专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

US20070293506A1 COMBINATION PREPARATIONS COMPRISING BIFEPRUNOX AND A DOPAMINE AGONIST 有权
标题翻译：包含BIFEPRUNOX和DOPAMINE AGONIST的组合制剂
公开(公告)号：US20070293506A1
公开(公告)日：2007-12-20
申请号：US11762239
申请日：2007-06-13
申请人： Andrew McCREARY , Gustaaf Van Scharrenburg , Martinus Tulp
发明人： Andrew McCREARY , Gustaaf Van Scharrenburg , Martinus Tulp
IPC分类号： A61K31/496 , A61K31/198 , A61K31/137
CPC分类号： A61K31/137 , A61K31/198 , A61K31/496 , A61K2300/00
摘要： The present invention relates to a composition containing bifeprunox or its N-oxide, or at least one pharmacologically acceptable salt thereof: and L-DOPA or at least one pharmacologically acceptable salt thereof, for simultaneous, separate or sequential use in the treatment of disorders requiring recovery of dopaminergic function, including Parkinson's disease and restless leg syndrome.
摘要翻译：本发明涉及含有双岐杆菌或其N-氧化物或其至少一种药理学可接受的盐的组合物：和L-DOPA或其至少一种药理学上可接受的盐，用于同时，分开或顺序地用于治疗所需疾病恢复多巴胺能功能，包括帕金森病和不宁腿综合征。

2. 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。

3. 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。

4. 发明申请

US20050215567A1 1-[2H-1-benzopyran-2-one-8-yl]-piperazine derivatives for the treatment of pain 审中-公开
标题翻译： 1- [2H-1-苯并吡喃-2-酮-8-基] - 哌嗪衍生物，用于治疗疼痛
公开(公告)号：US20050215567A1
公开(公告)日：2005-09-29
申请号：US11085193
申请日：2005-03-22
申请人： Cornelis Bakker , Jeffrey Glennon , Mayke Hesselink , Claudia Thaete , Andrew McCreary , Gustaaf Van Scharrenburg
发明人： Cornelis Bakker , Jeffrey Glennon , Mayke Hesselink , Claudia Thaete , Andrew McCreary , Gustaaf Van Scharrenburg
IPC分类号： A61K31/496
CPC分类号： A61K31/496
摘要： The invention relates to a novel use of known 1-[2H-1-benzopyran-2-one-8-yl]-piperazine derivatives, broad spectrum 5-HT receptor binding compounds, having amongst other functional serotonin receptor activities, potent 5-HT1A-agonistic as well as 5-HT1D-antagonistic activity. The compounds of the invention are useful for the preparation of medicaments for treating pain. The invention relates to compounds of the general formula (1) wherein the symbols have the meanings as given in the description
摘要翻译：本发明涉及已知的1- [2H-1-苯并吡喃-2-酮-8-基] - 哌嗪衍生物，具有其他功能性5-羟色胺受体活性的广谱5-HT受体结合化合物的新用途， HT 1A - 拮抗剂以及5-HT 1D拮抗活性。本发明的化合物可用于制备用于治疗疼痛的药物。本发明涉及通式（1）的化合物，其中符号具有说明书中给出的含义

5. 发明申请

US20050215551A1 1-[2H-1-benzopyran-2-one-8-yl]- piperazine derivatives for the treatment of movement disorders 审中-公开
标题翻译： 1- [2H-1-苯并吡喃-2-酮-8-基] - 哌嗪衍生物，用于治疗运动障碍
公开(公告)号：US20050215551A1
公开(公告)日：2005-09-29
申请号：US11079089
申请日：2005-03-15
申请人： Cornelis Bakker , Jeffrey Glennon , Mayke Hesselink , Claudia Thaete , Andrew McCreary , Gustaaf Van Scharrenburg
发明人： Cornelis Bakker , Jeffrey Glennon , Mayke Hesselink , Claudia Thaete , Andrew McCreary , Gustaaf Van Scharrenburg
IPC分类号： A61K31/00 , A61K31/496 , A61K31/5377
CPC分类号： A61K31/496 , A61K31/00
摘要： The invention relates to a novel use of known 1-[2H-1-benzopyran-2-one-8-yl]-piperazine derivatives, broad spectrum 5-HT receptor binding compounds, having amongst other functional serotonin receptor activities, potent 5-HT1A receptor agonistic activity, 5-Ht1D receptor antagonistic activity and 5-HT7 receptor agonistic activity. The compounds of the invention are useful for the preparation of medicaments for treating, ameliorating or preventing movement disorders. The invention relates to compounds of the general formula (1) wherein the symbols have the meanings as given in the description.
摘要翻译：本发明涉及已知的1- [2H-1-苯并吡喃-2-酮-8-基] - 哌嗪衍生物，具有其他功能性5-羟色胺受体活性的广谱5-HT受体结合化合物的新用途， HT 1A受体激动活性，5-HT 1受体拮抗活性和5-HT 7受体激动活性。本发明的化合物可用于制备用于治疗，改善或预防运动障碍的药物。本发明涉及通式（1）的化合物，其中符号具有说明书中给出的含义。

