公开(公告)号：US06727367B2

公开(公告)日：2004-04-27

申请号：US09953870

申请日：2001-09-18

申请人： Karel Pospisilik

发明人： Karel Pospisilik

IPC分类号： C07D27782

CPC分类号： C07D277/82 ,  C07B2200/07

摘要： A process for resolving or enriching (R,S) 2-amino-6-propylamino-4,5,6,7-tetrahydrobenzothiazole (pramipexole) into optical isomers uses a monovalent salt thereof, e.g. pramipexole monohydrochloride, as a substrate. The monovalent salt is treated with an optically active acid, e.g. with L(+)-tartaric acid, to yield a diastereomeric mixed salt. The mixed salt is subjected to fractional crystallization to yield an optically enriched mixed salt. The mixed salt can be treated with base to liberate the desired isomer of pramipexole.

公开(公告)号：US06770761B2

公开(公告)日：2004-08-03

申请号：US10380758

申请日：2003-08-07

申请人： Karel Pospisilik ,  Hans Jan Hoorn ,  Theodorus Hendricus Antonius Peters ,  Jacobus Maria Lemmens

发明人： Karel Pospisilik ,  Hans Jan Hoorn ,  Theodorus Hendricus Antonius Peters ,  Jacobus Maria Lemmens

IPC分类号： C07D27782

CPC分类号： C07D277/82 ,  C07B2200/07

摘要： A new process to obtain pramipexole and related products is described. The process involves the reaction of new compounds of formula (6), wherein R is hydrogen or acyl group, R3 and R4 are either the same and each of them represents an alkoxy group of 1-4 carbons or they together form a C2-C5 alkylenedioxy group or an oxo-group, with an alkylamine in the presence of a reducing agent or a hydrogen gas with hydrogenation catalyst. A process to obtain new compounds of formula (6) is also described.

摘要翻译： 描述了获得普拉克索及其相关产品的新方法。 该方法涉及新的式（6）化合物，其中R是氢或酰基，R 3和R 4相同，并且它们各自表示1-4个碳的烷氧基或它们一起形成C 2 -C 5 亚烷基二氧基或氧代基与烷基胺在还原剂或氢气与氢化催化剂存在下反应。 还描述了获得新的式（6）化合物的方法。

公开(公告)号：US06495693B2

公开(公告)日：2002-12-17

申请号：US09280966

申请日：1999-03-30

申请人： James E. Audia ,  Beverly K. Folmer ,  Varghese John ,  Lee H. Latimer ,  Jeffrey S. Nissen ,  Warren J. Porter ,  Eugene D. Thorsett ,  Jing Wu

发明人： James E. Audia ,  Beverly K. Folmer ,  Varghese John ,  Lee H. Latimer ,  Jeffrey S. Nissen ,  Warren J. Porter ,  Eugene D. Thorsett ,  Jing Wu

IPC分类号： C07D27782

CPC分类号： C07D215/38 ,  A61K31/00 ,  A61K31/198 ,  A61K31/223 ,  C07C237/08 ,  C07C237/10 ,  C07C237/12 ,  C07C271/22 ,  C07D209/20 ,  C07D233/64 ,  C07D277/62 ,  C07D277/82

摘要： Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

摘要翻译： 公开了抑制β-淀粉样蛋白肽释放和/或其合成的化合物，因此具有治疗阿尔茨海默病的效用。 还公开了包含抑制β-淀粉样蛋白肽释放和/或其合成的化合物的药物组合物以及用这种药物组合物预防性和治疗性地治疗阿尔茨海默病的方法。