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1. 发明申请

WO2009115515A1 ARYLSULFONYL PYRAZOLINE CARBOXAMIDINE DERIVATIVES AS 5-HT6 ANTAGONISTS 审中-公开
标题翻译：作为5-HT6拮抗剂的芳基磺酰基吡唑烷酮衍生物
公开(公告)号：WO2009115515A1
公开(公告)日：2009-09-24
申请号：PCT/EP2009/053133
申请日：2009-03-17
申请人： SOLVAY PHARMACEUTICALS B.V. , VAN LOEVEZIJN, Arnold , IWEMA BAKKER, Wouter I. , STOIT, Axel , RENSINK, Agatha A.M. , VENHORST, Jennifer , VAN DER NEUT, Martina A.W. , DE HAAN, Martin , KRUSE, Cornelis G.
发明人： VAN LOEVEZIJN, Arnold , IWEMA BAKKER, Wouter I. , STOIT, Axel , RENSINK, Agatha A.M. , VENHORST, Jennifer , VAN DER NEUT, Martina A.W. , DE HAAN, Martin , KRUSE, Cornelis G.
IPC分类号： C07D231/06 , C07D231/54 , C07D403/12 , C07D491/10 , A61K31/4155 , A61K31/416 , A61K31/4162 , A61P25/00
CPC分类号： C07D231/06 , A61K31/415 , A61K31/4155 , A61K31/4162 , A61K31/435 , A61K31/635 , A61K45/06 , C07D231/00 , C07D231/54 , C07D403/12 , C07D471/10 , C07D491/10 , C07D491/107
摘要： This invention concerns arylsulfonyl pyrazoline carboxamidine derivatives as antagonists of 5- HT 6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in Parkinson's disease, Huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, Alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, Irritable Bowel Syndrome, obesity and type-2 diabetes. The compounds have the general formula (1) wherein the symbols have the meanings given in the description.
摘要翻译：本发明涉及作为5-HT 6受体的拮抗剂的芳基磺酰基吡唑啉甲脒衍生物，制备这些化合物的方法和用于它们合成的新型中间体。本发明还涉及这些化合物和组合物的用途，特别是它们在给予患者以在帕金森病，亨廷顿氏舞蹈症，精神分裂症，焦虑症，抑郁症，躁狂抑郁症，精神病，癫痫，强迫症中的治疗效果方面的用途，情绪障碍，偏头痛，阿尔茨海默病，年龄相关认知衰退，轻度认知障碍，睡眠障碍，进食障碍，厌食症，贪食症，暴饮暴食症，惊恐发作，静坐不动，注意力缺陷多动障碍，注意力缺陷障碍，可卡因滥用，乙醇，尼古丁或苯并二氮杂，疼痛，与脊髓损伤或头部损伤相关的疾病，脑积水，功能性肠病，肠易激综合征，肥胖症和2型糖尿病。化合物具有通式（1），其中符号具有说明书中给出的含义。

2. 发明申请

WO2006061379A1 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：WO2006061379A1
公开(公告)日：2006-06-15
申请号：PCT/EP2005/056508
申请日：2005-12-06
申请人： SOLVAY PHARMACEUTICALS B.V. , FEENSTRA, Roelof W. , STOIT, Axel , TERPSTRA, Jan-Willem , PRAS-RAVES, Maria L. , MCCREARY, Andrew C. , VAN VLIET, Bernard J. , HESSELINK, Mayke B. , KRUSE, Cornelis G. , VAN SCHARRENBURG, Gustaaf J.M.
发明人： FEENSTRA, Roelof W. , STOIT, Axel , TERPSTRA, Jan-Willem , PRAS-RAVES, Maria L. , MCCREARY, Andrew C. , VAN VLIET, Bernard J. , HESSELINK, Mayke B. , KRUSE, Cornelis G. , VAN SCHARRENBURG, Gustaaf J.M.
IPC分类号： A61K31/423 , C07D413/12 , A61P25/00
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.
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

