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1. 发明申请

WO2004106298A1 INDOLE DERIVATIVES WITH AN IMPROVED ANTIPSYCHOTIC ACTIVITY 审中-公开
标题翻译：具有改善抗肌动蛋白活性的吲哚衍生物
公开(公告)号：WO2004106298A1
公开(公告)日：2004-12-09
申请号：PCT/EP2003/005789
申请日：2003-05-30
申请人： JANSSEN PHARMACEUTICA N.V. , BARTOLOMÉ-NEBREDA, José, Manuel , ANDRÉS-GIL, José, Ignacio
发明人： BARTOLOMÉ-NEBREDA, José, Manuel , ANDRÉS-GIL, José, Ignacio
IPC分类号： C07D98/04
CPC分类号： C07D491/04 , C07D405/14 , C07D498/04
摘要： The present invention relates to a novel indol derivative according to Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N -oxide form thereof or a quaternary ammonium salt thereof, wherein the variables R 1 , R 2 , R 3 , R 4 , R 5 , p, a 1 = a 2 -a 3 = a 4 , Z 1 -Z 2 , X and Y are defined as in claim 1. Said derivative exhibit a binding affinity towards dopamine receptors, in particular towards dopamine D 2 , D 3 and D 4 receptors, with selective serotonin reuptake inhibition properties and acting as 5-HT 1A agonists or partial agonists. The invention also relates to pharmaceutical compositions comprising the compounds according to the invention, the use thereof for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic disorders, most in particular schizophrenia and processes for their production.
摘要翻译：本发明涉及式（I）的新颖的吲哚衍生物，其药学上可接受的酸或碱加成盐，其立体化学异构形式，其N-氧化物形式或其季铵盐，其中变量R 1 R 2，R 3，R 4，R 5，p，a 1 = a 2 -a 3 = a 4，Z 1 -Z X和Y如权利要求1所定义。所述衍生物显示出对多巴胺受体，特别是对多巴胺D2，D3和D4受体的结合亲和力，具有选择性5-羟色胺再摄取抑制性质并且作为5-HT 1A激动剂或部分激动剂。本发明还涉及包含根据本发明的化合物的药物组合物，其用于预防和/或治疗一系列精神和神经障碍，特别是某些精神病性障碍，特别是精神分裂症和其制备方法的用途。

2. 发明申请

WO2011110545A1 IMIDAZO [1, 2 -A] PYRAZINE DERIVATIVES AND THEIR USE FOR THE PREVENTION OR TREATMENT OF NEUROLOGICAL, PSYCHIATRIC AND METABOLIC DISORDERS AND DISEASES 审中-公开
标题翻译：咪唑并[1,2-A]吡嗪衍生物及其用于预防或治疗神经，心理和代谢障碍和疾病的用途
公开(公告)号：WO2011110545A1
公开(公告)日：2011-09-15
申请号：PCT/EP2011/053445
申请日：2011-03-08
申请人： JANSSEN PHARMACEUTICA NV , BARTOLOMÉ-NEBREDA, José, Manuel , CONDE-CEIDE, Susana , MACDONALD, Gregor, James , PASTOR-FERNÁNDEZ, Joaquin , VAN GOOL, Michiel, Luc, Maria , MARTÍN-MARTÍN, María, Luz , VANHOOF, Greta, Constantia, Peter
发明人： BARTOLOMÉ-NEBREDA, José, Manuel , CONDE-CEIDE, Susana , MACDONALD, Gregor, James , PASTOR-FERNÁNDEZ, Joaquin , VAN GOOL, Michiel, Luc, Maria , MARTÍN-MARTÍN, María, Luz , VANHOOF, Greta, Constantia, Peter
IPC分类号： C07D487/04 , A61K31/4985 , A61P3/00 , A61P25/00
CPC分类号： C07D487/04 , A61K31/5377
摘要： The present invention relates to novel imidazo[1,2-a]pyrazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.
摘要翻译：本发明涉及作为磷酸二酯酶10酶（PDE10）的抑制剂的新的咪唑并[1,2-a]吡嗪衍生物，其可用于治疗或预防涉及PDE10酶的神经，精神和代谢紊乱。本发明还涉及包含这些化合物的药物组合物，以制备这些化合物和组合物以使用这些化合物或药物组合物来预防或治疗神经，精神和代谢疾病和疾病。

