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    Noncardiotoxic pharmaceutical compounds
    6.
    发明授权
    Noncardiotoxic pharmaceutical compounds 失效
    非心脏毒性药物化合物

    公开(公告)号：US08088918B2

    公开(公告)日：2012-01-03

    申请号：US11199866

    申请日：2005-08-09

    申请人： Donald L. Barbeau

    发明人： Donald L. Barbeau

    IPC分类号： C07D491/00 ,  C07D291/08 ,  C07D223/18

    CPC分类号： C07F9/2458 ,  C07F9/2462 ,  C07F9/2466 ,  C07F9/247 ,  C07F9/2475 ,  C07F9/5532 ,  C07F9/5535 ,  C07F9/5728 ,  C07F9/58 ,  C07F9/59 ,  C07F9/6506 ,  C07F9/650952 ,  C07F9/6533 ,  C07F9/6547 ,  C07F9/65517 ,  C07F9/65527 ,  C07F9/655345 ,  C07F9/65583 ,  C07F9/65586 ,  C07F9/6561

    摘要： The present invention relates to novel noncardiotoxic compounds and pharmaceutical compositions useful in the treatment of a variety of disorders including the treatment of depression, allergies, psychoses, cancer and gastrointestinal disorders. In particular, the present invention describes pharmaceutical compositions that mitigate life-threatening arrhythmias such as torsade de pointes. Torsade de pointes is a particular cardiac problem associated with many therapeutic agents and has been implicated as a possible cause of sudden death, particularly in those individuals with a past history of disturbances of cardiac rhythm, myocardial infarction, congenital repolarization abnormalities and cardiac risk factors such as hyperlipidemia and age. This arrhythmia is a variant of paroxysmal ventricular tachycardia associated with a prolonged QTc interval or prominent U waves on the ECG. Torsade de pointes is potentially lethal because it can progress to ventricular fibrillation, life-threatening arrhythmias or precipitate sudden death.

    摘要翻译： 本发明涉及用于治疗各种疾病的新型非心脏毒性化合物和药物组合物，包括治疗抑郁症，过敏反应，精神病，癌症和胃肠道疾病。 特别地，本发明描述了减轻危及生命的心律失常的药物组合物，例如尖端扭转型室性心律失常。 特征是与许多治疗剂相关的特定的心脏问题，并且已经被认为是猝死的可能原因，特别是在具有过去心律失调史，心肌梗死，先天性复极化异常和心脏危险因素的个体中 作为高脂血症和年龄。 这种心律失常是与心电图延长的QTc间期或突出的U波相关的阵发性室性心动过速的变体。 由于可能会导致心室纤维性颤动，危及生命的心律失常或突然猝死，可能导致脚部扭转。

    STABILIZATION OF CONJUGATES COMPRISING A THIOUREA LINKER
    7.
    发明申请
    STABILIZATION OF CONJUGATES COMPRISING A THIOUREA LINKER 审中-公开
    包含一个连接器的连接器的稳定性

    公开(公告)号：US20110112291A1

    公开(公告)日：2011-05-12

    申请号：US12323942

    申请日：2008-11-26

    申请人： Eva Hoess ,  Rene Blind ,  Gerhard Fink ,  Hans-Joachim Kytzia

    发明人： Eva Hoess ,  Rene Blind ,  Gerhard Fink ,  Hans-Joachim Kytzia

    IPC分类号： C07D223/18

    CPC分类号： G01N33/532 ,  A61K47/55

    摘要： The present invention discloses a composition containing a conjugate comprising two moieties covalently linked by a thiourea linker and thiourea or a derivative thereof in free form. It also relates to a method for stabilizing a conjugate comprising two moieties covalently linked by a thiourea linker is described the method comprising the steps of providing the conjugate, adding thereto thiourea or a derivative thereof in free form and thereby stabilizing the conjugate and to the use of a composition containing a conjugate comprising two moieties covalently linked by a thiourea linker and thiourea or a derivative thereof in free form.

    摘要翻译： 本发明公开了一种含有共轭物的组合物，其包含由硫脲接头和硫脲或其衍生物以游离形式共价连接的两个部分。 本发明还涉及一种用于稳定缀合物的方法，其包含由硫脲连接体共价连接的两个部分，所述方法包括以下步骤：提供缀合物，向其中加入游离形式的硫脲或其衍生物，从而稳定缀合物和使用 包含共轭物的组合物，其包含由硫脲接头和硫脲或其衍生物以游离形式共价连接的两个部分。

    THERAPEUTIC AMINE-ARYLSULFONAMIDE CONJUGATE COMPOUNDS
    9.
    发明申请
    THERAPEUTIC AMINE-ARYLSULFONAMIDE CONJUGATE COMPOUNDS 审中-公开
    治疗氨基磺酰氟联合化合物

    公开(公告)号：US20100311727A1

    公开(公告)日：2010-12-09

    申请号：US12796236

    申请日：2010-06-08

    申请人： Philip F. MORGAN ,  James L. KELLEY

    发明人： Philip F. MORGAN ,  James L. KELLEY

    IPC分类号： A61K31/55 ,  C07D307/52 ,  A61K31/341 ,  C07D413/12 ,  A61K31/5377 ,  C07D223/18 ,  A61P3/00 ,  A61P25/00 ,  A61P25/24 ,  A61P25/02 ,  A61P25/06 ,  A61P25/30 ,  A61P25/16 ,  A61P25/28 ,  A61P25/22 ,  A61P3/04

    CPC分类号： C07D307/14 ,  A61K47/55 ,  C07D413/12

    摘要： Therapeutic amine-arylsulfonamide conjugate compounds, of the general formula: wherein R′ is [D-W-], hydroxyl, or alkoxyl; R″ is independently [D-W′-], hydrogen, alkoxy, alkyl, cycloalkyl, alkenyl, alkynyl or aryl, or R″ and R″ together with the nitrogen atom to which they are attached form a 4-, 5-, 6-, 7- or 8-membered ring optionally containing one or two further heteroatoms independently selected from nitrogen, oxygen and sulfur; D is independently a therapeutic amine radical comprising at least one nitrogen atom and optionally at least one oxygen atom coupled to W or W′ by a nitrogen or oxygen atom; W and W′ are a chemical bond or linker; wherein either R′ is [D-W-] or at least one R″ is [D-W′-], and pharmaceutically acceptable esters, amides, salts or solvates thereof, pharmaceutical compositions containing same, methods for their preparation, and their use in treating psychiatric, neurologic and metabolic disorders are disclosed.

    摘要翻译： 治疗性胺 - 芳基磺酰胺缀合物，其通式为：其中R'为[D-W-]，羟基或烷氧基; R“独立地是[DW']，氢，烷氧基，烷基，环烷基，烯基，炔基或芳基，或R”和R“与它们所连接的氮原子一起形成4-， 任选地含有一个或两个独立地选自氮，氧和硫的其它杂原子的7-或8-元环; D独立地是包含至少一个氮原子和任选的至少一个与氮或氧原子与W或W'偶合的氧原子的治疗性胺基; W和W'是化学键或接头; 其中R'为[DW-]或至少一个R“为[DW'-]及其药学上可接受的酯，酰胺，盐或溶剂合物，含有它们的药物组合物，其制备方法及其在治疗精神病学 ，公开了神经和代谢紊乱。