哌哒甲酮(Pidazone) - 在研适应症：阿尔茨海默症，脑卒中_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点-

作用机制

神经炎抑制剂

治疗领域

在研适应症

非在研适应症

原研机构

在研机构

非在研机构

最高研发阶段临床1期

首次获批日期-

最高研发阶段(中国)临床1期

特殊审评特殊审批 (中国)

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结构

分子式C20H20N6O

InChIKeyZTJHTEHADIHZJS-UHFFFAOYSA-N

CAS号1252608-59-5

关联

6

项与哌哒甲酮相关的临床试验

NCT05806177 / Completed临床1期IIT

Safety, Tolerability and Pharmacokinetics of AD16 Tablets After Multiple Administration in Healthy Chinese Adult Subjects

This single-center, randomized, placebo-controlled, double-blind, dose-increasing study was designed to evaluate the safety, tolerability, and pharmacokinetics of multiple successive dosing in healthy Chinese adult subjects.In this study, 20 healthy adult subjects were enrolled in a multi-dose study in the 30mg and 40mg groups.

开始日期2020-05-26

申办/合作机构

中南大学湘雅医院

CTR20200977 / Completed临床1期

哌哒甲酮片在中国成人健康受试者中多次给药的安全性、耐受性及药代动力学研究

主要目的：评估中国成人健康受试者空腹条件下多次连续服用哌哒甲酮片后的安全性、耐受性;次要目的：评估中国成人健康受试者空腹条件下多次连续服用哌哒甲酮片后的药代动力学特性。

开始日期2020-05-26

申办/合作机构

广东华南新药创制中心

[+1]

CTR20191869 / Completed临床1期

评估高脂饮食对哌哒甲酮片在中国健康成人受试者中药代动力学影响研究

主要目的：评估高脂饮食对中国健康成人受试者单剂量服用哌哒甲酮片药代动力学特征的影响;次要目的：评估高脂饮食对中国健康成人受试者单剂量服用哌哒甲酮片的安全性的影响。

开始日期2019-09-18

申办/合作机构

广东华南新药创制中心

[+1]

100 项与哌哒甲酮相关的临床结果

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100 项与哌哒甲酮相关的转化医学

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100 项与哌哒甲酮相关的专利（医药）

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12

项与哌哒甲酮相关的文献（医药）

2024-09-01·Biomedicine & Pharmacotherapy

AD16 attenuates neuroinflammation induced by cerebral ischemia through down-regulating astrocytes A1 polarization

Article

作者: Huang, Cheng ; Huang, Zhihua ; Zhao, Guojian ; Luo, Zhengwei ; Tang, Xiaolu ; Liu, Gaigai ; Yu, Zining ; Feng, Zhong-Ping ; Sun, Hong-Shuo ; Yuan, Zhidong ; Su, Guangjun ; Zhang, Limei

A1 polarization of astrocytes mediated prolonged inflammation contributing to brain injury in ischemic stroke. We have previously shown that AD16 protects against neonatal hypoxic-ischemic brain damage in vivo and oxygen-glucose deprivation in vitro. More recently, AD16 has demonstrated safety, tolerability, and favorable pharmacokinetics in a randomized controlled phase I trial. In this study, we utilized a rat model of transient middle cerebral artery occlusion (tMCAO) to explore whether the anti-inflammatory compound AD16 protects against ischemic brain injury by regulating A1 polarization and its underlying mechanisms. Our results showed that AD16 treatment significantly reduced the brain infarcted volume and improved neurological function in tMCAO rats. GO analysis results show that differential genes among the Sham, tMCAO and AD16 treatment groups are involved in the regulation of cytokine and inflammatory response. KEGG enrichment pathways analysis mainly enriched in cytokine-cytokine receptor interaction, viral protein interaction with cytokine-cytokine receptor, TNF, chemokine, NF-κB and IL-17 signaling pathway. Furthermore, AD16 treatment decreased the permeability of the blood-brain barrier and suppressed neuroinflammation. AD16 treatment also significantly reduced the polarization of A1 and inhibited NF-κB and JAK2/STAT3 signaling pathways. This study demonstrates that AD16 protects against brain injury in ischemic stroke by reducing A1 polarization to suppress neuroinflammation through downregulating NF-κB and JAK2/STAT3 signaling. Our findings uncover a potential molecular mechanism for AD16 and suggest that AD16 holds promising therapeutic potential against cerebral ischemia.