3. 发明申请

WO2011051342A1 IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS 审中-公开
标题翻译：咪唑并[1,2-b]吡啶衍生物及其用作PDE10抑制剂
公开(公告)号：WO2011051342A1
公开(公告)日：2011-05-05
申请号：PCT/EP2010/066264
申请日：2010-10-27
申请人： JANSSEN PHARMACEUTICA NV , PASTOR-FERNÁNDEZ, Joaquin , BARTOLOMÉ-NEBREDA, José, Manuel , MACDONALD, Gregor, James , CONDE-CEIDE, Susana , DELGADO-GONZÁLEZ, Óscar , VANHOOF, Greta, Constantia, Peter , VAN GOOL, Michiel, Luc, Maria , MARTÍN-MARTÍN, María, Luz , ALONSO-DE DIEGO, Sergio-Alvar
发明人： PASTOR-FERNÁNDEZ, Joaquin , BARTOLOMÉ-NEBREDA, José, Manuel , MACDONALD, Gregor, James , CONDE-CEIDE, Susana , DELGADO-GONZÁLEZ, Óscar , VANHOOF, Greta, Constantia, Peter , VAN GOOL, Michiel, Luc, Maria , MARTÍN-MARTÍN, María, Luz , ALONSO-DE DIEGO, Sergio-Alvar
IPC分类号： C07D487/04 , A61K31/5025 , A61P3/00 , A61P25/00
CPC分类号： C07D487/04
摘要： The present invention relates to novel imidazo[1,2-b]pyridazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.
摘要翻译：本发明涉及作为磷酸二酯酶10酶（PDE10）的抑制剂的新的咪唑并[1,2-b]哒嗪衍生物，其可用于治疗或预防涉及PDE10酶的神经，精神和代谢紊乱。本发明还涉及包含这些化合物的药物组合物，以制备这些化合物和组合物以使用这些化合物或药物组合物来预防或治疗神经，精神和代谢疾病和疾病。

4. 发明申请

WO2010000456A1 SUBSTITUTED 6- (1-PIPERAZINYL) -PYRIDAZINES AS 5-HT6 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为5-HT6受体拮抗剂取代6-（1-哌嗪基） - 吡啶
公开(公告)号：WO2010000456A1
公开(公告)日：2010-01-07
申请号：PCT/EP2009/004745
申请日：2009-07-01
申请人： JANSSEN PHARMACEUTICA NV , BARTOLOMÉ-NEBREDA, José Manuel , MACDONALD, Gregor, James , VAN GOOL, Michiel, Luc, Maria , CONDE-CEIDE, Susana , DELGADO-JIMÉNEZ, Francisca
发明人： BARTOLOMÉ-NEBREDA, José Manuel , MACDONALD, Gregor, James , VAN GOOL, Michiel, Luc, Maria , CONDE-CEIDE, Susana , DELGADO-JIMÉNEZ, Francisca
IPC分类号： C07D237/20 , C07D237/22 , C07D401/12 , A61K31/501 , A61P3/04
CPC分类号： C07D237/22 , C07D237/20 , C07D401/12
摘要： The present invention is concerned with novel substituted 6-(1-piperazinyl)-pyridazines of Formula (I) wherein R 1 , R 2 , R 3 and X have the meaning defined in the claims, having 5 -HT 6 - antagonistic properties. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said novel compound as an active ingredient as well as the use of said compounds as a medicine.
摘要翻译：本发明涉及式（I）的新型取代的6-（1-哌嗪基） - 哒嗪，其中R 1，R 2，R 3和X具有权利要求中定义的含义，具有5-HT 6拮抗性质。本发明还涉及制备这种新化合物的方法，包含所述新化合物作为活性成分的药物组合物以及所述化合物作为药物的用途。

