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1. 发明授权

US07371769B2 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：US07371769B2
公开(公告)日：2008-05-13
申请号：US11294657
申请日：2005-12-06
申请人： Roelof van Hes , Pieter Smid , Cornelis G. Kruse , Martinus Th. M. Tulp
发明人： Roelof van Hes , Pieter Smid , Cornelis G. Kruse , Martinus Th. M. Tulp
IPC分类号： A01N43/64 , A61K31/41 , C07D209/04
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。

2. 发明授权

US07696383B2 N-oxides of venlafaxine and o-desmethylvenlafaxine as prodrugs 有权
标题翻译：文拉法辛和o-去甲基文拉法辛的N-氧化物作为前药
公开(公告)号：US07696383B2
公开(公告)日：2010-04-13
申请号：US12143919
申请日：2008-06-23
申请人： Lechoslaw A. Turski , Axel Stoit , Cornelis G. Kruse , Sander Vader , Martinus Th. M. Tulp
发明人： Lechoslaw A. Turski , Axel Stoit , Cornelis G. Kruse , Sander Vader , Martinus Th. M. Tulp
IPC分类号： C07C291/04 , A61K31/13
CPC分类号： C07C291/04
摘要： Embodiments of the invention relate to a compound of formula (1), or a tautomer, stereoisomer, hydrate, or solvate thereof, wherein R1 is H or CH3. Other embodiments of the invention relate to a pharmaceutical composition containing these compound, to methods for preparing these compounds, and to methods for preparing compositions containing these compounds. Yet other embodiments of the invention relate to the uses of these compounds and compositions containing it, such as for the manufacture of medicaments and pharmaceutical compositions for treating a condition chosen from depression, major depressive disorder, generalized anxiety disorder, obsessive compulsive disorder, social anxiety disorder, panic disorder, general depressive disorders, diabetic neuropathy, migraine and hot flashes.
摘要翻译：本发明的实施方案涉及式（1）的化合物或其互变异构体，立体异构体，水合物或溶剂合物，其中R 1为H或CH 3。本发明的其它实施方案涉及含有这些化合物的药物组合物，制备这些化合物的方法以及制备含有这些化合物的组合物的方法。本发明的其它实施方案涉及这些化合物和含有它们的组合物的用途，例如用于制备用于治疗选自抑郁症，重度抑郁障碍，广泛性焦虑症，强迫症，社会焦虑症的药物和药物组合物障碍，恐慌症，一般抑郁障碍，糖尿病性神经病，偏头痛和潮热。

3. 发明授权

US07915262B2 Combination preparations comprising SLV308 and a dopamine agonist 有权
标题翻译：包含SLV308和多巴胺激动剂的组合制剂
公开(公告)号：US07915262B2
公开(公告)日：2011-03-29
申请号：US12843967
申请日：2010-07-27
申请人： Andrew C McCreary , Gustaaf J. M. Van Scharrenburg , Martinus Th. M. Tulp
发明人： Andrew C McCreary , Gustaaf J. M. Van Scharrenburg , Martinus Th. M. Tulp
IPC分类号： A61K31/497 , A61K31/195 , A61K31/135
CPC分类号： A61K31/137 , A61K31/198 , A61K31/496 , A61K2300/00
摘要： A composition containing SLV308 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 using this composition, including Parkinson's disease and restless leg syndrome.
摘要翻译：含有SLV308或其N-氧化物或其至少一种药学上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，分别或顺序地用于治疗需要恢复多巴胺能功能的疾病，其使用这种组合物，包括帕金森病和不宁腿综合征。

