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1. 发明授权

US5670511A Indolepiperidine derivatives 失效
标题翻译：吲哚哌啶衍生物
公开(公告)号：US5670511A
公开(公告)日：1997-09-23
申请号：US586273
申请日：1996-01-16
申请人： Joachim Marz , Hartmut Greiner , Christoph Seyfried , Gerd Bartoszyk
发明人： Joachim Marz , Hartmut Greiner , Christoph Seyfried , Gerd Bartoszyk
IPC分类号： C07D401/12 , A61K31/4427 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/53 , A61K31/535 , A61K31/54 , A61K31/635 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , A61P43/00 , C07D401/04 , C07D401/14 , C07D417/12 , C07D471/04 , C07D471/16 , C07D498/16 , C07D513/16 , C07D513/04 , A61K31/395
CPC分类号： C07D401/04 , C07D401/14
摘要： Indolepiperidine derivatives of the formula I ##STR1## and their physiologically acceptable salts exhibit action on the central nervous system, in particular dopamine-agonistic or dopamine-antagonistic action.
摘要翻译：式I的吲哚哌啶衍生物及其生理上可接受的盐表现出对中枢神经系统的作用，特别是多巴胺激动剂或多巴胺拮抗作用。

2. 发明授权

US5324786A Process for preparation of a solid phase system 失效
标题翻译：制备固相体系的方法
公开(公告)号：US5324786A
公开(公告)日：1994-06-28
申请号：US695424
申请日：1991-05-03
申请人： Horst Kunz , Winfried Kosch , Joachim Marz
发明人： Horst Kunz , Winfried Kosch , Joachim Marz
IPC分类号： C07C271/22 , C07K1/04 , C08F257/02
CPC分类号： C07C271/22 , C07K1/042
摘要： The invention provides a method for the production of a solid phase system of the formula F--(--R.sup.3 --Y--CO--CR.sup.2 .dbd.CR.sup.1 --CH.sub.2 --X).sub.m using new allyl esters of the formula:X--CH.sub.2 --CR.sup.1 .dbd.CR.sup.2 --CO--Y--R.sup.3 --A (I).R.sup.1 and R.sup.2 are hydrogen, halogen, alkyl or aryl, R.sup.3 is a spacer, X is acyloxy where acyl is the residue of an aliphatic carboxylic acid or is RCO-- in which R is an organic group. Y is oxygen or sulphur or an --NH-- group and A is a grouping which can react with a solid carrier material F, which contains functional groups B. A and B are groups which react with one another with condensation and/or addition and formation of a linkage between the solid carrier material and X--CH.sub.2 --CR.sup.1 .dbd.CR.sup.2 --CO--Y--R.sup.3 --.
摘要翻译：本发明提供了使用新的下式的烯丙基酯制备式F - （ - R3-Y-CO-CR2 = CR1-CH2-X）m的固相体系的方法：X-CH2-CR1 = CR2 -CO-Y-R 3 -A（I）。 R 1和R 2是氢，卤素，烷基或芳基，R 3是间隔基，X是酰氧基，其中酰基是脂族羧酸的残基或是RCO-，其中R是有机基团。 Y是氧或硫或-NH-基团，A是可以与含有官能团B的固体载体材料F反应的基团.A和B是在缩合和/或添加和形成时彼此反应的基团固体载体材料与X-CH2-CR1 = CR2-CO-Y-R3-之间的连接。

