&bgr;3-adrenoreceptor agonists, agonist compositions and methods of making and using the same
    82.
    发明授权
    &bgr;3-adrenoreceptor agonists, agonist compositions and methods of making and using the same 失效
    β3-肾上腺素受体激动剂,激动剂组合物及其制备和使用方法

    公开(公告)号:US06593341B2

    公开(公告)日:2003-07-15

    申请号:US10149953

    申请日:2002-06-17

    IPC分类号: C07D22102

    CPC分类号: C07D217/18 C07D217/20

    摘要: The invention provides compounds useful as &bgr;3-adrenorecptor agonists and pharmaceutical compositions comprising such compounds. The invention further includes a method for stimulating, regulating, and modulating metabolism in fats of adipose tissue in mammals by administering an effective amount of a compound of the invention.

    摘要翻译: 本发明提供了可用作β3肾上腺素摄取激动剂的化合物和包含这些化合物的药物组合物。 本发明还包括通过施用有效量的本发明化合物来刺激,调节和调节哺乳动物脂肪组织脂肪代谢的方法。

    Drugs for the treatment of cardiac arrest and other shock states
    83.
    发明授权
    Drugs for the treatment of cardiac arrest and other shock states 失效
    用于治疗心脏骤停和其他休克状态的药物

    公开(公告)号:US5527830A

    公开(公告)日:1996-06-18

    申请号:US312665

    申请日:1994-09-26

    CPC分类号: C07C215/52 A61K31/137

    摘要: The invention relates to new drugs for augmenting perfusion pressure administered during cardiopulmonary resuscitation and other shock states. The compounds include phenylethanolamines and imidazolines, and fluorinated derivatives thereof, which act on adrenergic receptors in patients. The compounds of the invention enhance neurologic outcome and survival, and decrease ventricular dysrhythmias in patients suffering cardiac arrest and other shock states, relative to the outcomes, survival, and post defibrillation ventricular dysrhythmias in conventional therapy for use in resuscitation.

    摘要翻译: 本发明涉及用于增加在心肺复苏和其他休克状态期间施用的灌注压的新药物。 化合物包括苯乙醇胺和咪唑啉及其氟化衍生物,其作用于患者的肾上腺素能受体。 本发明的化合物相对于用于复苏的常规治疗中的结果,存活和除颤后室性心律失常,增加了心脏骤停和其他休克状态患者的神经学结果和存活,并降低了心室心律失常。

    5-fluoro-and 8-fluoro-trimetoquinol compounds and the processes for
their preparation
    84.
    发明授权
    5-fluoro-and 8-fluoro-trimetoquinol compounds and the processes for their preparation 失效
    5-氟 - 和8-氟 - 三甲基喹啉化合物及其制备方法

    公开(公告)号:US4737504A

    公开(公告)日:1988-04-12

    申请号:US890490

    申请日:1986-07-25

    IPC分类号: C07D217/20 A61K31/47

    CPC分类号: C07D217/20

    摘要: The present invention relates to novel 5-fluoro- and 8-fluoro-trimetoquinol compounds of the general formula I wherein X.sub.1 =F,X.sub.2 =H or X.sub.1 =H,X.sub.2 =F ##STR1## The present invention also relates to a process for making the 5-fluoro- and 8-fluoro-trimetoquinol compounds by condensation of an appropriately substituted phenethylamine to afford an appropriately substituted phenethylacetamide compound. The amides are cyclized to give appropriately substituted intermediate dihydroisoquinolines. Without isolation, the dihydroisoquinolines are reduced to give appropriately substituted tetrahydroisoqinolines. The hydrochloride salts of tetrahydroisoqinolines are prepared and subjected to hydrogenolysis, to give the fluorine substituted trimetoquinol compounds of the present invention. The present invention also encompasses the preparation of the phenethylamines by reducing appropriately substituted benzylcyanides and to the preparation of an intermediate benzylcyanide compound by converting a fluorine substituted methoxyphenol compound, under aminomethylation conditions into a N, N-dimethyl-4-hydroxy-3-methoxy-5-fluorobenzylamine. The benzylamine is converted to benzylnitrile and a functional group shuffle is carried out which yields the appropriately substituted benzylcyanide compound. In a composition aspect, the present invention encompasses novel pharmaceutical compositions comprising a compound of the formula I, together with a physiologically acceptable carrier or excipient, in an amount sufficient to increase .beta..sub.2 -adrenergic and antithrombotic activities while simultaneously decreasing the .beta..sub.1 -adrenergic activity in mammals, including humans. The compounds of the invention are useful in the treatment of pulmonary, cardiovascular or thromboembolic disorders.

