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    Biologically active eburnamenine derivatives, pharmaceutical compositions containing them and process for preparing same
    2.
    发明授权
    Biologically active eburnamenine derivatives, pharmaceutical compositions containing them and process for preparing same 失效
    生物活性白蛋白衍生物，含有它们的药物组合物及其制备方法

    公开(公告)号：US5510345A

    公开(公告)日：1996-04-23

    申请号：US351447

    申请日：1994-12-08

    申请人： Zoltan Tuba ,  Sandor Maho ,  Aniko Gere ,  Pal Vittay ,  Bela Kiss ,  Eva Palosi ,  Laszlo Szporny ,  Csaba Szantay ,  Ferenc Soti ,  Zsuzsa Baloghne Kardos ,  Maria Incze ,  Gabor Balogh ,  Maria Gazdag

    发明人： Zoltan Tuba ,  Sandor Maho ,  Aniko Gere ,  Pal Vittay ,  Bela Kiss ,  Eva Palosi ,  Laszlo Szporny ,  Csaba Szantay ,  Ferenc Soti ,  Zsuzsa Baloghne Kardos ,  Maria Incze ,  Gabor Balogh ,  Maria Gazdag

    IPC分类号： C07D471/00 ,  A61K31/495 ,  A61K31/505 ,  A61K31/55 ,  A61P9/08 ,  A61P9/10 ,  A61P13/02 ,  A61P15/00 ,  A61P25/28 ,  C07D239/00 ,  C07D295/00 ,  C07D461/00 ,  C07D401/14 ,  C07D403/14

    CPC分类号： C07D461/00

    摘要： The invention relates to novel eburnamenine derivatives of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 as well as R.sup.3 and R.sup.4, independently from each other, stand for hydrogen, C.sub.2-6 alkyl group, C.sub.2-6 alkenyl group; or a C.sub.3-10 alicyclic group involving 1 to 3 rings, and this latter group may be substituted by a C.sub.1-6 alkyl or C.sub.2-6 alkenyl group; or R.sup.1 and R.sup.2 and/or R.sup.3 and R.sup.4, together with the adjacent nitrogen atom and optionally with an additional oxygen or nitrogen atom, form a 4- to 6-membered, saturated or unsaturated cyclic group which may be substituted by a C.sub.1-6 alkyl or C.sub.2-6 alkenyl group; two of X, Y and Z are nitrogen whereas the third of them means a methine group; n is 1 or 2; W means oxygen or two hydrogen atoms; and the wavy line means .alpha.-/.alpha.-, .alpha.-/.beta.- or .beta.-/.alpha.- steric position, as well as their acid addition salts and solvates. The invention further relates to pharmaceutical compositions containing the above compounds as well as a process for preparing the compounds of formula (I). The compounds of formula (I) possess antioxidant effect and therefore, they are useful for inhibiting the peroxidation of lipids occurring in mammals (including human).

    摘要翻译： PCT No.PCT / Hu93 / 00036 Sec。 371日期1994年12月8日第 102（e）日期1994年12月8日PCT提交1993年6月8日PCT公布。 出版物WO93 / 25550 本发明涉及式（I）的新颖白蛋白衍生物：其中R 1和R 2以及R 3和R 4彼此独立地代表氢，C 2-6烷基 ，C 2-6烯基; 或含有1〜3个环的C 3〜10环亚烷基，后者可以被C 1-6烷基或C 2-6烯基取代; 或R 1和R 2和/或R 3和R 4与相邻的氮原子以及任选的另外的氧或氮原子一起形成可被C 1-6烷基取代的4-至6-元饱和或不饱和的环状基团 或C 2-6烯基; X，Y和Z中的两个是氮，而第三个是次甲基; n为1或2; W表示氧或两个氢原子; 波浪线表示α - /α - ，α - /β - 或β - / - - - 立体位置，以及它们的酸加成盐和溶剂合物。 本发明还涉及含有上述化合物的药物组合物以及制备式（I）化合物的方法。 式（I）化合物具有抗氧化作用，因此它们可用于抑制哺乳动物（包括人）中发生的脂质的过氧化反应。

    PROCESS FOR THE PREPARATION OF CHIRALLY PURE NATEGLINIDE
    4.
    发明申请
    PROCESS FOR THE PREPARATION OF CHIRALLY PURE NATEGLINIDE 审中-公开
    制备纯丙烯酰氯的方法

    公开(公告)号：US20100256414A1

    公开(公告)日：2010-10-07

    申请号：US12755572

    申请日：2010-04-07

    申请人： Maria Gazdag ,  Tibor Gizur ,  Bela Hegedus ,  Attila Szemzo ,  Gabor Tarkanyi ,  Jozsef Törley ,  Monika Babjak