WO2009000797A1 N-OXIDES OF VENLAFAXINE AND O-DESMETHYLVENLAFAXINE AS PRODRUGS 审中-公开
标题翻译：芬太尼氧化物和邻苯二甲酸氧氟沙星作为PRODRUGS
公开(公告)号：WO2009000797A1
公开(公告)日：2008-12-31
申请号：PCT/EP2008/057939
申请日：2008-06-23
申请人： SOLVAY PHARMACEUTICALS B.V. , TURSKI, Lechoslaw A. , STOIT, Axel , KRUSE, Cornelis G. , VADER, Sander , TULP, Martinus Th.M.
发明人： TURSKI, Lechoslaw A. , STOIT, Axel , KRUSE, Cornelis G. , VADER, Sander , TULP, Martinus Th.M.
IPC分类号： C07C291/04 , A61K31/135 , A61P25/24
CPC分类号： C07C291/04
摘要： The invention concerns venlafaxine-N-oxide and O-desmethylvenlafaxine-N-oxide as prodrugs of venlafaxine and its major (active) metabolite O-desmethylvenlafaxine respectively, to pharmaceutical compositions containing these N-oxides, to methods for preparing them, and methods for preparing compositions. The invention relates to N-oxide, having formula (1), wherein R 1 is H or CH 3 , and tautomers, stereoisomers, hydrates and solvates thereof. The invention also relates to the uses of the N-oxides and compositions, particularly for the manufacture of medicaments useful in the treatment of affections or diseases effectively treatable - albeit with side effects - with venlafaxine.
摘要翻译：本发明涉及文拉法辛-N-氧化物和O-去甲基文拉法辛-N-氧化物作为文拉法辛及其主要（活性）代谢物O-去甲基文拉法辛的前药，含有这些N-氧化物的药物组合物，及其制备方法制备组合物。本发明涉及具有式（1）的N-氧化物，其中R 1是H或CH 3，以及互变异构体，立体异构体，水合物和溶剂化物。本发明还涉及N-氧化物和组合物的用途，特别是用于制备可用于治疗与文拉法辛有效治疗的感染或疾病（尽管有副作用）的药物。

