| 摘要 |
FIELD: biotechnologies.SUBSTANCE: invention refers to a compound of formula (I):,where Rrepresents NRC(O)Ror NRR; Rrepresents hydrogen; Rrepresents halogen; Rrepresents hydrogen, halogen, cyano, hydroxy, Calkyl, Calkoxy, CF, OCF, Calkylthio, S(O)(Calkyl), S(O)(Calkyl), COH or CO(Calkyl); Rrepresents Calkyl (replaced with NRRor heterocyclyl that represents nonaromatic 5-7-membered ring containing 1 or 2 heteroatoms independently chosen from a group containing nitrogen, oxygen or sulphur); Rrepresents hydrogen, halogen, hydroxy, Calkoxy, COH or Calkyl (possibly replaced with NRRgroup, morpholinyl or thiomorpholinyl); Rrepresents hydrogen; Rrepresents Ccycloalkyl (possibly replaced with NRRgroup), phenyl or heteroaryl, which represents aromatic 5- or 6-membered ring containing 1 to 3 heteroatoms independently chosen from the group containing nitrogen, oxygen and sulphur, and which is probably condensed with one 6-membered aromatic or nonaromatic carbocyclic ring or with one 6-membered aromatic heterocyclic ring, where the above 6-membered aromatic heterocyclic ring includes 1 to 3 heteroatoms independently chosen from a group containing nitrogen, oxygen and sulphur; Rrepresents hydrogen or Calkyl (possibly replaced with pyrazolyl); Rrepresents Calkyl (possibly replaced with phenyl or heteroaryl group, which represents aromatic 5- or 6-membered ring containing 1 or 2 heteroatoms independently chosen from the group containing nitrogen, oxygen or sulphur, and which is possibly condensed with one 6-membered heterocyclic ring, where the above 6-membered aromatic heterocyclic ring contains 1 or 2 heteroatoms independently chosen from the group containing nitrogen, oxygen or sulphur; where the above phenyl and heteroaryl groups in R, Rand Rare possibly independently replaced with the following group: halogen, hydroxy, C(O)R, Calkyl, Chydroxyalkyl, Chalogenoalkyl, Calkoxy(C)alkyl or Ccycloalkyl; unless otherwise stated, heterocyclyl is possibly replaced with group of Calkyl, (Calkyl)OH, (Calkyl)C(O)NRRor pyrrolidinyl; Rrepresents Calkyl; R, Rand Rindependently represent Calkyl (possibly replaced with hydroxy or NRRgroup); R, R, R, R, R, Rand Rindependently represent hydrogen or Calkyl; or to its pharmaceutically acceptable salts.EFFECT: new compounds are obtained, which can be used in medicine for treatment of PDE4-mediated disease state.10 cl, 2 tbl, 202 ex |
