预约演示
更新于：2025-02-22
Pittsburgh Compound B
更新于：2025-02-22
概要
基本信息
在研机构 |
最高研发阶段临床2期 |
首次获批日期- |
最高研发阶段(中国)- |
特殊审评- |
登录后查看时间轴
结构/序列
分子式C14H12N2OS |
InChIKeyZQAQXZBSGZUUNL-BJUDXGSMSA-N |
CAS号566170-04-5 |
关联
39
项与 Pittsburgh Compound B 相关的临床试验NCT04542603
Neuroinflammation and Age-associated Brain Pathology: Two Potential Mechanisms of Cognitive Impairment in Ovarian Cancer
NCT06439992
Beta Amyloid PET Imaging for Alzheimer Disease: [18F]-Fluselenamyl (Alternative Vehicle) Comparison With [11C]-PIB (FSA-PIB AD)
NCT05911178
Impact of Microglial Activation on Synaptic Density in Alzheimer's Disease
100 项与 Pittsburgh Compound B 相关的临床结果
登录后查看更多信息
100 项与 Pittsburgh Compound B 相关的转化医学
登录后查看更多信息
100 项与 Pittsburgh Compound B 相关的专利（医药）
登录后查看更多信息
521
项与 Pittsburgh Compound B 相关的文献（医药）2024-11-18ChemMedChem
Benzofuran and Benzo[b]thiophene‐2‐Carboxamide Derivatives as Modulators of Amyloid Beta (Aβ42) Aggregation
Article
作者: Rao, Praveen P. N. ; Chowdary Karuturi, Rahul ; Hefny, Ahmed A. ; Zhao, Yusheng ; Shakeri, Arash ; Beazely, Mike A. ; Singh, Kartar
Abstract:
A group of N‐phenylbenzofuran‐2‐carboxamide and N‐phenylbenzo[b]thiophene‐2‐carboxamide derivatives were designed and synthesized as a novel class of Aβ42 aggregation modulators. In the thioflavin‐T based fluorescence aggregation kinetics study, compounds 4 a, 4 b, 5 a and 5 b possessing a methoxyphenol pharmacophore were able to demonstrate concentration dependent inhibition of Aβ42 aggregation with maximum inhibition of 54 % observed for compound 4 b. In contrast, incorporation of a 4‐methoxyphenyl ring in compounds 4 d and 5 d led to a significant increase in Aβ42 fibrillogenesis demonstrating their ability to accelerate Aβ42 aggregation. Compound 4 d exhibited 2.7‐fold increase in Aβ42 fibrillogenesis when tested at the maximum concentration of 25 μM. These results were further confirmed by electron microscopy studies which demonstrates the ability of compounds 4 a, 4 b, 4 d, 5 a, 5 b and 5 d to modulate Aβ42 fibrillogenesis. Compounds 5 a and 5 b provided significant neuroprotection to mouse hippocampal neuronal HT22 cells against Aβ42‐induced cytotoxicity. Molecular docking studies suggest that the orientation of the bicyclic aromatic rings (either benzofuran or benzo[b]thiophene) plays a major role in moderating their ability to either inhibit or accelerate Aβ42 aggregation. Our findings support the application of these novel derivatives as pharmacological tools to study the mechanisms of Aβ42 aggregation.
2024-10-01NEUROBIOLOGY OF AGING
Multimodal investigation of neuropathology and neurometabolites in mild cognitive impairment and late-life depression with 11C-PiB beta-amyloid PET and 7T magnetic resonance spectroscopy
Article
作者: Smith, Gwenn S ; Leoutsakos, Jeannie-Marie ; Barker, Peter B ; Kraut, Michael A ; Zöllner, Helge J ; Oeltzschner, Georg ; Workman, Clifford I ; Davies-Jenkins, Christopher W ; Hupfeld, Kathleen E
Positron emission tomography (PET) and magnetic resonance spectroscopy (1H-MRS) are complementary techniques that can be applied to study how proteinopathy and neurometabolism relate to cognitive deficits in preclinical stages of Alzheimer's disease (AD)-mild cognitive impairment (MCI) and late-life depression (LLD). We acquired beta-amyloid (Aβ) PET and 7 T 1H-MRS measures of GABA, glutamate, glutathione, N-acetylaspartate, N-acetylaspartylglutamate, myo-inositol, choline, and lactate in the anterior and posterior cingulate cortices (ACC, PCC) in 13 MCI and 9 LLD patients, and 13 controls. We used linear regression to examine associations between metabolites, Aβ, and cognitive scores, and whether metabolites and Aβ explained cognitive scores better than Aβ alone. In the ACC, higher Aβ was associated with lower GABA in controls but not MCI or LLD patients, but results depended upon MRS data quality control criteria. Greater variance in California Verbal Learning Test scores was better explained by a model that combined ACC glutamate and Aβ deposition than by models that only included one of these variables. These findings identify preliminary associations between Aβ, neurometabolites, and cognition.
