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1. 发明授权

US07423048B2 Compounds for treating fundic disaccomodation 有权
公开(公告)号：US07423048B2
公开(公告)日：2008-09-09
申请号：US11355402
申请日：2006-02-16
申请人： Kristol Van Emelen , Marcel Frans Leopold De Bruyn , Manuel Jesús Alcázar-Vaca , José Ignacio Andrés-Gil , Francisco Javier Fernández-Gadea , Maria Encamacion Matesanz-Ballesteros , José Manuel Bartolomé-Nebreda
发明人： Kristol Van Emelen , Marcel Frans Leopold De Bruyn , Manuel Jesús Alcázar-Vaca , José Ignacio Andrés-Gil , Francisco Javier Fernández-Gadea , Maria Encamacion Matesanz-Ballesteros , José Manuel Bartolomé-Nebreda
IPC分类号： C07D413/06 , C07D413/14 , C07D417/06 , C07D417/14 , C07D403/06 , C07D403/14 , A61K31/436 , A61P1/14
CPC分类号： C07D411/04 , C07D491/04
摘要： The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -a1═a2-a3═a4- is a bivalent radical wherein one or two of a1 to a4 are nitrogen and the remaining a1 to a4 are —CH═; -Z1-Z2- is a bivalent radical; -A- is a bivalent radical of formula —N(R6)-Alk2- or a 5, 6 or 7-membered saturated heterocycle containing one or two nitrogen atoms; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; Alk1 and Alk2 are optionally substituted C1-6alkanediyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ═NR9; Y2 is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a bivalent radical. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to disturbed fundic accomodation.

2. 发明授权

US07081453B2 Compounds for treating impaired fundic relaxation 有权
公开(公告)号：US07081453B2
公开(公告)日：2006-07-25
申请号：US10311612
申请日：2001-06-13
申请人： Kristof Van Emelen , Marcel Frans Leopold De Bruyn , Manuel Jesús Alcázar-Vaca , José Ignacio Andrés-Gil , Francisco Javier Fernández-Gadea , Maria Encarnacion Matesanz-Ballesteros , José Manuel Bartolomé-Nebreda
发明人： Kristof Van Emelen , Marcel Frans Leopold De Bruyn , Manuel Jesús Alcázar-Vaca , José Ignacio Andrés-Gil , Francisco Javier Fernández-Gadea , Maria Encarnacion Matesanz-Ballesteros , José Manuel Bartolomé-Nebreda
IPC分类号： A61K31/397
CPC分类号： C07D411/04 , C07D491/04
摘要： The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharma-ceutically acceptable acid addition salt thereof, wherein —a1═a2—a3═a4— is a bivalent radical wherein one or two of a1 to a4 are nitrogen and the remaining a1 to a4 are —CH═; —Z1—Z2— is a bivalent radical; —A— is a bivalent radical of formula —N(R6)—Alk2— or a 5, 6 or 7-membered saturated heterocycle containing one or two nitrogen atoms; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; Alk1 and Alk2 are optionally substituted C1-6alkanediyl; R5 is a radical of formula (d-1), (d-2), (d-3), (d-4), (d-5) wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ═NR9; Y2 is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a bivalent radical. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to disturbed fundic accomodation

3. 发明授权

US07476662B2 Substituted tetracyclic imidazole derivatives, processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine 有权
标题翻译：取代的四环咪唑衍生物，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：US07476662B2
公开(公告)日：2009-01-13
申请号：US10479839
申请日：2002-06-11
申请人： Frans Eduard Janssens , Joseph Elisabeth Leenaerts , Koenraad Arthur Van Rossem , Manuel Jesús Alcázar-Vaca , Pedro Martínez-Jiménez , José Manuel Bartolomé-Nebreda , Antonio Gómez-Sánchez , Francisco Javier Fernández-Gadea , Jos Van Reempts
发明人： Frans Eduard Janssens , Joseph Elisabeth Leenaerts , Koenraad Arthur Van Rossem , Manuel Jesús Alcázar-Vaca , Pedro Martínez-Jiménez , José Manuel Bartolomé-Nebreda , Antonio Gómez-Sánchez , Francisco Javier Fernández-Gadea , Jos Van Reempts
IPC分类号： A61K31/00 , A61P43/00 , C07D487/04 , C07D519/00 , C07D495/04 , C07D487/14
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-6H-benzimidazo[2,1-b][3]benzazepin-6-yl)-2-(phenyl-l-methyl)-1-piperidinyl]ethyl]-2,10-dimethyl pyrimido[1,2-α]benzimidazol-4(10H)-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及其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-1-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N- 氧化物形式。

