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1. 发明申请

US20060293313A1 New phenylpiperazines 有权
标题翻译：新的苯基哌嗪
公开(公告)号：US20060293313A1
公开(公告)日：2006-12-28
申请号：US11450323
申请日：2006-06-12
申请人： Roelof Hes , Johannes Van der Heijden , Cornelis Kruse , Tipker Jacobus , Martinus Tulp , Gerben Visser , Bernard Van Vliet
发明人： Roelof Hes , Johannes Van der Heijden , Cornelis Kruse , Tipker Jacobus , Martinus Tulp , Gerben Visser , Bernard Van Vliet
IPC分类号： A61K31/5415 , A61K31/538 , A61K31/496 , C07D417/14 , C07D413/14 , C07D405/14 , C07D403/14
CPC分类号： C07D401/12 , C07D209/34 , C07D209/40 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances in the dopaminergic and/or the serotonergic systems such as anxiety disorders, depression, Parkinson's disease, and schizophrenia. The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein: X is a group of formula 1, 2, 3, 4, 5, 6, or 7 as defined in the text, m has the value 2 to 6; n has the value 0-2; R5 and R6 are independently H or alkyl (1-3C); or R5+R6 represent a group —(CH2)—p wherein p has the value 3-5, and R7 is alkyl (1-3C), alkoxy (1-3C), halogen or cyano; or R6+R7 (R7 at position 7 of the indole group) represent a group —(CH2)q wherein q has the value 2-4, and salts thereof.
摘要翻译：本发明涉及具有令人感兴趣的药理学性质的新一组苯基哌嗪，例如对多巴胺D 2 O受体和/或5-羟色胺再摄取位点的高亲和力，以及治疗与多巴胺能和/或血清素能系统如焦虑障碍，抑郁症，帕金森病和精神分裂症。本发明涉及一组新的式（I）的苯基哌嗪衍生物：其中：X是本文定义的式1,2,3,4,5,6或7的基团，m的值为2 至6; n的值为0-2; R 5和R 6独立地是H或烷基（1-3C）; 或R 5 + R 6表示基团 - （CH 2）2 - ，其中p的值为3 -5和R 7是烷基（1-3C），烷氧基（1-3C），卤素或氰基; 或吲哚基的第7位上的R 6（R 7）表示 - （CH 2）2 - 其中q具有2-4，及其盐。

2. 发明申请

US20060122206A1 Tetrahydropyridin-4-yl indoles with a combination of affinity for dopamine-D2 receptors and serotonin reuptake sites 有权
标题翻译：具有对多巴胺-D2受体和5-羟色胺再摄取位点的亲和力的组合的四氢吡啶-4-基吲哚
公开(公告)号：US20060122206A1
公开(公告)日：2006-06-08
申请号：US11294657
申请日：2005-12-06
申请人： Roelof Hes , Pieter Smid , Cornelis Kruse , Martinus Tulp
发明人： Roelof Hes , Pieter Smid , Cornelis Kruse , Martinus Tulp
IPC分类号： A61K31/513 , C07D403/14
CPC分类号： C07D401/14
摘要： The present invention relates to a group of novel tetrahydropyridin-4-yl indoles with a dual mode of action: serotonin reuptake inhibition and affinity for dopamine-D2 receptors, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said tetrahydropyridin-4-yl indoles. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The invention relates to novel tetrahydropyridin-4-yl indoles of the formula. and tautomers, stereoisomers, prodrugs, N-oxides, pharmacologically acceptable salts, hydrates and solvates thereof, wherein: R1 is hydrogen, halogen, alkyl(C1-3) or alkoxy(C1-3), CN or CF3, R2 is hydrogen or alkyl(C1-3), R3 is hydrogen or alkyl(C1-3), Z is hydrogen or alkyl(C1-3), alkoxy(C1-3) or alkylthio(C1-3), A is hydrogen or alkyl(C1-3), or A and Z together form a saturated or (partly) unsaturated 5- or 6-membered ring which may be substituted with halogen, alkyl (C1-3) or phenyl, in which ring Z represents carbon, sulfur of nitrogen.
摘要翻译：本发明涉及一组具有双重作用方式的新的四氢吡啶-4-基吲哚：5-羟色胺再摄取抑制和对多巴胺-D 2受体的亲和性，制备这些化合物的方法和涉及可用于合成所述四氢吡啶-4-基吲哚的新型中间体。本发明还涉及本文公开的化合物在制备产生有益效果的药物中的用途。本发明涉及下式的新的四氢吡啶-4-基吲哚。和其互变异构体，立体异构体，前药，N-氧化物，其药理学上可接受的盐，水合物和溶剂化物，其中：R 1是氢，卤素，烷基（C 1-3 - 或烷氧基（C 1-3 - ），CN或CF 3 R 2，R 2是氢或烷基（C 1-3 - R 3是氢或烷基（C 1-3），Z是氢或烷基（C 1-3），烷氧基（C 1-3-3）或烷硫基（C 1-3-3），A是氢或烷基（C 1-3-3），或A和Z一起形成饱和或（部分）不饱和的5或6元环，其可被卤素，烷基（C 1-3-3）或苯基取代，其中环Z表示碳，硫氮。

