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    Oral anti-diabetic pharmaceutical forms and the preparation thereof
    1.
    发明授权
    Oral anti-diabetic pharmaceutical forms and the preparation thereof 失效
    口服抗糖尿病药物形式及其制备

    公开(公告)号：US4708868A

    公开(公告)日：1987-11-24

    申请号：US616010

    申请日：1984-05-31

    申请人： Rolf Brickl ,  Gottfried Schepky ,  Eckhard Rupprecht ,  Andreas Greischel

    发明人： Rolf Brickl ,  Gottfried Schepky ,  Eckhard Rupprecht ,  Andreas Greischel

    IPC分类号： A61K31/64 ,  A61K9/00 ,  A61K9/14 ,  A61K9/20 ,  A61K9/48 ,  A61K47/00 ,  A61P3/08 ,  A61K31/79 ,  A61K31/47 ,  A61K31/495 ,  A61K31/745

    CPC分类号： A61K9/146 ,  A61K9/2004 ,  Y10S514/861

    摘要： This invention is directed to novel galenic preparation forms for providing an oral anti-diabetic agent having an improved release of active substance and to processes for producing these preparation forms. The pharmaceutical compositions are characterized in that the onset of the activity and the duration of activity are adapted to the particular needs of diabetics with regard to proper control of metabolism and the associated proper release of insulin. A basic or acidic excipient in a solvent is added to the anti-diabetically active substance in a quantity such that the active substance is made soluble, and then a solubilizing agent is added. The solution is applied to a water-insoluble carrier, the solvent is evaporated, and the residue is further processed to yield the various preparation forms.

    摘要翻译： 本发明涉及用于提供具有改善的活性物质释放的口服抗糖尿病药物的新型盖仑制剂形式和用于制备这些制剂形式的方法。 药物组合物的特征在于活性的发作和活性的持续时间适应于糖尿病患者适当控制代谢和相关的胰岛素正确释放的特殊需要。 将溶剂中的碱性或酸性赋形剂加入到抗糖尿病活性物质中，其量使得活性物质可溶，然后加入增溶剂。 将溶液施加到水不溶性载体上，蒸发溶剂，并进一步处理残余物以产生各种制备形式。

    Anti-diabetic pharmaceutical forms and the preparation thereof
    2.
    发明授权
    Anti-diabetic pharmaceutical forms and the preparation thereof 失效
    抗糖尿病药物形式及其制备方法

    公开(公告)号：US4696815A

    公开(公告)日：1987-09-29

    申请号：US615892

    申请日：1984-05-31

    申请人： Gottfried Schepky ,  Rolf Brickl ,  Eckhard Rupprecht ,  Andreas Greischel

    发明人： Gottfried Schepky ,  Rolf Brickl ,  Eckhard Rupprecht ,  Andreas Greischel

    IPC分类号： A61K31/19 ,  A61K9/00 ,  A61K9/14 ,  A61K9/20 ,  A61K31/047 ,  A61K31/195 ,  A61K31/395 ,  A61K31/445 ,  A61K31/64 ,  A61K45/00 ,  A61K47/00 ,  A61P3/08 ,  A61K31/79 ,  A61K31/415 ,  A61K31/47 ,  A61K31/495

    CPC分类号： A61K9/2004 ,  A61K9/146 ,  Y10S514/866

    摘要： The invention is directed to novel galenic preparation forms for providing an oral anti-diabetic agent having an improved release of active substance and processes for producing these preparation forms. The novel pharmaceutical compositions are characterized in that the onset of the activity and the duration of activity are adapted to the particular needs of diabetics with regard to proper control of the metabolism and the associated proper release of insulin. A basic or acidic excipient in a solvent is added to the anti-diabetic active substance in a quantity such that the active substance is made soluble, and then a solubilizing agent is added. Polyvinyl pyrrolidone is dissolved as carrier in this solution, but the carrier may simultaneously serve as the solubilizing adjuvant. This solution is further processed with other excipients to form corresponding preparation forms.

