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1. 发明授权

US5180820A Brain-derived neurotrophic factor 失效
标题翻译：脑源性神经营养因子
公开(公告)号：US5180820A
公开(公告)日：1993-01-19
申请号：US400591
申请日：1989-08-30
申请人： Yves-Alain Barde , Joachim Leibrock , Friedrich Lottspeich , George Yancopoulos , Hans Thoenen
发明人： Yves-Alain Barde , Joachim Leibrock , Friedrich Lottspeich , George Yancopoulos , Hans Thoenen
IPC分类号： A61K38/00 , A61K38/18 , A61K38/27 , A61K39/395 , A61K49/00 , A61P25/00 , A61P25/02 , A61P25/28 , A61P35/00 , C07H15/12 , C07H21/04 , C07K14/00 , C07K14/18 , C07K14/47 , C07K14/475 , C07K14/48 , C07K14/52 , C07K14/71 , C07K16/00 , C07K16/22 , C07K16/28 , C12N1/19 , C12N1/21 , C12N5/00 , C12N5/10 , C12N15/00 , C12N15/09 , C12N15/12 , C12P21/00 , C12P21/02 , C12P21/08 , C12Q1/00 , C12Q1/68 , C12R1/01 , C12R1/645 , C12R1/91 , F02B75/02 , G01N33/53 , G01N33/577
CPC分类号： C07K14/48 , C07K14/475 , C07K14/71 , C07K16/22 , C07K16/2863 , A61K38/00 , F02B2075/027 , G01N2333/4709 , G01N2333/475
摘要： The present invention relates to nucleic acid sequences encoding brain derived neurotrophic factor (BDNF), as well as BDNF protein produced in quantity using these nucleic acid sequences, as well as fragments and derivatives thereof. In addition, the invention relates to pharmacologic compositions and therapeutic uses of BDNF, having provided, for the first time, the ability to generate sufficient quantities of substantially pure BDNF for clinical use. The invention also relates to antibodies directed toward BDNF or fragments thereof, having provided a method for generating sufficient immunogen. Further, by permitting a comparison of the nucleic acid sequences of BDNF and NGF, the present invention provides for the identification of homologous regions of nucleic acid sequence between BDNF and NGF, thereby defining a BDNF/NGF gene family; the invention provides a method for identifying an disolating additional members of this gene family.
摘要翻译：本发明涉及编码脑源性神经营养因子（BDNF）的核酸序列，以及使用这些核酸序列量产生的BDNF蛋白质，以及其片段和衍生物。此外，本发明涉及BDNF的药物组合物和治疗用途，BDNF首次提供产生足够量的基本上纯的BDNF用于临床应用的能力。本发明还涉及针对BDNF或其片段的抗体，其提供了产生足够免疫原的方法。此外，通过比较BDNF和NGF的核酸序列，本发明提供了鉴定BDNF和NGF之间的核酸序列的同源区，从而限定BDNF / NGF基因家族; 本发明提供了一种用于鉴定该基因家族的不成体的附加成员的方法。

2. 发明授权

US5453361A Method for producing biologically active human brain derived neurotrophic factor 失效
标题翻译：生物活性人脑源性神经营养因子的制备方法
公开(公告)号：US5453361A
公开(公告)日：1995-09-26
申请号：US823117
申请日：1992-01-21
申请人： George Yancopoulos , Yves-Alain Barde , Hans Thoenen , Friedrich Lottspeich , Joachim Leibrock
发明人： George Yancopoulos , Yves-Alain Barde , Hans Thoenen , Friedrich Lottspeich , Joachim Leibrock
IPC分类号： A61K38/00 , A61K38/18 , A61K38/27 , A61K39/395 , A61K49/00 , A61P25/00 , A61P25/02 , A61P25/28 , A61P35/00 , C07H15/12 , C07H21/04 , C07K14/00 , C07K14/18 , C07K14/47 , C07K14/475 , C07K14/48 , C07K14/52 , C07K14/71 , C07K16/00 , C07K16/22 , C07K16/28 , C12N1/19 , C12N1/21 , C12N5/00 , C12N5/10 , C12N15/00 , C12N15/09 , C12N15/12 , C12P21/00 , C12P21/02 , C12P21/08 , C12Q1/00 , C12Q1/68 , C12R1/01 , C12R1/645 , C12R1/91 , F02B75/02 , G01N33/53 , G01N33/577 , C12P21/06 , C07H17/00
CPC分类号： C07K14/48 , C07K14/475 , C07K14/71 , C07K16/22 , C07K16/2863 , A61K38/00 , F02B2075/027 , G01N2333/4709 , G01N2333/475
摘要： The present invention relates to nucleic acid sequences encoding brain derived neurotrophic factor (BDNF), as well as BDNF protein produced in quantity using these nucleic acid sequences, as well as fragments and derivatives thereof. In addition, the invention relates to pharmacologic compositions and therapeutic uses of BDNF, having provided, for the first time, the means to generate sufficient quantities of substantially pure BDNF for clinical use. The invention also relates to antibodies directed toward BDNF or fragments thereof, having provided a method for generating sufficient immunogen. Further, by permitting a comparison of the nucleic acid sequences of BDNF and NGF, the present invention provides for the identification of homologous regions of nucleic acid sequence between BDNF and NGF, thereby defining a BDNF/NGF gene family; the invention provides a method for identifying and isolating additional members of this gene family.
摘要翻译：本发明涉及编码脑源性神经营养因子（BDNF）的核酸序列，以及使用这些核酸序列量产生的BDNF蛋白质，以及其片段和衍生物。此外，本发明涉及BDNF的药物组合物和治疗用途，其首次提供了产生足够量的用于临床使用的基本上纯的BDNF的方法。本发明还涉及针对BDNF或其片段的抗体，其提供了产生足够免疫原的方法。此外，通过比较BDNF和NGF的核酸序列，本发明提供了鉴定BDNF和NGF之间的核酸序列的同源区，从而限定BDNF / NGF基因家族; 本发明提供了鉴定和分离该基因家族的其他成员的方法。