5. 发明申请

WO2008128996A1 THIA(DIA)ZOLES AS FAST DISSOCIATING DOPAMINE 2 RECEPTOR ANTAGONISTS 审中-公开
标题翻译： THIA（DIA）ZOLES作为快速解决DOPAMINE 2受体拮抗剂
公开(公告)号：WO2008128996A1
公开(公告)日：2008-10-30
申请号：PCT/EP2008/054732
申请日：2008-04-18
申请人： JANSSEN PHARMACEUTICA N.V. , MACDONALD, Gregor, James , BARTOLOMÉ-NEBREDA, José Manuel , VAN GOOL, Michiel, Luc, Maria
发明人： MACDONALD, Gregor, James , BARTOLOMÉ-NEBREDA, José Manuel , VAN GOOL, Michiel, Luc, Maria
IPC分类号： C07D417/12 , A61K31/454 , A61P25/18
CPC分类号： C07D401/12 , C07D417/12
摘要： The present invention relates to [1- (benzyl) -piperidin-4-yl] -( [1, 3,4] thiadiazol-2-yl) - amine and [1- (benzyl) -piperidin-4-yl] - (thiazol-2-yl) -amine derivatives of formula (I) that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.
摘要翻译：本发明涉及[1-（苄基） - 哌啶-4-基] - （[1,3,4]噻二唑-2-基） - 胺和[1-（苄基） - 哌啶-4-基] - （I）的（噻唑-2-基） - 胺衍生物，其是快速解离的多巴胺2受体拮抗剂，制备这些化合物的方法，包含这些化合物作为活性成分的药物组合物。该化合物可用作治疗或预防中枢神经系统疾病（例如精神分裂症）的药物，通过发挥抗精神病作用而没有运动副作用。

6. 发明申请

WO2006056600A1 ISOXAZOLINE-INDOLE DERIVATIVES WITH AN IMPROVED ANTIPSYCHOTIC AND ANXIOLYTIC A IVITY 审中-公开
标题翻译：具有改进的抗肌动蛋白和抗炎药物的ISOXAZOLINE-INDOLE衍生物
公开(公告)号：WO2006056600A1
公开(公告)日：2006-06-01
申请号：PCT/EP2005/056229
申请日：2005-11-25
申请人： JANSSEN PHARMACEUTICA N.V. , ANDRÉS-GIL, José, Ignacio , BARTOLOMÉ-NEBREDA, José, Manuel , ALCÁZAR-VACA, Manuel, Jesús , GARCIA-MARTIN, Maria de las Mercedes , MEGENS, Antonius, Adrianus, Hendrikus, Petrus
发明人： ANDRÉS-GIL, José, Ignacio , BARTOLOMÉ-NEBREDA, José, Manuel , ALCÁZAR-VACA, Manuel, Jesús , GARCIA-MARTIN, Maria de las Mercedes , MEGENS, Antonius, Adrianus, Hendrikus, Petrus
IPC分类号： C07D498/04 , A61K31/424 , A61P25/18 , A61P25/00
CPC分类号： C07D498/04
摘要： The present invention relates to novel isoxazoline-indole derivatives according to Formula (I), a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N -oxide form thereof or a quaternary ammonium salt thereof, w ith a binding affinity towards dopamine receptors, in particular towards dopamine D 2 and/or D 3 receptors, with selective serotonin reuptake inhibition (SSRI) properties and showing an affinity for the 5-HT 1A receptor, pharmaceutical compositions comprising the compounds according to the invention, the use thereof for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic disorders, most in particular schizophrenia and processes for their production, wherein the variables are further defined in the application.
摘要翻译：本发明涉及具有式（I）的新型异恶唑啉 - 吲哚衍生物，其药学上可接受的酸或碱加成盐，其立体异构体形式，其N-氧化物形式或其季铵盐，具有结合对多巴胺受体，特别是对多巴胺D 2和/或D 3 N受体的亲和力，具有选择性5-羟色胺再摄取抑制（SSRI）特性并显示出对5-HT的亲和力 1AA受体，包含根据本发明的化合物的药物组合物，其用于预防和/或治疗一系列精神和神经障碍，特别是某些精神障碍，特别是精神分裂症和其生产过程，其中在应用中进一步定义变量。

7. 发明申请

WO2010012758A1 PIPERAZIN-1-YL-TRIFLUOROMETHYL-SUBSTITUTED-PYRIDINES AS FAST DISSOCIATING DOPAMINE 2 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：哌嗪-1-基 - 三氟甲基取代的吡啶作为快速分解多巴胺2受体拮抗剂
公开(公告)号：WO2010012758A1
公开(公告)日：2010-02-04
申请号：PCT/EP2009/059788
申请日：2009-07-29
申请人： JANSSEN PHARMACEUTICA NV , BARTOLOMÉ-NEBREDA, José Manuel , MACDONALD, Gregor, James , VAN GOOL, Michiel, Luc, Maria
发明人： BARTOLOMÉ-NEBREDA, José Manuel , MACDONALD, Gregor, James , VAN GOOL, Michiel, Luc, Maria
IPC分类号： C07D213/74 , C07D213/84 , A61K31/496 , A61P25/00
CPC分类号： C07D213/74 , C07D213/84
摘要： The present invention relates to piperazin-1-yl-trifluoromethyl-substituted-pyridines that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects. Formula (I).
摘要翻译：本发明涉及快速解离多巴胺2受体拮抗剂的哌嗪-1-基 - 三氟甲基取代的吡啶，制备这些化合物的方法，包含这些化合物作为活性成分的药物组合物。该化合物可用作治疗或预防中枢神经系统疾病（例如精神分裂症）的药物，通过发挥抗精神病作用而没有运动副作用。式（I）。

