发明名称 N-SUBSTITUTED BENZAMIDES
摘要 Compounds of the general formula: <CHEM> wherein R<1> represents hydrogen, a C1-6 alkyl group or an acetyl group; R<2> represents halogen; R<3> represents a group of the formula: <CHEM> wherein R<5> represents hydrogen or a phenyl or non-aromatic cyclic ether group and n is 2 or 3; R<4> represents a C3-6 cycloalkyl, cyclohexenyl, C1-6 alkoxy, trifluoromethyl, tetrahydrofuryl, 1,3-dioxolanyl or phenoxy group; m is 0, 1, 2, 3 or 4 with the proviso that when m is 0, R<4> is only a C3-6 cycloalkyl or tetrahydrofuryl group; and pharmacologically acceptable acid addition salts, quaternary ammonium salts and N-oxides thereof have pharmacological properties rendering them useful as antiematic agents with reduced undesirable side-effects. Various methods are described for their preparation involving formation of the amide link, etherification of the 2-hydroxy derivative, introducing the R<5>CH2 group on the N-unsubstituted azabicyclooctane or nonane or, for 4-amino compounds, by hydrolysing a 4-acylamino derivative.
申请公布号 PH25048(A) 申请公布日期 1991.01.28
申请号 PH19290000373 申请日期 1988.08.02
申请人 FORDONAL S.A. 发明人 ARMANDO VEGA NOVEROLA;JOSE MANUEL PRIETO SOTO;FERNANDO PUJOL NOGUERA;JACINTO MORAGUES MAURI;ROBERT GEOFFREY WILLIAM SPICKETT
分类号 C07C1/00;A61K31/435;A61K31/46;A61P1/00;A61P1/08;A61P25/04;A61P25/20;C07D451/04;C07D451/14;C07D453/02;C07D487/08 主分类号 C07C1/00
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