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71. 发明申请

US20100197697A1 PIPERIDINE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS 有权
标题翻译：作为NK3受体拮抗剂的哌啶衍生物
公开(公告)号：US20100197697A1
公开(公告)日：2010-08-05
申请号：US12692680
申请日：2010-01-25
申请人： Henner Knust , Matthias Nettekoven , Hasane Ratni , Claus Riemer , Walter Vifian
发明人： Henner Knust , Matthias Nettekoven , Hasane Ratni , Claus Riemer , Walter Vifian
IPC分类号： A61K31/501 , A61K31/497 , A61K31/4523 , A61K31/4545 , C07D401/14 , C07D413/14 , A61P25/18 , A61P25/24
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14
摘要： The present invention relates to a compounds of formula I wherein A, Ar1, Ar2, R1, R2, R3, R4, R5, R6, m, n, o, p, s, t, and u are as defined herein or to a pharmaceutically active salt, a racemic mixture, an enantiomer, an optical isomer or a tautomeric form thereof. the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
摘要翻译：本发明涉及式I化合物，其中A，Ar1，Ar2，R1，R2，R3，R4，R5，R6，m，n，o，p，s，t和u如本文所定义，药物活性盐，外消旋混合物，对映体，旋光异构体或其互变异构形式。本发明化合物是用于治疗抑郁症，疼痛，精神病，帕金森病，精神分裂症，焦虑和注意缺陷多动障碍（ADHD）的高潜力NK-3受体拮抗剂。

72. 发明授权

US07671048B2 Substituted imidazo [1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives 失效
标题翻译：取代的咪唑并[1,5-a] [1,2,4]三唑并[1,5-d] [1,4]苯并二氮杂衍生物
公开(公告)号：US07671048B2
公开(公告)日：2010-03-02
申请号：US11245736
申请日：2005-10-07
申请人： Henner Knust , Heinz Stadler , Andrew William Thomas
发明人： Henner Knust , Heinz Stadler , Andrew William Thomas
IPC分类号： A61P25/28 , A61K31/5517 , C07D487/12
CPC分类号： A61K31/5517 , C07D487/14
摘要： The present invention is concerned with a method of treating a disease selected from the group consisting of cognitive disorders, anxiety, Alzheimer's disease, and schizophrenia comprising administering a therapeutically effective amount of a substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of the following formula wherein R1 is halogen, lower alkyl, lower alkynyl, cycloalkyl, lower alkoxy, OCF3, —NHR, —NHC(O)R or —NHSO2R; R2 is hydrogen, methyl or aryl which is unsubstituted or substituted by one or two substituents selected from the group consisting of halogen and lower alkoxy; R3 is hydrogen, lower alkyl, lower alkenyl, cycloalkyl, lower alkoxy, —O(CH2)n+1—O-lower alkyl, —(CH2)n-aryl which is optionally substituted by lower alkyl or halogen, heteroaryl, —NHR, —N(R)2, wherein each R can be the same or different, —NHCH2C≡CH, or pyrrolidin-1-one; R is hydrogen, lower alkyl, lower alkyl substituted by halogen, heteroaryl, —(CH2)nO-lower alkyl, —NH-lower alkyl, cycloalkyl or aryl, and n is 0, 1, 2 or 3; and with their pharmaceutically acceptable acid addition salts. The invention also provides novel compounds of formula I-A and pharmaceutical compositions containing them. The most preferred indication is Alzheimer's disease.
摘要翻译：本发明涉及治疗选自认知障碍，焦虑，阿尔茨海默氏病和精神分裂症的疾病的方法，其包括给予治疗有效量的取代的咪唑并[1,5-a] [1,2， 4]三唑并[1,5-d] [1,4]苯并二氮杂衍生物其中R1是卤素，低级烷基，低级炔基，环烷基，低级烷氧基，OCF3，-NHR，-NHC（O） NHSO2R; R2是氢，甲基或芳基，其未被取代或被一个或两个选自卤素和低级烷氧基的取代基取代; R3是氢，低级烷基，低级烯基，环烷基，低级烷氧基，-O（CH2）n + 1-O-低级烷基， - （CH2）n-芳基，其任选被低级烷基或卤素，杂芳基，-NHR ，-N（R）2，其中每个R可以相同或不同，-NHCH 2C≡CH或吡咯烷-1-酮; R为氢，低级烷基，被卤素取代的低级烷基，杂芳基， - （CH 2）n O-低级烷基，-NH-低级烷基，环烷基或芳基，n为0,1,2或3。和其药学上可接受的酸加成盐。本发明还提供新颖的式I-A化合物和含有它们的药物组合物。最优选的指征是阿尔茨海默病。