4. 发明授权

US07094779B2 Piperazine oxime dervatives having NK-1 receptor antagonistic activity 有权
标题翻译：具有NK-1受体拮抗活性的哌嗪肟衍生物
公开(公告)号：US07094779B2
公开(公告)日：2006-08-22
申请号：US10480542
申请日：2002-07-03
申请人： Wouter I. Iwema Bakker , Jan H. van Maarseveen , Hein K. A. C. Coolen , Martinus Th. M. Tulp , Arnoldus H. J. Herremans , Andrew C. Mccreary , Gustaaf J. M. van Scharrenburg , Adrianus van den Hoogenband
发明人： Wouter I. Iwema Bakker , Jan H. van Maarseveen , Hein K. A. C. Coolen , Martinus Th. M. Tulp , Arnoldus H. J. Herremans , Andrew C. Mccreary , Gustaaf J. M. van Scharrenburg , Adrianus van den Hoogenband
IPC分类号： A61K31/496 , C07D403/06 , C07D413/14 , C07D471/04
CPC分类号： C07D401/14 , C07D241/04 , C07D403/06 , C07D403/14 , C07D405/06 , C07D405/14 , C07D409/06 , C07D471/04
摘要： The present invention relates to a group of novel piperazine oxime derivatives having interesting NK-1 antagonistic activity. The invention relates to compounds of the general formula (1) wherein: X represents phenyl or pyridyl substituted with 1 or 2 substituents from the group CH3, CF3, OCH3, halogen, cyano and 5-CF3-tetrazol-1-yl; Y represents 2- or 3-indolyl, phenyl, 7-aza-indol-3-yl or 3-indazolyl, 2-naphthyl, 3-benzo[b]thiophenyl, 2-benzofuranyl, which groups may be substituted with one or more halogen or alkyl (1–3C); n has the value 0–3; m has the value 0–2; R1 represents NH2, NH-alkyl (1–3C), dialkyl (1–3C)N, morpholino or morpholino substituted with one or two methyl and/or methoxymethyl groups, thiomorpholino, 1,1-dioxothiomorpholino, 2-, 3- or 4-pyridyl or 4-CH3-piperazinyl; R2 is hydrogen, alkyl (1–4C) or phenyl, or R2 together with (CH2)m wherein m is 1, and the intermediate carbon, nitrogen and oxygen atoms forms an isoxazolyl or a 4,5-dihydroisoxazolyl group; R3 and R4 independently represent hydrogen or methyl, or R3 and R4 together are oxygen. The invention also relates to a method for the preparation of the novel compounds, and to pharmaceutical compositions comprising compounds with formula (1) as an active ingredient and the use of these compounds for the treatment of disorders in which neurokinin-1 receptors are involved
摘要翻译：本发明涉及一组具有有趣的NK-1拮抗活性的新型哌嗪肟衍生物。本发明涉及通式（1）的化合物，其中：X表示苯基或被1或2个取代基取代的吡啶基，其中CH 3，CF 3，OCH 3， N 3，卤素，氰基和5-CF 3 - 四唑-1-基; Y代表2-或3-吲哚基，苯基，7-氮杂 - 吲哚-3-基或3-吲唑基，2-萘基，3-苯并[b]噻吩基，2-苯并呋喃基，它们可以被一个或多个卤素或烷基（1-3C）; n的值为0-3; m的值为0-2; R 1表示NH 2，NH-烷基（1-3C），（1-3C）二烷基，吗啉代或吗啉基，被一或两个甲基和/或甲氧基甲基基团，硫代吗啉代，1,1-二氧代硫代吗啉代，2-，3-或4-吡啶基或4- CH 3 - 哌嗪基; R 2是氢，烷基（1-4C）或苯基，或R 2和（CH 2 CH 2）m，其中m为1，中间碳，氮和氧原子形成异恶唑基或4,5-二氢异恶唑基; R 3和R 4独立地代表氢或甲基，或R 3和R 4一起是氧。本发明还涉及一种制备新化合物的方法，以及包含式（1）化合物作为活性成分的药物组合物，以及这些化合物用于治疗涉及神经激肽-1受体的疾病的用途

5. 发明授权

US08106056B2 Combination preparations comprising bifeprunox and a dopamine agonist 有权
标题翻译：包含双歧杆菌和多巴胺激动剂的组合制剂
公开(公告)号：US08106056B2
公开(公告)日：2012-01-31
申请号：US11762239
申请日：2007-06-13
申请人： Andrew C. McCreary , Gustaaf J. M. Van Scharrenburg , Martinus Th. M. Tulp
发明人： Andrew C. McCreary , Gustaaf J. M. Van Scharrenburg , Martinus Th. M. Tulp
IPC分类号： A61K31/497 , A61K31/195 , A61K31/16 , A61K31/135
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。

6. 发明授权

US07786126B2 Combination preparations comprising SLV308 and a dopamine agonist 有权
标题翻译：包含SLV308和多巴胺激动剂的组合制剂
公开(公告)号：US07786126B2
公开(公告)日：2010-08-31
申请号：US11762206
申请日：2007-06-13
申请人： Andrew C. McCreary , Gustaaf J. M. Van Scharrenburg , Martinus Th. M. Tulp
发明人： Andrew C. McCreary , Gustaaf J. M. Van Scharrenburg , Martinus Th. M. Tulp
IPC分类号： A61K31/497 , A61K31/195 , A61K31/135
CPC分类号： A61K31/137 , A61K31/198 , A61K31/496 , A61K2300/00
摘要： A composition containing SLV308 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 using this composition, including Parkinson's disease and restless leg syndrome.
摘要翻译：含有SLV308或其N-氧化物或其至少一种药学上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，分别或顺序地用于治疗需要恢复多巴胺能功能的疾病，其使用这种组合物，包括帕金森病和不宁腿综合征。

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