公开(公告)号：US5084469A

公开(公告)日：1992-01-28

申请号：US612399

申请日：1990-11-09

申请人： Isabelle Lesieur ,  Said Yous ,  Michelle Devissaguet ,  Yannis Tsouderos

发明人： Isabelle Lesieur ,  Said Yous ,  Michelle Devissaguet ,  Yannis Tsouderos

IPC分类号： A61K31/425 ,  A61K31/428 ,  A61P7/02 ,  A61P9/00 ,  A61P25/04 ,  C07D277/68 ,  C07D417/06

CPC分类号： C07D277/68 ,  C07D417/06

摘要： Compounds of general formula (I): ##STR1## in which: R.sub.1 represents a hydrogen atom or a lower alkyl group, andR.sub.2 represents a substituted or unsubstituted alkyl, a phenyl or a substituted or unsubstituted heteroaryl,their enantiomers, diastereoisomers and epimers and their addition salts with a pharmaceutically acceptable base when R.sub.1 represents a hydrogen atom or when R.sub.2 comprises a carboxylic acid group. Medicinal products.

摘要翻译： 通式（I）的化合物：其中：R1表示氢原子或低级烷基，R2表示取代或未取代的烷基，苯基或取代或未取代的杂芳基，其对映体，非对映异构体 当R1表示氢原子或当R 2包含羧酸基团时，它们与药学上可接受的碱的差向异构体及其加成盐。 药用产品。

公开(公告)号：US4407801A

公开(公告)日：1983-10-04

申请号：US306224

申请日：1981-09-28

申请人： Jean-Claude Arnaud ,  Michelle Devissaguet

发明人： Jean-Claude Arnaud ,  Michelle Devissaguet

IPC分类号： A61K9/20 ,  A61K31/495 ,  A61K31/70

CPC分类号： A61K9/2018 ,  A61K31/495 ,  A61K9/2059

摘要： The subject of the invention is a novel pharmaceutical composition, especially having an anti-ischaemic action, containing, in combination, a high dosage (within the range of from 20 to 80 mg) of the dihydrochloride (or another mineral or organic salt) of 1-(2,3,4-trimethoxybenzyl)piperazine and a disintegrating agent, such as mannitol or sodium carboxymethyl starch, that has the effect of liberating the salt of 1-(2,3,4-trimethoxybenzyl)piperazine virtually instantaneously in the organism, this composition being, furthermore, advantageously enclosed in a thin coating film or held together by a binder that is itself readily disintegrated in situ in the organism in such a manner that it makes possible a "flash" action, that is to say a virtually instantaneous action, of the above-mentioned salt in situ. This composition is administered to the patient at a dosage of from 20 to 80 mg/day.

摘要翻译： 本发明的主题是特别是具有抗缺血作用的新型药物组合物，其组合含有二盐酸盐（或另一种矿物或有机盐）的高剂量（在20至80mg范围内） 1-（2,3,4-三甲氧基苄基）哌嗪和崩解剂，如甘露糖醇或羧甲基淀粉钠，其实际上可以瞬间释放1-（2,3,4-三甲氧基苄基）哌嗪的盐 此外，该组合物还有利地封闭在薄的涂膜中或通过粘合剂保持在一起，所述粘合剂本身容易在生物体中原位分解，使得可能发生“闪光”作用，也就是说 几乎瞬间作用，上述盐原位。 将该组合物以20至80mg /天的剂量施用于患者。