PDE4D Allosteric Modulators for Treating Cognitive Impairment
PDE4D Allosteric Modulators for Treating Cognitive Impairment
批准号:
8485701
负责人:
Mark E Gurney
金额:
$23.54万
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
关键词:
2-cyclopentyl-5-(5-isoquinolylsulfonyl)-6-nitro-1H-benzo(D)imidazoleActive SitesAffectAlzheimer&aposs DiseaseAnesthesia proceduresBindingBiochemicalBiological AssayBiological AvailabilityBoxingBrainBrain PartBuffersCellsCellular AssayCentral Nervous System DiseasesChemosensitizationClinicalClinical TrialsClinical dementia rating scaleCognitionCognitiveCollaborationsCrystallizationCyclic AMPCytochrome P450DementiaDemographic AgingDendritic SpinesDeveloped CountriesDoseDrug TargetingElderlyForskolinFunctional disorderGenerationsHealthHepatocyteHumanHumulusImpaired cognitionIn VitroInhibitory Concentration 50KetamineKineticsKnowledgeLeadLifeMedicalMemoryMental DepressionMetabolic ActivationMetabolismModelingMonkeysMusOralPathologyPatientsPersonsPharmaceutical PreparationsPhasePlasmaPopulationPropertyPublishingRetrievalRodentRolipramSafetySolubilityStructureSumSystemTestingTherapeuticToxic effectUnited States National Institutes of HealthVomitingXylazinebasecognitive functioncopingdesignexperiencegenotoxicityimprovedin vivoindexinginhibitor/antagonistmembermild cognitive impairmentmouse modelnovelobject recognitionphosphodiesterase 4Dphosphoric diester hydrolaseprogramsresponsescaffoldscreeningsynaptic functionworking group
中文摘要
点击翻译按钮获取中文摘要
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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