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1. 发明授权

US5698559A Disubstituted polycyclic systems as cognition enhancers 失效
标题翻译：二取代多环系统作为认知增强子
公开(公告)号：US5698559A
公开(公告)日：1997-12-16
申请号：US620643
申请日：1996-03-25
申请人： Wendell Wilkie Wilkerson , Christopher Allan Teleha
发明人： Wendell Wilkie Wilkerson , Christopher Allan Teleha
IPC分类号： C07D213/16 , C07D213/30 , C07D213/53 , C07D213/56 , C07D213/57 , C07D471/04 , C07D401/04 , A61K31/44 , A61K31/505 , C07D403/04
CPC分类号： C07D213/16 , C07D213/30 , C07D213/53 , C07D213/56 , C07D213/57 , C07D471/04
摘要： Compounds of Formula I have been shown to enhance the release of the neurotransmitter acetylcholine, and thus may be useful in the treatment of diseases of man, such as in Alzheimer's disease and other conditions involving learning and cognition, where subnormal levels of this neurochemical are found. The compounds of this invention can be described as shown in Formula I ##STR1## where Q is ##STR2## R.sup.1 is 4-, 3-, or 2-pyridyl, pyrimidyl, pyrazinyl, or fluoro-4-pyridyl; R.sup.2 and R.sup.3 are independently H, F, Cl, Br, NO.sub.2, OH, --R.sup.4, --O--R.sup.4, --CO.sub.2 R.sup.4, --COR.sup.4, --CONH.sub.2, --CONHR.sup.4, --CONR.sub.4 R.sup.4', --S(O).sub.m2 --R.sup.4, NH.sub.2, CF.sub.3, NHR.sup.4, NR.sup.4 R.sup.4' ; R.sup.4 and R.sup.4' are independently H, alkyl of 1 to 4 carbons, CH.sub.2 Phe-W or Phe-W; Phe is a phenyl group; R.sup.5 is --(CH.sub.2).sub.n --Y or --OCOR.sup.4 ; Y is H, OH, NH.sub.2, NHR.sup.4, NR.sup.4 R.sup.4', NHCOR.sup.4, NHCO.sub.2 R.sup.4, NHS(O).sub.2 R.sup.4 ; F, Cl, Br, OR.sup.4, S(O).sub.m R.sup.4, --CO.sub.2 H, --CO.sub.2 R.sup.4, --CN, --CONR.sup.4 R.sup.4', --CONHR.sup.4, --CONH.sub.2, --COR.sup.4 ; --CH.dbd.CHCO.sub.2 R.sup.4, --OCOR.sup.4, Phe, Phe--W, --C.tbd.CCO.sub.2 R.sup.4, --CH.dbd.CHR.sup.4, or --C.dbd.C--R.sup.4 ; W is F, Cl, Br, R.sup.4, OR.sup.4, NO.sub.2, NH.sub.2, NHR.sup.4, NR.sup.4 R.sup.4, CN, S(O).sub.m --R.sup.4 ; m is 0, 1 or 2; n is 1 to 7; and hydrates and physiologically suitable salts thereof.
摘要翻译：已经显示式I的化合物增强了神经递质乙酰胆碱的释放，因此可用于治疗人的疾病，例如阿尔茨海默病和涉及学习和认知的其它病症，其中发现该神经化学物质的次正常水平。本发明的化合物可以如式I的化学式I所述进行描述，其中Q是R 3是4-，3-或2-吡啶基，嘧啶基，吡嗪基或氟代 - 4-吡啶基; R2和R3独立地是H，F，Cl，Br，NO2，OH，-R4，-O-R4，-CO2R4，-COR4，-CONH2，-CONHR4，-CONR4R4'，-S（O） NH2，CF3，NHR4，NR4R4'; R4和R4'独立地是H，1至4个碳的烷基，CH2Phe-W或Phe-W; Phe是苯基; R5是 - （CH2）n-Y或-OCOR4; Y是H，OH，NH2，NHR4，NR4R4'，NHCOR4，NHCO2R4，NHS（O） F，Cl，Br，OR 4，S（O）m R 4，-CO 2 H，-CO 2 R 4，-CN，-CONR 4 R 4'，-CONHR 4，-CONH 2，-COR 4; -CH = CHCO 2 R 4，-OCOR 4，Phe，Phe-W，-C 3 D CCO 2 R 4，-CH = CHR 4或-C = C-R 4; W是F，Cl，Br，R4，OR4，NO2，NH2，NHR4，NR4R4，CN，S（O）m-R4; m为0,1或2; n为1〜7; 和水合物及其生理适合的盐。

