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35 条记录 (耗时 0.05 秒)

    Heteroaryl amide derivatives
    5.
    发明授权
    Heteroaryl amide derivatives 失效
    杂芳酰胺衍生物

    公开(公告)号：US08431593B2

    公开(公告)日：2013-04-30

    申请号：US12516480

    申请日：2007-11-27

    申请人： Alan J. Hutchison ,  Hongbin Li ,  Jianmin Mao ,  David J. Wustrow ,  Jun Yuan ,  He Zhao

    发明人： Alan J. Hutchison ,  Hongbin Li ,  Jianmin Mao ,  David J. Wustrow ,  Jun Yuan ,  He Zhao

    IPC分类号： A61K31/44 ,  A01N43/42 ,  C07D221/02

    CPC分类号： C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D491/113 ,  C07D519/00

    摘要： Heteroaryl amide derivatives are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

    摘要翻译： 提供了以下分子式的杂芳酰胺衍生物：其中变量如本文所述。 这些化合物是可用于在体内或体外调节特异性受体活性的配体，并且特别可用于治疗与人类，驯养伴侣动物和家畜中的病理受体激活相关的病症。 还提供了使用这些化合物治疗这种病症的药物组合物和方法，以及使用这些配体进行受体定位研究的方法。

    Bicyclic and tricyclic heteroaromatic compounds
    6.
    发明授权
    Bicyclic and tricyclic heteroaromatic compounds 失效
    双环和三环杂芳族化合物

    公开(公告)号：US07326709B2

    公开(公告)日：2008-02-05

    申请号：US11442812

    申请日：2006-05-30

    申请人： Jun Yuan ,  Pamela A. Albaugh ,  Kenneth Shaw ,  Alan J. Hutchison

    发明人： Jun Yuan ,  Pamela A. Albaugh ,  Kenneth Shaw ,  Alan J. Hutchison

    IPC分类号： C07D487/04 ,  A61K31/5025

    CPC分类号： C07D217/26 ,  C07D237/30 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00 ,  G01N2333/70571

    摘要： Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof, wherein W, Q, X, X1, Y and Z are as defined herein. These compounds bind with high selectivity and/or high affinity to the benzodiazepine site of GABAA receptors and are therefore useful in the treatment of central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples. Also disclosed are intermediates useful in the preparation of these compounds.

    摘要翻译： 公开了下式的化合物及其药学上可接受的盐，其中W，Q，X，X 1，Y和Z如本文所定义。 这些化合物以高选择性和/或高亲和力结合GABA A A受体的苯并二氮杂位点，因此可用于治疗中枢神经系统（CNS）疾病和用作GABA < 组织样品中的受体。 还公开了可用于制备这些化合物的中间体。

    Certain hetero phosphonic acid derivatives of 2-piperidine or 2-tetrahydropyridinecarboxylates and esters thereof which are useful for the treatment of disorders responsive to blockade of the NMDA receptor in mammals
    8.
    发明授权
    Certain hetero phosphonic acid derivatives of 2-piperidine or 2-tetrahydropyridinecarboxylates and esters thereof which are useful for the treatment of disorders responsive to blockade of the NMDA receptor in mammals 失效
    可用于治疗对哺乳动物中NMDA受体的阻断作出反应的病症的2-哌啶或2-四氢吡啶羧酸酯及其酯的某些异膦酸衍生物

    公开(公告)号：US4746653A

    公开(公告)日：1988-05-24

    申请号：US834672

    申请日：1986-02-28

    申请人： Alan J. Hutchison ,  Kenneth R. Shaw ,  Josef A. Schneider

    发明人： Alan J. Hutchison ,  Kenneth R. Shaw ,  Josef A. Schneider

    IPC分类号： C07F9/59 ,  C07F9/60 ,  C07F9/58 ,  C07F9/65 ,  A61K31/675

    CPC分类号： C07F9/592 ,  C07F9/598 ,  C07F9/60

    摘要： The present invention is concerned with the phosphonic acids of formula I ##STR1## wherein one or both of the acidic hydroxy groups of the phosphonic acid moiety may be functionalized in form of pharmaceutically acceptable mono- or di-esters; wherein Y represents optionally substituted 2-carboxypyrrolidinyl, 2-carboxy-2,5-dihydropyrrolyl, 2-carboxy-1,2,3,6-tetrahydropyridinyl, 2-carboxy-1,2,5,6-tetrahydropyridinyl, 2-carboxypiperidinyl, 2-carboxytetrahydroquinolinyl or 2-carboxyperhydroquinolinyl, 2-carboxy-2,3-dihydroindolyl, 2-carboxyperhydroindolyl, and in each of which the carboxy group may be functionalized in form of a pharmaceutically acceptable ester or amide; A represents B--X--D wherein B represents a direct bond, or straight chain or branched lower alkylene; X represents O, S, SO, SO.sub.2, CO--NR.sub.b, R.sub.b N--CO or N--Ra; Ra represents hydrogen, lower alkyl, aryl, aryl-lower alkyl or acyl; R.sub.b represents hydrogen, lower alkyl or aryl-lower alkyl; D represents straight chain or branched lower alkylene; and pharmaceutically acceptable salts thereof; which are useful in mammals as antagonists of the N-methyl-D-aspartate sensitive excitatory amino acid receptor.