    摘要翻译: 本发明涉及通式I的新的5-氟 - 和8-氟 - 三甲基喹诺酮化合物,其中X1 = F,X2 = H或X1 = H,X2 = F。本发明还涉及一种 通过适当取代的苯乙胺的缩合制备5-氟 - 和8-氟 - 三甲基喹啉化合物,得到适当取代的苯乙基乙酰胺化合物。 使酰胺环化,得到适当取代的中间体二氢异喹啉。 不分离,将二氢异喹啉还原,得到适当取代的四氢异喹啉。 制备四氢异喹啉的盐酸盐并进行氢解,得到本发明的氟取代的三甲基喹诺酮化合物。 本发明还包括通过在氨基甲基化条件下将氟取代的甲氧基苯酚化合物转化成N,N-二甲基-4-羟基-3-甲氧基的方法,通过还原适当取代的苄基氰化物和制备中间体苄基氰化合物来制备苯乙胺 -5-氟苄胺。 将苄胺转化为苄基腈,进行官能团混洗,产生适当取代的苄基氰化合物。 在组合物方面,本发明包括新颖的药物组合物,其包含式I化合物以及生理上可接受的载体或赋形剂,其量足以增加β2-肾上腺素能和抗血栓形成活性,同时降低β1-肾上腺素能 哺乳动物,包括人类的活动。 本发明的化合物可用于治疗肺,心血管或血栓栓塞障碍。

    Yohimbine dimers exhibiting binding selectivities for &agr;2 adrenergic receptors
    87.
    发明授权
    Yohimbine dimers exhibiting binding selectivities for &agr;2 adrenergic receptors 失效
    育亨宾二聚体显示α2肾上腺素能受体的结合选择性

    公开(公告)号:US06638943B2

    公开(公告)日:2003-10-28

    申请号:US10106521

    申请日:2002-03-25

    IPC分类号: A61K31475

    CPC分类号: C07D519/00

    摘要: The present invention relates to yohimbine dimer compounds, pharmaceutical compositions containing such dimer compounds, methods of making such dimer compounds, and uses thereof. The yohimbine dimer compounds include compounds of formula (I): where R is any linker molecule which affords a yohimbine dimer that has activity as an &agr;2-AR antagonist and has selectivity for an &agr;2-AR subtype over another &agr;2-AR subtype.

    摘要翻译: 本发明涉及育亨宾二聚体化合物,含有这种二聚体化合物的药物组合物,制备这种二聚体化合物的方法及其应用。 育亨宾二聚体化合物包括式(I)化合物:其中R是提供具有作为α2-AR拮抗剂的活性的育亨宾二聚体并且对α2-AR亚型具有对另一α2-AR亚型的选择性的任何连接分子。

    Regenerable MgO Promoted Metal Oxide Oxygen Carriers for Chemical Looping Combustion
    88.
    发明申请
    Regenerable MgO Promoted Metal Oxide Oxygen Carriers for Chemical Looping Combustion 有权
    用于化学循环燃烧的可再生MgO促进金属氧化物载体

    公开(公告)号:US20130316292A1

    公开(公告)日:2013-11-28

    申请号:US13477274

    申请日:2012-05-22

    IPC分类号: F23C13/00 F23C13/08

    摘要: The disclosure provides an oxygen carrier comprised of a plurality of metal oxide particles in contact with a plurality of MgO promoter particles. The MgO promoter particles increase the reaction rate and oxygen utilization of the metal oxide when contacting with a gaseous hydrocarbon at a temperature greater than about 725° C. The promoted oxide solid is generally comprised of less than about 25 wt. % MgO, and may be prepared by physical mixing, incipient wetness impregnation, or other methods known in the art. The oxygen carrier exhibits a crystalline structure of the metal oxide and a crystalline structure of MgO under XRD crystallography, and retains these crystalline structures over subsequent redox cycles. In an embodiment, the metal oxide is Fe2O3, and the gaseous hydrocarbon is comprised of methane.

    摘要翻译: 本公开提供了由与多个MgO促进剂颗粒接触的多个金属氧化物颗粒构成的氧载体。 当在大于约725℃的温度下与MgO气体烃接触时,MgO助催化剂颗粒增加了金属氧化物的反应速率和氧气利用率。促进的氧化物固体通常包含小于约25wt。 %MgO,并且可以通过物理混合,初始润湿浸渍或本领域已知的其它方法制备。 氧载体在XRD晶体学下表现出金属氧化物的结晶结构和MgO的结晶结构,并且在随后的氧化还原循环中保留这些晶体结构。 在一个实施方案中,金属氧化物是Fe 2 O 3,并且气态烃由甲烷组成。