FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention describes derivatives of piperazine of the general formula: 
or their pharmaceutically acceptable salts wherein Ra - R8a mean phenyl; R8b means pyridyl, or R8 means naphthyl; R1 means hydrogen atom; R2 - R9, R10, R11 mean substituted phenyl; R9, R10, R11 mean substituted pyridyl or pyrimidyl; R9, R10, R11 mean substituted pyridyl-N-oxide or pyrimidyl-N-oxide; R12, R13 mean substituted oxazolyl, naphthyl, fluorenyl, compounds of formulae 
, 
or 
; R3 means hydrogen atom, (C1-C6)-alkyl, (C1-C6)-alkoxy-(C1-C6)-alkyl, (C3-C10)-cycloalkyl, (C3-C10)-cycloalkyl-(C1-C6)-alkyl; R8 means phenyl; R8 means phenyl-(C1-C6)-alkyl, or R8 means thienyl-(C1-C6)-alkyl; R4, R5, R7 and R13 mean independently hydrogen atom or (C1-C6)-alkyl; R6 means hydrogen atom or (C1-C6)-alkyl; R8 means 1-3 substitutes that mean independently hydrogen atom, halogen atom, (C1-C6)-alkoxyl or -CF3; R8a means 1-3 substitutes that mean independently hydrogen atom, halogen atom, -CF3, -CF3O, -CN; R14 means phenyl, -NHCOCF3 and imidazolyl; R8b means 1-3 substitutes that mean independently hydrogen atom or halogen atom; R9 and R10 mean independently (C1-C6)-alkyl, halogen atom, -NR17R18, -OH, -CF3 and -OCH3; R11 means R9, hydrogen atom, phenyl, -NO2, -CN, -CH2F, -CHF2, -CHO, -CN=NOR17, pyridyl, pyridyl-N-oxide, pyrimidinyl, pyrazinyl, -N(R17)CONR18R19, -NHCONH-(chloro-(C1-C6)-alkyl), -NHCONH-((C3-C10)-cycloalkyl-(C1-C6)-alkyl), -NHCO-(C1-C6)-alkyl, -NHCOCF3, -NHSO2N-((C1-C6)-alkyl)2, -NHSO2-(C1-C6)-alkyl, -N(SO2CF3)2, -NHCO2-(C1-C6)-alkyl, (C3-C10)-cycloalkyl, -SR20, -OSO2-(C1-C6)-alkyl, -SO2CF3, hydroxy-(C1-C6)-alkyl, -CONR17R18, -CON(CH2CH2-O-CH3)2, -OCONH-(C1-C6)-alkyl, -Si(CH3)3 or -B(OC(CH3)2)2; R12 means (C1-C)-alkyl or R14-phenyl; R14 means 1-3 substitutes that mean independently hydrogen, (C1-C6)-alkyl, -CF3, -CO2R17, -CN, (C1-C6)-alkoxyl and halogen atom; R15 and R16 mean independently hydrogen atom and (C1-C6)-alkyl, or R15 and R16 mean in common (C2-C5)-alkylene group and in common with carbon atom to which they are bound form (C3-C6)-spiran ring; R17, R18 and R19 mean independently hydrogen atom or (C1-C6)-alkyl; R20 means (C1-C6)-alkyl. Also, invention describes pharmaceutical compositions containing these compounds and using novel compounds as CCR5 antagonists in treatment of HIV infection, arthritis, asthma, cerebrospinal sclerosis and other diseases.
EFFECT: valuable medicinal properties of compounds and pharmaceutical compositions.
29 cl, 30 tbl, 31 ex
| Title | Year | Author | Number |
|---|---|---|---|
| PYRROLIDINE AND PIPERIDINE DERIVATIVES | 2002 |
|
RU2326120C9 |
| COMPOUND, PHARMACEUTICAL COMPOSITION | 1999 |
|
RU2237060C2 |
| PIPERIDINYLPIPERAZINE DERIVATIVES APPLICABLE AS CHEMOKINE RECEPTOR INHIBITORS | 2006 |
|
RU2411241C2 |
| TRICYCLIC ANTITUMOR COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHOD FOR TREATMENT BASED ON THEREOF | 2001 |
|
RU2293734C9 |
| POLYCYCLIC COMPOUND, PHARMACEUTICAL COMPOSITION POSSESSING PROPERTY OF H RECEPTOR ANTAGONIST AND METHOD FOR TREATMENT BY ITS USING | 2001 |
|
RU2301231C2 |
| MACROCYCLIC COMPOUND AND METHOD FOR IDENTIFYING AGENT BASED ON THEREOF | 1999 |
|
RU2245335C2 |
| METHOD FOR TREATMENT OF ALLERGY BY USING SUBSTITUTED PYRAZOLES | 2001 |
|
RU2290179C2 |
| DERIVATIVES OF TETRAHYDROISOQUINOLINE, PHARMACEUTICAL COMPOSITION CONTAINING THEREOF, METHOD FOR INHIBITION OF SYNAPTIC UPTAKE OF DOPAMINE AND TREATMENT METHOD | 2000 |
|
RU2293728C2 |
| MACROCYCLIC ANALOGUES AND METHODS OF THEIR APPLICATION AND PREPARATION | 1999 |
|
RU2822750C2 |
| PYRAZOLE DERIVATIVES AND THEIR PHARMACEUTICALLY ACCEPTABLE SALTS | 1991 |
|
RU2076100C1 |
