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    • 5. 发明授权
    • 신규의히드록시믹산유도체,그를포함한약제학적조성물및그의제조방법
    • 신규의히드록시믹산유도체,그를포함한약제학적조성물및그의제조방법
    • KR100372312B1
    • 2003-05-09
    • KR1019960706277
    • 1995-05-04
    • 바이오렉스 쿠타토 에스 페레즈토 알티
    • 바라바스미할리마바니오스이드우로그디라즐로베렉키라즐로자슬릿츠라즐로비로카탈린제드나코비츠안드레아라드바니에르제베우드바르디-나기이스트바네
    • C07C259/02C07D213/78C07D295/088
    • C07D295/088C07C259/02C07C259/18C07D213/78
    • PCT No. PCT/HU95/00014 Sec. 371 Date Nov. 5, 1996 Sec. 102(e) Date Nov. 5, 1996 PCT Filed May 4, 1995 PCT Pub. No. WO95/30649 PCT Pub. Date Nov. 16, 1995Hydroximic 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): 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(R1)R2 group, wherein: R1 and R2 represent, independently from each other, hydrogen or an alkyl group; or R1 and R2, 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; and A 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: In formula II, the variables Z and R have the same definitions provided above.
    • PCT No.PCT / HU95 / 00014 Sec。 371日期1996年11月5日Sec。 102(e)日期1996年11月5日PCT提交日期1995年5月4日PCT Pub。 WO95 / 30649 PCT Pub。 日期1995年11月16日氢氧化肟酸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,如心肌缺血(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代表卤素; Z表示芳族基团,吡啶基,吡啶甲基或卢迪基; 并且R表示-A-N(R 1)R 2基团,其中:R 1和R 2彼此独立地表示氢或烷基; 或R1和R2与相邻的氮原子一起形成任选含有另外的氮,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代表直链或支链亚烷基,以及其药学上可接受的酸加成盐。 本发明进一步涉及制备上述化合物的方法,以及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。