3. 发明授权

US5214195A Allyl esters and the use thereof for the build-up of solid phase systems for solid phase reactions 失效
标题翻译：所有产品及其固体相系统建立用于固相反应的用途
公开(公告)号：US5214195A
公开(公告)日：1993-05-25
申请号：US576366
申请日：1990-08-31
申请人： Horst Kung , Winfried Kosch , Joachim Marz
发明人： Horst Kung , Winfried Kosch , Joachim Marz
IPC分类号： C07C271/22 , C07K1/04
CPC分类号： C07C271/22 , C07K1/042
摘要： The present invention provides new allyl esters of the general formula:X--CH.sub.2 --CR.sup.1 .dbd.CR.sup.2 --CO--Y--R.sup.3 --A (I)wherein R.sup.1 and R.sup.2, which can be the same or different, are hydrn or halogen atoms or alkyl or aryl radicals, R.sup.3 is a linking grouping (spacer), X is an acyloxy radical in which acyl in the acyloxy radical is the residue of an aliphatic carboxylic acid or is the radical RCO-- in which R is an organic radical, Y is an oxygen or sulphur atom or especially an --NH-- group and A is a grouping which can react with a solid carrier material F, which contains appropriate functional groups B, either after selective deblocking or directly, whereby A and B are atom groupings which react with one another with condensation and/or addition and formation of a linkage between the solid carrier material and the radical X--CH.sub.2 --CR.sup.1 .dbd.CR.sup.2 --CO--Y--R.sup.3 --.The present invention also provides processes for the preparation of these new allyl esters. The present invention is also concerned with the use of these new allyl esters for the build-up of solid phase systems, as well as with a process for the preparation of such solid phase systems.
摘要翻译：本发明提供新的具有以下通式的烯丙基酯：X-CH 2 -CR 1 = CR 2 -CO-Y-R 3 -A（I）其中R 1和R 2可相同或不同，为氢或卤素原子或烷基或芳基，R 3是连接基（间隔基），X是酰氧基，其中酰氧基中的酰基是脂族羧酸的残基或是其中R是有机基团的基团RCO-，Y是氧或硫原子，特别是-NH-基团，A是可以在选择性解封后或直接与包含适当的官能团B的固体载体材料F反应的基团，由此A和B是与在固体载体材料和基团X-CH2-CR1 = CR2-CO-Y-R3-之间形成连接，并进行缩合和/或添加。本发明还提供了制备这些新的烯丙基酯的方法。本发明还涉及这些新的烯丙基酯用于固相体系的建立以及制备这种固相体系的方法。

4. 发明授权

US5693655A 3-indolylpiperidines 失效
标题翻译： 3-吲哚基哌啶
公开(公告)号：US5693655A
公开(公告)日：1997-12-02
申请号：US426405
申请日：1995-04-21
申请人： Henning Bottcher , Joachim Marz , Christoph Seyfried , Hartmut Greiner , Gerd Bartoszyk
发明人： Henning Bottcher , Joachim Marz , Christoph Seyfried , Hartmut Greiner , Gerd Bartoszyk
IPC分类号： A61K31/4427 , A61K31/445 , A61K31/454 , A61P9/10 , A61P9/12 , A61P25/04 , A61P25/20 , A61P25/24 , A61P43/00 , C07D209/14 , C07D211/14 , C07D401/14 , C07D491/04 , C07D491/056
CPC分类号： C07D401/14 , C07D491/04
摘要： 3-Indolylpiperidines of the formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are in each case independently of one another H, A, OH, OA, F, Cl, Br, Z, CN, CF.sub.3, COOH, CONH.sub.2, CONHA, CONA.sub.2, or COOA, or R.sup.1 and R.sup.2 and also R.sup.3 and R.sup.4 in each case together are also methylenedioxy, R.sup.5 is H or OH, R.sup.6 is H or R.sup.5 and R.sup.6 together are also a bond, A is alkyl having 1 to 6 C atoms and n is 2, 3, 4, 5 or 6, and to their physiologically acceptable salts, exhibit action on the central nervous system, in particular dopamine-agonistic or dopamine-antagonistic action.
摘要翻译：式I的3-吲哚基哌啶其中R 1，R 2，R 3和R 4各自独立地为H，A，OH，OA，F，Cl，Br，Z，CN，CF 3，COOH，CONH 2 ，CONHA，CONA2或COOA，或者R 1和R 2以及R 3和R 4在一起也是亚甲二氧基，R 5是H或OH，R 6是H或R 5，R 6一起也是键，A是具有1至 6个C原子，n为2,3,4,5或6及其生理上可接受的盐，对中枢神经系统，特别是多巴胺激动剂或多巴胺拮抗作用表现出作用。

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