FIELD: pharmaceutical chemistry.
SUBSTANCE: invention relates to phenylpyridazine derivative of general formula I 
, wherein R1 represents C1-C12-alkyl optionally comprising cyclic C3-C6-alkyl structures and optionally substituted by phenyl, which may be substituted by 1-2 halogen atoms; or C1-C12-alkenyl substituted by optionally halogen-substituted phenyl; R2 and R3, independently form each other, represent hydrogen, C1-C12-alkyl, C1-C12-hydroxyalkyl, C1-C12-dihydroxyalkyl, or C1-C12-alkynyl; or R2 and R3, together with adjacent nitrogen atom form 5-6-membered saturated heterocyclic group containing 1-2 nitrogen atoms and optionally oxygen atom, indicated heterocyclic group being optionally substituted by C1-C12-alkyl group, C1-C12-alkoxydicarboxylic group or phenyl-C1-C7-alkyl group; X, Y, and Z, independently form each other, represent hydrogen, halogen, optionally halogen(s)-substituted C1-C12-alkyl, C1-C12-alkoxy, C1-C12-alkylthio, C1-C12-alkylsulfinyl, C1-C12-alkylsulfonyl, or phenyl; and n is a number from 0 to 5; provided that R2 and R3 cannot be simultaneously hydrogen atoms or identical C1-C3-alkyl groups when R1 is benzyl or C1-C3-alkyl group; and salts of compounds I. Foregoing compounds manifest inhibitory activity against production of interleukin IL-1β being well dissoluble in water and characterized by good oral absorption. Invention also relates to therapeutical agent inhibiting production of interleukin 1β, pharmaceutical composition, employment of above-defined compounds, a method for treating disease caused by interleukin 1β production stimulation as well as methods for treating immune system disturbances, inflammatory conditions, ischemia, osteoporosis, or septicemia using above compounds.
EFFECT: expanded therapeutical possibilities.
22 cl, 4 dwg, 2 tbl, 217 ex
| Title | Year | Author | Number |
|---|---|---|---|
| ACTIVATING AGENT FOR RECEPTOR ACTIVATED BY PEROXISOME GROWTH-STIMULATING AGENTS | 2009 |
|
RU2501794C2 |
| METHOD OF SYNTHESIS OF N-ACRYLOYLPIPERAZINE DERIVATIVES | 1990 |
|
RU2024513C1 |
| HERBICIDES FOR WEEDS RESISTANT TO SULFONYLUREA-BASE HERBICIDE, METHOD FOR CONTROL OF WEEDS RESISTANT TO SULFONYLUREA-BASE HERBICIDE, COMPOUNDS | 2003 |
|
RU2292139C2 |
| PIPERIDINE COMPOUND, METHOD FOR ITS PREPARING, PHARMACEUTICAL COMPOSITION AND METHOD FOR INHIBITION OF SODIUM CHANNELS AND POTASSIUM CHANNELS | 2001 |
|
RU2259365C2 |
| DERIVATIVES OF PYRIDAZINE-3-ONE AND MEDICINAL AGENTS COMPRISING THEREOF | 2000 |
|
RU2232755C2 |
| QUINOLINE AND QUINAZOLINE DERIVATIVES | 2000 |
|
RU2256654C2 |
| ANTAGONIST NPY Y5 | 2000 |
|
RU2264810C2 |
| CASR ANTAGONIST | 2004 |
|
RU2315036C2 |
| GLUCOPYRANOSYLOXYPYRAZOLE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THESE DERIVATIVES AND INTERMEDIATE COMPOUNDS FOR THEIR PREPARING | 2000 |
|
RU2232767C2 |
| PHENYLPYRIDAZINE COMPOUNDS AND MEDICINAL AGENTS COMPRISING THEREOF | 2001 |
|
RU2269519C2 |