4. 发明授权

US07732437B2 Use of anti-histaminics for acute reduction of elevated intracranial pressure 有权
标题翻译：使用抗组胺药物急性降低颅内压升高
公开(公告)号：US07732437B2
公开(公告)日：2010-06-08
申请号：US10494006
申请日：2002-11-22
申请人： Frank Tegtmeier , Frans Eduard Janssens , Joseph Elisabeth Leenaerts , Koenraad Arthur van Rossem , Manuel Jesús Alcázar-Vaca , Pedro Martínez-Jiménez , José Manuel Bartolomé-Nebreda , Antonio Gómez-Sánchez , Francisco Javier Fernández-Gadea , Jozef Leo Henri Van Reempts
发明人： Frank Tegtmeier , Frans Eduard Janssens , Joseph Elisabeth Leenaerts , Koenraad Arthur van Rossem , Manuel Jesús Alcázar-Vaca , Pedro Martínez-Jiménez , José Manuel Bartolomé-Nebreda , Antonio Gómez-Sánchez , Francisco Javier Fernández-Gadea , Jozef Leo Henri Van Reempts
IPC分类号： A61P9/10 , A61P37/02 , A61P37/08 , A61K31/415 , A61K31/425 , C07D519/00 , C07D487/04 , C07D471/04
CPC分类号： C07D471/00 , C07D487/00 , C07D519/00
摘要： The invention concerns a novel histamine receptor antagonist and the use of an histamine receptor antagonist for the reduction of intracranial pressure (ICP), in particular for the prevention and treatment of elevated intracranial pressure and/or secondary ischaemida, in particular caused by brain injury, more in particular caused by traumatic (TBI) and non-traumatic brain injury. 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-6H-benzimidazo[2,1-b][3]benzazepin-6-yl)-2-(phenyl-methyl)-1-piperidinyl]ethyl]-2,10-dimethyl pyrimido[1,2-α]benzimidazol-4(10H)-one, the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof. Also claimed is the novel use of commercially available histamine H1-and H2-receptor antagonists for the reduction of intracranial pressure (ICP).
摘要翻译：本发明涉及一种新的组胺受体拮抗剂和组胺受体拮抗剂用于降低颅内压（ICP）的用途，特别是用于预防和治疗颅内压升高和/或继发性白斑，特别是由脑损伤引起的，更特别是由创伤性（TBI）和非创伤性脑损伤引起的。新化合物包括根据通式（I）的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-氧化物形式的化合物。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N-氧化物形式其中。还要求的是市售的组胺H1和H2受体拮抗剂用于降低颅内压（ICP）的新颖用途。

5. 发明授权

US08592422B2 Bicyclic triazole and pyrazole lactams as allosteric modulators of mGluR5 receptors 失效
标题翻译：双环三唑和吡唑内酰胺作为mGluR5受体的变构调节剂
公开(公告)号：US08592422B2
公开(公告)日：2013-11-26
申请号：US13329025
申请日：2011-12-16
申请人： P. Jeffrey Conn , Craig W. Lindsley , Shaun R. Stauffer , José Manuel Bartolomé-Nebreda , Susana Conde-Ceide , Gregor James MacDonald , Han Min Tong , Carrie K. Jones , Manuel Jesús Alcázar-Vaca , José Ignacio Andrés-Gil , Chrysa Malosh
发明人： P. Jeffrey Conn , Craig W. Lindsley , Shaun R. Stauffer , José Manuel Bartolomé-Nebreda , Susana Conde-Ceide , Gregor James MacDonald , Han Min Tong , Carrie K. Jones , Manuel Jesús Alcázar-Vaca , José Ignacio Andrés-Gil , Chrysa Malosh
IPC分类号： A61K31/4985 , A61P25/00 , C07D487/04
CPC分类号： C07D487/04 , A61K31/40 , A61K31/4985 , A61K31/501 , A61K31/506 , A61K31/695 , A61K45/06 , C07F7/1804
摘要： In one aspect, the invention relates to bicyclic triazole and pyrazole lactams, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
摘要翻译：一方面，本发明涉及双代三唑和吡唑内酰胺，其衍生物和相关化合物，其可用作代谢型谷氨酸受体亚型5（mGluR5）的正变构调节剂; 制备化合物的合成方法; 包含该化合物的药物组合物; 以及使用所述化合物和组合物治疗与谷氨酸官能障碍相关的神经和精神障碍的方法。该摘要旨在作为用于在特定技术中进行搜索的扫描工具，而不意在限制本发明。

