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    NOVEL HYDROXIMIC ACID DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESS FOR PREPARING SAME
    1.
    发明申请
    NOVEL HYDROXIMIC ACID DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESS FOR PREPARING SAME 审中-公开
    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）。

    ORAL PHARMACEUTICAL COMPOSITION CONTAINING CYCLOSPORIN AND PROCESS FOR PREPARING SAME
    2.
    发明申请
    ORAL PHARMACEUTICAL COMPOSITION CONTAINING CYCLOSPORIN AND PROCESS FOR PREPARING SAME 审中-公开
    含有CYPOSPORIN的口服药物组合物及其制备方法

    公开(公告)号：WO1992009299A1

    公开(公告)日：1992-06-11

    申请号：PCT/HU1991000050

    申请日：1991-11-27

    申请人： BIOGAL GYOGYSZERGYAR RT. ,  ORBAN, Erno ,  TOMORI, Lászlóné ,  KÜRTHY, Mária ,  BALOGH, Tibor ,  JASZLITS, László ,  MORAVCSIK, Imre ,  KOVACS, István ,  JUSZTIN, Istvánné ,  JANCSO, Sándor ,  TAKACS, Erzsébet ,  KISS, Tamásné ,  KOVACS, Antalné

    发明人： BIOGAL GYOGYSZERGYAR RT.

    IPC分类号： A61K37/02

    CPC分类号： A61K47/10 ,  A61K38/13

    摘要： The invention relates to therapeutically usable novel oral solutions, containing cyclosporin as active ingredient, which possess advantageous absorption characteristics. The invention also relates to a process for preparing these solutions. The solutions according to the invention comprise 1 part by mass of one or more cyclosporin(s) dissolved in a mixture containing 4 to 50 parts by volume of propylene glycol, 0 to 25 parts by volume of ethanol and 0.01 to 5 parts by mass of a polyoxyethylene/polyoxypropylene block polymer in homogenized state. Based on examinations carried out at 100 DEG C, the stability of solutions prepared according to the invention does not differ from that of the commercially available Sandimmun oral solution.

    摘要翻译： 本发明涉及具有有利吸收特征的含有环孢菌素作为活性成分的治疗上可用的新型口服溶液。 本发明还涉及一种制备这些溶液的方法。 根据本发明的溶液包含1质量份溶解在含有4至50体积份丙二醇，0至25体积份乙醇和0.01至5质量份的乙醇的混合物中的一种或多种环孢菌素 均聚状态的聚氧乙烯/聚氧丙烯嵌段聚合物。 基于在100℃下进行的检查，根据本发明制备的溶液的稳定性与市售的Sandimmun口服溶液的稳定性没有不同。

    ANTI-ISCHAEMIC HYDROXYLAMINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS
    3.
    发明申请
    ANTI-ISCHAEMIC HYDROXYLAMINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS 审中-公开
    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。

    NOVEL 3(2H)-PYRIDAZINONES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESS FOR PREPARING SAME
    4.
    发明申请
    NOVEL 3(2H)-PYRIDAZINONES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESS FOR PREPARING SAME 审中-公开
    新的3（2H） - 吡啶酮，含有它们的药物组合物及其制备方法

    公开(公告)号：WO1992012137A1

    公开(公告)日：1992-07-23

    申请号：PCT/HU1991000054

    申请日：1991-12-20

    申请人： RICHTER GEDEON VEGYÉSZETI GYAR RT. ,  MATYUS, Péter ,  RABLOCZKY, György ,  JASZLITS, László ,  KOSARY, Judit ,  KÜRTHY, Mária ,  PAPPNÉ BEHR, Agnes ,  ZARA, Dénesné ,  KARPATI, Egon ,  KOVACS, Anikó ,  SEBESTYÉN, László ,  FARKAS, Lajos ,  CZAKO, Klára ,  VARGA, Ildikó ,  ELEK, Sándor ,  MAGO, Istvánné ,  MATHÉ, György ,  SZEDERKÉNYI, Ferenc ,  JEDNAKOVITS, Andrea ,  BODI, Ilona ,  PODANYI, Benjamin

    发明人： RICHTER GEDEON VEGYÉSZETI GYAR RT.

    IPC分类号： C07D237/22

    CPC分类号： C07D401/06 ,  C07D237/22 ,  C07D401/12 ,  C07D405/06

    摘要： The invention relates to novel, racemic and optically active 3(2H)-pyridazinone derivatives of general formula (I), wherein R means hydrogen; a C1-4alkyl group optionally substituted by an R R N- group where R and R , being the same or different, stand for a C1-4alkyl group or R R N- together represents a 6-membered heterocyclic group optionally containing an oxygen or an R N- moiety where R is a C1-4alkyl optionally substituted by a phenyoxy group or a C3-5alkenyl optionally substituted by a phenyl group; or a C1-4alkyl group substituted by a mono- or polysubstituted phenyl, phenoxy or benzyloxy group; or a C3-5alkenyl or C3-5alkynyl optionally substituted by an unsubstituted or optionally substituted phenyl group; or a phenyl group; R means hydrogen; or a C1-4alkyl optionally substituted by a morpholino, pyridyl, 1,4-benzodioxanyl or an optionally substituted phenyl group; R means hydrogen or an optionally substituted phenyl group; R means hydrogen; or R CO- group where R is a C1-4alkyl, phenyl or pyridyl group or an amino group substituted by a C1-4alkyl group; or an -SO3M moiety where M is hydrogen or an organic or inorganic cation; X means halogen; and n is 1, 2 or 3, with the proviso that R is different from a C1-4alkyl, alkenyl, aralkyl and phenyl group when n is 1, as well as their tautomers and the acid addition salts of these compounds. The invention further relates to pharmaceutical compositions containing as active ingredient a compound of general formula (I) as well as to a process for the preparation of compounds of general formula (I). The compounds of the invention possess a significant calmodulin-antagonizing effect, decrease the coronary resistance and are less toxic. Thus, these compounds are useful for treating cardiovascular diseases, particularly angina pectoris.

    摘要翻译： 本发明涉及通式（I）的新型外消旋和光学活性的3（2H） - 哒嗪酮衍生物，其中R 1表示氢; 任选被R 5 R 6 N-基团取代的C 1-4烷基，其中R 5和R 6相同或不同，代表C 1-4烷基或R 5 R N-一起表示任选含有氧或R 7 N-部分的6元杂环基，其中R 7是任选被苯氧基取代的C 1-4烷基或任选被 苯基; 或被一或多取代的苯基，苯氧基或苄氧基取代的C 1-4烷基; 或任选被未取代或任选取代的苯基取代的C3-5烯基或C3-5炔基; 或苯基; R 2表示氢; 或任选被吗啉代，吡啶基，1,4-苯并二恶烷基或任意取代的苯基取代的C 1-4烷基; R 3表示氢或任选取代的苯基; R 4表示氢; 或R 8 CO-基团，其中R 8是C 1-4烷基，苯基或吡啶基或​​被C 1-4烷基取代的氨基; 或其中M为氢或有机或无机阳离子的-SO 3 M部分; X表示卤素; n为1,2或3，条件是当n为1时，R 1不同于C 1-4烷基，烯基，芳烷基和苯基，以及它们互变异构体和这些化合物的酸加成盐。 本发明还涉及含有通式（I）化合物作为活性成分的药物组合物以及制备通式（I）化合物的方法。 本发明化合物具有显着的钙调素拮抗作用，降低冠状动脉阻力并且毒性较小。 因此，这些化合物可用于治疗心血管疾病，特别是心绞痛。