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    • 4. 发明授权
    • Methods for treating disorders associated with the central nervous
system using opticallly pure (+) cisapride
    • 使用光学纯(+)西沙必利治疗与中枢神经系统相关疾病的方法
    • US5629329A
    • 1997-05-13
    • US690242
    • 1996-07-19
    • Nancy M. GrayJames W. Young
    • Nancy M. GrayJames W. Young
    • C07D211/62A61K31/445A61K31/4468A61P1/00A61P1/08A61P1/10A61P1/14A61K31/395C07D409/06
    • A61K31/445A61K31/4468
    • Methods are disclosed utilizing the optically pure (+) isomer of cisapride. This compound is a potent drug for the treatment of gastro-esophageal reflux disease while substantially reducing the concomitant liability of adverse effects associated with the racemic mixture of cisapride. This compound is also useful in treating or preventing emesis while substantially reducing adverse effects associated with racemic cisapride. The optically pure (+) isomer of cisapride is also useful for the treatment of dyspepsia and such other conditions as may be related to the activity of (+) cisapride as a prokinetic agent, such as gastroparesis, constipation, post-operative ileus, and intestinal pseudo-obstruction, without the concomitant liability of adverse effects associated with the racemic mixture of cisapride. The (+) isomer of cisapride also exhibits longer duration of action than does racemic cisapride and is useful for treatment of disorders of the central nervous system.
    • 公开利用西沙必利的光学纯(+)异构体的方法。 该化合物是用于治疗胃食管反流疾病的有效药物,同时显着减少与西沙必利的外消旋混合物相关的副作用的伴随的责任。 该化合物也可用于治疗或预防呕吐,同时显着降低与西西沙必利素有关的不良反应。 西沙必利的光学纯的(+)异构体也可用于治疗消化不良和其它可能与(+)西沙必利作为促动力剂的活性相关的其它病症,例如胃轻瘫,便秘,手术后肠梗阻和 肠假性梗阻,没有与西沙必利的外消旋混合物相关的副作用的伴随的责任。 西沙必利的(+)异构体也表现出比外消旋西沙必利更长的作用时间,并且可用于治疗中枢神经系统疾病。
    • 6. 发明授权
    • Use of bridged tricyclic amine derivatives as anti-ischemic agents
    • 桥联三环胺衍生物作为抗缺血剂的用途
    • US5055468A
    • 1991-10-08
    • US428531
    • 1989-10-30
    • Nancy M. GrayPatricia C. Contreras
    • Nancy M. GrayPatricia C. Contreras
    • A61K31/135A61K31/16A61K31/445A61K31/495A61K31/505
    • A61K31/16A61K31/135A61K31/445A61K31/495A61K31/505
    • Certain bridged tricyclic amine compounds are described as being therapeutically effective in treatments of CNS disorders resulting from neurotoxic damage or neurodegenerative diseases, particularly those CNS disorders resulting from ischemic events. Compounds of particular interest for use as neuroprotective agents are those of the formula ##STR1## wherein each of R.sup.1 and R.sup.2 is independently selected from hydrido, loweralkyl, benzyl and phenyl; wherein each of R.sup.1 through R.sup.7 is independently selected from hydrido, loweralkyl, hydroxy, benzyl, phenyl, loweralkoxy, phenoxy, benzyloxy, halo and haloloweralkyl; wherein R.sup.18 may be selected from hydrido, loweralkyl, cycloalkyl of five or six carbon atoms, cycloalkylalkyl of six or seven carbon atoms, phenyl, hydroxyloweralkyl, and heteroaryl selected from saturated or fully unsaturated heterocyclic rings containing five to seven ring members of which one or two ring members are nitrogen atom; wherein each X is independently one or more groups selected from hydrido, hydroxy, loweralkyl, benzyl, phenyl, loweralkoxy, phenoxy, haloloweralkyl, halo, and lower-alkanoyl; and wherein each of R.sup.23 through R.sup.30 is independently selected from hydrido, lower alkyl, benzyl, phenyl and halo; wherein R.sup.18 together with one of R.sup.23, R.sup.24, R.sup.29 or R.sup.30 may form a fused heterocyclic ring containing five or six ring members; or a pharmaceutically-acceptable salt thereof.
    • 描述了某些桥连的三环胺化合物在治疗由神经毒性损伤或神经变性疾病,特别是由缺血事件引起的CNS障碍引起的CNS障碍中的治疗有效性。 用作神经保护剂的特别感兴趣的化合物是下式的化合物:其中R 1和R 2各自独立地选自氢,低级烷基,苄基和苯基; 其中R 1至R 7各自独立地选自氢,低级烷基,羟基,苄基,苯基,低级烷氧基,苯氧基,苄氧基,卤代和卤代低级烷基; 其中R 18可以选自氢或低级烷基,5或6个碳原子的环烷基,6或7个碳原子的环烷基烷基,苯基,羟基低级烷基和选自饱和或完全不饱和的含有5-7个环成员的杂环,其中一个或 两个环成员是氮原子; 其中每个X独立地是一个或多个选自氢,羟基,低级烷基,苄基,苯基,低级烷氧基,苯氧基,卤代低级烷基,卤素和低级烷酰基的基团。 并且其中R 23至R 30各自独立地选自氢,低级烷基,苄基,苯基和卤素; 其中R 18与R 23,R 24,R 29或R 30中的一个可以形成含有五个或六个环成员的稠合杂环; 或其药学上可接受的盐。