6. 发明申请

US20120225844A1 BICYCLIC TRIAZOLE AND PYRAZOLE LACTAMS AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS 失效
标题翻译：作为MGLUR5受体的独立调节剂的双相三唑和吡唑类
公开(公告)号：US20120225844A1
公开(公告)日：2012-09-06
申请号：US13329025
申请日：2011-12-16
申请人： P. Jeffrey Conn , Craig W. Lindsley , Shaun R. Stauffer , José Manuel Bartolomé-Nebreda , Susana Conde-Ceide , Gregor James Macdonald , Han Min Tong , Carrie K. Jones , Manuel Jesús Alcázar-Vaca , José Ignacio Andrés-Gil , Chrysa Malosh
发明人： P. Jeffrey Conn , Craig W. Lindsley , Shaun R. Stauffer , José Manuel Bartolomé-Nebreda , Susana Conde-Ceide , Gregor James Macdonald , Han Min Tong , Carrie K. Jones , Manuel Jesús Alcázar-Vaca , José Ignacio Andrés-Gil , Chrysa Malosh
IPC分类号： C07D487/04 , A61K31/695 , C07F7/08 , A61P35/04 , A61P25/20 , A61P25/18 , A61P25/08 , A61P25/28 , A61P25/06 , A61K31/4985 , A61P25/00
CPC分类号： C07D487/04 , A61K31/40 , A61K31/4985 , A61K31/501 , A61K31/506 , A61K31/695 , A61K45/06 , C07F7/1804
摘要： In one aspect, the invention relates to bicyclic triazole and pyrazole lactams, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
摘要翻译：一方面，本发明涉及双代三唑和吡唑内酰胺，其衍生物和相关化合物，其可用作代谢型谷氨酸受体亚型5（mGluR5）的正变构调节剂; 制备化合物的合成方法; 包含该化合物的药物组合物; 以及使用所述化合物和组合物治疗与谷氨酸官能障碍相关的神经和精神障碍的方法。该摘要旨在作为用于在特定技术中进行搜索的扫描工具，而不意在限制本发明。

7. 发明授权

US08466153B2 Piperidinylamino-pyridazines and their use as fast dissociating dopamine 2 receptor antagonists 有权
标题翻译：哌啶基氨基哒嗪及其作为快速解离多巴胺2受体拮抗剂的用途
公开(公告)号：US08466153B2
公开(公告)日：2013-06-18
申请号：US12516645
申请日：2007-12-05
申请人： Gregor James MacDonald , José Ignacio Andrés-Gil , Frans Alfons Maria Van Den Keybus , José Manuel Bartolomé-Nebreda , Michiel Luc Maria Van Gool
发明人： Gregor James MacDonald , José Ignacio Andrés-Gil , Frans Alfons Maria Van Den Keybus , José Manuel Bartolomé-Nebreda , Michiel Luc Maria Van Gool
IPC分类号： A61K31/501 , C07D237/20 , A61P25/28
CPC分类号： C07D401/12
摘要： The present invention relates to 6-(piperidin-4-ylamino)pyridazin-3-carbonitriles of the general formula (I); or a pharmaceutically acceptable salt thereof, or a stereoisomeric form, that are fast dissociating dopamine 2 receptor antagonists, as well as 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：本发明涉及通式（I）的6-（哌啶-4-基氨基）哒嗪-3-腈：或其药学上可接受的盐或立体异构形式，其是快速解离的多巴胺2受体拮抗剂，以及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。

