公开(公告)号：EP0619299A3

公开(公告)日：1996-03-06

申请号：EP94105517.0

申请日：1994-04-11

申请人： EGIS GYOGYSZERGYAR RT.

发明人： Bajnogel, Judit, Dr. ,  Blasko, Gábor, Dr. ,  Budai, Zoltán, Dr. ,  Schmidt, Eva ,  Egyed, András, Dr. ,  Fekete, Márton, Dr. ,  Gacsályi, István ,  Gyertyán, István, Dr. ,  Mezei, Tibor, Dr. ,  Reiter, Klára, Dr. born Esses ,  Simig, Gyula, Dr. ,  Szemerédi, Katalin, Dr. ,  Szirt, Enikö, born Kiszelly

IPC分类号： C07C251/58 ,  C07D295/12 ,  A61K31/15 ,  A61K31/445 ,  A61K31/495

CPC分类号： C07D207/08 ,  C07C251/58 ,  C07C2601/02 ,  C07C2601/14 ,  C07D295/088

摘要： A subject-matter of the invention are 1-(Phenyl)-3-[ω-(amino)-alkoxyimino]-alk-1-ene derivatives of general formula

wherein
R₁ and R₂ independently each stands for hydrogen, halogen or a C₁₋₄ alkoxy group or together represent a 3,4-methylenedioxy group, R stands for C₁₋₈ alkyl, R₃ represents hydrogen, C₁₋₄ alkyl or hydroxy, R₄ and R₅ independently each represents hydrogen, a C₁₋₁₂ alkyl group, optionally substituted by hydroxy, or a C₂₋₁₂ alkenyl or C₃₋₆ cycloalkyl group,
óóóor R₄ and R₅ together with the nitrogen atom to which they are attached form a 4- to 7-membered heterocyclic ring, optionally comprising an oxygen, sulfur or a further nitrogen atom, which latter optionally may carry a phenyl, benzyl or C₁₋₄ alkyl substituent
óóóand A represents a valency bond or a -CH₂-group, as well as stereo and optically active isomers and their mixtures, acid-addition salts and quaternary ammonium derivatives thereof. Furthermore the invention is concerned with a process for preparing these compounds as well as medicaments containing them and the use of them for preparing medicaments, particularly having ulcus and gastric-acid-secretion inhibiting and anxiolytic effects.

公开(公告)号：EP0619299A2

公开(公告)日：1994-10-12

申请号：EP94105517.0

申请日：1994-04-11

申请人： EGIS GYOGYSZERGYAR RT.

发明人： Bajnogel, Judit, Dr. ,  Blasko, Gábor, Dr. ,  Budai, Zoltán, Dr. ,  Schmidt, Eva ,  Egyed, András, Dr. ,  Fekete, Márton, Dr. ,  Gacsályi, István ,  Gyertyán, István, Dr. ,  Mezei, Tibor, Dr. ,  Reiter, Klára, Dr. born Esses ,  Simig, Gyula, Dr. ,  Szemerédi, Katalin, Dr. ,  Szirt, Enikö, born Kiszelly

IPC分类号： C07C251/58 ,  C07D295/12 ,  A61K31/15 ,  A61K31/445 ,  A61K31/495

CPC分类号： C07D207/08 ,  C07C251/58 ,  C07C2601/02 ,  C07C2601/14 ,  C07D295/088

摘要： A subject-matter of the invention are 1-(Phenyl)-3-[ω-(amino)-alkoxyimino]-alk-1-ene derivatives of general formula

wherein

R₁ and R₂ independently each stands for hydrogen, halogen or a C₁₋₄ alkoxy group or together represent a 3,4-methylenedioxy group,
R stands for C₁₋₈ alkyl,
R₃ represents hydrogen, C₁₋₄ alkyl or hydroxy,
R₄ and R₅ independently each represents hydrogen, a C₁₋₁₂ alkyl group, optionally substituted by hydroxy, or a C₂₋₁₂ alkenyl or C₃₋₆ cycloalkyl group,
óóóor
R₄ and R₅ together with the nitrogen atom to which they are attached form a 4- to 7-membered heterocyclic ring, optionally comprising an oxygen, sulfur or a further nitrogen atom, which latter optionally may carry a phenyl, benzyl or C₁₋₄ alkyl substituent
óóóand
A represents a valency bond or a -CH₂-group,
as well as stereo and optically active isomers and their mixtures, acid-addition salts and quaternary ammonium derivatives thereof.
Furthermore the invention is concerned with a process for preparing these compounds as well as medicaments containing them and the use of them for preparing medicaments, particularly having ulcus and gastric-acid-secretion inhibiting and anxiolytic effects.

摘要翻译： 本发明的主题是1-（苯基）-3- [Ω - （氨基）烷氧基亚氨基]通式 worin R1和R2的链-1-烯衍生物unabhängig各自表示氢，卤素或 C1-4烷氧基或一起代表3,4-亚甲二氧基，R代表C1-8烷基，R3 darstellt氢，C 1-4烷基或羟基，R4和R5各自独立地darstellt氢，C 1-12烷基 ，任选被羟基substituiertem，或C 2-12烯基或C 3-6环烷基，或R4和R5一起与氮原子到它们所连接形成4-至7-元杂环，其任选地包含氧，硫的 或氮原子。此外，后一种可任选地携带一个苯基，苄基或C 1-4烷基取代基，A表示一个价键或-CH 2基团，以及立体声和旋光异构体和它们的混合物，酸加成盐 它们的和季铵衍生物。 进一步，本发明涉及有用于制备合成化合物以及含有它们的药物和用于制备药物的用途其中，特别是具有ulcus和胃酸分泌抑制作用和抗焦虑作用的方法。

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。