2. 发明授权

US5990132A Polycyclic systems, and derivatives thereof, as neurotransmitter release enhancers useful in the treatment of cognitive disorders 失效
标题翻译：多环系统及其衍生物作为用于治疗认知障碍的神经递质释放增强剂
公开(公告)号：US5990132A
公开(公告)日：1999-11-23
申请号：US664631
申请日：1996-06-17
申请人： Christopher Allan Teleha , Wendell Wilkie Wilkerson , Richard Alan Earl
发明人： Christopher Allan Teleha , Wendell Wilkie Wilkerson , Richard Alan Earl
IPC分类号： A61K31/44 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61P25/00 , C07D213/06 , C07D213/61 , C07D401/14 , C07D405/14 , C07D407/00 , C07D409/06 , C07D409/14 , C07D471/04 , C07D487/04 , C07D487/14 , C07D491/04 , C07D491/052 , C07D495/04
CPC分类号： C07D401/14 , C07D213/61 , C07D405/14 , C07D409/06 , C07D409/14 , C07D471/04 , C07D487/04 , C07D487/14 , C07D491/04 , C07D495/04
摘要： Compounds of Formula (I) have been shown to enhance the release of the neurotransmitter acetylcholine, and thus may be useful in the treatment of diseases of man where subnormal levels of this neurochemical are found, such as in Alzheimer's disease, and other conditions involving learning and cognition. This invention describes compounds, pharmaceutical compositions and methods of treatment comprising compounds of Formula (I): ##STR1##
摘要翻译：已经显示式（I）化合物增强了神经递质乙酰胆碱的释放，因此可用于治疗发现该神经化学物质异常水平的人的疾病，例如在阿尔茨海默病中，以及涉及学习的其它病症和认知。本发明描述了包含式（I）化合物的化合物，药物组合物和治疗方法：

3. 发明授权

US5750528A Blockade of neuronal m-channels as a therapeutic approach to the treatment of neurological disease 失效
标题翻译：神经元m通道的阻断作为治疗神经系统疾病的治疗方法
公开(公告)号：US5750528A
公开(公告)日：1998-05-12
申请号：US384289
申请日：1995-02-01
申请人： Barry Stephen Brown , Simon Piers Aiken , Robert Zaczek , Paul Richard Hartig , Christopher Allan Teleha , Wendell Wilkie Wilkerson , Richard Alan Earl
发明人： Barry Stephen Brown , Simon Piers Aiken , Robert Zaczek , Paul Richard Hartig , Christopher Allan Teleha , Wendell Wilkie Wilkerson , Richard Alan Earl
IPC分类号： A61K31/00 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/498 , A61K31/517 , A61K31/50 , A61K31/38 , A61K31/445 , A61K31/505
CPC分类号： A61K31/517 , A61K31/00 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/498
摘要： Compounds which block neuronal M-channels are useful for treating conditions involving neurotransmitter deficiencies, traumatic brain injury, or the depressive phase of bipolar disorder. Compounds can be evaluated for utility in treating these conditions by determining whether they are capable of blocking neuronal M-channels.
摘要翻译：阻断神经元M通道的化合物可用于治疗涉及神经递质缺乏症，创伤性脑损伤或双相障碍抑郁期的病症。可以通过确定它们是否能够阻断神经元M通道来评价化合物在治疗这些病症中的效用。

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