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11.发明授权2[3-(4-Chlorophenyl)-1,2-dimethyl-1H-indol-5-yloxy]-2-methyl propanoic acid and hyperlipidemic or atheosclerotic use thereof 失效2 [3-（4-氯苯基）-1,2-二甲基-1H-吲哚-5-基氧基] -2-甲基丙酸和其高脂血症或动脉粥样硬化用途
公开(公告)号：US4343811A
公开(公告)日：1982-08-10
申请号：US126006
申请日：1980-02-29
申请人： Rudolf Hurnaus , Gerhart Griss , Wolfgang Grell , Robert Sauter , Bernhard Eisele , Nikolaus Kaubisch , Eckhard Rupprecht , Joachim Kahling
发明人： Rudolf Hurnaus , Gerhart Griss , Wolfgang Grell , Robert Sauter , Bernhard Eisele , Nikolaus Kaubisch , Eckhard Rupprecht , Joachim Kahling
IPC分类号： C07D401/04 , A61K31/40 , A61K31/403 , A61K31/44 , A61K31/4427 , A61P3/06 , A61P9/10 , C07D209/04 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/14 , C07D209/43 , C07D401/06 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/14 , C07D487/04 , Y10S514/824
摘要： This invention relates to novel indole derivatives of formula ##STR1## and the non-toxic, pharmacologically acceptable salts thereof. These compounds exhibit desirable pharmacological properties, especially lipid-level lowering and anti-atherosclerotic activity. The compounds of the invention may be prepared by, for example, alkylation of a corresponding hydroxy indole.
摘要翻译： 本发明涉及式IMA的新型吲哚衍生物及其无毒的药理学上可接受的盐。 这些化合物显示出所需的药理学性质，特别是脂质降低和抗动脉粥样硬化活性。 本发明的化合物可以通过例如相应的羟基吲哚的烷基化来制备。
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公开(公告)号：US4696815A
公开(公告)日：1987-09-29
申请号：US615892
申请日：1984-05-31
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。
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13.发明授权
公开(公告)号：US4873080A
公开(公告)日：1989-10-10
申请号：US103524
申请日：1987-09-30
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。
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公开(公告)号：US4863724A
公开(公告)日：1989-09-05
申请号：US76697
申请日：1987-07-23
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。
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公开(公告)号：US4708868A
公开(公告)日：1987-11-24
申请号：US616010
申请日：1984-05-31
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。
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