3. 发明申请

US20060122177A1 Phenylpiperazines with a combination of affinity for dopamine-D2 receptors and serotonin reuptake sites 审中-公开
标题翻译：具有与多巴胺-D2受体的亲合力和5-羟色胺再摄取位点的组合的苯基哌嗪
公开(公告)号：US20060122177A1
公开(公告)日：2006-06-08
申请号：US11294611
申请日：2005-12-06
申请人： Roelof Hes , Pieter Smid , Cornelis Kruse , Martinus Tulp
发明人： Roelof Hes , Pieter Smid , Cornelis Kruse , Martinus Tulp
IPC分类号： A61K31/538 , A61K31/496 , C07D413/02 , C07D405/02 , C07D403/02
CPC分类号： C07D263/58 , C07D307/79 , C07D319/18
摘要： The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and affinity for dopamine-D2 receptors and to methods for the preparation of these compounds. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1) wherein the symbols have the meanings given in the specification.
摘要翻译：本发明涉及一组具有双重作用方式的新型苯基哌嗪衍生物：5-羟色胺再摄取抑制和对多巴胺-D2受体的亲和性以及制备这些化合物的方法。本发明还涉及本文公开的化合物在制备产生有益效果的药物中的用途。化合物具有通式（1），其中符号具有说明书中给出的含义。

4. 发明申请

US20060122175A1 Benzdioxane piperazine derivatives with a combination of affinity for dopamine-D2 receptors and serotonin reuptake sites 审中-公开
标题翻译：具有对多巴胺-D2受体的亲合力和5-羟色胺再摄取位点的组合的二恶烷哌嗪衍生物
公开(公告)号：US20060122175A1
公开(公告)日：2006-06-08
申请号：US11294610
申请日：2005-12-06
申请人： Roelof Hes , Pieter Smid , Cornelis Kruse , Martinus Tulp
发明人： Roelof Hes , Pieter Smid , Cornelis Kruse , Martinus Tulp
IPC分类号： A61K31/5415 , A61K31/538 , A61K31/498 , A61K31/496 , C07D417/14 , C07D413/14 , C07D405/14 , C07D403/14
CPC分类号： C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to a group of novel 3-(2-piperidin-4-yl-ethyl)-1H-indole derivatives with a dual mode of action: serotonin reuptake inhibition and affinity for dopamine-D2 receptors and to methods for the preparation of these compounds. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1) wherein the symbols have the meanings given in the specification.
摘要翻译：本发明涉及一种具有双重作用方式的新型3-（2-哌啶-4-基 - 乙基）-1H-吲哚衍生物：5-羟色胺再摄取抑制和对多巴胺-D2- / >受体和制备这些化合物的方法。本发明还涉及本文公开的化合物在制备产生有益效果的药物中的用途。化合物具有通式（1），其中符号具有说明书中给出的含义。