4. 发明申请

WO2008129054A2 HETEROCYCLIC COMPOUNDS WITH AFFINITY TO MUSCARINIC RECEPTORS 审中-公开
标题翻译：具有对肌肉受体的亲和性的杂环化合物
公开(公告)号：WO2008129054A2
公开(公告)日：2008-10-30
申请号：PCT/EP2008/054897
申请日：2008-04-23
申请人： SOLVAY PHARMACEUTICALS B.V. , STOIT, Axel , COOLEN, Hein K.A.C. , KRUSE, Cornelis G. , TERWEL, Louise, heir of REINDERS, Jan H. (deceased)
发明人： STOIT, Axel , COOLEN, Hein K.A.C. , KRUSE, Cornelis G. , TERWEL, Louise, heir of REINDERS, Jan H. (deceased)
IPC分类号： C07D401/04 , C07D401/14 , C07D413/04 , C07D471/08 , A61K31/4439 , A61K31/4427 , A61K31/439 , A61P25/28 , C07D453/02
CPC分类号： C07D401/04 , C07D401/14 , C07D413/04 , C07D453/02 , C07D471/08
摘要： The present invention relates to heterocyclic compounds of the formula (I) wherein - the heterocycle comprises two double bonds which may be present at several positions, represented by the dashed lines ( -- ); - the heterocycle contains two heteroatoms, - W being N or NH; - Y being CH, O or NH, wherein if Y is O, X 1 is CH and X 2 is the residue C-Z-R2 or C-R3, wherein Z is NH, O, or S; and if Y is CH or NH, one of X 1 and X 2 is CH or N, the other being the residue C-Z-R2 or C-R3, wherein Z is NH or S; - R1 is selected from the structures (a), (b) and (c): - R2 is selected from (C 1 -C 10 )alkyl, (C 2 -C 10 )alkenyl and (C 2 -C 10 )alkynyl, optionally independently substituted with one or more substituents selected from halogen, hydroxy, cyano, oxo, (C 1 -C 6 )alkoxy, (C 1 -C 6 )alkylthio, (C 1 -C 6 )alkenyloxy, (C 1 -C 6 )alkenylthio, (C 1 -C 4 )alkoxy(C 1 -C 4 )alkoxy, (C 5 -C 7 )cycloalkyl, a 5-membered unsaturated heterocycle (optionally substituted with halogen), phenyl, phenyloxy and phenylthio, wherein the phenyl group is optionally substituted with halogen; or - R2 is an unbranched (C 2 -C 8 )alkyl substituted at the Za-symbol of a group with the formula (Ia) wherein if X 1 is CH or N 1 X 1 is CH or N and X 2 a is C-Za-, or if X 1 is C-Z-R2, X 1 a is C-Za- and X 2 a is CH or N; and the symbols Wa, Ya and Za and the substituent R1a have the same meanings as defined previously for the symbols W, Y and Z and the substituent R1, and are not independently selected, each of the symbols Wa, Ya and Za and the substituent R1 a representing identical symbols and substituents, respectively, as the symbols W, Y and Z and the substituent R1 in the other part of the structure of formula (I); - R3 is selected from (C 4 -C 10 ) alkyl, (C 2 -C 10 ) alkenyl and (C 2 -C 10 ) alkynyl, optionally independently substituted with one or more substituents selected from halogen, hydroxy, cyano, (C 1 C 6 ) alkoxy, (C 1 C 6 ) alkylthio, (C 1 C 6 )alkenyloxy, (C 1 C 6 ) alkenylthio, (C 1 -C 4 ) alkoxy (C 1 -C 4 ) alkoxy, (C 5 -C 7 ) cycloalkyl, a 5-membered unsaturated heterocycle optionally substituted with halogen, phenyl, phenyloxy and phenylthio, wherein the phenyl group is optionally substituted with halogen; or a pharmaceutically acceptable salt, a solvate or hydrate thereof. The compounds of the invention have affinity to muscarinic receptors and may be used in the treatment, alleviation or prevention of muscarinic receptor mediated diseases and conditions.
摘要翻译：本发明涉及式（I）的杂环化合物，其中 - 杂环包含两个双键，其可以存在于由虚线（ - ）表示的几个位置。 - 杂环含有两个杂原子，-W为N或NH; - Y是CH，O或NH，其中如果Y是O，则X 1是CH且X 2是残基CZ-R2或C-R3，其中Z是 NH，O或S; 并且如果Y是CH或NH，则X 1和X 2中的一个是CH或N，另一个是残基CZ-R2或C-R3，其中Z是 NH或S; - R 1选自结构（a），（b）和（c）：-R 2选自（C 1 -C 10）烷基，（C 1 -C 10）（C 2 -C 10 -C 10）链烯基和（C 2 -C 10 -C 10）炔基，任选地独立地被一个或多个取代基选自卤素，羟基，氰基，氧代，（C 1 -C 6 - ）烷氧基，（C 1 -C 6 - （C 1 -C 6 -C 6）烷氧基，（C 1 -C 6）烷硫基，（C 1 -C 6 -C 6）烷氧基，（C 1 -C 6 - ）链烯硫基，（C 1 -C 4 -C 4）烷氧基（C 1 -C 4）烷氧基，（C 5元不饱和杂环（任选被卤素取代），苯基，苯氧基和苯硫基，其中苯基任选被卤素取代; 或 - R 2是在具有式（Ia）的基团的Za符号处被取代的未支化的（C 2 -C 8 -C 8）烷基，其中如果X 1 CH或N 1 X 1是CH或N，X 2是C-Z a，或者如果X < A 1是CZ-R 2，X 1 a是C 1 -C 8，X 2是CH或N; 并且符号Wa，Ya和Za以及取代基R 1a具有与前面对符号W，Y和Z以及取代基R所定义的相同的含义，并且不是独立地选择，每个符号Wa，Ya和Za以及取代基 R1a分别表示与式（I）结构的另一部分中的符号W，Y和Z以及取代基R 1相同的符号和取代基; R 3选自（C 1 -C 10 -C 10）烷基，（C 2 -C 10 -C 10）链烯基（C 1 -C 10）炔基，任选独立地被一个或多个选自卤素，羟基，氰基，（C 1 -C 10）（C 1 -C 6）烷硫基，（C 1 -C 6）烷氧基，（C 1 -C 6）烷硫基，（C 1 -C 6）（C 1 -C 6）链烯硫基，（C 1 -C 4 -C 4）烷氧基，（C 1 -C 6）烷硫基，（C 1 -C 6）（C 1 -C 4 - ）烷氧基，（C 5 -C 7 -C 7）环烷基，5元环任选被卤素，苯基，苯氧基和苯硫基取代的不饱和杂环，其中苯基任选被卤素取代; 或其药学上可接受的盐，溶剂合物或水合物。本发明的化合物对毒蕈碱受体具有亲和力，可用于治疗，缓解或预防毒蕈碱受体介导的疾病和病症。

