申请人:JANSSEN PHARMACEUTICA N.V.
公开号:EP0727421A1
公开(公告)日:1996-08-21
A chemical compound having the formula
the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof,
R1 and R2each independently are hydrogen or C1-6alkyl;
Xis C1-6alkyl, hydroxyC1-6alkyl, C1-6alkyloxyC1-6alkyl, aminocarbonyl, mono- and di(C1-6alkyl)aminocarbonyl, carboxyl, C1-6alkyloxycarbonyl, (aminocarbonyl)C1-6alkyl, [mono- and di(C1-6alkyl)aminocarbonyl]C1-6alkyl, carboxylC1-6alkyl, (C1-6alkyloxycarbonyl)C1-6alkyl or (hydroxyC1-6alkyl)aminocarboxyl;
mis 1 or 2; n is 1 to 4;
Aris optionally substituted phenyl; optionally substituted pyridinyl; optionally substituted pyrazolyl; or a radical of formula
Q' is arylethyl, arylethenyl, aryloxymethyl, diarylmethoxy, 2,2-diarylethenyl, diarylmethylcarbonyl, arylcarbonylmethyl, mono- and diarylaminocarbonyl, diarylethyl or arylaminomethyl.
Process for preparing said compounds and pharmaceutical compositions comprising them are also disclosed.
一种化合物,其化学式为
药学上可接受的酸加成盐及其立体异构体、
R1和R2各自独立地为氢或C1-6烷基;
X是C1-6烷基、羟基C1-6烷基、C1-6烷氧基C1-6烷基、氨基羰基、单-和二(C1-6烷基)氨基羰基、羧基、C1-6烷氧基羰基、(氨基羰基)C1-6烷基、[单-和二(C1-6烷基)氨基羰基]C1-6烷基、羧基C1-6烷基、(C1-6烷氧基羰基)C1-6烷基或(羟基C1-6烷基)氨基羰基;
mis为1或2;n为1至4;
Aris 任选取代的苯基;任选取代的吡啶基;任选取代的吡唑基;或式中的一个基团
Q'是芳基乙烷基、芳基乙烯基、芳基氧甲基、二芳基甲氧基、2,2-二芳基乙烯基、二芳基甲基羰基、芳基羰基甲基、单芳基和二芳基氨基羰基、二芳基乙烷基或芳基氨基甲基。
此外,还公开了制备上述化合物的工艺和包含这些化合物的药物组合物。