    发明人： Maria Gazdag ,  Tibor Gizur ,  Bela Hegedus ,  Attila Szemzo ,  Gabor Tarkanyi ,  Jozsef Törley ,  Monika Babjak

    IPC分类号： C07C229/36

    CPC分类号： C07C233/63 ,  C07C231/12 ,  C07C231/24

    摘要： The invention relates to N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanine (nateglinide) in the novel crystalline form “G” and a process for the preparation thereof. A process for the preparation of chirally pure nateglinide by treating a lower alkyl ester thereof with a base to yield an alkali salt and liberating the product from said salt by proper addition of an acid, is also provided. Still another aspect of the invention is a process for the preparation of nateglinide in the crystalline form “H” from other crystalline modifications of nateglinide.

    摘要翻译： 本发明涉及新型晶型“G”中的N-（反式-4-异丙基环己基羰基）-D-苯丙氨酸（那格列奈）及其制备方法。 还提供了通过用碱处理其低级烷基酯以产生碱金属盐并通过适当添加酸从所述盐释放产物来制备手性纯奈格列奈的方法。 本发明的另一方面是从那格列奈的其他结晶修饰物制备结晶形式“H”的那格列奈的方法。

    Parenteral solvent and a process for the preparation of stable solutions containing same
    5.
    发明授权
    Parenteral solvent and a process for the preparation of stable solutions containing same 失效
    肠胃外溶剂和制备含有它们的稳定溶液的方法

    公开(公告)号：US4344950A

    公开(公告)日：1982-08-17

    申请号：US201509

    申请日：1980-10-28

    申请人： Geza T. Nagy ,  Gabor Szepesi ,  Maria Gazdag

    发明人： Geza T. Nagy ,  Gabor Szepesi ,  Maria Gazdag

    IPC分类号： A61K31/435 ,  A61K9/00 ,  A61K9/08 ,  A61K31/475 ,  A61K47/00 ,  A61P25/28

    CPC分类号： A61K9/0019 ,  A61K31/475

    摘要： A parenteral solvent suitable for injectable solutions of eburnamenines and dihydroeburnamenines is disclosed, said solvent containing a buffer having the ability to buffer the injectable solutions at given pH values, at least one stabilizing agent which includes parenterally acceptable aliphatic alcohols containing one or more hydroxy groups or water-miscible ethers thereof, 30 to 70% by weight water and optional preservatives, anaesthetics, and antioxidants.

    摘要翻译： 公开了一种适用于本戊胺和二氢巴西那宁的可注射溶液的肠胃外溶剂，所述溶剂含有缓冲液，其具有在给定pH值下缓冲注射溶液的能力，至少一种稳定剂，其包含含有一个或多个羟基的肠胃外可接受的脂族醇或 水混溶性醚，30-70％重量水和任选的防腐剂，麻醉剂和抗氧化剂。

    Process for the preparation of chirally pure N-(trans-4-is)
    6.
    发明授权
    Process for the preparation of chirally pure N-(trans-4-is) 失效
    手性纯N-（反式-4-异构体）的制备方法

    公开(公告)号：US07767847B2

    公开(公告)日：2010-08-03

    申请号：US10564017

    申请日：2004-07-08

    申请人： Maria Gazdag ,  Tibor Gizur ,  Bela Hegedus ,  Attila Szemzo ,  Gabor Tarkanyi ,  Jozsef Törley ,  Monika Babjak

    发明人： Maria Gazdag ,  Tibor Gizur ,  Bela Hegedus ,  Attila Szemzo ,  Gabor Tarkanyi ,  Jozsef Törley ,  Monika Babjak

    IPC分类号： C07C229/00

    CPC分类号： C07C233/63 ,  C07C231/12 ,  C07C231/24

    摘要： The invention relates to N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanine (nateglinide) in the novel crystalline form “G” and a process for the preparation thereof. A process for the preparation of chirally pure nateglinide by treating a lower alkyl ester thereof with a base to yield an alkali salt and liberating the product from said salt by proper addition of an acid, is also provided. Still another aspect of the invention is a process for the preparation of nateglinide in the crystalline form “H” from other crystalline modifications of nateglinide.

