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    PHARMACEUTICAL COMPOSITIONS CONTAINING BISARAMIL INHIBITING RADICAL PRODUCTION AND PROCESS FOR PREPARING SAME
    2.
    发明申请
    PHARMACEUTICAL COMPOSITIONS CONTAINING BISARAMIL INHIBITING RADICAL PRODUCTION AND PROCESS FOR PREPARING SAME 审中-公开
    含有BISARAMIL抑制生产的药物组合物及其制备方法

    公开(公告)号：WO1996022096A1

    公开(公告)日：1996-07-25

    申请号：PCT/HU1996000003

    申请日：1996-01-18

    申请人： RICHTER GEDEON VEGYÉSZETI GYAR RT. ,  PELLIONISZ-PAROCZAI, Margit ,  KARPATI, Egon ,  REGO"e;S-SZABO, Katalin ,  RO"e;TH, Erzsébet

    发明人： RICHTER GEDEON VEGYÉSZETI GYAR RT.

    IPC分类号： A61K31/445

    CPC分类号： A61K31/451

    摘要： The invention relates to free radical production-inhibitory pharmaceutical compositions containing as active ingredient 3-methyl-7-ethyl-9 alpha -(4-chlorobenzoyloxy)-3,7-diazabicyclo[3,3,1]-nonane prepared in a known manner or a therapeutically acceptable salt thereof together with fillers, diluents and other formulation-promoting additives known in se and commonly used in the preparation of pharmaceutical compositions. Furthermore, the invention relates also to a process for the preparation of these compositions, to their use for the preparation of pharmaceutical compositions having free radical production inhibitory effect and for a method for treating clinical conditions in patients induced by oxidative stress or weakening or exhaustion of the endogenous antioxidant protection of the organism.

    摘要翻译： 本发明涉及含有作为活性成分的3-甲基-7-乙基-9α-（4-氯苯甲酰氧基）-3,7-二氮杂双环[3,3,1]壬烷的活性成分的自由基生成抑制药物组合物 方式或其治疗上可接受的盐以及已知的并且通常用于制备药物组合物的填充剂，稀释剂和其它制剂促进添加剂。 此外，本发明还涉及制备这些组合物的方法，其用于制备具有自由基产生抑制作用的药物组合物的用途，以及用于治疗由氧化应激诱导的患者的临床病症或弱化或消耗的方法 生物体内源性抗氧化保护。

    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。

    NOVEL N-HYDROXYALKYL-SUBSTITUTED 1,2,3,6-TETRAHYDROPYRIDINE AND PIPERIDINE DERIVATIVES
    5.
    发明申请
    NOVEL N-HYDROXYALKYL-SUBSTITUTED 1,2,3,6-TETRAHYDROPYRIDINE AND PIPERIDINE DERIVATIVES 审中-公开
    新型N-羟基烷基取代的1,2,3,6-四氢吡啶和哌啶衍生物

    公开(公告)号：WO1993011107A1

    公开(公告)日：1993-06-10

    申请号：PCT/HU1992000050

    申请日：1992-12-01

    申请人： RICHTER GEDEON VEGYÉSZETI GYAR RT. ,  HARSANYI, Kálmán ,  GIZUR, Tibor ,  AGAI-CSONGOR, Éva ,  KALLAY-SOHONYAI, Anna ,  KAPOLNAS-PAP, Márta ,  CSIZÉR, Éva ,  HEGEDÜS, Béla ,  SZPORNY, László ,  KISS, Béla ,  KARPATI, Egon ,  PALOSI, Éva ,  SZOMBATHELYI, Zsolt ,  SARKADI, Adám ,  GERE, Anikó ,  BODO, Mihály ,  CSOMOR, Katalin ,  LASZY, Judit ,  SZENTIRMAI, Zsolt ,  LAPIS, Erzsébet ,  SZABO, Sándor ,  BOD, Péter ,  CSEHI, Attila

    发明人： RICHTER GEDEON VEGYÉSZETI GYAR RT.

