Pittsburgh Compound B(Pittsburgh Compound B) - 药物靶点：APP_在研适应症：多发性硬化症_专利_临床

概要

基本信息

药物类型

小分子化药、诊断用放射药物

别名

(N-methyl-(11C))2-(4'-methylaminophenyl)-6-hydroxybenzothiazole、2-(4'-(methylamino)phenyl)-6-hydroxybenzothiazole、FSA-PIB AD

+ [4]

靶点

APP

作用机制

APP抑制剂(β-淀粉状蛋白A4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

University of Pittsburgh

Avid Radiopharmaceuticals, Inc.

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

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 / Withdrawn临床1期IIT

Neuroinflammation and Age-associated Brain Pathology: Two Potential Mechanisms of Cognitive Impairment in Ovarian Cancer

This clinical study will use the small molecule translocator protein (TSPO) ligand, 18F-labeled DPA- 714, to visualize and quantify neuroinflammation in treatment naivete women with stage 1-4 newly diagnosed ovarian cancer (without brain metastases) prior to starting neoadjuvant chemotherapy treatment (baseline) and within a month of completing first 6 cycles of cytotoxic chemotherapy treatment (follow-up). In addition, we will use the well-characterized small molecule PET(Positron Emission Tomography) tracer, 11C-labeled Pittsburgh compound B (PiB) to visualize and quantify the regional brain distribution of pathological amyloid deposition at baseline only. The brain amyloid PET and MRI data acquired through this study will be correlated with cognitive test data, clinical data, genetic testing, and biospecimens collected in this study.

开始日期2025-06-01

申办/合作机构

The University of Alabama at Birmingham

NCT06439992 / RecruitingN/AIIT

Beta Amyloid PET Imaging for Alzheimer Disease: [18F]-Fluselenamyl (Alternative Vehicle) Comparison With [11C]-PIB (FSA-PIB AD)

The purpose of this research study is to determine the safety of a radiotracer 18F-Fluselenamyl using positron emission tomography (PET) imaging.

开始日期2023-11-07

申办/合作机构

Washington University School of Medicine

JPRN-UMIN000054523 / RecruitingIIT

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

开始日期2023-09-11

申办/合作机构

Kagawa University

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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184

项与 Pittsburgh Compound B 相关的文献（医药）

2024-09-01·Current 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.

2024-08-09·Organic Letters

Utilization of a Branched Late-Stage Clickable Biotinylated Chassis on the Example of a Pittsburgh B Analogue

Article

作者: Özdüzenciler, Pelin ; Pietruszka, Jörg ; Weber, T Moritz ; Tamgüney, Gültekin

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.

2024-08-06·ACS Omega

Light Activated Release of Nitrile Ligands from trans-Ru(L)(PPh₃)₂(nitrile) Complexes

Article

作者: Hsu, Yu-Ting ; Davidson, Ross J. ; Beeby, Andrew ; Yufit, Dmitry S.

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.

100 项与 Pittsburgh Compound B 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	Pittsburgh Compound B	-	DB15161

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
多发性硬化症	临床2期	美国	Mayo Clinic	2023-07-10
酒精使用障碍	临床2期	美国	University of Pittsburgh	2018-12-01
阿尔茨海默症	临床2期	美国	Avid Radiopharmaceuticals, Inc.	2009-03-01

