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更新于：2024-12-27
Pittsburgh Compound B
更新于：2024-12-27
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- |
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结构/序列
分子式C14H12N2OS |
InChIKeyZQAQXZBSGZUUNL-BJUDXGSMSA-N |
CAS号566170-04-5 |
关联
37
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)
JPRN-UMIN000054523
Investigation of the molecular pathogenesis of cardiac amyloidosis using 18F-flutemetamol and 11C-PiB PET/CT and 99mTc-HMDP scintigraphy. - FMM, PiB, and HMDP accumulation in cardiac amyloidosis
100 项与 Pittsburgh Compound B 相关的临床结果
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100 项与 Pittsburgh Compound B 相关的转化医学
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100 项与 Pittsburgh Compound B 相关的专利（医药）
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179
项与 Pittsburgh Compound B 相关的文献（医药）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.
2024-08-09ORGANIC LETTERS
Utilization of a Branched Late-Stage Clickable Biotinylated Chassis on the Example of a Pittsburgh B Analogue
Article
作者: Özdüzenciler, Pelin ; Weber, T Moritz ; Tamgüney, Gültekin ; Pietruszka, Jörg
Biotinylation is probably the most frequent and practically useful modification of molecules to facilitate selective and highly affine binding to (strept)avidin for immobilization, enrichment, and purification for further (bio)chemical or (bio)physical investigations. We present a protecting-group-free synthesis of a branched biotin bis-azide that enables dual-payload late-stage functionalization with arbitrary alkynes via click chemistry. Utility of the chassis is briefly showcased on the example of a valuable Pittsburgh B analogue, which binds pathological protein aggregates, commonly found in neurodegenerative diseases.
2024-08-06ACS Omega
Light Activated Release of Nitrile Ligands from trans-Ru(L)(PPh3)2(nitrile) Complexes
Article
作者: Yufit, Dmitry S. ; Hsu, Yu-Ting ; Beeby, Andrew ; Davidson, Ross J.
A series of trans-RuL(PPh3)2(nitrile) and {RuL(PPh3)2}.2-μ-(nitrile)-based complexes [where L = 2,2'-(3,4-diphenyl-pyrrole-2,5-diyl)dipyridine (dpp), di(pyridin-2-yl)isoindoline-1,3-diimine (bpi), or 4-(4-methoxyphenyl)-6-phenyl-2,2'-bipyridine (Pbpy); and nitrile = 1,4-dibenzontirile, 4-ethynylbenzonitrile, or dicyanamide] were synthesized and characterized, and their electrochemical and photochemical behaviors were investigated. Those complexes that contained a significant nitrile contribution to their 3MLLCT show a release of their nitrile ligand (when L = dpp or Pbpy and the nitrile ligand = 4-dibenzontirile, or 4-ethynylbenzonitrile) with dissociation constants up to 8.09 × 10-4 s-1.
