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    • 1. 发明申请
    • USE OF FINASTERIDE, DUTASTERIDE AND RELATED COMPOUNDS FOR THE PREVENTION OR TREATMENT OF NEUROLOGICALLY-ASSOCIATED DISORDERS
    • 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
    • WO2006058781A2
    • 2006-06-08
    • PCT/EP2005/012925
    • 2005-12-02
    • PROTEOSYS AGSOSKIC, VukicSCHRATTENHOLZ, André
    • SOSKIC, VukicSCHRATTENHOLZ, André
    • A61K31/58A61K31/568A61P25/00A61P25/28A61P25/16A61P25/24A61P25/18A61P25/08
    • C07J73/005A61K31/568A61K31/58A61K45/06A61K2300/00
    • 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.
    • 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,精神分裂症或癫痫症。 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。
    • 6. 发明申请
    • MUSCARINIC ANTAGONISTS WITH PARP AND SIR MODULATNG ACTIVITY AS AGENTS FOR INFLAMMATORY DISEASES
    • 具有PARP和SIR调节剂活性的炎症拮抗剂作为炎症性疾病的代理
    • WO2006008119A1
    • 2006-01-26
    • PCT/EP2005/007805
    • 2005-07-18
    • PROTEOSYS AGSCHRATTENHOLZ, André
    • SCHRATTENHOLZ, André
    • A61K31/5513
    • A61K31/554A61K31/55A61K31/551A61K31/5513A61K31/5517A61K31/553
    • x 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.
    • 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,特别是作为药物 预防和/或治疗与重要炎症成分相关的常见肺部疾病中的至少一种,例如严重败血症,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, 系统性硬化症,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。