6. 发明申请

US20050070548A1 Hexa-and octahydro-pyrido[1,2-a]pyrazine derivatives with NK1 antagonistic activity 失效
标题翻译：具有NK1拮抗活性的六氢 - 八氢吡啶并[1,2-a]吡嗪衍生物
公开(公告)号：US20050070548A1
公开(公告)日：2005-03-31
申请号：US10946176
申请日：2004-09-22
申请人： Wouter Iwema Bakker , Gustaaf Van Scharrenburg , Adrianus Van Den Hoogenband , Andrew McCreary
发明人： Wouter Iwema Bakker , Gustaaf Van Scharrenburg , Adrianus Van Den Hoogenband , Andrew McCreary
IPC分类号： A61P1/08 , A61P29/00 , C07D471/04 , A61K31/498 , C07D487/04
CPC分类号： C07D471/04
摘要： The invention relates to hexahydro-pyrido[1,2-a]pyrazine derivatives having interesting neurokinin-NK1 receptor antagonistic activity. The invention also relates to methods for the preparation of these compounds, to pharmaceutical compositions containing a pharmacologically active amount of at least one of these compounds as an active ingredient, as well as to the use of these compositions for the treatment of disorders in which neurokinin receptors are involved. The invention relates to compounds represented by the general formula (1) wherein the symbols have the meanings as given in the description.
摘要翻译：本发明涉及具有感兴趣的神经激肽NK1受体拮抗活性的六氢 - 吡啶并[1,2-a]吡嗪衍生物。本发明还涉及制备这些化合物的方法，含有药理学活性量的这些化合物中的至少一种作为活性成分的药物组合物，以及这些组合物用于治疗神经激肽受体参与。本发明涉及由通式（1）表示的化合物，其中符号具有说明书中给出的含义。

7. 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。

8. 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。

9. 发明申请

US20050070528A1 Benzimidazolone and quinazolinone derivatives as agonists on human ORL1 receptors 有权
标题翻译：苯并咪唑酮和喹唑啉酮衍生物作为人类ORL1受体的激动剂
公开(公告)号：US20050070528A1
公开(公告)日：2005-03-31
申请号：US10946177
申请日：2004-09-22
申请人： Jacobus Den Hartog , Gustaaf Van Scharrenburg , Herman Van Stuivenberg , Tinka Tuinstra , Jan-Willem Terpstra
发明人： Jacobus Den Hartog , Gustaaf Van Scharrenburg , Herman Van Stuivenberg , Tinka Tuinstra , Jan-Willem Terpstra
IPC分类号： A61P25/00 , C07C251/20 , C07D401/04 , C07D451/04 , A61K31/5513 , A61K31/454 , A61K31/519 , C07D43/04
CPC分类号： C07C251/20 , C07C2603/28 , C07D401/04 , C07D451/04
摘要： The invention relates to a group of novel benzimidazolone and quinazolinone derivatives which are agonists on human ORL1 (nociceptin) receptors. The invention also relates to the preparation of these compounds, to pharmaceutical compositions containing a pharmacologically active amount of at least one of these imidazolone and quinazolinone derivatives as an active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which ORL1 receptors are involved. The invention relates to compounds of the general formula (1): wherein the symbols have the meanings as given in the description.
摘要翻译：本发明涉及一组新的苯并咪唑酮和喹唑啉酮衍生物，它们是人类ORL1（伤害感受素）受体的激动剂。本发明还涉及这些化合物的制备，含有药理活性量的这些咪唑啉酮和喹唑啉酮衍生物中的至少一种作为活性成分的药物组合物，以及这些药物组合物在治疗疾病中的用途哪个ORL1受体参与。本发明涉及通式（1）的化合物：其中符号具有说明书中给出的含义。

10. 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。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式