    摘要翻译： 本发明涉及用于提供具有改善的活性物质释放的口服抗糖尿病药物和用于制备这些制剂形式的新型盖仑制剂形式。 新型药物组合物的特征在于活性的发作和活性的持续时间适应于糖尿病患者适当控制代谢和相关的胰岛素正确释放的特殊需要。 将溶剂中的碱性或酸性赋形剂添加到抗糖尿病活性物质中，其量使得活性物质可溶，然后加入增溶剂。 聚乙烯吡咯烷酮作为载体溶解在该溶液中，但载体可以同时用作增溶助剂。 该溶液进一步用其它赋形剂处理以形成相应的制备形式。

    Oral anti-diabetic pharmaceutical compositions and the preparation thereof
    3.
    发明授权
    Oral anti-diabetic pharmaceutical compositions and the preparation thereof 失效
    口服抗糖尿病药物组合物及其制备

    公开(公告)号：US4873080A

    公开(公告)日：1989-10-10

    申请号：US103524

    申请日：1987-09-30

    申请人： Rolf Brickl ,  Gottfried Schepky ,  Eckhard Rupprecht ,  Andreas Greischel

    发明人： Rolf Brickl ,  Gottfried Schepky ,  Eckhard Rupprecht ,  Andreas Greischel

    IPC分类号： A61K31/64 ,  A61K9/00 ,  A61K9/14 ,  A61K9/20 ,  A61K9/48 ,  A61K47/00 ,  A61P3/08

    CPC分类号： A61K9/146 ,  A61K9/2004 ,  Y10S514/861

    摘要： Galenic compositions containing an oral antidiabetic agent and having an improved release of active substance as well as processes for producing these compositions are provided. The pharmaceutical compositions are characterized in that the onset of the activity and the duration of activity are adapted to the particular needs of diabetics with regard to proper control of metabolism and the associated proper release of insulin. A basic or acidic excipient in a solvent is added to the anti-diabetically active substance in a quantity such that the active substance is made soluble, and then a solubilizing agent is added. The solution is applied to a water-insoluble carrier, the solvent is evaporated, and the residue is further processed to yield the various compositions.

    摘要翻译： 提供了含有口服抗糖尿病药物和具有改善的活性物质释放的Galenic组合物以及制备这些组合物的方法。 药物组合物的特征在于活性的发作和活性的持续时间适应于糖尿病患者适当控制代谢和相关的胰岛素正确释放的特殊需要。 将溶剂中的碱性或酸性赋形剂加入到抗糖尿病活性物质中，其量使得活性物质可溶，然后加入增溶剂。 将溶液施加到水不溶性载体上，蒸发溶剂，并进一步处理残余物以得到各种组合物。

    Anti-diabetic pharmaceutical compositions and the preparation thereof
    4.
    发明授权
    Anti-diabetic pharmaceutical compositions and the preparation thereof 失效
    抗糖尿病药物组合物及其制备

    公开(公告)号：US4863724A

    公开(公告)日：1989-09-05

    申请号：US76697

    申请日：1987-07-23

    申请人： Gottfried Schepky ,  Rolf Brickl ,  Eckhard Rupprecht ,  Andreas Greischel

    发明人： Gottfried Schepky ,  Rolf Brickl ,  Eckhard Rupprecht ,  Andreas Greischel

    IPC分类号： A61K31/19 ,  A61K9/00 ,  A61K9/14 ,  A61K9/20 ,  A61K31/047 ,  A61K31/195 ,  A61K31/395 ,  A61K31/445 ,  A61K31/64 ,  A61K45/00 ,  A61K47/00 ,  A61P3/08

    CPC分类号： A61K9/2004 ,  A61K9/146 ,  Y10S514/866

    摘要： Galenic compositions containing an oral antidiabetic agent and having an improved release of active substance are provided, as well as processes for producing these compositions. The compositions are characterized in that the onset of the activity and the duration of activity are adapted to the particular needs of diabetics with regard to proper control of the metabolism and the associated proper release of insulin. A basic or acidic excipient in a solvent is added to the antidiabetic active substance in a quantity such that the active substance is made soluble, and then a solubilizing agent is added. Polyvinylpyrrolidone is dissolved as carrier in this solution, but the carrier may simultaneously serve as the solubilizing adjuvant. This solution is further processed with other excipients to form pharmaceutical compositions.

