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11. 发明授权

EP1940832B1 NOVEL 1-AZA BICYCLOALKYL DERIVATIVES FOR THE TREATMENT OF PSYCHOTIC AND NEURODEGENERATIVE DISORDERS 有权
标题翻译：新型1-AZA-BIZYKLOALKYL衍生物用于治疗和PSYCHO TISCHER神经退行性疾病
公开(公告)号：EP1940832B1
公开(公告)日：2011-12-07
申请号：EP06806403.9
申请日：2006-10-19
申请人： Novartis AG
发明人： FEUERBACH, Dominik , FREDERIKSEN, Mathias , MARZI, Martin , ROY, Bernard, Lucien
IPC分类号： C07D453/02 , A61K31/435 , A61P25/00
CPC分类号： C07D453/02
摘要： The present invention provides a compound of formula (I), where X, R, Y, D, A and B are as defined herein. These compounds are suitable as nic-alpha 7 agonists and as such for the treatment of psychotic or neurodegenerative disorders.

12. 发明公开

EP1966208A1 (1-AZA-BICYCLOÝ3.3.1¨N0N-4-YL)-Ý5-(IH-INDOL-5-YL)-HETEROARYL¨-AMINES AS CHOLINERGIC LIGANDS OF THE N-ACHR FOR THE TREATMENT OF PSYCHOTIC AND NEURODEGENERATIVE DISORDERS 失效
标题翻译：（1-氮杂双环[3.3.1]壬-4-基） - [5-（-1H-吲哚-5-基）杂芳基] - 胺，胆碱能配体的N-乙酰胆碱受体对于精神病和神经变性疾病
公开(公告)号：EP1966208A1
公开(公告)日：2008-09-10
申请号：EP06840977.0
申请日：2006-12-14
申请人： Novartis AG
发明人： FREDERIKSEN, Mathias , FEUERBACH, Dominik , HURTH, Konstanze , KOLLER, Manuel , ROY, Bernard, Lucien
IPC分类号： C07D471/08 , A61K31/439 , A61P25/00
CPC分类号： C07D471/08 , A61K31/429
摘要： The present invention relates to compounds of formula (I) wherein n represents 0, 1, 2, 3, 4 or 5, R represents independent from each other hydroxyl, cyano, nitro, halogen, alkyl, alkoxy alkylcarbonyl, alkoxycarbonyl, alkylamine, dialkylamine, alkylcarbonylamine, alkylcarbamate Y represents one of the following groups: (Ia) in free base or acid addition salt form, to processes for their production, to pharmaceutical compositions comprising them and their use in the manufacture of a medicament for the treatment and/or delay of progression of psychotic and neurodegenerative disorders.

13. 发明公开

EP2456763A1 OXAZINE DERIVATIVES AND THEIR USE AS BACE INHIBITORS FOR THE TREATMENT OF NEUROLOGICAL DISORDERS 有权
标题翻译：恶嗪衍生物及其作为BACE抑制剂神经病症的治疗用途
公开(公告)号：EP2456763A1
公开(公告)日：2012-05-30
申请号：EP10737870.5
申请日：2010-07-23
申请人： Novartis AG
发明人： BADIGER, Sangamesh , CHEBROLU, Murali , FREDERIKSEN, Mathias , HOLZER, Philipp , HURTH, Konstanze , LUEOEND, Rainer Martin , MACHAUER, Rainer , MOEBITZ, Henrik , NEUMANN, Ulf , RAMOS, Rita , RUEEGER, Heinrich , TINTELNOT-BLOMLEY, Marina , VEENSTRA, Siem Jacob , VOEGTLE, Markus , SCHAEFER, Michael
IPC分类号： C07D265/30 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , A61K31/5377 , A61K31/553 , A61P25/00 , A61P9/00
CPC分类号： C07D487/04 , A61K31/5377 , A61K31/553 , A61K45/06 , C07D265/30 , C07D267/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04
摘要： The invention relates to novel heterocyclic compounds of the formula (I) in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their medical use as BACE inhibitors for the treatment of Alzheimer and to medicaments comprising them.

14. 发明授权

EP1761533B8 1-AZA-BICYCLO[3.3.1]NONANES 失效转让
标题翻译： 1-氮杂 - 二环[3.3.1]壬烷
公开(公告)号：EP1761533B8
公开(公告)日：2011-10-12
申请号：EP05771214.3
申请日：2005-06-17
申请人： Novartis AG
发明人： FEUERBACH, Dominik , MÜLLER, Werner , ROY, Bernard, Lucien , TROXLER, Thomas, J. , HURTH, Konstanze , FREDERIKSEN, Mathias
IPC分类号： C07D471/04 , A61K31/439 , A61P25/00
CPC分类号： C07D471/08

15. 发明公开

EP1761533A1 1-AZA-BICYCLO[3.3.1]NONANES 失效转让
标题翻译： 1-氮杂 - 二环[3.3.1]壬烷
公开(公告)号：EP1761533A1
公开(公告)日：2007-03-14
申请号：EP05771214.3
申请日：2005-06-17
申请人： Novartis AG , NOVARTIS-PHARMA GMBH
发明人： FEUERBACH, Dominik , MÜLLER, Werner , ROY, Bernard, Lucien , TROXLER, Thomas, J. , HURTH, Konstanze , FREDERIKSEN, Mathias
IPC分类号： C07D471/04 , A61K31/439 , A61P25/00
CPC分类号： C07D471/08
摘要： The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I); wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them. Formula (I), wherein A represents O or N(R1); Y represents a group of formula, or wherein the left bond is attached to the A group and the right bond is attached to the R group; R represents a substituted or unsubstituted C5- C10aryl, substituted or unsubstituted hetero-C5-C10aryl, a group N(R1)(R4), or a group N(R2)(CHP3R4); R represent a hydrogen, C1-C4alkyl, or CF3; R2 represents hydrogen, C1-C4alkyl, or CF3; R3 represents hydrogen, C1-C4alkyl, or CF3; R4 represents a substituted or unsubstituted C5-C10 aryl or a substituted or unsubstituted C5-C10heteroaryl; in free base or acid addition salt form.