3. 发明授权

US5438121A Brain derived neurotrophic factor 失效
标题翻译：脑源性神经营养因子
公开(公告)号：US5438121A
公开(公告)日：1995-08-01
申请号：US691612
申请日：1991-04-25
申请人： Yves-Alain Barde , Joachim Leibrock , Friedrich Lottspeich , David Edgar , George Yancopoulos , Hans Thoenen
发明人： Yves-Alain Barde , Joachim Leibrock , Friedrich Lottspeich , David Edgar , George Yancopoulos , Hans Thoenen
IPC分类号： A61K38/00 , C07K14/475 , C07K14/48 , C07K14/71 , C07K16/22 , C07K16/28 , F02B75/02 , A61K38/22 , A23J1/00 , C07K1/00 , C12P21/06
CPC分类号： C07K14/71 , C07K14/475 , C07K14/48 , C07K16/22 , C07K16/2863 , A61K38/00 , F02B2075/027 , G01N2333/4709 , G01N2333/475
摘要： The present invention relates to nucleic acid sequences encoding brain derived neurotrophic factor (BDNF), as well as BDNF protein produced in quantity using these nucleic acid sequences, as well as fragments and derivatives thereof. In addition, the invention relates to pharmacologic compositions and therapeutic uses of BDNF, having provided, for the first time, the means to generate sufficient quantities of substantially pure BDNF for clinical use. In a specific embodiment, BDNF may be used to promote the survival of substantia nigra dopaminergic neurons and basal forebrain cholinergic neurons, thereby providing a method for treating, respectively, Parkinson's disease and Alzheimer's disease. The invention also relates to antibodies directed toward BDNF or fragments thereof, having provided a method for generating sufficient immunogen. Further, by permitting a comparison of the nucleic acid sequences of BDNF and NGF, the present invention provides for the identification of homologous regions of nucleic acid sequence between BDNF and NGF, thereby defining a BDNF/NGF gene family; the invention provides a method for identifying and isolating additional members of this gene family.
摘要翻译：本发明涉及编码脑源性神经营养因子（BDNF）的核酸序列，以及使用这些核酸序列量产生的BDNF蛋白质，以及其片段和衍生物。此外，本发明涉及BDNF的药物组合物和治疗用途，其首次提供了产生足够量的用于临床使用的基本上纯的BDNF的方法。在一个具体实施方案中，BDNF可用于促进黑质多巴胺能神经元和基础前脑胆碱能神经元的存活，从而提供分别治疗帕金森病和阿尔茨海默氏病的方法。本发明还涉及针对BDNF或其片段的抗体，其提供了产生足够免疫原的方法。此外，通过比较BDNF和NGF的核酸序列，本发明提供了鉴定BDNF和NGF之间的核酸序列的同源区，从而限定BDNF / NGF基因家族; 本发明提供了鉴定和分离该基因家族的其他成员的方法。