5. 发明申请

US20060089366A1 New piperazine and piperidine compounds 有权
标题翻译：新的哌嗪和哌啶化合物
公开(公告)号：US20060089366A1
公开(公告)日：2006-04-27
申请号：US11129465
申请日：2005-05-16
申请人： Roelof Feenstra , Johannes van der Heijden , Cornelis Kruse , Stephen Long , Gustaaf van Scharrenburg
发明人： Roelof Feenstra , Johannes van der Heijden , Cornelis Kruse , Stephen Long , Gustaaf van Scharrenburg
IPC分类号： A61K31/496 , A61K31/454 , C07D413/02 , C07D417/02
CPC分类号： C07D263/58 , C07D413/12
摘要： The invention relates to a group of novel piperazine and piperidine derivatives of the formula wherein Y is hydrogen, halogen, alkyl (1-3C), or CN, CF3, OCF3, SCF3, alkoxy(1-3C), amino or mono- or dialkyl(1-3C) substituted amino or hydroxy, X is O, S, SO or SO2, ---Z represents -C, =C or -N, R1 and R2 independently represent hydrogen or alkyl (1-3C), Q is benzyl or 2-, 3- or 4-pyridylmethyl, wich groups may be substited with one or more more substituents from the group halogen, nitro, cyano, amino, mono- or di (1-3C)alkylamino, (1-3C) alkoxy, CF3, OCF3, SCF3, (1-4C)-alkyl, (1-3C)alkylsulfonyl or hydroxy, and salts and prodrugs thereof. It has been found that these compounds have interesting pharmacological properties due to a combination of (partial) agonism towards the members of the dopamine D2-receptor subfamily and affinity for relevant serotonin and/or noradrenergic receptors.
摘要翻译：本发明涉及下式的一组新的哌嗪和哌啶衍生物其中Y是氢，卤素，烷基（1-3C）或CN，CF 3，OCF 3， >，SCF 3，烷氧基（1-3C），氨基或单或二烷基（1-3C）取代的氨基或羟基，X是O，S，SO或SO 2， Z代表-C，= C或-N，R 1和R 2独立地代表氢或烷基（1-3C），Q是苄基或2-，3-或4-吡啶基甲基，其可以被一个或多个取代基取代为卤素，硝基，氰基，氨基，单或二（1-3C）烷基氨基，（1-3C）烷氧基，CF 3 3，OCF 3，SCF 3，（1-4C） - 烷基，（1-3C）烷基磺酰基或羟基，和盐及其前体药物。已经发现，这些化合物由于（多）向多巴胺D 2受体亚家族的成员的组合以及对相关的5-羟色胺和/或去甲肾上腺素能受体的亲和力而具有令人感兴趣的药理学性质。

6. 发明申请

US20060247256A1 Phenylpiperazine derivatives with a combination of partial dopamine-D2 receptor agonism and serotonin reuptake inhibition 审中-公开
标题翻译：具有部分多巴胺-D2受体激动剂和5-羟色胺再摄取抑制组合的苯基哌嗪衍生物
公开(公告)号：US20060247256A1
公开(公告)日：2006-11-02
申请号：US11294615
申请日：2005-12-06
申请人： Roelof Feenstra , Axel Stoit , Jan-Willem Terpstra , Maria Pras-Raves , Andrew McCreary , Bernard Van Vliet , Mayke Hesselink , Cornelis Kruse , Gustaaf Van Scharrenburg
发明人： Roelof Feenstra , Axel Stoit , Jan-Willem Terpstra , Maria Pras-Raves , Andrew McCreary , Bernard Van Vliet , Mayke Hesselink , Cornelis Kruse , Gustaaf Van Scharrenburg
IPC分类号： A61K31/496 , C07D413/14
CPC分类号： C07D413/12
摘要： The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine-D2 receptors. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1): wherein the symbols have the meanings given in the specification.
摘要翻译：本发明涉及一组具有双重作用方式的新型苯基哌嗪衍生物：5-羟色胺再摄取抑制和对多巴胺-D 2受体的部分激动作用。本发明还涉及本文公开的化合物在制备产生有益效果的药物中的用途。化合物具有通式（1）：其中符号具有说明书中给出的含义。

