Chloro- and alkoxy-substituted-2,4-diaminoquinazolines and pharmaceutical compositions containing them
申请人:PFIZER INC.
公开号:EP0028473A1
公开(公告)日:1981-05-13
2,4-Diaminoquinazolinesoftheformula:
and the pharmaceutically acceptable salts thereof are disclosed and claimed as novel compounds having useful antihypertensive activity wherein: Y' is hydrogen or chloro, Y2 is OR and Y' is hydrogen or OR, such that when Y' is hydrogen, Y3 is OR and when Y' is chloro, Y3 is hydrogen or OR; R represents an alkyl group having from one to three carbon atoms; when taken separately, R1 and R2 are each hydrogen, alkyl having from one to five carbon atoms, cycloalkyl having from three to eight carbon atoms, alkenyl or alkynyl each having from three to five carbon atoms or hydroxy substituted alkyl having from two to five carbon atoms; when taken together with the nitrogen atom to which they are attached, R and R2 form any one of a number of specified substituted or unsubstituted heterocyclic groups optionally containing also an atom of oxygen, sulfur or a second atom of nitrogen as a ring member. Also disclosed and claimed are pharmaceutical compositions containing such compounds, and novel intermediates for their production, having the formulae:
and
2,4-Diaminoquinazolinesoftheformula:
及其药学上可接受的盐类公开并声称是具有有用的抗高血压活性的新型化合物,其中:Y'是氢或氯,Y2是OR,Y'是氢或OR,这样,当Y'是氢时,Y3是OR,当Y'是氯时,Y3是氢或OR;R代表具有1至3个碳原子的烷基;当单独使用时,R1和R2各自是氢、具有1至5个碳原子的烷基、具有3至8个碳原子的环烷基、各自具有3至5个碳原子的烯基或炔基或具有2至5个碳原子的羟基取代的烷基;当 R 和 R2 与它们所连接的氮原子结合在一起时,R 和 R2 形成若干指定的取代或未取代的杂环基团中的任一个,这些杂环基团还可选择含有一个氧原子、硫原子或第二个氮原子作为环成员。本发明还公开了含有此类化合物的药物组合物,以及用于生产此类化合物的新型中间体,其结构式为
和