Muscarinic antagonists with PARP and SIR modulating activity as agents for inflammatory diseases
    1.
    发明授权
    Muscarinic antagonists with PARP and SIR modulating activity as agents for inflammatory diseases 失效
    具有PARP和SIR调节活性的毒蕈碱拮抗剂作为炎性疾病的药剂

    公开(公告)号:US08039464B2

    公开(公告)日:2011-10-18

    申请号:US11632648

    申请日:2005-07-18

    摘要: The present invention relates generally to the cytoprotective activity of mixed muscarinic inhibition/PARP modulation and in particular to the use of dual inhibitors of M1 muscarinic receptor and poly(ADP-ribose) polymerase (PARP) as epithelioprotective medicaments, particularly as medicaments for the prevention and/or treatment of at least one of the common lung diseases associated with a significant inflammatory component such as severe sepsis, acute lung injury, acute respiratory distress syndrome, cystic fibrosis, asthma, allergic rhinitis, chronic obstructive pulmonary disease, pulmonary fibrosis, systemic sclerosis, pneumoconiosis or lung cancer. Particularly preferred compounds are condensed diazepinones, e.g. condensed benzodiazepinones such as pirenzepine or compounds which are metabolized to condensed benzodiazepinones such as olanzapine.

    摘要翻译: 本发明一般涉及混合毒蕈碱抑制/ PARP调节的细胞保护活性,特别涉及使用M1毒蕈碱受体和聚(ADP-核糖)聚合酶(PARP)的双重抑制剂作为上皮保护药物,特别是作为预防药物的药物 和/或治疗与显着的炎症成分相关的常见肺部疾病中的至少一种,例如严重脓毒症,急性肺损伤,急性呼吸窘迫综合征,囊性纤维化,哮喘,过敏性鼻炎,慢性阻塞性肺病,肺纤维化,全身性 硬化症,肺尘埃沉着病或肺癌。 特别优选的化合物是缩合的二氮杂酮,例如 缩合苯并二氮杂酮如哌仑西平或代谢为缩合苯并二氮杂酮如奥氮平的化合物。

    Use of finasteride, dutasteride and related compounds for the prevention or treatment of neurologically-associated disorders
    2.
    发明授权
    Use of finasteride, dutasteride and related compounds for the prevention or treatment of neurologically-associated disorders 失效
    使用非那雄胺,度他雄胺和相关化合物预防或治疗神经系统相关疾病

    公开(公告)号:US07998970B2

    公开(公告)日:2011-08-16

    申请号:US11720650

    申请日:2005-12-02

    摘要: The present invention relates to new pharmaceutical uses of 4-azasteroid compounds, in particular of Finasteride/Dutasteride/Dutasteride and Dutasteride, particularly preferred of Finasteride/Dutasteride/Dutasteride, and its pharmaceutically acceptable derivatives, and combinations comprising said compounds. The invention also features generally the use of a modulator compound of neuroprotective conditions via beta subunits of shaker-type voltage-gated potassium channels and/or via members of solute carriers family 25, in particular Aralar (member 12) and adenine-nucleotide translocators 1 & 2 (member 4 & 5) and/or via a 4-nitrophenylphosphatase domain and non-neuronal SNAP25-like protein homolog 1 (NIPSNAP 1) as a neuroprotective medicament, particularly as a medicament for the prevention and/or treatment of neurological diseases such as dementia, Parkinson, Alzheimer, schizophrenia or epilepsy. The demonstrated inhibition of the MPTP appears to constitute a novel principle applicable to all pathological conditions which have underlying excitotoxic/mitochondrial mechanisms, like: amyotrophic lateral sclerosis, Alzheimer's disease, depression, epilepsy, multiple sclerosis, pain, Parkinson's disease, schizophrenia, traumatic brain and spinal chord injury, stroke and other ischemic conditions in the brain.