5. 发明申请

WO2009000798A1 SILDENAFIL N-OXIDE AS PRODRUG 审中-公开
标题翻译： SILDENAFIL N-OXIDE作为PRODRUG
公开(公告)号：WO2009000798A1
公开(公告)日：2008-12-31
申请号：PCT/EP2008/057940
申请日：2008-06-23
申请人： SOLVAY PHARMACEUTICALS B.V. , TURSKI, Lechoslaw A. , STOIT, Axel , KRUSE, Cornelis, G. , VADER, Sander , TULP, Martinus Th., M.
发明人： TURSKI, Lechoslaw A. , STOIT, Axel , KRUSE, Cornelis, G. , VADER, Sander , TULP, Martinus Th., M.
IPC分类号： C07D487/04 , A61P15/10 , A61K31/519 , A61P11/00
CPC分类号： C07D487/04
摘要： The invention concerns sildenafil N-oxide as prodrug, to pharmaceutical compositions containing this compound, to methods for preparing it, and methods for preparing compositions. The invention relates to 1-[[3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-ethoxyphenyl]sulfonyl]-4-methyl-4-oxido-piperazine having formula (1 A ) and pharmacologically acceptable salts, hydrates and solvates thereof. The invention also relates to uses of the compound, and compositions containing it, particularly for the manufacture of medicaments useful in the treatment of affections or diseases effectively treatable - albeit with side effects - with sildenafil.
摘要翻译：本发明涉及西地那非N-氧化物作为前药，含有该化合物的药物组合物，其制备方法和制备组合物的方法。本发明涉及1 - [[3-（6,7-二氢-1-甲基-7-氧代-3-丙基-1H-吡唑并[4,3-d]嘧啶-5-基）-4-乙氧基苯基] 磺酰基] -4-甲基-4-氧代 - 哌嗪及其药理学上可接受的盐，水合物和溶剂化物。本发明还涉及该化合物和含有它的组合物的用途，特别是用于制备可用于治疗感染或有效治疗的疾病的药物 - 尽管有副作用 - 西地那非。

6. 发明申请

WO2006061378A1 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：WO2006061378A1
公开(公告)日：2006-06-15
申请号：PCT/EP2005/056507
申请日：2005-12-06
申请人： SOLVAY PHARMACEUTICALS B.V. , FEENSTRA, Roelof, W. , STOIT, Axel , TERPSTRA, Jan-Willem , PRAS-RAVES, Maria, L. , MCCREARY, Andrew, C. , VAN VLIET, Bernard, J. , HESSELINK, Mayke, B. , KRUSE, Cornelis, G. , VAN SCHARRENBURG, Gustaaf, J., M.
发明人： FEENSTRA, Roelof, W. , STOIT, Axel , TERPSTRA, Jan-Willem , PRAS-RAVES, Maria, L. , MCCREARY, Andrew, C. , VAN VLIET, Bernard, J. , HESSELINK, Mayke, B. , KRUSE, Cornelis, G. , VAN SCHARRENBURG, Gustaaf, J., M.
IPC分类号： A61K31/423 , C07D263/58 , A61P25/00
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 -D 2 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）：其中符号具有本说明书中给出的含义，以及其互变异构体，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，水合物和溶剂合物和其互变异构体，立体异构体和N-氧化物。

7. 发明申请

WO2006061377A1 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：WO2006061377A1
公开(公告)日：2006-06-15
申请号：PCT/EP2005/056506
申请日：2005-12-06
申请人： SOLVAY PHARMACEUTICALS B.V. , FEENSTRA, Roelof, W. , STOIT, Axel , TERPSTRA, Jan-Willem , PRAS-RAVES, Maria, L. , MCCREARY, Andrew, C. , VAN VLIET, Bernard, J. , HESSELINK, Mayke, B. , KRUSE, Cornelis, G. , VAN SCHARRENBURG, Gustaaf, J., M.
发明人： FEENSTRA, Roelof, W. , STOIT, Axel , TERPSTRA, Jan-Willem , PRAS-RAVES, Maria, L. , MCCREARY, Andrew, C. , VAN VLIET, Bernard, J. , HESSELINK, Mayke, B. , KRUSE, Cornelis, G. , VAN SCHARRENBURG, Gustaaf, J., M.
IPC分类号： A61K31/423 , C07D263/58 , C07D413/12 , A61P25/00
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 -D 2 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

