Hydroximic acid derivatives, pharmaceutical compositions containing
them, and processes for preparing the same
    7.
    发明授权
    Hydroximic acid derivatives, pharmaceutical compositions containing them, and processes for preparing the same 失效
    含羟基酸衍生物,含有它们的药物组合物及其制备方法

    公开(公告)号:US5919796A

    公开(公告)日:1999-07-06

    申请号:US737168

    申请日:1996-11-05

    摘要: Hydroximic acid derivatives possess anti-ischemic effects, and therefore, they are useful for treating ischemic states and diseases, such as myocardial ischemia (which may be induced by occlusion of coronary arteries). These derivatives include compounds of formula (I): ##STR1## wherein: X represents a halogen; Z represents an aromatic group, a pyridinyl group, a picolyl group, or a lutidyl group; and R represents an --A--N(R.sub.1)R.sub.2 group, wherein:R.sub.1 and R.sub.2 represent, independently from each other, hydrogen or an alkyl group;or R.sub.1 and R.sub.2, together with the adjacent nitrogen atom, form a 5- to 7-membered,saturated heterocyclic group optionally containing an additional nitrogen, oxygen,or sulfur atom, the heterocyclic group optionally being substituted by at least one alkyl group; andA represents a straight or branched chain alkylene group, as well as pharmaceutically acceptable acid addition salts thereof. The invention further relates to processes for preparing the above noted compounds, and pharmaceutical compositions containing these compounds or their pharmaceutically acceptable acid addition salts as an active ingredient. Additionally, the invention relates to intermediate compounds of formula II used in preparing the compounds of formula I. Formula II is as follows: ##STR2## In formula II, the variables Z and R have the same definitions provided above.

    摘要翻译: PCT No.PCT / HU95 / 00014 Sec。 371日期:1996年11月5日 102(e)日期1996年11月5日PCT提交1995年5月4日PCT公布。 公开号WO95 / 30649 日期1995年11月16日海洛因衍生物具有抗缺血作用,因此它们可用于治疗缺血状态和疾病,例如心肌缺血(其可能由冠状动脉闭塞引起)。 这些衍生物包括式(I)的化合物:其中:X表示卤素; Z表示芳基,吡啶基,吡啶甲基或联脂基; 并且R表示-A-N(R1)R2基团,其中:R1和R2彼此独立地表示氢或烷基; 或R 1和R 2与相邻的氮原子一起形成任选地含有另外的氮,氧或硫原子的5至7元饱和杂环基,所述杂环基任选被至少一个烷基取代; A表示直链或支链亚烷基,以及其药学上可接受的酸加成盐。 本发明还涉及制备上述化合物的方法和含有这些化合物或其药学上可接受的酸加成盐作为活性成分的药物组合物。 此外,本发明涉及用于制备式I化合物的式II的中间体化合物。式II如下:在式II中,变量Z和R具有与上述相同的定义。