8. 发明申请

WO2004016621A1 C-SUBSTITUTED TRICYCLIC ISOXAZOLINE DERIVATIVES AND THEIR USE AS ANTI-DEPRESSANTS 审中-公开
标题翻译： C-取代的三羟甲基吗啉衍生物及其作为抗坏血酸的用途
公开(公告)号：WO2004016621A1
公开(公告)日：2004-02-26
申请号：PCT/EP2003/050374
申请日：2003-08-12
申请人： JANSSEN PHARMACEUTICA N.V. , ANDRÉS-GIL, José, Ignacio , BARTOLOMÉ-NEBREDA, José, Manuel , ALVAREZ-ESCOBAR, Rosa, Maria , BAKKER, Margaretha, Henrica, Maria , MEGENS, Antonius, Adrianus, Hendrikus, Petrus
发明人： ANDRÉS-GIL, José, Ignacio , BARTOLOMÉ-NEBREDA, José, Manuel , ALVAREZ-ESCOBAR, Rosa, Maria , BAKKER, Margaretha, Henrica, Maria , MEGENS, Antonius, Adrianus, Hendrikus, Petrus
IPC分类号： C07D498/04
CPC分类号： C07D498/04
摘要： The invention concerns substituted tricyclic isoxazoline derivatives according to Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N -oxide form thereof, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisoxazoline , dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on the phenylpart of the tricyclic moiety with at least one radical that is attached to the phenyl radical by a carbon-carbon bond as well as processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for treating depression, anxiety, movement disorders, psychosis, Parkinson's disease and body weight disorders including anorexia nervosa and bulimia, wherin all variables are defined in Claim 1. (I) The compounds have surprisingly been shown to have selective serotonine (5-HT) reuptake inhibitor activity in combination with additional α 2 -adrenoceptor antagonist activity and show a strong anti-depressant and/or anxiolytic activity and/or antipsychotic and/or a body weight control activity without being sedative. Also, in view of their selective serotonine (5-HT) reuptake inhibitor as well as α 2 -adrenoceptor antagonist activity, compounds according to the invention are also suitable for treatment and/or prophylaxis in diseases where either one of the activities alone or the combination of said activities may be of therapeutic use.
摘要翻译：本发明涉及取代的式（I）三环异恶唑啉衍生物，其药学上可接受的酸或碱加成盐，其立体化学异构形式及其N-氧化物形式，更特别地三环二氢苯并吡喃恶唑啉，二氢喹啉基异恶唑啉，二氢萘并恶唑啉和二氢苯并噻喃并恶唑啉衍生物取代在具有至少一个通过碳 - 碳键连接到苯基的基团的三环部分的苯基上，以及它们的制备方法，包含它们的药物组合物及其作为药物的用途，特别是用于治疗抑郁症，焦虑，运动障碍，精神病，帕金森病和包括神经性厌食症和贪食症的体重障碍，所有变量均在权利要求1中定义。（I）化合物令人惊奇地显示具有选择性5-羟色胺（5-HT）再摄取抑制剂活性 combinat 具有额外的α2-肾上腺素能受体拮抗剂活性，并显示强烈的抗抑郁和/或抗焦虑活性和/或抗精神病和/或体重控制活性而不需要镇静。此外，考虑到它们的选择性5-羟色胺再摄取抑制剂以及α2-肾上腺素能受体拮抗剂活性，根据本发明的化合物也适用于治疗和/或预防疾病，其中单独的一种活性或组合的所述活动可能具有治疗用途。