    摘要翻译： 提供了含有口服抗糖尿病药物并具有改善的活性物质释放的Galenic组合物，以及制备这些组合物的方法。 组合物的特征在于活性的发作和活性的持续时间适应糖尿病患者在适当控制代谢和相关的胰岛素正确释放方面的特殊需要。 将溶剂中的碱性或酸性赋形剂加入到抗糖尿病活性物质中，其量使得活性物质可溶，然后加入增溶剂。 聚乙烯吡咯烷酮作为载体溶解在该溶液中，但载体可以同时用作增溶助剂。 该溶液进一步用其它赋形剂处理以形成药物组合物。

    Azepine derivatives and their anti-thrombotic compositions and methods
    6.
    发明授权
    Azepine derivatives and their anti-thrombotic compositions and methods 失效
    Azepine衍生物及其抗血栓形成和方法

    公开(公告)号：US4414225A

    公开(公告)日：1983-11-08

    申请号：US348496

    申请日：1982-02-12

    申请人： Robert Sauter ,  Gerhart Griss ,  Wolfgang Grell ,  Rudolf Hurnaus ,  Bernhard Eisele ,  Walter Haarmann ,  Eckhard Rupprecht

    发明人： Robert Sauter ,  Gerhart Griss ,  Wolfgang Grell ,  Rudolf Hurnaus ,  Bernhard Eisele ,  Walter Haarmann ,  Eckhard Rupprecht

    IPC分类号： C07D487/02 ,  A61K31/55 ,  A61P3/06 ,  A61P7/02 ,  C07D223/06 ,  C07D487/04 ,  C07D491/02 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  A61K31/40

    CPC分类号： C07D487/04 ,  C07D223/06 ,  C07D491/04 ,  C07D495/04

    摘要： Compounds of the formula ##STR1## wherein n and m are each 1, 2 or 3, and the sum of n+m is 4;R.sub.1 is alkyl; alkenyl; unsubstituted, mono- or di-substituted aralkyl; unsubstituted, mono- or di-substituted benzoyl; alkoxycarbonyl; aralkoxycarbonyl; or, when m and n are each 2 and/or R.sub.2 and R.sub.3 are other than both hydrogen at the same time, also hydrogen;one of R.sub.2 and R.sub.3 is hydrogen or amino, and the other is carboxyl or alkoxycarbonyl; or, when R.sub.3 is hydrogen,R.sub.2 is hydrogen; amino; alkoxycarbonyl-amino; (unsubstituted or mono-substituted phenyl)-aminocarbonyl-; (unsubstituted or mono-substituted phenyl)ethylaminocarbonyl; azidocarbonyl; or hydrazinocarbonyl;X is oxygen, sulfur or ##STR2## where R.sub.4 is hydrogen; alkyl; phenyl-alkyl; or phenyl; non-toxic, pharmacologically acceptable acid addition salts thereof; and, when R.sub.2 or R.sub.3 is carboxyl, non-toxic, pharmacologically acceptable salts thereof formed with inorganic or organic bases. The compounds as well as their salts are useful as antithrombotics.

    摘要翻译： 其中n和m各自为1,2或3，并且n + m的和为4; R1是烷基; 烯基; 未取代的，单或二取代的芳烷基; 未取代的，单或二取代的苯甲酰基; 烷氧基羰基 芳烷氧羰基; 或者当m和n各自为2和/或R 2和R 3不同时为氢时，也为氢; R2和R3之一是氢或氨基，另一个是羧基或烷氧基羰基; 或当R3为氢时，R2为氢; 氨基; 烷氧基羰基 - 氨基; （未取代或单取代的苯基） - 氨基羰基 - ; （未取代或单取代的苯基）乙基氨基羰基; 叠氮羰基; 或肼基羰基; X是氧，硫或者其中R 4是氢; 烷基; 苯基 - 烷基; 或苯基; 无毒，药理学上可接受的酸加成盐; 并且当R 2或R 3为羧基时，与无机或有机碱形成的无毒的药学上可接受的盐。 化合物及其盐可用作抗血栓形成剂。