    摘要翻译： 本发明涉及新型晶型“G”中的N-（反式-4-异丙基环己基羰基）-D-苯丙氨酸（那格列奈）及其制备方法。 还提供了通过用碱处理其低级烷基酯以产生碱金属盐并通过适当添加酸从所述盐释放产物来制备手性纯奈格列奈的方法。 本发明的另一方面是从那格列奈的其他结晶修饰物制备结晶形式“H”的那格列奈的方法。

    Process for the preparation of chirally pure n-(trans-4-is
    7.
    发明申请
    Process for the preparation of chirally pure n-(trans-4-is 失效
    手性纯的n-（反式-4-异构体）的制备方法

    公开(公告)号：US20070043117A1

    公开(公告)日：2007-02-22

    申请号：US10564017

    申请日：2004-07-08

    申请人： Maria Gazdag ,  Tibor Gizur ,  Bela Hegedus ,  Attila Szemzo ,  Gabor Tarkanyi ,  Jozsef Torley ,  Monika Babjak

    发明人： Maria Gazdag ,  Tibor Gizur ,  Bela Hegedus ,  Attila Szemzo ,  Gabor Tarkanyi ,  Jozsef Torley ,  Monika Babjak

    IPC分类号： A61K31/198 ,  C07C237/20

    CPC分类号： C07C233/63 ,  C07C231/12 ,  C07C231/24

    摘要： The invention relates to N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanine (nateglinide) in the novel crystalline form “G” and a process for the preparation thereof. A process for the preparation of chirally pure nateglinide by treating a lower alkyl ester thereof with a base to yield an alkali salt and liberating the product from said salt by proper addition of an acid, is also provided. Still another aspect of the invention is a process for the preparation of nateglinide in the crystalline form “H” from other crystalline modifications of nateglinide.

    摘要翻译： 本发明涉及新型晶型“G”中的N-（反式-4-异丙基环己基羰基）-D-苯丙氨酸（那格列奈）及其制备方法。 还提供了通过用碱处理其低级烷基酯以产生碱金属盐并通过适当添加酸从所述盐释放产物来制备手性纯奈格列奈的方法。 本发明的另一方面是从那格列奈的其他结晶修饰物制备结晶形式“H”的那格列奈的方法。

    Metal complexes of bis-indole compounds and aqueous pharmaceutical compositions containing them
    9.
    发明授权
    Metal complexes of bis-indole compounds and aqueous pharmaceutical compositions containing them 失效
    双吲哚化合物的金属络合物和含有它们的含水药物组合物

    公开(公告)号：US4684638A

    公开(公告)日：1987-08-04

    申请号：US782492

    申请日：1985-10-01

    申请人： Geza T. Nagy ,  Gabor Szepesi ,  Maria Gazdag ,  Zsofia Papp nee Sziklay ,  Kalman Burger

    发明人： Geza T. Nagy ,  Gabor Szepesi ,  Maria Gazdag ,  Zsofia Papp nee Sziklay ,  Kalman Burger

    IPC分类号： A61K9/00 ,  A61K9/08 ,  A61K31/475 ,  A61K31/555 ,  A61K47/26 ,  A61P35/00 ,  C07D519/04 ,  C07F3/02 ,  C07F3/04 ,  C07F3/06

    CPC分类号： A61K9/0019 ,  A61K31/475 ,  A61K47/26 ,  C07D519/04

    摘要： The invention relates to new aqueous pharmaceutical compositions containing as active ingredient a pharmaceutically acceptable complex of a bis-indole compound with a bi- or multivalent metal ion in a therapeutically effective amount. The invention further relates to complexes formed between a bis-indole compound and a bi- or multivalent metal ion.According to another aspect of the invention there is provided a process for the preparation of a pharmaceutically acceptable metal complex of a bis-indole compound and optionally stable aqueous pharmaceutical compositions containing said metal complex, in which a solution of a bis-indole compound or a pharmaceutically acceptable salt thereof in an aqueous medium is reacted with a non-toxic water soluble salt of a bi- or multivalent metal capable of complexation, at a pH of 3.0 to 6.0, optionally in the presence of or followed by the addition of a conventional pharmaceutical carrier and/or further additive, or, if desired, the obtained complex is isolated.The aqueous pharmaceutical compositions according to the invention have substantially increased stability.

    摘要翻译： 本发明涉及含有治疗有效量的双吲哚化合物与双价或多价金属离子的药学上可接受的复合物作为活性成分的新的含水药物组合物。 本发明还涉及在双吲哚化合物和二价或多价金属离子之间形成的络合物。 根据本发明的另一方面，提供了制备双 - 吲哚化合物和任选的包含所述金属络合物的任选稳定的含水药物组合物的药学上可接受的金属络合物的方法，其中将双吲哚化合物或 其药学上可接受的盐在水性介质中与无毒的水溶性二价或多价金属盐在3.0至6.0的pH下反应，任选在存在或随后加入常规 药物载体和/或另外的添加剂，或者如果需要，分离获得的复合物。 根据本发明的水性药物组合物具有显着提高的稳定性。