MODULATORS OF THE G PROTEIN-COUPLED FORMYL PEPTIDE RECEPTOR-LIKE 2 AND THEIR THERAPEUTIC USE AGAINST CELL DEATH-RELATED DISORDERS
    9.
    发明公开
    MODULATORS OF THE G PROTEIN-COUPLED FORMYL PEPTIDE RECEPTOR-LIKE 2 AND THEIR THERAPEUTIC USE AGAINST CELL DEATH-RELATED DISORDERS 审中-公开
    G蛋白调节剂的耦合甲酰肽受体样2和它的治疗用途针对细胞死亡相关疾病的

    公开(公告)号:EP1604212A2

    公开(公告)日:2005-12-14

    申请号:EP04757576.6

    申请日:2004-03-15

    摘要: The present invention relates to methods of identifying whether a candidate compound is a modulator of a G protein-coupled receptor (GPCR). In certain embodiments, the GPCR is human. In certain embodiments, the GPCR is expressed endogenously by neuronal cells or muscle cells. In certain embodiments, the GPCR is neuroprotective or myoprotective. In certain embodiments, the GPCR is a Humanin receptor. The present invention also relates to methods of using a modulator of said GPCR. A preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of neurodegenerative diseases in general, including Alzheimer's disease, Parkinson's disease, prion-associated disease, stroke and motor-neuron disease in particular, peripheral neuropathy, cerebral amyloid beta-protein angiopathy, and ischemic heart disease, including myocardial infarction and congestive heart failure. Podocarpa-8, 11, 13-trien-16-amide derivatives carrying at least a substituent on the aromatic ring are the identified modulators.

    摘要翻译: 本发明涉及标识是否候选化合物是G蛋白偶联受体(GPCR)的调节剂的方法。 在某些实施例中,GPCR是人。 在某些实施例中,GPCR是由神经元细胞或肌肉细胞内源性过表达。 在某些实施例中,GPCR是神经保护或肌肉保护。 在某些实施例中,GPCR是Humanin受体。 因此,本发明涉及使用所述GPCR的调节剂的方法。 优选的调节剂是激动剂。 本发明的激动剂是作为用于预防或治疗神经变性疾病,一般包括阿尔茨海默氏病,帕金森氏病,朊病毒相关病,中风,特别是运动神经元疾病,外周神经病变,脑淀粉样β蛋白血管病的治疗剂有用的 和缺血性心脏疾病,心肌梗死包含和充血性心脏衰竭。