| 摘要 |
The present invention concerns compounds of general formula (I):in which:Rrepresents hydrogen, R, -C(=Y)-NHR, -SONHR, -C(=Z1)-R, -SO-Ror -C(=Z1)-OR;Rrepresents hydrogen, cyano, halogen or -C≡C-R;Rrepresents hydrogen, acyl, alkoxycarbonyl, alkyl, aroyl, aryl, aryloxycarbonyl, carboxy, cycloalkenyl, cycloalkyl, heteroaroyl, heteroaryl, heterocycloalkyl or -C(=O)-NYY;Rrepresents optionally substituted alkyl, cycloalkyl, cycloalkenyl ,heterocycloalkyl, aryl or heteroaryl;Rrepresents hydrogen or alkyl;Rrepresents alkyl, acyl, alkoxycarbonyl, alkylsulfonyl, aryl, arylsulfonyl, aroyl, cycloalkyl, cycloalkenyl, heteroaryl, heteroarylsulfonyl, heteroaroyl and heterocycloalkyl;Rrepresents optionally substituted alkyl, cycloalkyl or cycloalkylalkyl;Rrepresents hydrogen, alkyl, alkenyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl;Rrepresents alkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkylalkyl;Rrepresents hydrogen or lower alkyl;Rrepresents alkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkylalkyl; or alkyl optionally substituted by –NYY;Rrepresents aryl or heteroaryl; or alkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl or heterocycloalkylalkyl each optionally substituted;Y represents O, S or NCN;Yand Y(Yand Y) are independently in particular hydrogen, alkyl, aryl, cycloalkyl, cycloalkenyl, heteroaryl or heterocycloalkyl; or the group –NYYmay form 5-7 membered ring or the group –NYY(-NYY) may form a cyclic amine;Z (Z)represents O or S;Zrepresents O or S(O);n is zero or an integer 1 or 2;m is 1 or 2;p is 1 or 2;and their corresponding N-oxides, their prodrugs; their pharmaceutically acceptable salts and solvates (e.g. hydrates), also together with one or more pharmaceutically acceptable carriers or excipients, such novel indolizines derivatives with inhibitory effects towards kinase proteins and especially for use for preventing or treating diseases that may be modulated by the inhibition of such kinase proteins and particularly solid tumours. |