4. 发明授权

US5229500A Brain derived neurotrophic factor 失效
标题翻译：脑源性神经营养因子
公开(公告)号：US5229500A
公开(公告)日：1993-07-20
申请号：US570657
申请日：1990-08-20
申请人： Yves-Alain Barde , Joachim Leibrock , Friedrich Lottspeich , David Edgar , George Yancopoulos , Hans Thoenen
发明人： Yves-Alain Barde , Joachim Leibrock , Friedrich Lottspeich , David Edgar , George Yancopoulos , Hans Thoenen
IPC分类号： A61K38/00 , C07K14/475 , C07K14/48 , C07K14/71 , C07K16/22 , C07K16/28 , F02B75/02
CPC分类号： C07K14/71 , C07K14/475 , C07K14/48 , C07K16/22 , C07K16/2863 , A61K38/00 , F02B2075/027 , G01N2333/4709 , G01N2333/475
摘要： The present invention relates to nucleic acid sequences encoding brain derived neurotrophic factor (BDNF), as well as BDNF protein produced in quantity using these nucleic acid sequences, as well as fragments and derivatives thereof. In addition, the invention relates to pharmacologic compositions and therapeutic uses of BDNF, having provided, for the first time, the means to generate sufficient quantities of substantially pure BDNF for clinical use. In a specific embodiment, BDNF may be used to promote the survival of substantia nigra dopaminergic neurons and basal forebrain cholinergic neurons, thereby providing a method for treating, respectively, Parkinson's disease and Alzheimer's disease. The invention also relates to antibodies directed toward BDNF or fragments thereof, having provided a method for generating sufficient immunogen. Further, by permitting a comparison of the nucleic acid sequences of BDNF and NGF, the present invention provides for the identification of homologous regions of nucleic acid sequence between BDNF and NGF, thereby defining a BDNF/NGF gene family; the invention provides a method for identifying and isolating additional members of this gene family.
摘要翻译：本发明涉及编码脑源性神经营养因子（BDNF）的核酸序列，以及使用这些核酸序列量产生的BDNF蛋白质，以及其片段和衍生物。此外，本发明涉及BDNF的药物组合物和治疗用途，其首次提供了产生足够量的用于临床使用的基本上纯的BDNF的方法。在一个具体实施方案中，BDNF可用于促进黑质多巴胺能神经元和基础前脑胆碱能神经元的存活，从而提供分别治疗帕金森病和阿尔茨海默氏病的方法。本发明还涉及针对BDNF或其片段的抗体，其提供了产生足够免疫原的方法。此外，通过比较BDNF和NGF的核酸序列，本发明提供了鉴定BDNF和NGF之间的核酸序列的同源区，从而限定BDNF / NGF基因家族; 本发明提供了鉴定和分离该基因家族的其他成员的方法。

5. 发明申请

US20090247584A1 PHENOXY-PIPERIDINES FOR THE TREATMENT OF DISEASES SUCH AS SCHIZOPHRENIA AND DEPRESSION 审中-公开
标题翻译：用于治疗疾病的苯氧基苯丙胺，如抗抑郁药和抑郁症
公开(公告)号：US20090247584A1
公开(公告)日：2009-10-01
申请号：US12393480
申请日：2009-02-26
申请人： Gunter HOLZEMANN , Helmut Prucher , Kai Schiemann , Joachim Leibrock , Hartmut Greiner , Christa Burger , Laurie von Melchner
发明人： Gunter HOLZEMANN , Helmut Prucher , Kai Schiemann , Joachim Leibrock , Hartmut Greiner , Christa Burger , Laurie von Melchner
IPC分类号： A61K31/445 , A61P25/28 , A61P25/18
CPC分类号： C07D211/46 , A61K31/445 , A61K2300/00
摘要： Compounds of the formula (I), in which R1, R2′, R2″, R2′″, R3 and n are as defined in Claim 1, are effectors of the nicotinic and/or muscarinic acetylcholine receptor and are suitable for the prophylaxis or treatment of schizophrenia, depression, anxiety states, dementia, Alzheimer's disease, Lewy bodies dementia, neurodegenerative diseases, Parkinson's disease, Huntington's disease, Tourette's syndrome, learning and memory impairments, age-related memory impairment, amelioration of withdrawal symptoms in nicotine dependence, strokes or brain damage by toxic compounds.
摘要翻译：式（I）化合物，其中R 1，R 2'，R 2“，R 2”'，R 3和n如权利要求1所定义，是烟碱和/或毒蕈碱性乙酰胆碱受体的作用剂，并且适用于预防或治疗精神分裂症，抑郁症，焦虑状态，痴呆，阿尔茨海默病，路易体痴呆，神经退行性疾病，帕金森病，亨廷顿氏病，杜氏综合征，学习记忆障碍，年龄相关记忆障碍，尼古丁依赖戒断症状改善，中风或脑损伤的有毒化合物。