    摘要翻译: 本发明涉及4-氮杂甾族化合物,特别是非那雄胺/度他雄胺/度他雄胺和度他雄胺,特别优选非那雄胺/度他雄胺/度他雄胺及其药学上可接受的衍生物以及包含所述化合物的组合的新药用途。 本发明还通常特征在于通过振动筛型电压门控钾通道的β亚基和/或通过溶质载体家族25,特别是Aralar(成员12)和腺嘌呤核苷酸转运体1的成员通过神经保护条件的调节剂化合物的使用 &2(成员4&5)和/或通过4-硝基苯基磷酸酶结构域和非神经元SNAP25样蛋白同系物1(NIPSNAP 1)作为神经保护药物,特别是作为预防和/或治疗神经疾病的药物 如痴呆症,帕金森病,阿尔茨海默病,精神分裂症或癫痫。 所显示的MPTP的抑制似乎构成适用于具有潜在兴奋性毒素/线粒体机制的所有病理状况的新颖原理,例如:肌萎缩性侧索硬化,阿尔茨海默病,抑郁症,癫痫,多发性硬化,疼痛,帕金森病,精神分裂症,创伤性脑 和脊髓损伤,脑卒中等缺血状况。

    Use of neuregulin-β as an indicator and/or target
    4.
    发明授权
    Use of neuregulin-β as an indicator and/or target 失效
    使用神经调节蛋白-β作为指标和/或靶标

    公开(公告)号:US07538197B2

    公开(公告)日:2009-05-26

    申请号:US10203450

    申请日:2001-02-09

    IPC分类号: A61K38/18 C07K14/475

    CPC分类号: C07K14/4756 A61K38/00

    摘要: The invention relates, inter alia, to the use of neuregulin-β as a target in a screening method for active compounds, in particular for exerting an influence on changes in calcium concentration which are mediated by glutamate receptors.The invention furthermore relates to the use of neuregulins, preferably a neuregulin isoform having an isoelectric point in the range from pH 4.3 to 5.0, as a target for detecting and/or exerting an influence on neuronal processes, in particular for exerting an influence on long-term memory. Neuregulins, in particular neuregulin-β and also substances which exert an influence on the status, i.e. the expression and/or post-translational modification, of neuregulin-β, can therefore be used as agents for controlling the course of, treating and/or alleviating neuronal diseases, e.g. Alzheimer's disease.

    摘要翻译: 本发明特别涉及在活性化合物的筛选方法中使用神经调节蛋白-β作为靶标,特别是对由谷氨酸受体介导的钙浓度变化的影响。 本发明还涉及使用神经调节蛋白,优选具有等电点在pH 4.3至5.0范围内的神经调节蛋白同种型作为检测和/或发挥对神经元过程的影响的目标,特别是对长时间的影响 - 记忆 因此,神经调节蛋白,特别是神经调节蛋白β以及对神经调节蛋白-β的状态(即表达和/或翻译后修饰)产生影响的物质可用作控制治疗和/或治疗的过程, 减轻神经元疾病,例如 阿尔茨海默氏病。

    USE OF NEUREGULIN-ß AS AN INDICATOR AND/OR TARGET
    6.
    发明申请
    USE OF NEUREGULIN-ß AS AN INDICATOR AND/OR TARGET 失效
    用作神经元ß作为指示剂和/或目标

    公开(公告)号:US20110244507A1

    公开(公告)日:2011-10-06

    申请号:US13035352

    申请日:2011-02-25

    IPC分类号: C12Q1/02 C12N5/079

    CPC分类号: C07K14/4756 A61K38/00

    摘要: The invention relates, inter alia, to the use of neuregulin-β as a target in a screening method for active compounds, in particular for exerting an influence on changes in calcium concentration which are mediated by glutamate receptors.The invention furthermore relates to the use of neuregulins, preferably a neuregulin isoform having an isoelectric point in the range from pH 4.3 to 5.0, as a target for detecting and/or exerting an influence on neuronal processes, in particular for exerting an influence on long-term memory. Neuregulins, in particular neuregulin-β and also substances which exert an influence on the status, i.e. the expression and/or post-translational modification, of neuregulin-β, can therefore be used as agents for controlling the course of, treating and/or alleviating neuronal diseases, e.g. Alzheimer's disease.

