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45 条记录 (耗时 0.037 秒)

    (2-azabicyclo[2.2.1]hept-7yl) methanol derivatives as nicotinic acetylcholine receptor agonists
    32.
    发明授权
    (2-azabicyclo[2.2.1]hept-7yl) methanol derivatives as nicotinic acetylcholine receptor agonists 失效

    公开(公告)号：US07008955B2

    公开(公告)日：2006-03-07

    申请号：US10380064

    申请日：2001-09-11

    申请人： Kai Schiemann ,  Joachim Leibrock

    发明人： Kai Schiemann ,  Joachim Leibrock

    IPC分类号： A61K31/44 ,  A61K31/435 ,  C07D211/06

    CPC分类号： C07D401/12 ,  C07D209/52

    摘要： The present invention relates to substances of the general formula (I) in which X is selected from the group consisting of NH, NR4, O and S, R1 is selected from the group consisting of hydrogen, linear and branched, substituted and unsubstituted C1–C10-alkyl groups, substituted and unsubstituted C5–C10-aryl groups, substituted and unsubstituted C4–C10-heteroaryl groups, acyl groups, thioacyl groups, carbonylcarboxy groups, N-organyl-substituted carbamoyl groups and organosulfonyl groups, R2, R3 are selected, independently of one another, from the group consisting of C1–C10-alkyl groups, C5–C12-aryl groups and C4–C12-heteroaryl groups, these groups being unsubstituted or having one or more substituents which are selected, independently of one another, from the group consisting of halogens, alkoxy groups, aryloxy groups, nitro groups, C1–C5-alkoxycarbonyl groups, optionally fluorine-substituted alkyl or acyl groups and cyano groups, R4 is selected from the group consisting of hydrogen, linear and branched, substituted and unsubstituted C1–C10-alkyl groups, substituted and unsubstituted C5–C10-aryl groups, substituted and unsubstituted C4–C10-heteroaryl groups, aryl groups, thioacryl group, carbonylcarboxy groups, N-organyl-substituted carbamoyl groups and organosulfonyl groups, or a physiologically acceptable salt thereof.

    Piperidine derivatives
    34.
    发明申请
    Piperidine derivatives 失效
    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）。

    Piperidine derivatives
    35.
    发明授权
    Piperidine derivatives 失效
    哌啶衍生物

    公开(公告)号：US07834032B2

    公开(公告)日：2010-11-16

    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 ,  C07D401/02

    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-HT2A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，阿尔茨海默氏病，亨廷顿病，进食障碍，如妊娠症，神经性厌食症，经前期综合征和/或积极影响强迫症（OCD）。

    Benzylpiperidine derivatives
    38.
    发明授权
    Benzylpiperidine derivatives 失效
    苄基哌啶衍生物

    公开(公告)号：US5698553A

    公开(公告)日：1997-12-16

    申请号：US550105

    申请日：1995-10-30

    申请人： Helmut Prucher ,  Rudolf Gottschlich ,  Joachim Leibrock ,  Harry Schwartz

    发明人： Helmut Prucher ,  Rudolf Gottschlich ,  Joachim Leibrock ,  Harry Schwartz

    IPC分类号： C07D413/12 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/47 ,  A61P9/10 ,  A61P25/00 ,  A61P25/04 ,  A61P25/18 ,  A61P25/28 ,  A61P43/00 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D413/06 ,  C07D417/06

    CPC分类号： C07D401/06 ,  C07D413/06 ,  C07D417/06

    摘要： A benzylpiperidine compound of formula I ##STR1## in which R.sup.1 is H, Hal or nitro, R.sup.2 is a benzyl group, which is unsubstituted or substituted by Hal on the aromatic portion, in the 2-, 3- or 4-position of the piperidine ring, with the proviso that R.sup.2 is not in the 4-position if X is --CO--, Y and Z are --CH.sub.2 and R.sup.1 is H, R.sup.3 is H or A, X is --O--, --S--, --NH--, --CO-- or --SO.sub.2 --, Y is --CH.sub.2 --, --NH--, --O--, --S--, --NH-- or alternatively --CO-- if X is --CO-- and Z is --NH-- or --NA--, Z is --CH.sub.2 --, --C(A).sub.2-, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --CO--, --NH--, --NA--, --O--, --S-- or a bond, wherein X--Y or Y--Z is not --O--, --S--S--, --NH--O--, --O--NH--, --NH--NH--, --O--S-- or --S--O, A is alkyl having 1-6 C atoms, B is O or both H and OH, i.e., ##STR2## together with the carbon atom to which B is bonded, Hal is F, Cl, Br or I and n is 0, 1 or 2 or a physiologically acceptable salt thereof, and their salts show a high affinity for binding sites of amino acid receptors and are suitable for the treatment of neurodegenerative disorders.

    摘要翻译： 式I的苄基哌啶化合物其中R 1是H，Hal或硝基，R 2是未取代的或被芳族部分上的Hal取代的苄基，在2-，3-或4- 哌啶环的位置，条件是如果X是-CO-，则R2不在4-位，Y和Z是-CH2，R1是H，R3是H或A，X是-O - ， - S - ，-NH-，-CO-或-SO 2 - ，Y是-CH 2 - ， - NH - ， - O - ， - S - ， - NH-或者-CO-，如果X是-CO-，Z是 - NH-或-NH-，Z是-CH 2 - ， - C（A）2 - ， - CH 2 CH 2 - ， - CH = CH-，-CO-，-NH-，-NA-，-O-，-S- 或键，其中XY或YZ不是-O-，-SS-，-NH-O-，-O-NH-，-NH-NH-，-OS-或-SO，A是具有1-6个 C原子，B为O或H和OH两者，即，与IMA键合的碳原子一起，Hal为F，Cl，Br或I，n为0,1或2，或生理上可接受的盐 并且其盐对氨基酸受体的结合位点显示出高亲和力，并且适用于治疗神经变性疾病。

    Brain derived neurotrophic factor
    40.
    发明授权
    Brain derived neurotrophic factor 失效
    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。