| 摘要 |
FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to new derivatives of then[2,3-d]- pyrimidine-2,4-(1H,3H)-done of the general formula (I) or their pharmaceutically acceptable salts eliciting immunosuppressive activity. Invention relates also to pharmaceutical composition, method for its preparing, method for immunosuppression and method for treatment or reducing risk of obstruction of respiratory ways. In compounds of the general formula (I) R represents -C(O)-Ar1, -C(R4)(R5)Ar1 or Ar2 wherein Ar1 represents naphthyl, quaintly, isoquinolyl or benzofuranyl; or Ar1 represents phenyl optionally substituted with one or some substituents taken among: C1-4-alkyl, C1-4-alkoxy-group, halogen atom, trifluoromethyl, amino-, nitro-, cyano-, trifluoromethoxy-, phenoxy-group, -CH2N(R6)2, -NHSO2CF3, C1-4-alkylsulfonylamino-group, -NHC(O)R6a, CO2R7 or -C(O)NR8R8a; R4 represents hydrogen atom; R5 represents hydrogen atom or OH; each R6 and R7 represents hydrogen atom or C1-4- alkyl; R6a represents hydrogen atom, C1-6-alkyl, aryl or aryl-C1-4-alkyl wherein alkyl group or aryl moiety in arylalkyl group represents phenyl or pyridyl being each of them can be substituted optionally with one or some substituents; R8 and R8a each represents independently hydrogen atom, C1-4-alkyl, phenyl or pyridyl; Ar2 represents acenaphthenyl, indanyl, iminodihydrobenzofuranyl or fluorenyl and each of them can be substituted optionally with one or some substituents; R1 and R2 represent independently C1-6-alkyl, C3-6-alkenyl, CH2C3-5-cycloalkyl or C3-6-cycloalkyl; R3 represents hydrogen atom, X-R9 or X-Ar3 wherein X represents S(O)n, C(O)NR10, C(O)O, NH(CO)NR10, NH(CO)O or SO2NR10; n = 0, 1 or 2; X, R9 and R10 are given in the invention claim; Ar3 represents phenyl, pyridyl or pyridine N-oxide and each of them can be substituted optionally with one or some substituents taken among: OH, NO2, NH2, NHSO2CF3, C1-4-alkoxy-group, bis-C1-4-alkanesulfonylamino-group, C1-4- alkylcarbonylamino-group or C1-4-alkoxycarbonylamino-group. EFFECT: improved preparing and treatment methods, valuable medicinal properties of compounds. 17 cl, 95 ex _ |