2022-08-01·Neuroscience Bulletin2区 · 医学

AD-16 Protects Against Hypoxic-Ischemic Brain Injury by Inhibiting Neuroinflammation

2区 · 医学

Article

作者: Feng, Zhong-Ping ; Wan, Jiangfan ; Luo, Zhengwei ; Hu, Wenhui ; Ovcjak, Andrea ; Chen, Nai-Hong ; Huang, Zhihua ; Sun, Hong-Shuo

Neuroinflammation is a key contributor to the pathogenic cascades induced by hypoxic-ischemic (HI) insult in the neonatal brain. AD-16 is a novel anti-inflammatory compound, recently found to exert potent inhibition of the lipopolysaccharide-induced production of pro-inflammatory and neurotoxic mediators. In this study, we evaluated the effect of AD-16 on primary astrocytes and neurons under oxygen-glucose deprivation (OGD) in vitro and in mice with neonatal HI brain injury in vivo. We demonstrated that AD-16 protected against OGD-induced astrocytic and neuronal cell injury. Single dose post-treatment with AD-16 (1 mg/kg) improved the neurobehavioral outcome and reduced the infarct volume with a therapeutic window of up to 6 h. Chronic administration reduced the mortality rate and preserved whole-brain morphology following neonatal HI. The in vitro and in vivo effects suggest that AD-16 offers promising therapeutic efficacy in attenuating the progression of HI brain injury and protecting against the associated mortality and morbidity.

2020-12-11·ACS Pharmacology & Translational Science

Compound AD16 Reduces Amyloid Plaque Deposition and Modifies Microglia in a Transgenic Mouse Model of Alzheimer’s Disease

Article

作者: Ou, Yitao ; Hu, Wenhui ; Sun, Ping ; Yue, Hu ; Zhong, Xiaofen ; Pan, Guangjin ; Xing, Qi ; Deng, Wenmin

Microglial dysfunction is involved in the pathological cascade of Alzheimer's disease (AD). The regulation of microglial function may be a novel strategy for AD therapy. We previously reported the discovery of AD16, an antineuroinflammatory molecule that could improve learning and memory in the AD model. Here, we studied its properties of microglial modification in the AD mice model. In this study, AD16 reduced interleukin-1β (IL-1β) expression in the lipopolysaccharide-induced IL-1β-Luc transgenic mice model. Compared with mice receiving placebo, the group treated with AD16 manifested a significant reduction of microglial activation, plaque deposition, and peri-plaques microgliosis, but without alteration of the number of microglia surrounding the plaque. We also found that AD16 decreased senescent microglial cells marked with SA-β-gal staining. Furthermore, altered lysosomal positioning, enhanced Lysosomal Associated Membrane Protein 1 (LAMP1) expression, and elevated adenosine triphosphate (ATP) concentration were found with AD16 treatment in lipopolysaccharide-stimulated BV2 microglial cells. The underlying mechanisms of AD16 might include regulating the microglial activation/senescence and recovery of its physiological function via the improvement of lysosomal function. Our findings provide new insights into the AD therapeutic approach through the regulation of microglial function and a promising lead compound for further study.

100 项与哌哒甲酮相关的药物交易

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研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
阿尔茨海默症	药物发现	中国	广东华南新药创制中心	2019-01-30
认知障碍	药物发现	中国	中国科学院广州生物医药与健康研究院	2019-01-28
认知障碍	药物发现	中国	广东华南新药创制中心	2019-01-28
记忆障碍	药物发现	中国	中国科学院广州生物医药与健康研究院	2019-01-28
记忆障碍	药物发现	中国	广东华南新药创制中心	2019-01-28
轻度痴呆	药物发现	中国	中国科学院广州生物医药与健康研究院	2019-01-28
轻度痴呆	药物发现	中国	广东华南新药创制中心	2019-01-28
中度痴呆	药物发现	中国	广东华南新药创制中心	2019-01-28
中度痴呆	药物发现	中国	中国科学院广州生物医药与健康研究院	2019-01-28
脑卒中	药物发现	中国	中国科学院广州生物医药与健康研究院	2017-11-23