公开(公告)号：EP0468825B1

公开(公告)日：1997-01-08

申请号：EP91306934.0

申请日：1991-07-29

申请人： Richter Gedeon Vegyészeti Gyár R.T.

发明人： Farkas, Sàndor ,  Földeák, Sándor ,  Kárpáti, Egon ,  Hegyes, Péter ,  Kreidl, János ,  Szporny, Lászlo ,  Czibula, László ,  Petofi Vassné, Szilvia

IPC分类号： C07F7/08 ,  A61K31/695

CPC分类号： C07F7/0812 ,  C07F7/0818

公开(公告)号：EP0472304A3

公开(公告)日：1992-04-22

申请号：EP91306935.7

申请日：1991-07-29

申请人： Richter Gedeon Vegyészeti Gyár R.T.

发明人： Farkas, Sándor ,  Földeák, Sándor ,  Kárpáti, Egon ,  Hegyes, Péter ,  Kreidl, János ,  Szporny, László ,  Czibula, László ,  Vassné Petofi, Szilvia

IPC分类号： A61K31/695

CPC分类号： A61K31/695

摘要： The invention relates to pharmaceutical compositions containing an active ingredient at least one known organosilane derviative of formula (I),
wherein
R 1 represents a hydrogen or halogen atom ; A represents oxygen or =CH 2 or NR group, wherein R represents a hydrogen atom or a C 1-4 alkyl group ; m is 1, 2 or 3; and n is 1 or 2,
or a pharmaceutically acceptable salt thereof in admixture with one or more pharmaceutically acceptable carriers, excipients and/or diluents. The compositions of the invention possess muscle relaxant and antiparkinsonic effects, thus, they can be used for the treatment or prevention of diseases and conditions accompanied by hyperreflexia of the central nervous system and/or an increase of the muscular tone as well as nervous system injuries, degenerative nervous system disoders, sclerosis multiplex, myelopathies, rachicele, articular pains and Parkinson's disease in mammals including man.

摘要翻译： 本发明涉及含有活性成分至少一种式（I）的已知有机硅烷衍生物的药物组合物，其中R 1表示氢或卤原子; A表示氧或= CH 2或NR基，其中R表示氢原子或C 1-4烷基; m为1,2或3; 和n为1或2，或其药学上可接受的盐与一种或多种药学上可接受的载体，赋形剂和/或稀释剂混合。 本发明的组合物具有肌肉松弛剂和抗帕金森病作用，因此可用于治疗或预防伴有中枢神经系统反射亢进的疾病和病症和/或肌肉紧张度增加以及神经系统损伤 ，退行性神经系统解剖器，硬化症多发性，脊髓病，球形，关节痛和包括人在内的哺乳动物的帕金森病。

公开(公告)号：EP0472304A2

公开(公告)日：1992-02-26

申请号：EP91306935.7

申请日：1991-07-29

申请人： Richter Gedeon Vegyészeti Gyár R.T.

发明人： Farkas, Sándor ,  Földeák, Sándor ,  Kárpáti, Egon ,  Hegyes, Péter ,  Kreidl, János ,  Szporny, László ,  Czibula, László ,  Vassné Petofi, Szilvia

IPC分类号： A61K31/695

CPC分类号： A61K31/695

摘要： The invention relates to pharmaceutical compositions containing an active ingredient at least one known organosilane derviative of formula (I),
wherein

R 1 represents a hydrogen or halogen atom ;
A represents oxygen or =CH 2 or NR group, wherein R represents a hydrogen atom or a C 1-4 alkyl group ;
m is 1, 2 or 3; and
n is 1 or 2,

or a pharmaceutically acceptable salt thereof in admixture with one or more pharmaceutically acceptable carriers, excipients and/or diluents.
The compositions of the invention possess muscle relaxant and antiparkinsonic effects, thus, they can be used for the treatment or prevention of diseases and conditions accompanied by hyperreflexia of the central nervous system and/or an increase of the muscular tone as well as nervous system injuries, degenerative nervous system disoders, sclerosis multiplex, myelopathies, rachicele, articular pains and Parkinson's disease in mammals including man.

摘要翻译： 本发明涉及含有活性成分的式（I）中的至少一个已知的有机硅烷derviative worin R1 darstellt一个氢或卤原子的药物组合物; 甲darstellt氧或= CH 2或NR基团，worinřdarstellt氢原子或C 1-4烷基; m为1，2或3; 且n是1或2，或与一种或多种药学上可接受的载体，赋形剂和/或稀释剂混合的药学上可接受的盐。 本发明的组合物具有肌肉松弛和antiparkinsonic的影响，因此，它们可以用于伴有中枢神经系统和/或增加肌张力的以及神经系统损伤的反射亢进的治疗或预防的疾病和症状 ，退行性神经系统disoders，多重硬化，脊髓病，rachicele，关节痛和帕金森氏病的哺乳动物，包括你。

公开(公告)号：EP0468825A1

公开(公告)日：1992-01-29

申请号：EP91306934.0

申请日：1991-07-29

申请人： Richter Gedeon Vegyészeti Gyár R.T.

发明人： Farkas, Sàndor ,  Földeák, Sándor ,  Kárpáti, Egon ,  Hegyes, Péter ,  Kreidl, János ,  Szporny, Lászlo ,  Czibula, László ,  Petofi Vassné, Szilvia

IPC分类号： C07F7/08 ,  A61K31/695

CPC分类号： C07F7/0812 ,  C07F7/0818

摘要： The invention relates to novel organosilanes of the formula (I)

wherein
m is 1, 2 or 3;
R¹ and/or R² represents hydrogen, a straight or branched C₁₋₄alkyl, C₁₋₄alkoxy, C₅₋₇cycloalkyl group or halogen;
B represents a 5- or 6-membered saturated or unsaturated heterocyclic group which contains one or more nitrogen atoms and optionally an additional oxygen or sulfur atom or -NH or -NR group, wherein R represents a C₁₋₅alkyl or (C₁₋₅ alkyl)carbonyl group, said heterocyclic group being bound through a nitrogen atom to the (CH₂) m group and optionally substituted by a C₁₋₄alkyl or (C₁₋₄alkoxy)carbonyl group;
and acid addition salts thereof.
The compounds of the formula (I) show a strong muscle relaxant effect and antiparkinsonic properties; thus, they are useful for the treatment of Parkinson's disease, spastic, rigid muscular hypertonicity, stroke, nervous system laesions, sclerosis multiplex, myelopathies, rachicele or particular pains.
A process for the preparation of compound of formula (I) and pharmaceutical compositions containing them are also described.

摘要翻译： 本发明涉及式（I） worin m为1，2或3的有机硅烷新颖; [R <1>和/或R <2> darstellt氢，直链或支链C 1-4烷基，C 1-4烷氧基，C 5-7环烷​​基或卤素; 乙darstellt的5-或6-元饱和或含有一个或多个氮原子和任选的（一个额外的氧或硫原子或-NH或-NR基的不饱和杂环基，worinřdarstellt一个C 1-5烷基或C 1-5烷基 ）羰基，所述杂环基为通过氮原子成由C 1-4烷基或（C 1-4烷氧基）羰基的（CH 2）M组和任选substituiertem约束; 和酸加成盐。 式（I）表现出很强的肌肉松弛效果和antiparkinsonic性质的化合物; 因此，他们是帕金森氏病，痉挛，肌肉僵化高渗，中风，神经系统病变的治疗，多重硬化，脊髓病，rachicele或特别痛苦。 一种用于式（I）和含有它们的药物组合物的化合物的制备方法，如此所述。