| 摘要 |
FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to new bicyclic derivatives. Invention describes bicyclic derivatives of the general formula (I): wherein R1 means pyrimidinyl or pyridyl and each is substituted optionally independently with one, two or three substituents taken among alkyl, alkoxy, alkylthio, halogen atom, nitro-group, hydroxyamino-group, -NRR' (wherein R and R' mean independently each of other hydrogen atom, alkyl, carboxyalkyl or heteroalkyl) or -NHC(O)Rb [wherein Rb means alkyl, -(alkylene)-X wherein X means alkoxy, alkylamino, dialkylamino, heterocyclyl or heteroaryl]; --- means a bond between or B either CR1, or Q and CR1 therefore (I) when --- means a bond between Q and CR1 then: B means nitrogen atom; R2 means halogenphenyl or pyridyl and Q means CH-, and (II) when --- means a bond between b and CR1 then B means carbon atom; R2 phenyl optionally substituted with halogen atom, alkyl, alkoxy or halogenalkyl and Q means -NR4- or O- wherein R4 means hydrogen atom, alkyl, halogenalkyl, heteroalkyl, heteroaralkyl, heterocyclylalkyl, OR5 (wherein R5 means hydrogen atom, alkyl, heteroalkyl or heterocyclylalkyl), -SO2R'' (wherein R'' means alkyl), -(alkylene)-Z or -(alkylene)-CO-Z wherein Z means cyano-group; -COOR7 wherein R7 means hydrogen atom or alkyl, -CONR8R9 wherein R8 means hydrogen atom or alkyl; R9 means hydrogen atom, alkyl, alkoxy or (alkylene)--COOR7, -C(=NH)NH2; or -COR13 wherein R13 means alkyl, group of formulas: (S) , (T) , (U) , (V) or (W) wherein R6 means hydrogen atom, alkyl, heteroalkyl, halogen atom, alkoxy, monoalkylamino-group (optionally substituted with hydroxy, alkoxy or amino), dialkylamino, alkylthio, -NHC(O)R'' [wherein R'' means alkyl]; R3 means hydrogen atom, alkyl, halogenalkyl being "alkyl" and "alkylene" in all cases and each "alkoxy" comprise six carbon atoms, not above; "heteroalkyl" means alkyl group comprising six carbon atoms, not above and having one or two substituents taken among hydroxy, hydroxyalkyl, alkoxy, alkylthio, -NRfRb and -SO3X+ wherein Ra means hydrogen atom, alkyl, cyanoalkyl, hydroxyalkyl, aminoalkyl or dialkylaminoalkyl; X+ means alkali metal ion; "heteroaryl" means imidazolyl group that can be substituted with alkyl or nitro; "heterocyclyl" means cyclic saturated radical comprising from 3 to 8 ring atoms wherein 1 or 2 ring atoms represent heteroatoms taken among nitrogen and oxygen atoms and that can be substituted with one or two substituents taken independently among alkyl, hydroxyalkyl, hydroxy, amino and carbamoyl; and their pharmaceutically acceptable salts, individual isomers and mixtures of isomers also. Invention describes also pharmaceutical composition based on compounds of the formula (I) designated for treatment and prophylaxis of inflammatory diseases and intermediate compounds. Invention provides preparing new compounds eliciting useful biological properties. EFFECT: valuable medicinal properties of compounds. 15 cl, 8 tbl - |