7. 发明申请

US20060122190A1 Phenylpiperazine derivatives with a combination of partial dopamine-D2 receptor agonism and serotonin reuptake inhibition 有权
标题翻译：具有部分多巴胺-D2受体激动剂和5-羟色胺再摄取抑制组合的苯基哌嗪衍生物
公开(公告)号：US20060122190A1
公开(公告)日：2006-06-08
申请号：US11294603
申请日：2005-12-06
申请人： Roelof Feenstra , Axel Stoit , Jan-Willem Terpstra , Maria Pras-Raves , Andrew McCreary , Bernard Van Vliet , Mayke Hesselink , Cornelis Kruse , Gustaaf Van Scharrenburg
发明人： Roelof Feenstra , Axel Stoit , Jan-Willem Terpstra , Maria Pras-Raves , Andrew McCreary , Bernard Van Vliet , Mayke Hesselink , Cornelis Kruse , Gustaaf Van Scharrenburg
IPC分类号： A61K31/496 , C07D413/02
CPC分类号： C07D263/58 , C07D413/12
摘要： The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine-D2 receptors. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1): wherein the symbols have the meanings given in the specification, and tautomers, stereoisomers and N-oxides thereof, as well as pharmacologically acceptable salts, hydrates and solvates of said compounds of formula (1) and its tautomers, stereoisomers and N-oxides.
摘要翻译：本发明涉及一组具有双重作用方式的新型苯基哌嗪衍生物：5-羟色胺再摄取抑制和对多巴胺-D 2受体的部分激动作用。本发明还涉及本文公开的化合物在制备产生有益效果的药物中的用途。所述化合物具有通式（1）：其中符号具有说明书中给出的含义及其互变异构体，立体异构体和N-氧化物，以及所述式（1）化合物的药理学上可接受的盐，水合物和溶剂化物，其互变异构体，立体异构体和N-氧化物。

8. 发明申请

US20070142397A2 PHENYPIPERAZINE DERIVATIVES WITH A COMBINATION OF PARTIAL DOPAMINE-D2 RECEPTOR AGONISM AND SEROTONIN REUPTAKE INHIBITION 审中-公开
标题翻译：具有局部多巴胺-D2受体激动剂和丝氨酸蛋白酶抑制剂组合的苯并吡啶衍生物
公开(公告)号：US20070142397A2
公开(公告)日：2007-06-21
申请号：US11294615
申请日：2005-12-06
申请人： Roelof Feenstra , Axel Stoit , Jan-Willem Terpstra , Maria Pras-Raves , Andrew McCreary , Bernard Van Vliet , Mayke Hesselink , Cornelis Kruse , Gustaaf Van Scharrenburg
发明人： Roelof Feenstra , Axel Stoit , Jan-Willem Terpstra , Maria Pras-Raves , Andrew McCreary , Bernard Van Vliet , Mayke Hesselink , Cornelis Kruse , Gustaaf Van Scharrenburg
IPC分类号： A61K31/496 , C07D413/14
CPC分类号： C07D413/12
摘要： The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine-D2 receptors. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1): wherein the symbols have the meanings given in the specification.
摘要翻译：本发明涉及一组具有双重作用方式的新型苯基哌嗪衍生物：5-羟色胺再摄取抑制和对多巴胺-D 2受体的部分激动作用。本发明还涉及本文公开的化合物在制备产生有益效果的药物中的用途。化合物具有通式（1）：其中符号具有说明书中给出的含义。