WO2008003736A1 AZAINDOLE DERIVATIVES WITH A COMBINATION OF PARTIAL NICOTINIC ACETYLCHOLINE RECEPTOR AGONISM AND DOPAMINE REUPTAKE INHIBITION 审中-公开
标题翻译：具有部分NICOTINIC乙酰胆碱受体激动剂和多巴胺反复抑制组合的联合衍生物
公开(公告)号：WO2008003736A1
公开(公告)日：2008-01-10
申请号：PCT/EP2007/056792
申请日：2007-07-05
申请人： SOLVAY PHARMACEUTICALS B.V. , STOIT, Axel , COOLEN, Hein K.A.C. , VAN DER NEUT, Martina A.W. , KRUSE, Cornelis G.
发明人： STOIT, Axel , COOLEN, Hein K.A.C. , VAN DER NEUT, Martina A.W. , KRUSE, Cornelis G.
IPC分类号： C07D471/04 , C07D487/04 , C07D519/00 , A61P25/16 , A61P25/28 , A61P25/30 , A61K31/445 , A61K31/40
CPC分类号： C07D471/04 , C07D487/04 , C07D519/00
摘要： The invention concerns azaindole derivatives having the general formula (I) wherein the symbols have the meanings given in the specification. These compounds have a combination of partial nicotinic acetylcholine receptor agonism and dopamine reuptake inhibition. The invention also relates to pharmaceutical compositions containing these compounds, to methods for preparing them, methods for preparing novel intermediates useful for their synthesis, methods for preparing compositions, and uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in disorders in which nicotinic receptors and/or dopamine transporters are involved, or that can be treated via manipulation of those receptors.
摘要翻译：本发明涉及具有通式（I）的氮杂吲哚衍生物，其中符号具有说明书中给出的含义。这些化合物具有部分烟碱乙酰胆碱受体激动和多巴胺再摄取抑制的组合。本发明还涉及含有这些化合物的药物组合物，其制备方法，制备用于其合成的新中间体的方法，制备组合物的方法，以及这些化合物和组合物的用途，特别是其用于给患者施用在其中涉及烟碱受体和/或多巴胺转运蛋白的病症中的治疗效果，或者可以通过这些受体的操纵来治疗。

9. 发明申请

WO2006061376A1 ARYLOXYETHYLAMINE DERIVATIVES WITH A COMBINATION OF PARTIAL D0PAMINE-D2 RECEPTOR AGONISM AND SEROTONIN REUPTAKE INHIBITION 审中-公开
标题翻译：具有部分D0PAMINE-D2受体激动剂和丝氨酸蛋白酶重复抑制组合的芳基乙酰胺衍生物
公开(公告)号：WO2006061376A1
公开(公告)日：2006-06-15
申请号：PCT/EP2005/056505
申请日：2005-12-06
申请人： SOLVAY PHARMACEUTICALS B.V. , FEENSTRA, Roelof W. , STOIT, Axel , TERPSTRA, Jan-willem , PRAS-RAVES, Maria L. , MCCREARY, Andrew C. , VAN VLIET, Bernard J. , HESSELINK, Mayke B. , KRUSE, Cornelis G. , VAN SCHARRENBURG, Gustaaf J.m.
发明人： FEENSTRA, Roelof W. , STOIT, Axel , TERPSTRA, Jan-willem , PRAS-RAVES, Maria L. , MCCREARY, Andrew C. , VAN VLIET, Bernard J. , HESSELINK, Mayke B. , KRUSE, Cornelis G. , VAN SCHARRENBURG, Gustaaf J.m.
IPC分类号： A61K31/423 , C07D263/58 , C07D413/12 , A61P25/00
CPC分类号： C07D263/58 , C07D413/12
摘要： The invention relates to a group of novel aryloxyethylamine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine -D 2 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): Z-T-Ar wherein: Z is a fragment of the general formula (2): and wherein the other 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模式的新型芳氧基乙胺衍生物：5-羟色胺再摄取抑制和对多巴胺-D2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）：ZT-Ar其中：Z是通式（2）的片段：其中，其它符号具有本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. 发明公开

EP2041131A1 AZAINDOLE DERIVATIVES WITH A COMBINATION OF PARTIAL NICOTINIC ACETYLCHOLINE RECEPTOR AGONISM AND DOPAMINE REUPTAKE INHIBITION 有权
标题翻译： WITH部分激动AM烟碱乙酰胆碱受体的组合，并且多巴胺复苏的抑制氮杂吲哚衍生物
公开(公告)号：EP2041131A1
公开(公告)日：2009-04-01
申请号：EP07787088.9
申请日：2007-07-05
申请人： Solvay Pharmaceuticals B.V.
发明人： STOIT, Axel , COOLEN, Hein K.A.C. , VAN DER NEUT, Martina A.W. , KRUSE, Cornelis G.
IPC分类号： C07D471/04 , C07D487/04 , C07D519/00 , A61P25/16 , A61P25/28 , A61P25/30 , A61K31/445 , A61K31/40
CPC分类号： C07D471/04 , C07D487/04 , C07D519/00
摘要： The invention concerns azaindole derivatives having the general formula (I) wherein the symbols have the meanings given in the specification. These compounds have a combination of partial nicotinic acetylcholine receptor agonism and dopamine reuptake inhibition. The invention also relates to pharmaceutical compositions containing these compounds, to methods for preparing them, methods for preparing novel intermediates useful for their synthesis, methods for preparing compositions, and uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in disorders in which nicotinic receptors and/or dopamine transporters are involved, or that can be treated via manipulation of those receptors.

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