73. 发明申请

US20090197875A1 ARYL-ISOXAZOLO-4-YL-OXADIAZOLE DERIVATIVES 失效
公开(公告)号：US20090197875A1
公开(公告)日：2009-08-06
申请号：US12422317
申请日：2009-04-13
申请人： Bernd Buettelmann , Bo Han , Henner Knust , Andreas Koblet , Andrew Thomas
发明人： Bernd Buettelmann , Bo Han , Henner Knust , Andreas Koblet , Andrew Thomas
IPC分类号： A61K31/541 , C07D413/14 , A61K31/5377 , C07D417/14
CPC分类号： C07D413/04 , C07D413/14
摘要： The present invention is concerned with isoxazol-4-yl-oxadiazole derivatives of formula wherein R1, R2, and R3, are as defined in the specification and pharmaceutically acceptable acid addition salts thereof. This class of compounds has high affinity and selectivity for GABA A α5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.
摘要翻译：本发明涉及下式的异恶唑-4-基 - 恶二唑衍生物，其中R 1，R 2和R 3如说明书中所定义及其药学上可接受的酸加成盐。这类化合物对GABA Aα5受体结合位点具有高亲和力和选择性，可用作认知增强剂或用于治疗认知障碍如阿尔茨海默病。

74. 发明授权

US07501422B2 Prolinamide-tetrazole derivatives as NK3 receptor antagonists 失效
标题翻译：脯氨酰胺 - 四唑衍生物作为NK3受体拮抗剂
公开(公告)号：US07501422B2
公开(公告)日：2009-03-10
申请号：US12129720
申请日：2008-05-30
申请人： Bo Han , Henner Knust , Matthias Nettekoven , Hasane Ratni , Xihan Wu
发明人： Bo Han , Henner Knust , Matthias Nettekoven , Hasane Ratni , Xihan Wu
IPC分类号： A61K31/496 , C07D403/04
CPC分类号： C07D403/12
摘要： The present invention relates to a compound of formula I wherein R1, R2, R3, and n are as defined herein or to a pharmaceutically acceptable acid addition salt thereof. These compounds are NK3 receptor antagonists, useful for the treatment of such disorders as depression, pain, bipolar disorders, psychosis, Parkinson's disease, schizophrenia, anxiety, and attention deficit hyperactivity disorder (ADHD).
摘要翻译：本发明涉及其中R 1，R 2，R 3和n如本文所定义或其药学上可接受的酸加成盐的式I化合物。这些化合物是NK3受体拮抗剂，可用于治疗抑郁症，疼痛，双相性精神障碍，精神病，帕金森病，精神分裂症，焦虑和注意缺陷多动障碍（ADHD）等疾病。

75. 发明申请

US20090054644A1 PYRROLIDINE ARYL-ETHER AS NK3 RECEPTOR ANTAGONISTS 失效
标题翻译：吡咯烷酮ARYL-ETHER作为NK3受体拮抗剂
公开(公告)号：US20090054644A1
公开(公告)日：2009-02-26
申请号：US12195545
申请日：2008-08-21
申请人： Philippe Jablonski , Kenichi Kawasaki , Henner Knust , Anja Limberg , Matthias Nettekoven , Hasane Ratni , Claus Riemer , Xihan Wu
发明人： Philippe Jablonski , Kenichi Kawasaki , Henner Knust , Anja Limberg , Matthias Nettekoven , Hasane Ratni , Claus Riemer , Xihan Wu
IPC分类号： C07D498/04 , C07D403/06 , C07D401/06 , C07D413/06 , C07D403/14
CPC分类号： C07D401/14 , C07D207/08 , C07D401/06 , C07D403/06 , C07D403/14 , C07D487/04 , C07D491/04 , C07D491/10
摘要： The invention relates to a compound of general formula wherein Ar, R1, R2, R3, R4, n, o, p, s, X and are as defined herein or to a pharmaceutically active salt thereof, including all stereoisomeric forms, individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures thereof. The compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
摘要翻译：本发明涉及通式的化合物，其中Ar，R 1，R 2，R 3，R 4，n，o，p，s，X和如本文所定义或其药物活性盐，包括所有立体异构形式，各个非对映异构体和式（I）化合物的对映异构体以及其外消旋和非外消旋混合物。这些化合物是用于治疗抑郁症，疼痛，精神病，帕金森病，精神分裂症，焦虑和注意缺陷多动障碍（ADHD）的高潜力NK-3受体拮抗剂。