9. 发明申请

WO2002100862A2 NOVEL SUBSTITUTED TETRACYCLIC IMIDAZOLE DERIVATIVES, PROCESSES FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS COMPRISING THEM AND THEIR USE AS A MEDICINE 审中-公开
标题翻译：新型取代的四唑咪唑衍生物，其制备方法，包含它们的药物组合物及其作为药物的用途
公开(公告)号：WO2002100862A2
公开(公告)日：2002-12-19
申请号：PCT/EP2002/006576
申请日：2002-06-11
申请人： JANSSEN PHARMACEUTICA N.V. , JANSSENS, Frans, Eduard , LEENAERTS, Joseph, Elisabeth , VAN ROSSEM, Koenraad, Arthur , ALCÁZAR-VACA, Manuel, Jesús , MARTÍNEZ-JIMÉNEZ, Pedro , BARTOLOMÉ-NEBREDA, José, Manuel , GÓMEZ-SÁNCHEZ, Antonio , FERNÁNDEZ-GADEA, Francisco, Javier , VAN REEMPTS, Jos
发明人： JANSSENS, Frans, Eduard , LEENAERTS, Joseph, Elisabeth , VAN ROSSEM, Koenraad, Arthur , ALCÁZAR-VACA, Manuel, Jesús , MARTÍNEZ-JIMÉNEZ, Pedro , BARTOLOMÉ-NEBREDA, José, Manuel , GÓMEZ-SÁNCHEZ, Antonio , FERNÁNDEZ-GADEA, Francisco, Javier , VAN REEMPTS, Jos
IPC分类号： C07D487/00
CPC分类号： C07D487/04 , C07D471/04
摘要： The invention concerns novel substituted tetracyclic imidazole derivatives useful for the treatment of elevated intracranial pressure (ICP) and/or secondary ischaemia, in particular caused by brain injury, more in particular caused by traumatic (TBI) and non-traumatic brain injury, processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine. The novel compounds comprise compounds according to the general Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N -oxide form thereof. In particular, the preferred compound is 3-[2-[4-(11,12-dihydro-6 H -benzimidazo[2,1-b][3]benzazepin-6-yl)-2-(phenylmethyl)-1-piperidinyl]ethyl]-2,10-dimethyl pyrimido[1,2- a ]benzimidazol-4(10 H )-one, the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N -oxide form thereof.
摘要翻译：本发明涉及可用于治疗升高的颅内压（ICP）和/或继发性缺血的新型取代的四环咪唑衍生物，特别是由脑损伤引起的，特别是由创伤性（TBI）和非创伤性脑损伤引起的其制备方法，包含它们的药物组合物及其作为药物的用途。新化合物包括根据通式（I）的化合物，其药学上可接受的酸或碱加成盐，其立体化学异构形式和其N-氧化物形式。特别地，优选的化合物是3- [2- [4-（11,12-二氢-6H-苯并咪唑并[2,1-b] [3]苯并氮杂-6-基） - 2-（苯基甲基）-1-哌啶基]乙基] -2,10-二甲基嘧啶并[1,2-a]苯并咪唑-4（10H） - 酮，其药学上可接受的酸或碱加成盐，其立体化学异构形式和其N-氧化物形式。

10. 发明申请

WO2008128995A1 4-ALKOXYPYRIDAZINE DERIVATIVES AS FAST DISSOCIATING DOPAMINE 2 RECEPTOR ANTAGONISTS 审中-公开
标题翻译： 4-烷氧基吡啶衍生物作为快速分解多巴胺2受体拮抗剂
公开(公告)号：WO2008128995A1
公开(公告)日：2008-10-30
申请号：PCT/EP2008/054731
申请日：2008-04-18
申请人： JANSSEN PHARMACEUTICA N.V. , MACDONALD, Gregor, James , BARTOLOMÉ-NEBREDA, José Manuel
发明人： MACDONALD, Gregor, James , BARTOLOMÉ-NEBREDA, José Manuel
IPC分类号： C07D401/12 , A61K31/501 , A61P25/18
CPC分类号： C07D401/12
摘要： The present invention relates to (1-benzyl-piperidin-4-yl) - (4-alkoxy-pyridazin-3-yl) - amines of formula (I) that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.
摘要翻译：本发明涉及快速解离多巴胺2受体拮抗剂的式（I）的（1-苄基 - 哌啶-4-基） - （4-烷氧基 - 哒嗪-3-基） - 胺，制备这些化合物的方法，包含这些化合物作为活性成分的药物组合物。该化合物可用作治疗或预防中枢神经系统疾病（例如精神分裂症）的药物，通过发挥抗精神病作用而没有运动副作用。

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