9. 发明申请

US20060122189A1 Phenylpiperazine derivatives with a combination of partial dopamine-D2 receptor agonism and serotonin reuptake inhibition 审中-公开
标题翻译：具有部分多巴胺-D2受体激动剂和5-羟色胺再摄取抑制组合的苯基哌嗪衍生物
公开(公告)号：US20060122189A1
公开(公告)日：2006-06-08
申请号：US11294602
申请日：2005-12-06
申请人： Roelof Feenstra , Axel Stoit , Jan-Willem Terpstra , Maria Pras-Raves , Andrew McCreary , Bernard Van Vliet , Mayke Hesselink , Cornelis Kruse , Gustaaf Van Scharrenburg
发明人： Roelof Feenstra , Axel Stoit , Jan-Willem Terpstra , Maria Pras-Raves , Andrew McCreary , Bernard Van Vliet , Mayke Hesselink , Cornelis Kruse , Gustaaf Van Scharrenburg
IPC分类号： A61K31/496 , C07D413/14 , C07D413/02
CPC分类号： C07D263/58 , C07D413/12
摘要： The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine-D2 receptors. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1): wherein the symbols have the meanings given in the specification. and tautomers, stereoisomers and N-oxides thereof, as well as pharmacologically acceptable salts, hydrates and solvates of said compounds of formula (1) and its tautomers, stereoisomers and N-oxides.
摘要翻译：本发明涉及一组具有双重作用方式的新型苯基哌嗪衍生物：5-羟色胺再摄取抑制和对多巴胺-D 2受体的部分激动作用。本发明还涉及本文公开的化合物在制备产生有益效果的药物中的用途。化合物具有通式（1）：其中符号具有说明书中给出的含义。和其互变异构体，立体异构体和N-氧化物，以及所述式（1）化合物及其互变异构体，立体异构体和N-氧化物的药理学上可接受的盐，水合物和溶剂化物。

10. 发明申请

US20070072870A2 PHENYLPIPERAZINE DERIVATIVES WITH A COMBINATION OF PARTIAL DOPAMINE-D2 RECEPTOR AGONISM AND SEROTONIN REUPTAKE INHIBITION 审中-公开
标题翻译：具有部分多巴胺-D2受体激动剂和丝氨酸蛋白酶重复抑制的组合的苯基哌嗪衍生物
公开(公告)号：US20070072870A2
公开(公告)日：2007-03-29
申请号：US11294602
申请日：2005-12-06
申请人： Roelof Feenstra , Axel Stoit , Jan-Willem Terpstra , Maria Pras-Raves , Andrew McCreary , Bernard Van Vliet , Mayke Hesselink , Cornelis Kruse , Gustaaf Van Scharrenburg
发明人： Roelof Feenstra , Axel Stoit , Jan-Willem Terpstra , Maria Pras-Raves , Andrew McCreary , Bernard Van Vliet , Mayke Hesselink , Cornelis Kruse , Gustaaf Van Scharrenburg
IPC分类号： A61K31/496 , C07D413/14 , C07D413/02
CPC分类号： C07D263/58 , C07D413/12
摘要： The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine-D2 receptors. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1): wherein the symbols have the meanings given in the specification. and tautomers, stereoisomers and N-oxides thereof, as well as pharmacologically acceptable salts, hydrates and solvates of said compounds of formula (1) and its tautomers, stereoisomers and N-oxides.
摘要翻译：本发明涉及一组具有双重作用方式的新型苯基哌嗪衍生物：5-羟色胺再摄取抑制和对多巴胺-D 2受体的部分激动作用。本发明还涉及本文公开的化合物在制备产生有益效果的药物中的用途。化合物具有通式（1）：其中符号具有说明书中给出的含义。和其互变异构体，立体异构体和N-氧化物，以及所述式（1）化合物及其互变异构体，立体异构体和N-氧化物的药理学上可接受的盐，水合物和溶剂化物。

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