76. 发明申请

US20080306089A1 PROLINAMIDE-TETRAZOLE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS 失效
标题翻译：作为NK3受体拮抗剂的丙酰胺 - 四唑衍生物
公开(公告)号：US20080306089A1
公开(公告)日：2008-12-11
申请号：US12129720
申请日：2008-05-30
申请人： Bo Han , Henner Knust , Matthias Nettekoven , Hasane Ratni , Xihan Wu
发明人： Bo Han , Henner Knust , Matthias Nettekoven , Hasane Ratni , Xihan Wu
IPC分类号： A61K31/496 , C07D403/14 , A61P25/00
CPC分类号： C07D403/12
摘要： The present invention relates to a compound of formula I wherein R1, R2, R3, and n are as defined herein or to a pharmaceutically acceptable acid addition salt thereof. These compounds are NK3 receptor antagonists, useful for the treatment of such disorders as depression, pain, bipolar disorders, psychosis, Parkinson's disease, schizophrenia, anxiety, and attention deficit hyperactivity disorder (ADHD).
摘要翻译：本发明涉及其中R 1，R 2，R 3和n如本文所定义或其药学上可接受的酸加成盐的式I化合物。这些化合物是NK3受体拮抗剂，可用于治疗抑郁症，疼痛，双相性精神障碍，精神病，帕金森病，精神分裂症，焦虑和注意缺陷多动障碍（ADHD）等疾病。

77. 发明授权

US07432256B2 Substitued imidazo [1,5-A][1,2,4]triazolo[1,5-D][1,4]benzodiazepine derivatives 失效
标题翻译：取代的咪唑并[1,5-A] [1,2,4]三唑并[1,5-D] [1,4]苯并二氮杂衍生物
公开(公告)号：US07432256B2
公开(公告)日：2008-10-07
申请号：US11297691
申请日：2005-12-08
申请人： Bernd Buettelmann , Henner Knust , Andrew William Thomas
发明人： Bernd Buettelmann , Henner Knust , Andrew William Thomas
IPC分类号： A61P25/28 , A61K31/551 , C07D487/12
CPC分类号： C07D487/14
摘要： The present invention is concerned with substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of the formula I wherein R1 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, nitro, cycloalkyl, —O(CH2)mO(CH2)mOH or —C≡C—R′; R2 is hydrogen or methyl; R3 is lower alkyl, lower alkyl substituted by halogen, lower alkenyl, lower alkenyl substituted by halogen, lower alkynyl, —(CH2)n-cycloalkyl, —(CR′R″)m—CH3, phenyl that is unsubstituted or substituted by halogen, pyridinyl or thienyl each of which is unsubstituted or substituted by lower alkyl, —(CH2)n—NH-cycloalkyl, lower alkenyl-cycloalkyl, lower alkynyl-(CR′R″)mOH, or lower alkynyl-phenyl wherein the phenyl ring is unsubstituited or substituted by halogen, CF3, lower alkyl or lower alkoxy; R′ is hydrogen or lower alkyl; R″ is hydrogen, hydroxy or lower alkyl; n is 0, 1 or 2; m is 1, 2 or 3; and o is 1 or 2; and pharmaceutically acceptable acid addition salts thereof. This class of compounds have high affinity and selectivity for GABA A α5 receptor binding sites. Thus, the invention also relates to methods of enhancing cognition and treating cognitive disorders like Alzheimer's disease.
摘要翻译：本发明涉及式I的取代的咪唑并[1,5-a] [1,2,4]三唑并[1,5-d] [1,4]苯并二氮杂衍生物，其中R 1， >是氢，卤素，低级烷基，被卤素取代的低级烷基，低级烷氧基，被卤素取代的低级烷氧基，硝基，环烷基，-O（CH 2 CH 2）m O （CH 2）2 OH或-C≡C-R'; R 2是氢或甲基; R 3是低级烷基，被卤素取代的低级烷基，低级烯基，被卤素取代的低级链烯基，低级炔基， - （CH 2 SO 2）n