    IPC分类号： C07D211/06

    CPC分类号： C07D211/52 ,  C07D211/14 ,  C07D211/70

    摘要： The invention relates to novel N-hydroxy-substituted 1,2,3,6-tetrahydropyridine and piperidine derivatives of formula (I) wherein A stands for hydrogen or halogen; alkoxy; cyano; phenyl; phenyl monosubstituted by halogen; benzyl; benzyl monosubstituted by halogen; 2-phenylethyl monosubstituted by halogen on the phenyl moiety; or 2-picolyl group; B represents hydrogen; alkoxy or nitro group; D represents hydrogen or halogen; or alkoxy group; or B and D together stand for a -CH=CH-CH=CH- group; R represents hydrogen; alkyl or phenyl group; G is hydrogen; I stands for hydrogen or hydroxy group; or G and I together represent a single chemical bond; E stands for hydrogen or halogen; alkoxy or trifluoromethyl group; and m is 0, 1 or 2, with the proviso that: m is 0 or 2, or both G and I mean hydrogen, when A stands for benzyl or halogen-monosubstituted benzyl group; and m is 1, when A stands for 2-picolyl group, as well as their acid addition salts. The invention further relates to pharmaceutical compositions containing these compounds as active ingredients as well as to a process for the preparation of compounds of formula (I) and their intermediates. The compounds of formula (I) are useful for enhancing the tolerance of mammals (including man) against hypoxic and/or ischaemic states as well as for treating the degenerative and functional disturbances arising from hypoxic and/or ischaemic insults.

    摘要翻译： 本发明涉及式（I）的新型N-羟基取代的1,2,3,6-四氢吡啶和哌啶衍生物，其中A代表氢或卤素; 烷氧基; 氰基; 苯基; 被卤素单取代的苯基; 苄基; 被卤素单取代的苄基; 在苯基部分被卤素单取代的2-苯基乙基; 或2-吡啶甲基; B表示氢; 烷氧基或硝基; D表示氢或卤素; 或烷氧基; 或B和D一起代表-CH = CH-CH = CH-基团; R代表氢; 烷基或苯基; G是氢; 我代表氢或羟基; 或G和I一起代表单一化学键; E代表氢或卤素; 烷氧基或三氟甲基; m为0,1或2，条件是：m为0或2，或者G和I均为氢，A表示苄基或卤素 - 单取代苄基; 并且当A代表2-吡啶甲基时，m为1，以及它们的酸加成盐。 本发明还涉及含有这些化合物作为活性成分的药物组合物以及制备式（I）化合物及其中间体的方法。 式（I）化合物可用于增强哺乳动物（包括人）对缺氧和/或缺血状态的耐受性，以及用于治疗由缺氧和/或缺血损伤引起的退行性和功能障碍。

    NOVEL 14-(N-SUBSTITUTED AMINOMETHYL)EBURNANE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND COMPOSITIONS CONTAINING THEM
    9.
    发明申请
    NOVEL 14-(N-SUBSTITUTED AMINOMETHYL)EBURNANE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND COMPOSITIONS CONTAINING THEM 审中-公开
    新型14-（N-取代氨基甲基）衍生物衍生物及其制备方法及其组合物

    公开(公告)号：WO1992010495A1

    公开(公告)日：1992-06-25

    申请号：PCT/HU1991000051

    申请日：1991-12-06

    申请人： RICHTER GEDEON VEGYÉSZETI GYAR RT. ,  SZPORNY, László ,  KISS, Béla ,  KARPATI, Egon ,  PALOSI, Éva ,  SZOMBATHELYI, Zsolt ,  SARKADI, Adám ,  GERE, Anikó ,  BODO, Mihály ,  CSOMOR, Katalin ,  LASZY, Judit ,  SZENTIRMAY, Zsolt ,  LAPIS, Erzsébet ,  SZABO, Sándor ,  KREIDL, János ,  VISKY, György ,  CZIBULA, László ,  NEMES, András

    发明人： RICHTER GEDEON VEGYÉSZETI GYAR RT.

    IPC分类号： C07D461/00

    CPC分类号： C07D461/00

    摘要： The invention relates to novel, optically active cis and trans 14-(N-substituted aminomethyl)eburnane derivatives of formula (I), wherein R1 stands for hydrogen, a C1-6alkyl or C2-6alkenyl group; R2 means a C1-6alkyl, C2-6alkenyl or a hydroxy-C1-6alkyl group; or R1 and R2 represent together with the adjacent nitrogen atom to which they are attached, a 5 to 7-membered saturated ring, optionally containing one oxygen atom and/or one optionally substituted nitrogen atom as heteroatom; and n is 2 or 3, as well as pharmaceutically acceptable salts of these compounds. The compounds of the invention possess an antioxidative (lipid peroxidation-inhibiting) effect and therefore, they are useful for treating diseases connected with lipid peroxidation, such as ischaemic intestinal diseases, myocardial ischaemia, ischaemic cerebrovascular disturbances as well as some diseases of connective tissues, e.g. rheumatoid arthritis. The compounds of the invention are also suitable for treating or preventing cognitive disorders.