6. 发明申请

US20080051394A1 6H-Oxazolo[4,5 e]indole derivatives as nicotinic acetylcholine receptor ligands and/or serotonergic ligands 失效
标题翻译： 6H-恶唑并[4,5 e]吲哚衍生物作为烟碱乙酰胆碱受体配体和/或5-羟色胺能配体
公开(公告)号：US20080051394A1
公开(公告)日：2008-02-28
申请号：US11928961
申请日：2007-10-30
申请人： Kai Schiemann , Henning Bottcher , Joachim Leibrock
发明人： Kai Schiemann , Henning Bottcher , Joachim Leibrock
IPC分类号： A61K31/424 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28
CPC分类号： C07D498/04 , C07D519/00
摘要： Compounds of the formula I in which R1, R2, R3 and R4 are as defined in Claim 1, are ligands of the nicotinic acetylcholine receptor and/or serotonergic ligands and are suitable for the prophylaxis or treatment of psychoses, schizophrenia, depression, anxiety states, dementia, in particular Alzheimer's disease and Lewy bodies dementia, neurodegenerative disorders, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, Tourette's syndrome, learning and memory restrictions, bulimia, anorexia nervosa or other eating disorders, compulsive behaviour, premenstrual syndrome, age-induced memory impairment, amelioration of withdrawal symptoms in nicotine dependence, strokes or brain damage by toxic compounds, and for the treatment of disorders which are characterised by an excess of circulating serotonin or by serotonergic hyperactivity.
摘要翻译：其中R 1，R 2，R 3和R 4的式I化合物如权利要求1是烟酸乙酰胆碱受体和/或血清素能配体的配体，并且适用于预防或治疗精神病，精神分裂症，抑郁症，焦虑症，痴呆，特别是阿尔茨海默病和路易体痴呆，神经变性疾病，帕金森病，肌萎缩性侧索硬化，亨廷顿舞蹈病，Tourette综合征，学习和记忆限制，贪食症，神经性厌食症或其他饮食失调，强迫行为，经前综合征，年龄引起的记忆障碍，尼古丁依赖性戒断症状的改善，中毒或脑损伤的毒性化合物和用于治疗以循环血清素过量为特征或通过血清素过多活性的疾病的治疗。

7. 发明申请

US20070197596A1 Piperidine derivatives 失效
标题翻译：哌啶衍生物
公开(公告)号：US20070197596A1
公开(公告)日：2007-08-23
申请号：US10590912
申请日：2005-02-14
申请人： Timo Heinrich , Henning Boettcher , Joachim Leibrock
发明人： Timo Heinrich , Henning Boettcher , Joachim Leibrock
IPC分类号： A61K31/454 , C07D401/08
CPC分类号： C07D401/06
摘要： Compounds of the formula (I), in which R1, R2, Q, X, Y, m and n have the meanings indicated in Claim (1), are potent 5-HT2A antagonists and are suitable for the treatment of psychoses, schizophrenia, depression, neurological disorders, memory disorders, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Huntington's disease, eating disorders, such as bulimia, anorexia nervosa, of premenstrual syndrome and/or for positively influencing obsessive-compulsive disorder (OCD).
摘要翻译：其中R 1，R 2，Q，X，Y，m和n具有权利要求（1）所示的含义的式（I）化合物是有效的5-HT 2A 2A拮抗剂，适用于治疗精神病，精神分裂症，抑郁症，神经障碍，记忆障碍，帕金森病，肌萎缩性侧索硬化，阿尔茨海默病，亨廷顿病，进食障碍妊娠症，神经性厌食症，经前期综合征和/或积极影响强迫症（OCD）。

8. 发明申请

US20060116405A1 Indol derivatives and their use as 5-ht ligands 失效
标题翻译：吲哚衍生物及其作为5-ht配体的用途
公开(公告)号：US20060116405A1
公开(公告)日：2006-06-01
申请号：US10538639
申请日：2003-11-17
申请人： Gunter Hoelzemann , Helene Crassier , Henning Bottcher , Timo Heinrich , Kai Schiemann , Joachim Leibrock , Chrisoph Van Amsterdam , Gerd Bartoszyk , Christoph Seyfried
发明人： Gunter Hoelzemann , Helene Crassier , Henning Bottcher , Timo Heinrich , Kai Schiemann , Joachim Leibrock , Chrisoph Van Amsterdam , Gerd Bartoszyk , Christoph Seyfried
IPC分类号： A61K31/433 , A61K31/4245 , C07D417/02 , C07D413/02
CPC分类号： C07D413/12 , C07D417/12
摘要： The invention relates to indol derivatives of Formula (I) in which R1, R2, R3, X, A, n, m and p have the meanings indicated above.
摘要翻译：本发明涉及式（I）的吲哚衍生物，其中R 1，R 2，R 3，X，A，n，m和p具有上述含义。