    摘要翻译： 本发明涉及式I（I）的膦酸，其中膦酸部分的一个或两个酸性羟基可以以药学上可接受的单酯或二酯的形式官能化; 其中Y表示任选取代的2-羧基吡咯烷基，2-羧基-2,5-二氢吡咯基，2-羧基-1,2,3,6-四氢吡啶基，2-羧基-1,2,5,6-四氢吡啶基，2-羧基哌啶基 ，2-羧基四氢喹啉基或2-羧基全氢化喹啉基，2-羧基-2,3-二氢吲哚基，2-羧基全氢吲哚基，其中羧基可以以药学上可接受的酯或酰胺的形式官能化; A表示B-X-D，其中B表示直接键，或直链或支链低级亚烷基; X表示O，S，SO，SO2，CO-NRb，RbN-CO或N-Ra; R a表示氢，低级烷基，芳基，芳基 - 低级烷基或酰基; Rb表示氢，低级烷基或芳基 - 低级烷基; D表示直链或支链低级亚烷基; 及其药学上可接受的盐; 其在哺乳动物中作为N-甲基-D-天冬氨酸敏感性兴奋性氨基酸受体的拮抗剂是有用的。

    N.sub.9 -cyclopentyl-substituted adenine derivatives useful as adenosine receptor agonists
    10.
    发明授权
    N.sub.9 -cyclopentyl-substituted adenine derivatives useful as adenosine receptor agonists 失效

    公开(公告)号：US5063233A

    公开(公告)日：1991-11-05

    申请号：US531499

    申请日：1990-05-31

    申请人： Jen Chen ,  Alan J. Hutchison

    发明人： Jen Chen ,  Alan J. Hutchison

    IPC分类号： C07D303/46 ,  C07D473/00 ,  C07D473/16

    CPC分类号： C07D473/00 ,  C07D303/46 ,  C07D473/16

    摘要： The compound of the formula I ##STR1## wherein R, R.sub.3 and R.sub.5 independently represent hydrogen or hydroxy provided that at least one of R, R.sub.3 and R.sub.5 represents hydroxy; R.sub.1 represents hydrogen, lower alkyl, C.sub.3 -C.sub.7 -alkenyl, hydroxy-lower alkyl, optionally substituted cycloalkyl or optionally substituted cycloalkyl-lower alkyl, bicycloalkyl, bicycloalkyl-lower alkyl, adamantyl, tetrahydropyranyl, tetrahydrothiopyranyl, tetrahydropyranyl-lower alkyl, tetrahydrothiopyranyl-lower alkyl, adamantyl-lower alkyl, aryl-hydroxy-lower alkyl, aryl, aryl-lower alkyl, aryl-C.sub.3 -C.sub.6 -cycloalkyl, 9-fluorenyl, 9-fluorenyl-lower alkyl or cycloalkenyl-lower alkyl; or R.sub.1 represents a bicyclic benzo-fused 5 or 6-membered saturated carbocyclic radical or a benz-fused 5 or 6-membered saturated heterocyclic radical containing a heteroatom selected from oxygen and sulfur directly attached to the fused benzene ring, any said bicyclic radicals being optionally substituted on the benzo portion by lower alkyl, lower alkoxy or halogen, or R.sub.1 represents any said bicyclic radical substituted-lower alkyl; R.sub.2 represents hydrogen, halogen, --S--R.sub.1 ', --NR.sub.b --R.sub.1 ', or --NH--R.sub.1 ' in each of which R.sub.1 ' has meaning as defined for R.sub.1 provided that R.sub.1 ' in --SR.sub.1 ' does not represent hydrogen; R.sub.b represents lower alkyl; R.sub.4 represents hydroxymethyl provided that R.sub.2 does not represent either hydrogen or --NHR.sub.1 ' in which R.sub.1 ' represents either hydrogen or lower alkyl; or R.sub.4 represents lower alkoxymethyl or lower alkylthiomethyl; or R.sub.4 represents --CONHR.sub.6 in which R.sub.6 represents lower alkyl, aryl-lower alkyl, C.sub.3 -C.sub.6 -cycloalkyl or hydroxy-lower alkyl; pharmaceutically acceptable ester derivatives thereof in which free hydroxy groups are esterified in form of a pharmaceutically acceptable ester; and pharmaceutically acceptable salts thereof; methods for their preparation; and their use as adenosine receptor agonists are disclosed.