    摘要翻译: 本发明特别涉及使用神经调节蛋白 - 作为活性化合物的筛选方法的目标,特别是对由谷氨酸受体介导的钙浓度变化的影响。 本发明还涉及使用神经调节蛋白,优选具有等电点在pH 4.3至5.0范围内的神经调节蛋白同种型作为检测和/或发挥对神经元过程的影响的目标,特别是对长时间的影响 - 记忆 神经调节蛋白,特别是神经调节蛋白 并且因此也可以使用对神经调节蛋白 - bgr的状态,即表达和/或翻译后修饰产生影响的物质,作为用于控制神经元疾病进程,治疗和/或缓解神经元疾病的药剂。 阿尔茨海默氏病。

    USE OF FINASTERIDE, DUTASTERIDE AND RELATED COMPOUNDS FOR THE PREVENTION OR TREATMENT OF NEUROLOGICALLY-ASSOCIATED DISORDERS
    10.
    发明申请
    USE OF FINASTERIDE, DUTASTERIDE AND RELATED COMPOUNDS FOR THE PREVENTION OR TREATMENT OF NEUROLOGICALLY-ASSOCIATED DISORDERS 失效
    杀虫剂,杀虫剂及相关化合物用于预防或治疗神经病学相关疾病的使用

    公开(公告)号:US20090170889A1

    公开(公告)日:2009-07-02

    申请号:US11720650

    申请日:2005-12-02

    摘要: The present invention relates to new pharmaceutical uses of 4-azasteroid compounds, in particular of Finasteride/Dutasteride/Dutasteride and Dutasteride, particularly preferred of Finasteride/Dutasteride/Dutasteride, and its pharmaceutically acceptable derivatives, and combinations comprising said compounds. The invention also features generally the use of a modulator compound of neuroprotective conditions via beta subunits of shaker-type voltage-gated potassium channels and/or via members of solute carriers family 25, in particular Aralar (member 12) and adenine-nucleotide translocators 1 & 2 (member 4 & 5) and/or via a 4-nitrophenylphosphatase domain and non-neuronal SNAP25-like protein homolog 1 (NIPSNAP 1) as a neuroprotective medicament, particularly as a medicament for the prevention and/or treatment of neurological diseases such as dementia, Parkinson, Alzheimer, schizophrenia or epilepsy. The demonstrated inhibition of the MPTP appears to constitute a novel principle applicable to all pathological conditions which have underlying excitotoxic/mitochondrial mechanisms, like: amyotrophic lateral sclerosis, Alzheimer's disease, depression, epilepsy, multiple sclerosis, pain, Parkinson's disease, schizophrenia, traumatic brain and spinal chord injury, stroke and other ischemic conditions in the brain.

    摘要翻译: 本发明涉及4-氮杂甾族化合物,特别是非那雄胺/度他雄胺/度他雄胺和度他雄胺,特别优选非那雄胺/度他雄胺/度他雄胺及其药学上可接受的衍生物以及包含所述化合物的组合的新药用途。 本发明还通常特征在于通过振动筛型电压门控钾通道的β亚基和/或通过溶质载体家族25,特别是Aralar(成员12)和腺嘌呤核苷酸转运体1的成员通过神经保护条件的调节剂化合物的使用 &2(成员4&5)和/或通过4-硝基苯基磷酸酶结构域和非神经元SNAP25样蛋白同系物1(NIPSNAP 1)作为神经保护药物,特别是作为预防和/或治疗神经疾病的药物 如痴呆症,帕金森病,阿尔茨海默病,精神分裂症或癫痫。 所显示的MPTP的抑制似乎构成适用于具有潜在兴奋性毒素/线粒体机制的所有病理状况的新颖原理,例如:肌萎缩性侧索硬化,阿尔茨海默病,抑郁症,癫痫,多发性硬化,疼痛,帕金森病,精神分裂症,创伤性脑 和脊髓损伤,脑卒中等缺血状况。