2024-09-01Current radiopharmaceuticals
Automated Synthesis of [11C]PiB via [11CH3OTf]-as Methylating Agent for
PET Imaging of β-Amyloid
Article
作者: Dixit, Manish ; Singh, Akhilesh K. ; Gambhir, Sanjay
Aim:::
Efficient synthesis of precursor from commercially available starting materials
and automated radiosynthesis of [11C]PiB using commercially available dedicated [11C]-
Chemistry module from the synthesized precursor.
Background:::
[11C]PiB is a promising radiotracer for PET imaging of β-Amyloid,
advancing Alzheimer's disease research. The availability of precursors and protocols
for efficient radiolabelling foster the applications of any radiotracer. Efficient synthesis
of PiB precursor was performed using anisidine and 4-nitrobenzoyl chloride as starting
materials in 5 steps, having addition, substitutions, and cyclization chemical methodologies.
This precursor was used for fully automated radiosynthesis of [11C]PiB in a commercially
available synthesizer, MPS-100 (SHI, Japan). The synthesized [11C]PiB was purified via
solid-phase methodology, and its quality control was performed by the quality and safety criteria
required for clinical use.
Methods:::
The synthesis of desired precursors and standard authentic compounds started
with commercially available materials with 70-80% yields. The standard analytical methods
were characterized all synthesized compounds. The fully automated [11C]-chemistry synthesizer
(MPS-100) used for radiosynthesis of [11C]PiB with [11C]CH3OTf acts as a methylating agent.
For radiolabelling, varied amounts of precursor and time of reaction were explored. The resulting
crude product underwent purification through solid-phase cartridges. The synthesized radiotracer
was analyzed using analytical tools such as radio TLC, HPLC, pH endo-toxicity, and
half-life.
Results:::
The precursor for radiosynthesis of [11C]PiB was achieved in excellent yield using
simple and feasible chemistry. A protocol for radiolabelling of precursor to synthesized
[11C]PiB was developed using an automated synthesizer. The crude radiotracer was purified by
solid-phase cartridge, with a decay-corrected radiochemical yield of 40±5% and radiochemical
purity of more than 97% in approx 20 minutes (EOB). The specific activity was calculated and
found in a 110-121 mCi/μmol range.
Conclusion:::
A reliable methodology was developed for preparing precursor followed by
fully automated radiolabeling using [11C]MeOTf as a methylating agent to synthesize
[11C]PiB. The final HPLC-free purification yielded more than 97% radiochemical purity
tracer within one radionuclide half-life. The method was reproducible and efficient for any
clinical center.
1
项与 Pittsburgh Compound B 相关的新闻（医药）2024-11-03
·奇点网
临床结果
100 项与 Pittsburgh Compound B 相关的药物交易
登录后查看更多信息
外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| - | Pittsburgh Compound B | - |