17. 发明授权

EP1966208B1 (1-AZA-BICYCLO[3.3.1]NON-4-YL)-[5-(1H-INDOL-5-YL)-HETEROARYL]-AMINES AS CHOLINERGIC LIGANDS OF THE N-AChR FOR THE TREATMENT OF PSYCHOTIC AND NEURODEGENERATIVE DISORDERS 失效
标题翻译：（1-氮杂双环[3.3.1]壬-4-基） - [5-（-1H-吲哚-5-基）杂芳基] - 胺，胆碱能配体的N-乙酰胆碱受体对于精神病和神经变性疾病
公开(公告)号：EP1966208B1
公开(公告)日：2011-11-02
申请号：EP06840977.0
申请日：2006-12-14
申请人： Novartis AG
发明人： FREDERIKSEN, Mathias , FEUERBACH, Dominik , HURTH, Konstanze , KOLLER, Manuel , ROY, Bernard, Lucien
IPC分类号： C07D471/08 , A61K31/439 , A61P25/00
CPC分类号： C07D471/08 , A61K31/429
摘要： The present invention relates to compounds of formula (I) wherein n represents 0, 1, 2, 3, 4 or 5, R represents independent from each other hydroxyl, cyano, nitro, halogen, alkyl, alkoxy alkylcarbonyl, alkoxycarbonyl, alkylamine, dialkylamine, alkylcarbonylamine, alkylcarbamate Y represents one of the following groups: (Ia) in free base or acid addition salt form, to processes for their production, to pharmaceutical compositions comprising them and their use in the manufacture of a medicament for the treatment and/or delay of progression of psychotic and neurodegenerative disorders.

18. 发明授权

EP1761533B1 1-AZA-BICYCLO[3.3.1]NONANES 失效转让
标题翻译： 1-氮杂 - 二环[3.3.1]壬烷
公开(公告)号：EP1761533B1
公开(公告)日：2011-04-20
申请号：EP05771214.3
申请日：2005-06-17
申请人： Novartis AG
发明人： FEUERBACH, Dominik , MÜLLER, Werner , ROY, Bernard, Lucien , TROXLER, Thomas, J. , HURTH, Konstanze , FREDERIKSEN, Mathias
IPC分类号： C07D471/04 , A61K31/439 , A61P25/00
CPC分类号： C07D471/08
摘要： The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I); wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them. Formula (I), wherein A represents O or N(R1); Y represents a group of formula, or wherein the left bond is attached to the A group and the right bond is attached to the R group; R represents a substituted or unsubstituted C5- C10aryl, substituted or unsubstituted hetero-C5-C10aryl, a group N(R1)(R4), or a group N(R2)(CHP3R4); R represent a hydrogen, C1-C4alkyl, or CF3; R2 represents hydrogen, C1-C4alkyl, or CF3; R3 represents hydrogen, C1-C4alkyl, or CF3; R4 represents a substituted or unsubstituted C5-C10 aryl or a substituted or unsubstituted C5-C10heteroaryl; in free base or acid addition salt form.
摘要翻译：本发明涉及式（I）的1-氮杂 - 二环烷基衍生物; 其中取代基如说明书中所定义，涉及其制备方法，其作为药物的用途以及包含它们的药物组合物。式（I），其中A代表O或N（R1）; Y代表式的基团，或者其中左键连接至A基团并且右键连接至R基团; R代表取代或未取代的C 5 -C 10芳基，取代或未取代的杂-C 5 -C 10芳基，基团N（R 1）（R 4）或基团N（R 2）（CHP 3 R 4）。 R代表氢，C 1 -C 4烷基或CF 3; R2代表氢，C1-C4烷基或CF3; R3代表氢，C1-C4烷基或CF3; R4代表取代或未取代的C5-C10芳基或取代或未取代的C5-C10杂芳基; 以游离碱或酸加成盐形式。

20. 发明授权

EP1966209B1 [ 1H- INDOL- 5 -YL) -HETEROARYLOXY] - (1-AZA-BICYCLO [3.3.1] NONANES AS CHOLINERGIC LIGANDS OF THE N-ACHR FOR THE TREATMENT OF PSYCHOTIC AND NEURODEGENERATIVE DISORDERS 有权
标题翻译： [1H-吲哚-5-基）杂芳基氧基] - （1-氮杂 - 二环[3.3.1] - 壬烷的N ACHR的AS胆碱能配体用于治疗和神经退行性精神病LEIDEN
公开(公告)号：EP1966209B1
公开(公告)日：2011-10-19
申请号：EP06846986.5
申请日：2006-12-14
申请人： Novartis AG
发明人： FEUERBACH, Dominik , FREDERIKSEN, Mathias , HURTH, Konstanze , ROY, Bernard, Lucien , WAGNER, Beatrix
IPC分类号： C07D471/08 , A61K31/439 , A61P25/00
CPC分类号： C07D471/08 , A61K31/439 , A61K31/501 , A61K31/506 , A61K45/06
摘要： The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I) wherein the substituents are as defined in the specification and to processes for their production to pharmaceutical compositions comprising them and to their use in the manufacture of a medicament for the treatment and/ or delay of progression of psychotic and nemodegenerative disorders.

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