8. 发明授权

US07465741B2 C-substituted tricyclic isoxazoline derivatives and their use as anti-depressants 有权
标题翻译： C-取代三环异恶唑啉衍生物及其作为抗抑郁剂的用途
公开(公告)号：US07465741B2
公开(公告)日：2008-12-16
申请号：US10524197
申请日：2003-08-12
申请人： José Ignacio Andrés-Gil , José Manuel Bartolomé-Nebreda , Rosa Maria Alvarez-Escobar , Margaretha Henrica Maria Bakker , Antonius Adrianus Hendrikus Petrus Megens
发明人： José Ignacio Andrés-Gil , José Manuel Bartolomé-Nebreda , Rosa Maria Alvarez-Escobar , Margaretha Henrica Maria Bakker , Antonius Adrianus Hendrikus Petrus Megens
IPC分类号： A61K31/44 , C07D401/00 , C07D491/00 , C07D498/00 , C07D515/00 , C07D513/00
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 α2-adrenocptor antagonist activity and show a strong antidepressant 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 α2-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，所有变量都在权利要求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）再摄取抑制剂活性组合具有额外的α2-肾上腺素能拮抗剂活性，并且显示强的抗抑郁药和/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

US20100076187A1 FAST DISSOCIATING DOPAMINE 2 RECEPTOR ANTAGONISTS 有权
标题翻译：快速分解多巴胺2受体拮抗剂
公开(公告)号：US20100076187A1
公开(公告)日：2010-03-25
申请号：US12516645
申请日：2007-12-05
申请人： Gregor James MacDonald , José Ignacio Andrés-Gil , Frans Alfons Maria Van Den Keybus , José Manuel Bartolomé-Nebreda , Michiel Luc Maria Van Gool
发明人： Gregor James MacDonald , José Ignacio Andrés-Gil , Frans Alfons Maria Van Den Keybus , José Manuel Bartolomé-Nebreda , Michiel Luc Maria Van Gool
IPC分类号： C07D401/14 , C07D401/12
CPC分类号： C07D401/12
摘要： The present invention relates to 6-(piperidin-4-ylamino)pyridazin-3-carbonitriles 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6-（哌啶-4-基氨基）哒嗪-3-腈，其制备方法，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。

10. 发明授权

US07635696B2 Isoxazoline-indole derivatives with an improved antipsychotic and anxiolytic activity 失效
标题翻译：具有改善的抗精神病和抗焦虑活性的异恶唑啉 - 吲哚衍生物
公开(公告)号：US07635696B2
公开(公告)日：2009-12-22
申请号：US11791510
申请日：2005-11-25
申请人： José Ignacio Andrés-Gil , José Manuel Bartolomé-Nebreda , Manuel Jesus Alcázar-Vaca , Maria de las Mercedes Garcia-Martin , Antonius Adrianus Hendrikus Petrus Megens
发明人： José Ignacio Andrés-Gil , José Manuel Bartolomé-Nebreda , Manuel Jesus Alcázar-Vaca , Maria de las Mercedes Garcia-Martin , Antonius Adrianus Hendrikus Petrus Megens
IPC分类号： A61K31/535 , A61K31/445 , A61K31/44 , C07D261/20 , C07D413/00
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, with a binding affinity towards dopamine receptors, in particular towards dopamine D2 and/or D3 receptors, with selective serotonin reuptake inhibition (SSRI) properties and showing an affinity for the 5-HT1A 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：本发明涉及具有结合亲和力的式（I）的异恶唑啉 - 吲哚衍生物，其药学上可接受的酸或碱加成盐，其立体化学异构形式，其N-氧化物形式或其季铵盐针对多巴胺受体，特别是多巴胺D2和/或D3受体，具有选择性5-羟色胺再摄取抑制（SSRI）性质并显示出对5-HT 1A受体的亲和力，包含本发明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，多数特别是精神分裂症及其生产过程，其中变量在本申请中被进一步定义。

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