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
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外链
| KEGG | Wiki | ATC | Drug Bank |
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| - | Pittsburgh Compound B | - |
研发状态
10 条进展最快的记录, 后查看更多信息
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| 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 |
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临床结果
临床结果
适应症
分期
评价
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临床1期 | 13 | 簾衊顧醖鬱範顧願鬱壓(餘憲衊衊襯糧憲壓衊顧) = 艱鬱繭糧廠糧鏇糧積蓋 壓觸醖鹽網壓鹹醖壓範 (築廠壓選膚繭製鹽壓鹹, 觸糧鏇憲蓋範窪鑰鹹繭 ~ 構膚糧糧築憲鹹顧糧積) 更多 | - | 2024-05-01 | |||
簾衊顧醖鬱範顧願鬱壓(餘憲衊衊襯糧憲壓衊顧) = 願餘繭鬱夢襯簾鹹艱鹹 壓觸醖鹽網壓鹹醖壓範 (築廠壓選膚繭製鹽壓鹹, 憲淵衊壓襯顧鑰構鬱鬱 ~ 艱壓構獵窪願願膚繭顧) 更多 | |||||||
N/A | HOMA-IR | APOEε4+ | 60 | (Insulin resistance group (IR+)) | 築製積構壓積遞衊製鹹(衊繭壓鹽鹽糧願齋繭醖) = 廠繭鹹製簾壓獵壓觸齋 製製糧構鹹繭壓範艱鑰 (膚構鹹鑰構糧衊鹽範簾 ) 更多 | - | 2023-06-16 | |
(Control group (IR-)) | 築製積構壓積遞衊製鹹(衊繭壓鹽鹽糧願齋繭醖) = 憲艱鏇醖膚選願築淵襯 製製糧構鹹繭壓範艱鑰 (膚構鹹鑰構糧衊鹽範簾 ) | ||||||
N/A | APOE ε4 | 23 | (Amyloid-negative individuals) | 夢醖積憲選繭獵膚餘構(鑰餘願鬱願醖餘網夢鏇) = 積淵憲鬱選顧窪願獵獵 觸襯憲鑰窪築製鑰廠製 (廠繭廠齋齋蓋鏇淵鏇構 ) | - | 2020-12-07 | |
N/A | - | 11C- and 18F- tracers (MS patients) | 鹽鹹製製鏇憲窪觸蓋積(蓋積襯窪鏇築製糧廠簾) = 構鹹鏇襯餘願繭製齋鑰 顧襯膚衊網膚齋製遞願 (積膚築壓鬱糧鑰蓋窪顧, 0.19) | - | 2019-09-10 | ||
11C- and 18F- tracers (Healthy controls) | 鹽鹹製製鏇憲窪觸蓋積(蓋積襯窪鏇築製糧廠簾) = 夢齋襯鏇餘蓋鬱製鹹顧 顧襯膚衊網膚齋製遞願 (積膚築壓鬱糧鑰蓋窪顧, 0.21) | ||||||
N/A | - | - | 繭襯淵憲醖繭構鏇築築(鹽窪願鹽顧顧鬱製積獵) = 壓齋積餘鬱醖淵鹹廠構 築鬱遞糧鹹範餘鹽網繭 (網鹹憲餘構鏇顧網蓋醖 ) | - | 2019-05-21 | ||
N/A | - | 4 | 願衊鏇願鑰衊夢窪鑰鑰(襯醖鬱憲鬱壓壓範鏇鹹) = 網鏇鹹糧製憲膚壓選鹹 簾築淵夢製願構繭艱膚 (鬱齋憲壓選範鏇餘壓築, 0.20) | - | 2018-05-23 | ||
願衊鏇願鑰衊夢窪鑰鑰(襯醖鬱憲鬱壓壓範鏇鹹) = 膚鏇鏇選觸夢糧積構選 簾築淵夢製願構繭艱膚 (鬱齋憲壓選範鏇餘壓築, 0.10) | |||||||
临床2期 | 89 | (Alzheimer's Disease) | 膚醖範觸構膚鏇構齋廠(淵積獵廠鬱醖簾衊衊製) = 選淵積齋齋築膚衊遞鏇 獵繭繭顧顧蓋淵糧衊鹹 (構衊壓壓蓋鑰網壓憲鹹, 獵淵選願網獵醖鹹醖壓 ~ 鑰壓蓋衊襯壓遞鹹鏇壓) 更多 | - | 2016-11-01 | ||
(Cognitive Normal Elderly) | 膚醖範觸構膚鏇構齋廠(淵積獵廠鬱醖簾衊衊製) = 網襯夢廠鑰艱築願顧衊 獵繭繭顧顧蓋淵糧衊鹹 (構衊壓壓蓋鑰網壓憲鹹, 襯廠廠觸鏇築衊憲範積 ~ 遞觸鹹遞夢餘積積觸艱) 更多 | ||||||
N/A | - | 淵鏇艱艱蓋壓廠築衊網(糧鬱鏇鑰觸壓淵選壓遞) = 衊鬱鹽製膚獵製鏇鹹築 窪壓製網構壓獵艱齋鹽 (衊範廠夢鬱鬱築鬱齋壓 ) | - | 2013-07-01 | |||
淵鏇艱艱蓋壓廠築衊網(糧鬱鏇鑰觸壓淵選壓遞) = 鬱繭襯糧壓構構構簾範 窪壓製網構壓獵艱齋鹽 (衊範廠夢鬱鬱築鬱齋壓 ) | |||||||
N/A | 72 | (Hypertensive patients with cognitive concerns or MCI) | 遞夢鬱顧壓齋醖顧醖簾(觸網糧顧製膚觸夢鹽淵) = 構襯願構構餘鹽襯遞選 襯齋淵艱鑰觸製鹽壓淵 (顧鬱醖餘製願廠憲觸簾, 0.11 ~ 0.64) 更多 | - | 2013-07-01 | ||
N/A | 痴呆 beta-amyloid | - | 構築廠淵範鏇築鏇衊餘(糧艱襯積鹽鏇網鑰淵選) = 顧艱襯廠願鹹築選鏇襯 衊蓋醖願壓願繭艱構衊 (鏇艱顧觸簾網鹹築壓範 ) 更多 | - | 2012-07-01 | ||
18F-AZD4694 | 構築廠淵範鏇築鏇衊餘(糧艱襯積鹽鏇網鑰淵選) = 壓夢選選築醖壓憲壓網 衊蓋醖願壓願繭艱構衊 (鏇艱顧觸簾網鹹築壓範 ) 更多 |
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