用于治疗认知障碍的 PDE4D 变构调节剂-猫眼课题宝

用于治疗认知障碍的 PDE4D 变构调节剂

批准号：

8675970

负责人：

Mark E Gurney

金额：

$23.54万

依托单位：

TETRA DISCOVERY PARTNERS, INC.

依托单位国家：

美国

项目类别：

财政年份：

2012

资助国家：

美国

项目状态：

已结题

起止时间：

2012-06-15 至 2017-05-31

来源：

https://reporter.nih.gov/project-details/8675970

关键词：

Activities of Daily Living Address Adult Affect Aftercare Alzheimer&apos s Disease Amyloid Amyloid beta-Protein Aricept Binding Biochemical Biological Assay Biological Availability Biological Markers Boxing Brain Brain Part CREB1 gene Central Nervous System Diseases Cholinesterase Inhibitors Clinical Clinical Trials Clinical dementia rating scale Cocrystallography Cognition Cognitive Collaborations Cyclic AMP-Dependent Protein Kinases Cytochrome P450 Dementia Demographic Aging Dendritic Spines Deposition Developed Countries Diagnostic Dimensions Dose Drug Targeting Elderly Enrollment Functional disorder Funding Generations Goals Health Hepatocyte Hippocampus (Brain)Human Impaired cognition In Vitro Individual Knowledge Lead Life Long-Term Potentiation Measures Medical Memory Mental Depression Metabolic Activation Metabolism Modeling Monkeys Morphology National Institute on Aging Oral Outcome Paired-Associate Learning Pathology Pathway interactions Patients Peptides Persons Pharmaceutical Preparations Phase Phase III Clinical Trials Plasma Population Prevention Property Publishing Recommendation Retrieval Rodent Rolipram Sales Senile Plaques Short-Term Memory Solubility Structure Sum System Testing Therapeutic Toxic effect United States National Institutes of Health Vomiting base cerebral atrophy clinical research site clinically significant cognitive function cooperative study coping design drug market experience genotoxicity impression improved in vivo inhibitor/antagonist instrument member mental state mild cognitive impairment mouse model neurochemistry neuroimaging neuron loss phosphodiesterase 4D phosphoric diester hydrolase pre-clinical programs scaffold screening synaptic function working group

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中文摘要

翻译

描述（由申请人提供）：由于美国人口老龄化，阿尔茨海默氏病（AD）是一种日益增加的医疗负担。 AD 是老年人中最常见的痴呆症，它会影响大脑中对记忆形成和检索很重要的部分，严重损害一个人独立生活和应对日常活动的能力。我们与 NIH 蓝图神经治疗计划合作，寻求开发 4 型磷酸二酯酶 (PDE4) 变构调节剂，以根据下面的目标产品简介改善认知。理想情况下，该治疗将改善 MCI 患者的认知并影响 AD 病理生理学，从而减缓向可能 AD 的转化。药物特性最低可接受结果理想结果主要药物适应症改善因可能 ADS 导致的轻度认知障碍 (MCI) 患者的认知能力从 MCI 到可能 AD 的转化速度减慢患者人群根据 NIAA/AA 工作组标准因可能 AD 导致 MCI 患者根据 NIAA/AA 工作组标准因可能 AD 导致 MCI 患者交付模式口服口服治疗持续时间慢性慢性治疗方案口服，每日一次口服，每日一次

英文摘要

DESCRIPTION (provided by applicant): Alzheimer's disease (AD) is an increasing medical burden due to the aging demographics of the US population. The most common form of dementia among older adults, AD affects parts of the brain important for memory formation and retrieval, seriously impairing a person's ability to live independently and cope with daily activities. In collaboration with the NIH Blueprint Neurotherapeutics Program, we seek to develop phosphodiesterase Type 4 (PDE4) allosteric modulators for improving cognition in accordance with the Target Product Profile below. Ideally, the therapeutic will improve cognition in MCI patients and impact AD pathophysiology, thereby slowing conversion to probable AD. Drug PropertiesMinimum Acceptable ResultIdeal ResultPrimary Drug IndicationImprovement of cognition in persons with Mild Cognitive Impairment (MCI) due to probable ADSlowing of conversion from MCI to probable ADPatient PopulationPatients with MCI due to probable AD according to the NIAA/AA working group criteriaPatients with MCI due to probable AD according to the NIAA/AA working group criteriaDelivery ModeOralOralTreatment DurationChronicChronicRegimenOral, once dailyOral, once daily

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