发明名称 Novel phenethanolamines
摘要 The tertiary amines of the formula <IMAGE> I wherein n represents a whole number of 1 to 5; X1 represents phenyl or phenyl mono-, di- or tri-substituted by R1, R2 and R3; X2 represents hydrogen, lower-alkyl, phenyl or phenyl mono-, di- or tri-substituted by R1, R2 and R3; Y represents hydrogen, lower-alkyl, hydroxymethyl, carboxy or lower-alkoxycarbonyl; Z represents a group of the formula <IMAGE> (Z) R1, R2 and R3 represent hydrogen, halogen, hydroxy, benzyloxy, lower-alkyl, lower-alkoxy, hydroxymethyl, amino, acylamino, lower-alkoxybenzylamino, nitro, carbamoyl, trifluoromethyl or lower-alkylsulphonylmethyl; R4, R5 and R51 represent hydrogen, lower-alkyl, lower-alkoxy, lower alkanoyl, carboxy, cyano, hydroxy, hydroxy-lower-alkyl, acyloxy or a group -C(R6)=C(R7)COOR8, -SO2R9, -C(O)R9 or -CH2R10, with the proviso that R4 does not represent hydrogen when R5 represents hydroxy, lower-alkyl or lower-alkoxy; R6, R7 and R8 represent hydrogen or lower-alkyl; R9 represents amino, mono-lower-alkylamino or a group R; R represents di-lower-alkylamino, piperidino, morpholino, thiamorpholino, piperazino or the ether group of a lower aliphatic, cycloaliphatic or araliphatic alcohol or of a phenol; and R10 represents a group R and, where R1, R2 and R3 represent hydrogen, halogen, hydroxy, benzyloxy, lower-alkyl, lower-alkoxy, hydroxymethyl, amino, lower-alkoxybenzylamino or trifluoromethyl and simultaneously Y represents hydrogen, lower-alkyl or hydroxymethyl, R10 can also represent amino or mono-lower-alkylamino, have hypoglycaemic activity and reduce glycosuria. They are manufactured from corresponding primary or secondary amines.
申请公布号 US4585796(A) 申请公布日期 1986.04.29
申请号 US19830518990 申请日期 1983.08.01
申请人 HOFFMANN-LA ROCHE INC. 发明人 ALIG, LEO;MUELLER, MARCEL
分类号 A61K31/165;C07C13/18;C07C229/38;C07C233/00;C07C309/63;C07C311/15;C07C317/04;C07D333/20;C07D333/22;C07D333/24;C07D333/38;(IPC1-7):A61K31/165;A61K31/38;C07C103/28 主分类号 A61K31/165
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