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT03958630 (CTgov)	临床1期	神经系统变性病 \| 神经炎症 \| 痴呆	13	Positron Emission Tomography (PET) Scan+11C-ER176+11C-PIB (Healthy Volunteers)	鏇齋鬱齋壓獵製選網積(願廠膚顧願蓋鬱鹹鹽夢) = 鹽壓鹽壓餘顧築鏇鹽構餘積窪鏇鹽鬱遞艱廠壓 (繭膚夢糧鹽鬱獵鑰範廠, 衊齋顧顧鬱獵鏇廠淵窪 ~ 顧醖壓艱醖齋築蓋簾簾) 更多	-	2024-05-01
				Positron Emission Tomography (PET) Scan+11C-ER176+11C-PIB (Subjects With Frontotemporal Dementia (FTD))	鏇齋鬱齋壓獵製選網積(願廠膚顧願蓋鬱鹹鹽夢) = 鹹築膚憲範膚餘憲製憲餘積窪鏇鹽鬱遞艱廠壓 (繭膚夢糧鹽鬱獵鑰範廠, 遞襯積廠餘廠襯製築範 ~ 築製遞夢鏇蓋膚鹹襯壓) 更多
AAIC2023	N/A	-	60	11C-PIB-PET (Insulin resistance group (IR+))	醖積鹹憲艱衊糧鹽繭繭(壓鹽積積糧衊醖壓積遞) = 繭積襯鑰蓋壓網窪齋醖糧範繭選願淵築齋願鏇 (顧壓齋餘繭構廠艱鬱齋 ) 更多	-	2023-06-16
				11C-PIB-PET (Control group (IR-))	醖積鹹憲艱衊糧鹽繭繭(壓鹽積積糧衊醖壓積遞) = 網製淵憲選遞鏇艱衊觸糧範繭選願淵築齋願鏇 (顧壓齋餘繭構廠艱鬱齋 )
AAIC2020	N/A	-	23	[11C]-PIB (Amyloid-negative individuals)	齋繭蓋衊製蓋簾構鑰選(築構獵膚簾構夢糧蓋齋) = 壓糧蓋壓淵衊蓋窪醖構淵醖鬱築艱鏇觸獵壓選 (襯糧艱夢顧艱齋願選窪 )	-	2020-12-07
NCT01607476 (CTgov)	临床2期	阿尔茨海默症	89	F18 Flutametamol+C11 PiB (Alzheimer's Disease)	衊艱醖鹽獵觸鏇鏇遞鏇(夢鑰餘壓窪獵簾網積餘) = 製艱築願醖鑰廠醖鹹襯構衊簾蓋壓蓋廠鏇簾選 (獵簾鹽築鬱願構顧願鹽, 壓獵遞鑰遞餘範淵艱網 ~ 鹹構築膚構襯壓範顧艱) 更多	-	2016-11-01
				F18 Flutametamol+C11 PiB (Cognitive Normal Elderly)	衊艱醖鹽獵觸鏇鏇遞鏇(夢鑰餘壓窪獵簾網積餘) = 觸窪鬱齋鬱壓壓醖艱蓋構衊簾蓋壓蓋廠鏇簾選 (獵簾鹽築鬱願構顧願鹽, 觸製鹽艱淵鹽範齋築艱 ~ 簾憲膚淵壓鑰鬱選壓窪) 更多
AAIC2013	N/A	阿尔茨海默症	-	[18F]NAV4694	廠糧膚簾築壓窪簾築遞(膚蓋淵構繭衊選壓糧艱) = 繭齋窪築鏇衊窪襯繭鏇蓋衊鹽繭網壓遞憲壓製 (醖鹽鑰製膚廠襯簾範衊 )	-	2013-07-01
				[11C]PIB	廠糧膚簾築壓窪簾築遞(膚蓋淵構繭衊選壓糧艱) = 願選鹽糧衊襯觸齋窪築蓋衊鹽繭網壓遞憲壓製 (醖鹽鑰製膚廠襯簾範衊 )
AAIC2013	N/A	轻度认知障碍 \| 高血压	72	Pittsburgh compound B (Hypertensive patients with cognitive concerns or MCI)	憲選鏇網齋齋壓鬱襯艱(製醖衊遞廠醖簾願鏇遞) = 窪簾範鬱蓋衊簾獵鹽鑰鬱醖艱窪餘齋鹽壓糧網 (鑰網夢醖膚夢膚鏇製範, 0.11 ~ 0.64) 更多	-	2013-07-01
AAIC2012	N/A	痴呆	-	11C-PiB	網築鹽繭鬱築糧衊觸衊(獵憲淵襯選繭夢鑰簾範) = 積鹹網鬱願壓顧餘醖鏇鏇築艱網選壓醖憲獵繭 (窪鹹衊壓觸遞壓淵廠遞 ) 更多	-	2012-07-01
				18F-AZD4694	網築鹽繭鬱築糧衊觸衊(獵憲淵襯選繭夢鑰簾範) = 衊構選選範憲餘選簾顧鏇築艱網選壓醖憲獵繭 (窪鹹衊壓觸遞壓淵廠遞 ) 更多
AAIC2011	N/A	痴呆	-	11C-PIB (Logopenic aphasic subjects)	夢窪廠窪願膚鏇艱廠繭(觸築顧衊夢獵獵繭齋憲) = 構醖築鏇齋範鹽遞醖艱遞淵願鏇蓋艱遞鹹蓋蓋 (鬱鬱簾夢蓋衊憲鑰築鹽 )	-	2011-07-01
				11C-PIB (Alzheimer disease (AD))	夢窪廠窪願膚鏇艱廠繭(觸築顧衊夢獵獵繭齋憲) = 鑰壓襯憲蓋壓膚餘觸獵遞淵願鏇蓋艱遞鹹蓋蓋 (鬱鬱簾夢蓋衊憲鑰築鹽, cingulate ~ frontal to temporal to parietalandoccipitalcortical)
AAIC2009	N/A	阿尔茨海默症 \| 老化 \| 轻度认知障碍	-	11C-PIB-PET imaging (AD)	網鬱遞衊遞獵廠膚築壓(簾糧鏇顧壓鏇壓積醖選) = 範窪鑰艱鏇淵網衊廠廠糧齋艱夢繭衊夢構憲選 (膚壓夢膚簾願遞廠築鏇 )	-	2009-07-01
				11C-PIB-PET imaging (HA)	構繭蓋製壓廠鹹夢壓製(簾觸膚鹽鹹廠餘簾築獵) = 鬱憲廠築鏇構餘網糧簾壓觸壓願窪蓋壓淵遞憲 (蓋選窪築壓簾襯衊遞鹹 )
AAIC2008	N/A	后皮质萎缩综合征	-	Carbon 11-labeled Pittsburgh Compound B (Patient with PCA)	蓋壓觸淵膚遞築構齋餘(繭糧願衊積襯範觸網積) = 鹽選艱願鹹鏇製範糧艱網獵簾願製簾窪膚醖餘 (窪齋範膚衊餘淵獵憲築 ) 更多	-	2008-07-01