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    • 1. 发明申请
    • NONCARDIOTOXIC PHARMACEUTICAL COMPOUNDS
    • 非药用药物化合物
    • WO2006020573A3
    • 2009-04-16
    • PCT/US2005028137
    • 2005-08-09
    • BARBEAU DONALD L
    • BARBEAU DONALD L
    • C07F9/06A61K31/41A61K31/435C07F9/02C07F9/08C07F9/28
    • C07F9/2458C07F9/2462C07F9/2466C07F9/247C07F9/2475C07F9/5532C07F9/5535C07F9/5728C07F9/588C07F9/591C07F9/65061C07F9/650958C07F9/6533C07F9/6547C07F9/65517C07F9/65527C07F9/655345C07F9/65583C07F9/65586C07F9/6561
    • 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.
    • 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。
    • 2. 发明申请
    • BIOADHESIVE PHARMACEUTICAL COMPOSITIONS
    • 生物药物组合物
    • WO2004064754A8
    • 2006-07-20
    • PCT/US2004001536
    • 2004-01-21
    • BARBEAU DONALD L
    • BARBEAU DONALD L
    • C07H5/04
    • C07H5/04
    • Disclosed are compounds having the formula (I) wherein R 2 is hydrogen, a monomeric glycoside or an oligomeric glycoside, R 3 is hydrogen, a monomeric glycoside, an oligomeric glycoside, or a group having the formula (II), R is a lower alkylene, R' is selected from the group consisting of moieties having the formula (III), (IV) and (V) where X = 0 or 1, Y = 0 or 1, R 1 is hydrogen or a pharmacologically active drug residue, R 8 a pharmacologically active drug residue, R 4 , R 5 , and R 6 are independently hydrogen, alkyl, aryl, aralkyl, and cycloalkyl or together form a nitrogen-containing ring, and R 7 is hydroxyl or hydroxyalkyl.
    • 公开了具有式(I)的化合物,其中R 2 2是氢,单体糖苷或低聚糖苷,R 3是氢,单糖苷,低聚糖苷, 或具有式(II)的基团,R是低级亚烷基,R'选自具有式(III),(IV)和(V)的部分,其中X = 0或1,Y = 0 或1,R 1是氢或药理活性药物残基,R 8是药理学活性药物残基,R 4,R 3, R 5和R 6独立地是氢,烷基,芳基,芳烷基和环烷基,或一起形成含氮环,并且R 7是羟基或 羟。