, phenylcarbamoyl, phenyl-thiocarbamoyl, phenylglyoxyloyl, carbamoyl, morpholinylcarbonyl, indolyl- -(lower)-alkanoyl; R5 - H or lower alkyl, or its pharmaceutically acceptable salt. Compounds of the formula (I) can be used as drug for prophylactic and therapeutic treatment of patients with diseases mediated by IL-1 and TNF, for example, chronic inflammatory diseases, specific autoimmune diseases, human or animal organ damages caused by sepsis. EFFECT: improved method of synthesis, enhanced effectiveness. 7 cl, 14 dwg 28 ex

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RU 2 124 517 C1

Authors

Esio Kavai

Khitosi Jamazaki

Khirokazu Tanaka

Teruo Oku

Dates

1999-01-10Published

1994-02-09Filed