    摘要翻译： 本发明涉及式（I）的新型光学活性顺式和反式14-（N-取代氨基甲基）艾本烷衍生物，其中R1代表氢，C1-6烷基或C2-6烯基; R 2表示C 1-6烷基，C 2-6烯基或羟基-C 1-6烷基; 或R 1和R 2与它们所连接的相邻氮原子一起表示5至7元饱和环，任选地含有一个氧原子和/或一个任选取代的氮原子作为杂原子; 和n为2或3，以及这些化合物的药学上可接受的盐。 本发明的化合物具有抗氧化（脂质过氧化抑制）效果，因此可用于治疗与脂质过氧化相关的疾病，例如缺血性肠病，心肌缺血，缺血性脑血管障碍以及结缔组织的一些疾病， 例如 类风湿关节炎。 本发明的化合物也适用于治疗或预防认知障碍。

    PROCESS FOR THE PREPARATION OF AN ANTIPSORIATIC PHARMACEUTICAL COMPOSITION
    10.
    发明申请
    PROCESS FOR THE PREPARATION OF AN ANTIPSORIATIC PHARMACEUTICAL COMPOSITION 审中-公开
    制备抗药性药物组合物的方法

    公开(公告)号：WO1988009662A1

    公开(公告)日：1988-12-15

    申请号：PCT/HU1988000042

    申请日：1988-06-10

    申请人： RICHTER GEDEON VEGYÉSZETI GYAR RT. ,  KEVE, Tibor ,  SZPORNY, László ,  KIRALY, Arpád ,  FEKETE, György ,  FORGACS, Lilla ,  STEFKO, Béla ,  ZSADON, Béla ,  GALAMBOS, János ,  BALAZSNÉ ZAYER, Mária ,  Hangay, György ,  KELEN, András ,  BUKOVECZNÉ BARTA, Margit ,  KARPATI, Egon ,  KISS, Béla ,  SOS, Gyöngyvér

    发明人： RICHTER GEDEON VEGYÉSZETI GYAR RT.

    IPC分类号： A61K31/475

    CPC分类号： A61K31/475 ,  A61K9/0014 ,  A61K47/10 ,  A61K47/12

    摘要： The invention relates to a process for the preparation of an antipsoriatic pharmaceutical composition containing 17,18-dehydroapovincaminol 3',4',5'-trimethoxybenzoate or its pharmaceutically acceptable acid addition salts, which comprises dissolving one equivalent of 17,18-dehydroapovincaminol 3',4',5'-trimethoxybenzoate or its pharmaceutically acceptable acid addition salt in 1.1 to 50, preferably 5 to 20, equivalents of an organic acid containing no basic group and being soluble in water or in a water-miscible monovalent or polyvalent alcohol or in a mixture thereof, or in a solution prepared from the organic acid with water or with a water-miscible monovalent or polyvalent alcohol or with a mixture thereof, and a) formulating the solution to a pharmaceutical composition as such or, if desired, together with therapeutically active agents showing no synergism with the active ingredient and/or with pharmaceutical auxiliary materials (additives), or b) diluting the solution with 5 to 50 parts by weight of water and formulating the thus-obtained gel, containing the active ingredient in a homogenous molecular distribution, as such or together with therapeutically active agents showing no synergism with the active ingredient and/or with a pharmaceutically acceptable auxiliary materials to a pharmaceutical composition.

    摘要翻译： 本发明涉及一种制备含有17,18-脱氢氨铂醇3'，4'，5'-三甲氧基苯甲酸酯或其药学上可接受的酸加成盐的抗牛皮癣药物组合物的方法，其包括将1当量的17,18-脱氢氨基嘌呤醇3 '，4'，5'-三甲氧基苯甲酸酯或其药学上可接受的酸加成盐在1.1至50，优选5至20当量的不含碱性基团的有机酸中并且可溶于水或水溶性单价或多价醇 或以其混合物，或由有机酸与水或与水混溶的单价或多价醇或其混合物制备的溶液，以及a）将溶液配制成药物组合物，或如果需要， 以及与活性成分和/或与药物辅助材料（添加剂）无协同作用的治疗活性剂，或b）用5至5 将0重量份的水配制成如此获得的含有均匀分子分布的活性成分的凝胶，或与治疗活性成分一起显示与活性成分和/或药学上可接受的辅助材料与 药物组成。