研发状态
10 条进展最快的记录, 后查看更多信息
登录
| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 多发性硬化症 | 临床2期 | 美国 | 2023-07-10 | |
| 阿尔茨海默症 | 临床2期 | 美国 | 2009-03-01 | |
| 酒精使用障碍 | 临床1期 | 美国 | 2018-12-01 | |
| 后皮质萎缩综合征 | 临床1期 | 美国 | 2012-11-01 | |
| 经皮质运动性失语 | 临床1期 | 美国 | 2010-03-01 | |
| 原发性进行性非流利性失语症 | 临床1期 | 美国 | 2010-03-01 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
N/A | - | C-11 Pittsburgh compound B (PiB) | 窪範製蓋顧簾繭遞憲顧(襯網遞壓獵蓋網憲網艱) = 構膚遞選膚鏇廠築襯襯 鏇觸繭選觸蓋窪廠積鏇 (獵獵衊壓窪選鏇襯顧鏇, 6.08) | - | 2024-06-09 | ||
F-18 flutemetamol (FMM) | 窪範製蓋顧簾繭遞憲顧(襯網遞壓獵蓋網憲網艱) = 糧繭蓋憲網壓鏇鏇鏇積 鏇觸繭選觸蓋窪廠積鏇 (獵獵衊壓窪選鏇襯顧鏇, 3.79) | ||||||
N/A | - | [11C]PiB LAFOV (Cerebral amyloid negative) | 鬱觸觸衊膚網壓構憲網(繭網網憲鑰膚鏇膚網憲) = 願觸襯選鹽鑰網積淵夢 衊鹹憲餘積觸製膚夢餘 (艱繭淵淵壓糧觸顧繭廠, 0.64 ~ 1.18) 更多 | - | 2023-08-28 | ||
[11C]PiB LAFOV (Cerebral amyloid positive) | 鬱觸觸衊膚網壓構憲網(繭網網憲鑰膚鏇膚網憲) = 壓選鏇範膚壓網鏇膚鹹 衊鹹憲餘積觸製膚夢餘 (艱繭淵淵壓糧觸顧繭廠, 0.57 ~ 1.25) 更多 | ||||||
N/A | - | Beta-amyloid (Down Syndrome (DS) cohort) | 鏇繭繭鏇獵夢壓醖獵遞(構選選衊壓夢衊繭獵選) = 夢膚蓋襯醖憲壓鏇膚餘 鑰網簾夢衊鑰糧鹹壓構 (鬱鏇鑰鏇鏇積製構鏇廠, 0.027) | - | 2023-08-28 | ||
Beta-amyloid (Neurotypical (NT) cohort) | 鏇繭繭鏇獵夢壓醖獵遞(構選選衊壓夢衊繭獵選) = 鏇選夢壓醖壓醖蓋選窪 鑰網簾夢衊鑰糧鹹壓構 (鬱鏇鑰鏇鏇積製構鏇廠, 0.009) | ||||||
N/A | - | 11C-Pittsburgh B (Amyloidosis group) | 獵鹽鑰壓觸獵獵衊窪獵(糧觸積餘製願衊齋壓衊) = PiB uptake in the liver was negatively correlated with ALP (r=-0.373) 憲獵遞憲觸廠構範顧鏇 (簾糧製淵淵廠齋夢選餘 ) 更多 | - | 2023-08-28 | ||
11C-Pittsburgh B (Control group) | |||||||
N/A | HOMA-IR | APOEε4+ | 60 | (Insulin resistance group (IR+)) | 襯願襯鹹憲襯顧範選構(餘範觸餘齋鑰廠獵齋鹽) = 遞窪廠鏇顧繭憲網蓋範 齋鏇壓範選積鏇鬱構觸 (選鹹範積積糧鹹選糧醖 ) 更多 | - | 2023-06-16 | |
(Control group (IR-)) | 襯願襯鹹憲襯顧範選構(餘範觸餘齋鑰廠獵齋鹽) = 壓顧衊遞網憲積網夢餘 齋鏇壓範選積鏇鬱構觸 (選鹹範積積糧鹹選糧醖 ) | ||||||
N/A | - | - | Bayesian Penalized Likelihood Reconstruction (OSEM reconstruction) | 壓窪糧夢製蓋艱膚蓋觸(遞鬱膚獵廠範艱蓋艱蓋) = 積膚蓋衊觸網蓋襯鏇衊 構壓鹹獵觸鹽鑰淵鏇淵 (衊範築壓襯襯壓夢遞衊, 0.5) | - | 2021-05-18 | |
Bayesian Penalized Likelihood Reconstruction (BPL reconstruction) | 壓窪糧夢製蓋艱膚蓋觸(遞鬱膚獵廠範艱蓋艱蓋) = 顧鏇築餘艱選鹽膚糧製 構壓鹹獵觸鹽鑰淵鏇淵 (衊範築壓襯襯壓夢遞衊, 0.5) | ||||||
N/A | APOE ε4 | 23 | (Amyloid-negative individuals) | 鏇艱築鏇齋簾糧網築積(衊壓願夢鬱鏇顧鏇憲鑰) = 淵廠鬱膚醖簾鹹鹹鬱膚 鹽糧鑰製艱醖觸簾廠鬱 (襯繭願積遞鏇夢糧獵鑰 ) | - | 2020-12-07 | |
N/A | - | 11C- and 18F- tracers (MS patients) | 觸衊糧積顧壓艱繭醖鑰(膚獵選醖糧積鏇廠鑰網) = 繭齋鹹蓋襯廠獵鏇壓糧 衊遞憲簾艱築範鹽獵醖 (獵願鹹壓廠積夢衊襯繭, 0.19) | - | 2019-09-10 | ||
11C- and 18F- tracers (Healthy controls) | 觸衊糧積顧壓艱繭醖鑰(膚獵選醖糧積鏇廠鑰網) = 齋顧顧獵餘積艱廠齋遞 衊遞憲簾艱築範鹽獵醖 (獵願鹹壓廠積夢衊襯繭, 0.21) | ||||||
N/A | 262 | Amyloid-PET (Aβ- group) | 鹹窪鏇觸憲鏇蓋網衊蓋(鬱夢夢糧築膚窪簾鬱艱) = 鬱淵壓網憲壓鑰蓋夢築 範積網糧鹽襯齋壓鏇構 (鬱網遞衊簾鏇鑰夢積壓 ) | 积极 | 2017-05-24 | ||
临床2期 | 89 | (Alzheimer's Disease) | 憲醖積壓鏇願選窪鏇鹹(繭鹽窪鏇鹽範製窪鹹廠) = 願齋蓋餘衊範襯襯廠襯 網觸衊築醖鹽鹽鹹襯獵 (糧網窪衊範膚蓋蓋餘糧, 衊窪築獵積網壓觸憲築 ~ 蓋繭顧遞鏇簾觸範鬱獵) 更多 | - | 2016-11-01 | ||
(Cognitive Normal Elderly) | 憲醖積壓鏇願選窪鏇鹹(繭鹽窪鏇鹽範製窪鹹廠) = 觸鬱鏇蓋膚醖蓋鏇構糧 網觸衊築醖鹽鹽鹹襯獵 (糧網窪衊範膚蓋蓋餘糧, 遞觸艱鹹膚網憲衊壓廠 ~ 網簾範鏇衊願鏇衊築艱) 更多 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
来和芽仔聊天吧
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用