    Phenylethanolamines, their use as pharmaceuticals and as performance enhancers in animals
    10.
    发明授权
    Phenylethanolamines, their use as pharmaceuticals and as performance enhancers in animals 失效
    苯乙醇胺，它们用作药物和作为动物中的性能增强剂

    公开(公告)号：US5232946A

    公开(公告)日：1993-08-03

    申请号：US572969

    申请日：1990-08-20

    申请人： Rudolf Hurnaus ,  Manfred Reiffen ,  Robert Sauter ,  Wolfgang Grell ,  Eckhard Rupprecht

    发明人： Rudolf Hurnaus ,  Manfred Reiffen ,  Robert Sauter ,  Wolfgang Grell ,  Eckhard Rupprecht

    IPC分类号： A61K31/13 ,  A61K31/135 ,  A61K31/16 ,  A61K31/19 ,  A61K31/195 ,  A61K31/215 ,  A61K31/22 ,  A61K31/275 ,  A61K31/40 ,  A61P3/00 ,  A61P43/00 ,  C07C213/00 ,  C07C215/30 ,  C07C215/32 ,  C07C215/48 ,  C07C215/54 ,  C07C215/68 ,  C07C217/56 ,  C07C217/62 ,  C07C221/00 ,  C07C225/16 ,  C07C227/00 ,  C07C229/38 ,  C07C233/43 ,  C07C237/30 ,  C07C253/30 ,  C07C255/53 ,  C07C255/59

    CPC分类号： C07C255/00 ,  C07C229/38

    摘要： The invention relates to new phenylethanolamines of general formula ##STR1## wherein A represents a straight-chained or branched alkylene group,B represents a bond, an alkylene group, a carbonyl or hydroxymethylene group,R.sub.1 represents a hydrogen atom, a halogen atom or a trifluoromethyl group,R.sub.2 represents a hydrogen atom or an amino group,R.sub.3 represents a cyano group, a hydrogen, chlorine or bromine atom andR.sub.4 represents a hydrogen or halogen atom, an alkyl, hydroxy, alkoxy, carboxy, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl or dialkylaminocarbonyl group or an alkoxy group substituted in the end position by a carboxy, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, hydroxy, alkoxy, amino, alkylamino, dialkylamino, pyrrolidino, piperidino or hexamethyleneimino group,the optical isomers and diastereoisomers and acid addition salts thereof.The new compounds of formula I, the optical isomers and diastereoisomers and acid addition salts thereof, particularly the physiologically acceptable acid addition salts thereof with inorganic or organic acids, have valuable pharmacological properties, namely an effect on the metabolism, preferably the effect of lowering blood sugar and reducing body fat and they may also be used as performance enhancers in animals.The new compounds of general formula I above may be prepared by methods known per se.

    摘要翻译： PCT No.PCT / EP88 / 01083 Sec。 371日期1990年8月20日 102（e）1990年8月20日日期PCT提交1988年11月29日PCT公布。 WO90 / 06299 PCT出版物 日本1990年6月14日。本发明涉及通式为（I）的新型苯乙醇胺，其中A表示直链或支链亚烷基，B表示键，亚烷基，羰基或羟基亚甲基，R1 表示氢原子，卤原子或三氟甲基，R 2表示氢原子或氨基，R 3表示氰基，氢，氯或溴原子，R 4表示氢或卤素原子，烷基，羟基， 烷氧基羰基，烷氧基羰基，氨基羰基，烷基氨基羰基或二烷基氨基羰基或由羧基，烷氧基羰基，氨基羰基，烷基氨基羰基，二烷基氨基羰基，羟基，烷氧基，氨基，烷基氨基，二烷基氨基，吡咯烷子基，哌啶子基或六亚甲基亚氨基取代的烷氧基。 光学异构体和非对映异构体及其酸加成盐。 式I的新化合物，其光学异构体和非对映异构体及其酸加成盐，特别是其与无机或有机酸的生理上可接受的酸加成盐具有有价值的药理学性质，即对代谢的影响，优选降低血液的作用 糖和减少身体脂肪，并且它们也可以用作动物中的性能增强剂。 上述通式I的新化合物可以通过本身已知的方法制备。