公开(公告)号：EP0736534A1

公开(公告)日：1996-10-09

申请号：EP96107729.4

申请日：1994-12-09

申请人： EGIS GYOGYSZERGYAR RT.

发明人： Szántay, Csaba, Dr. ,  Balogh née kardos, Zsuzsanna, Dr. ,  Moldvai, István, Dr. ,  Temesvári née Major, Eszter, Dr. ,  Szántay Jr., Csaba, Dr. ,  Mándi, Attila, Dr. ,  Blask , Gábor, Dr. ,  Simig, Gyula, Dr. ,  lax, Györgyi, Dr. ,  Drabant, Sándor, Dr. ,  Szállási, Tamás, Dr. ,  Fekete, Márton, Dr. ,  Gigler, Gábor

IPC分类号： C07D487/08 ,  A61K31/44

CPC分类号： C07D487/08

摘要： The subject-matter of the invention is a process for preparing racemic or optically active epibatidine of formula
which comprises cyclising a 1-[diacylamino]-2-[6'-chloro)-pyrid-3'-yl]-4-[amino]-cyclohexane of general formula
wherein

Ac stands for an acyl group.

The advantage of the process is that readily available starting materials are used and the procedure is suitable for industrial scale productions, too.

摘要翻译： 本发明的主题是制备式（CHEM）的外消旋或光学活性的表阿巴定的方法，该方法包括使1-偕二酰基氨基-2-Ä6'-氯） - 吡啶-3'-基-4'-氨基环己烷 通式其中Ac代表酰基。 该方法的优点是使用容易获得的原料，并且该方法也适用于工业规模生产。

公开(公告)号：EP0751137A1

公开(公告)日：1997-01-02

申请号：EP96110220.9

申请日：1996-06-25

申请人： EGIS GYOGYSZERGYAR RT.

发明人： Szántay, Csaba, Dr. ,  Novák, Lajos, Dr. ,  Kovács, Péter ,  Gado, Klára, Dr. ,  Gigler, Gábor ,  Takács born Julianna Bitai, Gáborné, Dr. ,  Egyed, András, Dr. ,  Bozsing, Dániel, Dr. ,  Pirok, György ,  Szemerédi, Katalin, Dr. ,  Csörgö, Margit, Dr. ,  Drabant, Sándor, Dr. ,  Blasko, Gábor, Dr. ,  Simig, Gyula, Dr. ,  Kovács, Gábor, Dr.

IPC分类号： C07D307/91 ,  A61K31/34 ,  C07D307/93

CPC分类号： C07D307/91 ,  C07D307/93

摘要： A subject-matter of the invention are oxaindene derivatives of general formula
wherein

R 1 represents a C 1-4 -alkyl, C 1-4 -alkoxy or C 3-6 -cycloalkyl group,
R 2 stands for hydrogen or a C 1-4 -alkyl or C 3-6 -cycloalkyl group,
R 3 represents hydrogen or a C 1-4 -alkyl, C 1-4 -alkoxy or benzyloxy group,
X means hydrogen, an aliphatic C 1-4 -acyl or benzoyl or naphthoyl group, optionally substituted by 1 or more nitro or C 1-4 -alkoxy group(s) or a group of formula
in which latter
R 7 stands for a C 1-4 -alkylene group
   and
R 5 and R 6 each represents a C 1-4 -alkyl group
   or
R 5 and R 6 together with the nitrogen atom to which they are attached form a piperidyl or morpholinyl group,
A and B together form an ethylene or a vinylene group
   and
n is 1, 2 or 3,
and their stereoisomers and their mixtures as well as acid addition salts of these compounds.
Moreover there are provided for a process for preparing these compounds, medicaments containing them and the use of these compounds.
They have a strong 5-lipoxygenase enzyme inhibiting activity.

摘要翻译： 本发明的主题是通式 worin R1 darstellt一个C 1-4烷基的oxaindene衍生物，C 1-4烷氧基或C 3-6环烷基，R2代表氢或C 1-4烷基 或C 3-6 - 环烷基，R 3 darstellt氢或C 1-4 - 烷基，C 1-4 - 烷氧基或苄氧基，X表示氢在脂肪族C 1-4酰基或苯甲酰基或萘基，任选被1或取代 多个硝基或C 1-4烷氧基（一个或多个）或下式基团的在后一种R7代表一个C 1-4的亚烷基基团和R 5和R 6各自darstellt C 1-4烷基或R5和R6 一起与氮原子到它们所连接形成哌啶基或吗啉基，A和B一起形成亚乙基或亚乙烯基的和n是1，2或3，和其立体异构体和它们的混合物以及将酸加成盐 合成化合物。 更上方设置有用于制备合成的化合物，药物含有它们和使用合成的化合物的方法。 他们有强烈的5-脂氧合酶抑制活性。