54914-17-9Relevant academic research and scientific papers
Iodinated Choline Transport-Targeted Tracers
?vec, Pavel,Novy, Zbyněk,Ku?ka, Jan,Pet?ík, Milo?,Sedlá?ek, Ond?ej,Kucha?, Martin,Li?ková, Barbora,Medvedíková, Martina,Kolouchová, Kristyna,Groborz, Ond?ej,Loukotová, Lenka,Konefa?, Rafa? ?.,Hajdúch, Marián,Hruby, Martin
supporting information, p. 15960 - 15978 (2020/12/23)
We present a novel series of radioiodinated tracers and potential theranostics for diseases accompanied by pathological function of proteins involved in choline transport. Unlike choline analogues labeled with 11C or 18F that are currently used in the clinic, the iodinated compounds described herein are applicable in positron emission tomography, single-photon emission computed tomography, and potentially in therapy, depending on the iodine isotope selection. Moreover, favorable half-lives of iodine isotopes result in much less challenging synthesis by isotope exchange reaction. Six of the described compounds were nanomolar ligands, and the best compound possessed an affinity 100-fold greater than that of choline. Biodistribution data of 125I-labeled ligands in human prostate carcinoma bearing (PC-3) mice revealed two compounds with a biodistribution profile superior to that of [18F]fluorocholine.
Discovery of Diphenoxy Derivatives with Flexible Linkers as Ligands for β-Amyloid Plaques
Jia, Jianhua,Zhang, Longfei,Song, Jia,Dai, Jiapei,Cui, Mengchao
, p. 4089 - 4100 (2020/12/13)
The highly rigid and planar scaffolds with π-conjugated systems have been widely considered to be indispensable for β-amyloid (Aβ) binding ligands. In this study, a library of diphenoxy compounds with different types of more flexible linkers as Aβ ligands were synthesized and evaluated. Most of them displayed good affinity (Ki1-42aggregates, and some ligands even showed values of Kiless than 10 nM. Structure-activity relationship analysis revealed that modification on the linkers or substituents tolerated great flexibility, which challenged the long-held belief that rigid and planar structures are exclusively favored for Aβ binding. Three ligands were labeled by iodine-125, and they exhibited good properties in vitro and in vivo, which further supported that this flexible scaffold was potential and promising for the development of Aβ imaging agents.
INDOLO-SUBSTITUTED-PIPERIDINE COMPOUNDS AS ESTROGEN RECEPTOR DEGRADING AGENT
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Paragraph 0135, (2019/02/09)
Disclosed is a new indole compound, in particular, the compound as shown in formula (I), and a preparation method, pharmaceutical composition and use thereof as an estrogen receptor down-regulator in preparing drugs for treating estrogen receptor-positive breast cancer.
Diphenoxyl flexible molecules with high affinity with A[beta] plaque and preparation method and applications thereof
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Paragraph 0230; 0231, (2017/12/09)
The invention discloses diphenoxyl flexible molecules with high affinity with A[beta] plaque and a preparation method and applications thereof. After the molecules are labeled by radionuclide, the molecules can be used as an A[beta] plaque developing agen
TETRASUBSTITUTED ALKENE COMPOUNDS AND THEIR USE
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Page/Page column 0410; 0411, (2016/12/22)
Disclosed herein are compounds, or pharmaceutically acceptable salts thereof, and methods of using the compounds for treating breast cancer by administration to a subject in need thereof a therapeutically effective amount of the compounds or pharmaceutically acceptable salts thereof. The breast cancer may be an ER-positive breast cancer and/or the subject in need of treatment may express a mutant ER-α protein.
Fabrication of fluorescent silica nanoparticles hybridized with AIE luminogens and exploration of their applications as nanobiosensors in intracellular imaging
Faisal, Mahtab,Hong, Yuning,Liu, Jianzhao,Yu, Yong,Lam, Jacky W. Y.,Qin, Anjun,Lu, Ping,Tang, Ben Zhong
experimental part, p. 4266 - 4272 (2010/07/02)
Highly emissive inorganicorganic nanoparticles with core-shell structures are fabricated by a one-pot, surfactant-free hybridization process. The surfactant-free sol-gel reactions of tetraphenylethene- (TPE) and silolefunctionalized siloxanes followed by
Aminoalcohol derivatives
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Page/Page column 17, (2010/02/12)
The present invention relates to a compound formula[I]: wherein X is bond, —CH2—, —O— or —NH—, R1 and R12 are each independently hydrogen, halogen, lower alkyl, etc., R2 is hydrogen or optionally substituted lower alkyl, R3 is hydrogen or an amino protective group, R4, R5 and R6 are each independently hydrogen or optionally substituted lower alkyl, R7 is -Z-R13, in which Z is bond, etc., and R13 is carboxy, lower alkoxycarbonyl, (lower alkylsulfonyl)carbamoyl or lower alkanoylsulfamoyl, R8 is —Y—R9, in which Y is bond, —CH2—, —O—, —S—, etc., and R9 is hydrogen, lower alkyl, cyclo(lower)alkyl, etc., and R11 is hydrogen, lower alkyl, lower alkoxy, etc., or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiurea or urinary incontinence.
Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity
Lewis, Timothy A.,Young, Michelle A.,Arrington, Mark P.,Bayless, Lynn,Cai, Xiong,Collart, Philippe,Eckman, Joseph B.,Ellis, James L.,Ene, Doina G.,Libertine, Lyn,Nicolas, Jean-Marie,Scannell, Ralph T.,Wels, Bruce F.,Wenberg, Karen,Wypij, Donna M.
, p. 5591 - 5594 (2007/10/03)
Three different histaminergic H1 scaffolds were attached by various linkers to a single 5-LO scaffold. Both activities were observed in vitro. Pharmacokinetic properties of the compounds were evaluated and both a cetirizine-based compound and a
Trifluoromethyl ketone analogs as selective cPLA2 inhibitors
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, (2008/06/13)
Selective inhibitors of the cPLA2enzymes are provided which are of use in controlling a wide variety of inflammatory diseases. The inhibitors of the present invention have the general formula where (R′), p, D, Y, Z, Ra, Rband A are as defined in the specification.
Compounds and methods for treatment of asthma, allergy and inflammatory disorders
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, (2008/06/13)
The present invention provides 1,4 substituted piperazines, 1,4 substituted piperidines, and 1-substituted, 4-alkylidenyl peperidines compounds. The compounds of the invention are dual acting molecules having both leukotriene inhibition properties as well
