Quinazolin-4-one AMPA antagonists
    4.
    发明授权
    Quinazolin-4-one AMPA antagonists 失效
    喹唑啉-4-酮AMPA拮抗剂

    公开(公告)号:US06627755B1

    公开(公告)日:2003-09-30

    申请号:US09079420

    申请日:1998-05-14

    IPC分类号: C07D40104

    摘要: The present invention relates to novel quinazolin-4-one derivatives of the formula wherein A is a benzo or thieno fused aromatic ring; B is phenyl, pyridyl or pyrimidyl; X is N or CH; and Y-Z is —CH2NH— or —NHCH2—; and to pharmaceutical compositions containing such compounds, and the use of such compounds to treat neurodegenerative, psychotropic, and drug and alcohol induced central and peripheral nervous system disorders.

    摘要翻译: 本发明涉及式Ⅳ的新颖喹唑啉-4-酮衍生物是苯并或噻吩并茂芳香环; B是苯基,吡啶基或嘧啶基; X为N或CH; Y-Z为-CH 2 NH-或-NHCH 2 - ; 以及含有这些化合物的药物组合物,以及这些化合物用于治疗神经变性,精神药物和药物和酒精诱导的中枢和周围神经系统疾病的用途。

    Atropisomers of 2,3-disubstituted-(5.6)-heteroaryl fused-pyrimidin-4-ones
    5.
    发明授权
    Atropisomers of 2,3-disubstituted-(5.6)-heteroaryl fused-pyrimidin-4-ones 失效
    2,3-二取代 - (5.6) - 杂芳基稠合 - 嘧啶-4-酮的阻转异构体

    公开(公告)号:US06323208B1

    公开(公告)日:2001-11-27

    申请号:US09259413

    申请日:1998-07-23

    IPC分类号: C07D49104

    摘要: The present invention relates to novel atropisomers of 2,3-disubstituted-(5,6)-heteroarylfused-pyrimidin-4-ones, pharmaceutical compositions containing such compounds the use of such compounds to treat neurodegenerative, psychotropic, and drug and alcohol induced central and peripheral nervous system disorders.

    摘要翻译: 本发明涉及2,3-二取代 - (5,6) - 杂芳基稠合嘧啶-4-酮的新型阻转异构体,含有这些化合物的药物组合物使用这些化合物来治疗神经变性,精神药物和药物和醇诱发的中枢 和周围神经系统疾病。

    Imidazo-pyrimidines and triazolo-pyrimidines: benzodiazepine receptor ligands
    8.
    发明授权
    Imidazo-pyrimidines and triazolo-pyrimidines: benzodiazepine receptor ligands 有权
    咪唑并 - 嘧啶和三唑并嘧啶:苯并二氮杂受体配体

    公开(公告)号:US07271170B2

    公开(公告)日:2007-09-18

    申请号:US10898690

    申请日:2004-07-23

    CPC分类号: C07D487/04

    摘要: Compounds of Formula I are provided, as are methods for their preparation. The variables Z1, Z2, Z3, R4, R5, R6, R7, R8 and Ar in the above formula are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).

    摘要翻译: 提供了式I化合物,以及其制备方法。 变量Z 1,Z 2,Z 3,R 4,R 5,/或 >,R 6,R 7,R 8和Ar如上所定义。 这样的化合物可用于在体内或体外调节配体与GABA A A受体的结合,并且特别可用于治疗人类中的各种中枢神经系统(CNS)紊乱,驯养伴侣动物 和牲畜。 本文提供的化合物可以单独施用或与一种或多种其它CNS剂组合施用,以增强其它CNS剂的作用。 还提供了用于治疗这种病症的药物组合物和方法,以及使用这种配体检测GABA A受体的方法(例如,受体定位研究)。

    Method for treating spinal cord trauma with phenolic
2-piperidino-1-alkanols
    9.
    发明授权
    Method for treating spinal cord trauma with phenolic 2-piperidino-1-alkanols 失效
    用酚类2-哌啶子基-1-链烷醇治疗脊髓创伤的方法

    公开(公告)号:US5594007A

    公开(公告)日:1997-01-14

    申请号:US195797

    申请日:1994-02-14

    摘要: A method of blocking N-methyl-D-aspartic acid (NMDA) receptor sites in a mammal in need thereof with an effective NMDA blocking (neuroprotective and antiischemic) amount of prodrug esters of 2-piperidino-1-alkanol derivatives and prodrug esters of 2-azabicyclo-1-alkanol derivatives and analogs and pharmaceutically acceptable salts thereof; methods of using these compounds in the treatment of stroke, spinal cord trauma, traumatic brain injury, multiinfarct dementia, CNS degenerative diseases such as Alzheimer's disease, senile dementia of the Alzheimer's type, Huntington's disease, Parkinson's disease, epilepsy, amyotrophic lateral sclerosis, pain, AIDS dementia, psychotic conditions, drug addictions, migraine, hypoglycemia, anxiolytic conditions, urinary incontinence and an ischemic event arising from CNS surgery, open heart surgery or any procedure during which the function of the cardiovascular system is compromised.

    摘要翻译: 在有需要的哺乳动物中封闭N-甲基-D-天冬氨酸(NMDA)受体位点的方法,其具有有效的NMDA阻断(神经保护和抗缺血)量的2-哌啶子基-1-链烷醇衍生物的前药酯和前药酯 2-氮杂双环-1-链烷醇衍生物及其类似物及其药学上可接受的盐; 使用这些化合物治疗中风,脊髓创伤,创伤性脑损伤,多发性痴呆,中枢神经系统退行性疾病如阿尔茨海默病,老年痴呆症,亨廷顿氏病,帕金森病,癫痫,肌萎缩性侧索硬化,疼痛 ,艾滋病痴呆,精神病症状,药物成瘾症,偏头痛,低血糖症,抗焦虑症状,尿失禁和CNS手术引起的局部缺血事件,开心手术或心血管系统功能受损的任何程序。

    Intermediates for 2-piperidino-1-alkanol derivatives
    10.
    发明授权
    Intermediates for 2-piperidino-1-alkanol derivatives 失效
    中间体2-哌啶子基-1-链烷醇衍生物

    公开(公告)号:US5527912A

    公开(公告)日:1996-06-18

    申请号:US411030

    申请日:1995-03-27

    摘要: 2-(8-Azabicyclo[3.2.1]oct-8-yl)alkanols of the formula ##STR1## wherein Q is S or CH.dbd.CH; X is H, OH or another aromatic substituent; R is hydrogen, alkyl, alkenyl or alkynyl; Y and Y.sup.1 are taken together and are arylmethylene or aralkylmethylene (or a corresponding epoxy derivative) or Y and Y.sup.1 are taken separately and Y is hydrogen or OH, and Y.sup.1 is aryl, aralkyl, arylthio, or aryloxy; and structurally related 2-(piperidino) alkanols; pharmaceutical compositions thereof; methods of treating CNS disorders therewith; and intermediates useful in the preparation of said compounds.

    摘要翻译: 式(I)的2-(8-氮杂双环[3.2.1]辛-8-基)链烷醇其中Q是S或CH = CH; X是H,OH或其它芳族取代基; R是氢,烷基,烯基或炔基; Y和Y1一起取代,分别为芳基亚甲基或芳烷基亚甲基(或相应的环氧衍生物)或Y和Y1分别取代,Y为氢或OH,Y1为芳基,芳烷基,芳硫基或芳氧基; 和结构相关的2-(哌啶子基)链烷醇; 其药物组合物; 治疗CNS疾病的方法; 和可用于制备所述化合物的中间体。