78. 发明授权

US07414061B2 Aryl-isoxazol-4-yl-imidazole derivatives 失效
标题翻译：芳基异恶唑-4-基 - 咪唑衍生物
公开(公告)号：US07414061B2
公开(公告)日：2008-08-19
申请号：US11640622
申请日：2006-12-18
申请人： Bernd Buettelmann , Bo Han , Henner Knust , Andrew Thomas
发明人： Bernd Buettelmann , Bo Han , Henner Knust , Andrew Thomas
IPC分类号： A61K31/506 , A61K31/4439 , A61K31/42 , C07D413/14
CPC分类号： C07D413/04
摘要： The present invention is concerned with aryl-isoxazol-4-yl-imidazole derivatives of formula I: wherein R1 to R6 are as defined in the specification and pharmaceutically acceptable acid addition salts thereof. This class of compounds has high affinity and selectivity for GABA A α5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.
摘要翻译：本发明涉及式I的芳基 - 异恶唑-4-基 - 咪唑衍生物：其中R 1至R 6如本说明书和药学上可接受的酸所定义其加成盐。这类化合物对GABA Aα5受体结合位点具有高亲和力和选择性，可用作认知增强剂或用于治疗认知障碍如阿尔茨海默病。

79. 发明授权

US07378435B2 Aryl-isoxazole-4-carbonyl-indole-carboxylic acid amide derivatives 失效
标题翻译：芳基异恶唑-4-羰基 - 吲哚羧酸酰胺衍生物
公开(公告)号：US07378435B2
公开(公告)日：2008-05-27
申请号：US11543178
申请日：2006-10-04
申请人： Bernd Buettelmann , Bo Han , Henner Knust , Matthias Nettekoven , Andrew Thomas
发明人： Bernd Buettelmann , Bo Han , Henner Knust , Matthias Nettekoven , Andrew Thomas
IPC分类号： A61K31/42 , C07D413/02
CPC分类号： C07D413/14
摘要： The present invention is concerned with aryl-isoxazole-4-carbonyl-indole-carboxylic acid amide derivatives of formula I wherein R1, R2, R3, R4, and R5 are as defined in the specification and claims and with their pharmaceutically acceptable acid addition salts. The invention also relates to methods for preparing such compounds. This class of compounds has a high affinity and selectivity for GABA A α5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease. Thus, the invention also is concerned with pharmaceutical compositions containing compounds of formula I or their pharmaceutically acceptable acid addition salts and methods for the treatment of GABA Aα5 mediated diseases, including Alzheimer's disease.
摘要翻译：本发明涉及式I的芳基 - 异恶唑-4-羰基 - 吲哚 - 羧酸酰胺衍生物，其中R 1，R 2，R 3， R 4，R 4和R 5如说明书和权利要求书及其药学上可接受的酸加成盐所定义。本发明还涉及制备这些化合物的方法。这类化合物对GABA Aα5受体结合位点具有高亲和力和选择性，可能作为认知增强剂或治疗阿尔茨海默病等认知障碍。因此，本发明还涉及含有式I化合物或其药学上可接受的酸加成盐和用于治疗包括阿尔茨海默病在内的GABA Aalpha5介导的疾病的方法的药物组合物。

80. 发明申请

US20070287739A1 Aryl-4-ethynyl-isoxazole derivatives 失效
标题翻译：芳基-4-乙炔基 - 异恶唑衍生物
公开(公告)号：US20070287739A1
公开(公告)日：2007-12-13
申请号：US11805640
申请日：2007-05-24
申请人： Bernd Buettelmann , Henner Knust , Andrew Thomas
发明人： Bernd Buettelmann , Henner Knust , Andrew Thomas
IPC分类号： A61K31/42 , C07D261/06
CPC分类号： C07D413/06 , C07D261/08 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/14 , C07D471/04
摘要： The present invention is concerned with aryl-4-ethynyl-isoxazole derivatives of formula I wherein R1 to R5 are as described in the specification and pharmaceutically acceptable salt thereof. This class of compounds has high affinity and selectivity for GABA A α5 receptor binding sites, being useful as a cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.
摘要翻译：本发明涉及式I的芳基-4-乙炔基 - 异恶唑衍生物，其中R 1至R 5如说明书及其药学上可接受的盐所述。这类化合物对GABA Aα5受体结合位点具有高亲和力和选择性，可用作认知增强剂或用于治疗认知障碍如阿尔茨海默病。

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