NEUROPROTECTIVE MULTIFUNCTIONAL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM
    6.
    发明申请
    NEUROPROTECTIVE MULTIFUNCTIONAL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM 审中-公开
    神经保护性多功能化合物和包含它们的药物组合物

    公开(公告)号:WO2010086860A3

    公开(公告)日:2011-02-24

    申请号:PCT/IL2010000080

    申请日:2010-01-31

    摘要: Multifunctional compounds are provided, comprising two or more functional moieties selected from: (i) a moiety that imparts an iron chelator function; (ii) a moiety that imparts a neuroprotective function; (iii) a moiety that imparts combined antiapoptotic, neuroprotective and/or neurorestorative functions; (iv) a moiety that imparts brain MAO inhibition, preferably with little or no MAO inhibition in liver and small intestine; (v) a moiety that imparts cholinesterase inhibitory function; and (vi) a moiety that imparts an N-methyl-D-aspartic acid receptor (NMDAR) inhibition, and pharmaceutically acceptable salts and optical isomers thereof. The multifunctional compounds are useful in the treatment or prevention of diseases, disorders or conditions that can be prevented and/or treated by iron chelation therapy, and/or neuroprotection and/or neurorestoration, and/or apoptosis inhibition and/or MAO inhibition and/or cholinesterase inhibition and/or NMADR inhibition. The present invention encompasses compounds of the formulas I to Vl.

    摘要翻译: 提供多官能化合物,其包含两个或多个选自以下的官能部分:(i)赋予铁螯合剂功能的部分; (ii)赋予神经保护功能的部分; (iii)赋予组合的抗细胞凋亡,神经保护和/或神经恢复功能的部分; (iv)赋予脑MAO抑制的部分,优选在肝脏和小肠中几乎没有MAO抑制作用; (v)赋予胆碱酯酶抑制功能的部分; 和(vi)赋予N-甲基-D-天冬氨酸受体(NMDAR)抑制的部分及其药学上可接受的盐和旋光异构体。 多官能化合物可用于治疗或预防可通过铁螯合治疗和/或神经保护和/或神经恢复,和/或凋亡抑制和/或MAO抑制和/或MAO抑制和/或治疗的/ 或胆碱酯酶抑制和/或NMADR抑制。 本发明包括式I至VI的化合物。

    NEUROPROTECTIVE IRON CHELATORS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM
    7.
    发明申请
    NEUROPROTECTIVE IRON CHELATORS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM 审中-公开
    神经保护性铁器钳和包含它们的药物组合物

    公开(公告)号:WO2004041151A2

    公开(公告)日:2004-05-21

    申请号:PCT/IL2003/000932

    申请日:2003-11-07

    IPC分类号: A61K

    摘要: Novel iron chelators exhibiting neuroprotective and good transport properties are useful in iron chelation therapy for treatment of a disease, disorder or condition associated with iron overload and oxidative stress, eg. a neurodegenerative or cerebrovascular disease or disorder, a neoplastic disease, hemochromatosis, thalassemia, a cardiovascular disease, diabetes, a inflammatory disorder, anthracycline cardiotoxicity, a viral infection, a protozoal infection, a yeast infection, retarding ageing, and prevention and/or treatment of skin ageing and skin protection against sunlight and/or UV light. The iron chelator function is provided by a 8-hydroxyquinoline, a hydroxypyridinone or a hydroxamate moiety, the neuroprotective function is imparted to the compound e.g. by a neuroprotective peptide, and a combined antiapoptotic and neuroprotective function by a propargyl group.

    摘要翻译: 显示出神经保护和良好转运性质的新型铁螯合剂可用于铁螯合治疗用于治疗与铁过载和氧化应激相关的疾病,病症或病症,例如, 神经变性或脑血管疾病或病症,肿瘤性疾病,血色素沉着病,地中海贫血,心血管疾病,糖尿病,炎性病症,蒽环类心脏毒性,病毒感染,原生动物感染,酵母感染,延迟衰老以及预防和/或治疗 的皮肤老化和皮肤防晒防晒和/或紫外线。 铁螯合剂功能由8-羟基喹啉,羟基吡啶酮或异羟肟酸盐部分提供,神经保护功能被赋予化合物例如 通过神经保护肽,以及由炔丙基组合的抗细胞凋亡和神经保护功能。

    USE OF R-ENANTIOMER OF N-PROPARGYL-1-AMINOINDAN, SALTS, AND COMPOSITIONS THEREOF
    10.
    发明申请
    USE OF R-ENANTIOMER OF N-PROPARGYL-1-AMINOINDAN, SALTS, AND COMPOSITIONS THEREOF 审中-公开
    N-丙基-1-氨基茚的R-增效剂,其盐及其组合物的使用

    公开(公告)号:WO1996037199A1

    公开(公告)日:1996-11-28

    申请号:PCT/US1996007465

    申请日:1996-05-22

    IPC分类号: A61K31/135

    摘要: The subject invention provides R(+)-N-propargyl-1-aminoindan and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions containing same. The subject invention also provides methods of treating a subject afflicted with Parkinson's disease, a memory disorder, dementia, depression, hyperactive syndrome, an effective illness, a neurodegenerative disease, a neurotoxic injury, stroke, brain ischemia, a head trauma injury, a spinal trauma injury, neurotrauma, schizophrenia, an attention deficit disorder, multiple sclerosis, or withdrawal symptoms, using R(+)-N-propargyl-1-aminoindan or the pharmaceutically acceptable salt of the subject invention. The subject invention further provides a method of preventing nerve damage in a subject. Finally, the subject invention provides methods of preparing R(+)-N-propargyl-1-aminoindan, a salt thereof, and racemic N-propargyl-1-aminoindan.

    摘要翻译: 本发明提供了R(+) - N-炔丙基-1-氨基茚满及其药学上可接受的盐,以及含有它们的药物组合物。 本发明还提供了治疗患有帕金森病,记忆障碍,痴呆,抑郁症,多动症综合征,有效疾病,神经变性疾病,神经毒性损伤,中风,脑缺血,头部创伤损伤,脊髓损伤的受试者的方法 使用R(+) - N-炔丙基-1-氨基茚满或本发明的药学上可接受的盐,创伤,神经损伤,精神分裂症,注意力缺陷障碍,多发性硬化或戒断症状。 本发明进一步提供一种预防受试者的神经损伤的方法。 最后,本发明提供了制备R(+) - N-炔丙基-1-氨基茚满其盐和外消旋的N-炔丙基-1-氨基茚满的方法。