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1. 发明申请

WO1995030649A1 NOVEL HYDROXIMIC ACID DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESS FOR PREPARING SAME 审中-公开
标题翻译：新型羟基酸衍生物，含有它们的药物组合物及其制备方法
公开(公告)号：WO1995030649A1
公开(公告)日：1995-11-16
申请号：PCT/HU1995000014
申请日：1995-05-04
申请人： BIOREX KUTATO ÉS FEJLESZTO"e; RT. , BARABAS, Mihály , MARVANYOS, Ede , ÜRÖGDI, László , VERECZKEY, László , JASZLITS, László , BIRO, Katalin , JEDNAKOVITS, Andrea , RADVANYI, Erzsébet , UDVARDY-NAGY, Istvánné
发明人： BIOREX KUTATO ÉS FEJLESZTO"e; RT.
IPC分类号： C07C259/02
CPC分类号： C07D295/088 , C07C259/02 , C07C259/18 , C07D213/78
摘要： The invention relates to novel compounds of formula (I), wherein X means halogen; Z stands for an aromatic group, pyridinyl group or the like; and R represents an alkyl or phenylalkyl group or an -A-N(R1)R2 group, and in the latter R1 and R2 stand, independently from each other, for hydrogen or 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, said heterocyclic group optionally being substituted by at least one alkyl group; and A stands for a straight or branched chain alkylene group, as well as the pharmaceutically acceptable acid addition salts thereof; furthermore, to processes for the preparation of the above novel compounds, and pharmaceutical compositions containing these compounds or their pharmaceutically acceptable acid addition salts as active ingredients. Further, the invention relates to certain novel intermediates of formula (II). The compounds of formula (I) possess anti-ischaemic effect and therefore, they are useful for treating ischaemic states and diseases, e.g. myocardial ischaemia (induced e.g. by occlusion of the coronary arteries).
摘要翻译：本发明涉及新的式（I）化合物，其中X表示卤素; Z表示芳基，吡啶基等; 并且R表示烷基或苯基烷基或-A-N（R 1）R 2基团，并且在后面的R 1和R 2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; 此外，涉及制备上述新化合物的方法，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，本发明涉及式（II）的某些新型中间体。式（I）化合物具有抗缺血作用，因此它们可用于治疗缺血状态和疾病，例如，心肌缺血（例如通过冠状动脉闭塞诱发）。

2. 发明申请

WO1997000251A1 ANTI-ISCHAEMIC HYDROXYLAMINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS 审中-公开
标题翻译：抗间歇羟基胺衍生物和药物组合物
公开(公告)号：WO1997000251A1
公开(公告)日：1997-01-03
申请号：PCT/HU1996000033
申请日：1996-06-14
申请人： BIOREX KUTATO ES FEJLESZTO RT. , ÜROGDI, László , MARVANYOS, Ede , BARABAS, Mihály , JASZLITS, László , BIRO, Katalin , JEDNAKOVITS, Andrea , RADVANYNÉ HEGEDÜS, Erzsébet , KÜRTHY, Mária , UDVARDY NAGY, Istvánné
发明人： BIOREX KUTATO ES FEJLESZTO RT.
IPC分类号： C07D295/092
CPC分类号： C07D213/75 , C07C275/64 , C07D295/088
摘要： The invention relates to novel hydroxylamine derivatives represented by general formula (I), the pharmaceutically acceptable acid addition salts thereof as well as the pharmaceutical compositions containing the same as active ingredient. Another object of the invention is the preparation of the hydroxylamine derivatives and salts thereof. The compounds according to the invention possess anti-ischaemic effect. In the above formula (I) X is O, -NH or a group of the formula -NR'-, wherein R and R', independently from each other, are alkyl, cycloalkyl, phenylalkyl; a phenyl group optionally substituted with halo, haloalkyl, alkyl, alkoxy or nitro; or an N-containing hetero ring; R is H or alkanoyl; R is H or hydroxy optionally acylated with alkanoyl; and R is a group of the formula -N(R )R wherein R and R , independently from each other, may be H, alkyl or a group of the formula -C(O)-NH-R wherein R is as defined above, or R and R , when taken together with the adjacent nitrogen attached thereto, form a 5 to 7-membered hetero ring which may contain one additional hetero atom selected from nitrogen, oxygen and sulfur and which is optionally substituted with alkyl of phenylalkyl.
摘要翻译：本发明涉及由通式（I）表示的新型羟胺衍生物，其药学上可接受的酸加成盐以及含有与活性成分相同的药物组合物。本发明的另一个目的是制备羟胺衍生物及其盐。根据本发明的化合物具有抗缺血作用。在上式（I）中，X是O，-NH或式-NR'-的基团，其中R和R'彼此独立地是烷基，环烷基，苯基烷基; 任选被卤素，卤代烷基，烷基，烷氧基或硝基取代的苯基; 或含N的杂环; R 1是H或烷酰基; R 2是任选用烷酰基进行酰化的H或羟基; 并且R 3是式-N（R 4）R 5的基团，其中R 4和R 5彼此独立地可以是H，烷基或式 -C（O）-NH-R，其中R如上定义，或R 4和R 5与连接在其上的相邻氮原子一起形成5至7元杂环，其可以含有一个选自氮，氧和硫的另外的杂原子，其任选被苯基烷基的烷基取代。

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