9. 发明申请

US20050101649A1 6H-oxazolo[4,5-e]indole derivatives as nicotinic acetylcholine receptor ligands and/or serotonergic ligands 失效
标题翻译： 6H-恶唑并[4,5-e]吲哚衍生物作为烟碱乙酰胆碱受体配体和/或血清素能配体
公开(公告)号：US20050101649A1
公开(公告)日：2005-05-12
申请号：US10476306
申请日：2002-04-05
申请人： Kai Schiemann , Henning Bottcher , Joachim Leibrock
发明人： Kai Schiemann , Henning Bottcher , Joachim Leibrock
IPC分类号： A61K31/439 , A61K31/454 , A61K31/496 , A61P1/14 , A61P3/04 , A61P5/24 , A61P15/00 , A61P21/00 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/34 , A61P43/00 , C07D498/04 , C07D519/00 , A61K31/424 , A61K31/5377 , A61K31/541
CPC分类号： C07D498/04 , C07D519/00
摘要： Compounds of the formula I in which R1, R2, R3 and R4 are as defined in claim 1, are ligands of the nicotinic acetylcholine receptor and/or serotonergic ligands and are suitable for the prophylaxis or treatment of psychoses, schizophrenia, depression, anxiety states, dementia, in particular Alzheimer's disease and Lewy bodies dementia, neurodegenerative disorders, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, Tourette's syndrome, learning and memory restrictions, bulimia anorexia nervosa or other eating disorders, compulsvie behaviour, premenstrual syndrome, age-induced memory impairment, amelioration of withdrawal symptoms in nicotine dependence, strokes or brain damage by toxic compounds, and for the treatment of disorders which are characterised by an excess of circulating serotonin or by serotonergic hyperactivity.
摘要翻译：其中R 1，R 2，R 3和R 4的式I化合物如权利要求1是烟酸乙酰胆碱受体和/或血清素能配体的配体，并且适用于预防或治疗精神病，精神分裂症，抑郁症，焦虑状态，痴呆，特别是阿尔茨海默病和路易体痴呆，神经变性疾病，帕金森病，肌萎缩性侧索硬化，亨廷顿舞蹈病，Tourette综合征，学习和记忆限制，贪食症神经性食欲障碍或其他饮食失调，强迫行为，经前综合征，年龄引起的记忆障碍，尼古丁依赖性戒断症状改善，中毒或脑损伤，以及用于治疗以循环血清素过量为特征的血清素多动障碍。

10. 发明授权

US07829565B2 Indole derivatives as serotonin reuptake inhibitors 有权
标题翻译：吲哚衍生物作为血清素再摄取抑制剂
公开(公告)号：US07829565B2
公开(公告)日：2010-11-09
申请号：US10560734
申请日：2004-05-24
申请人： Timo Heinrich , Henning Böttcher , Kai Schiemann , Günter Hölzemann , Christoph van Amsterdam , Gerd Bartoszyk , Joachim Leibrock , Christoph Seyfried
发明人： Timo Heinrich , Henning Böttcher , Kai Schiemann , Günter Hölzemann , Christoph van Amsterdam , Gerd Bartoszyk , Joachim Leibrock , Christoph Seyfried
IPC分类号： A61K31/497 , A61K31/445 , C07D295/00 , C07D241/04 , C07D211/00 , A01N43/40
CPC分类号： C07D405/12
摘要： Compounds of the formula (I), the use thereof for the preparation of a medicament for the treatment of diseases associated with the serotonin receptor and/or serotonin reuptake, in particular for the preparation of a medicament as anxiolytic, antidepressant, neuroleptic and/or antihypertonic and/or for positively influencing obsessive-compulsive disorder (OCD), sleeping disorders, tardive dyskinesia, learning disorders, age-dependent memory disorders, eating disorders, such as bulimia, and/or sexual dysfunctions. The compounds bind to the 5-HT1A receptor.
摘要翻译：式（I）的化合物，其用于制备用于治疗与5-羟色胺受体和/或5-羟色胺再摄取有关的疾病的药物的用途，特别是制备抗焦虑药，抗抑郁药，精神安定药和/或和/或积极影响强迫症（OCD），睡眠障碍，迟发性运动障碍，学习障碍，年龄依赖性记忆障碍，进食障碍如贪食症和/或性功能障碍。该化合物与5-HT1A受体结合。

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