864680-64-8Relevant articles and documents
IRAK DEGRADERS AND USES THEREOF
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Paragraph 2433; 2436, (2019/07/10)
The present invention provides compounds, compositions thereof, and methods of using the same.
COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ENHANCER OF ZESTE HOMOLOG 2 POLYPEPTIDE
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Paragraph 1106, (2018/07/15)
The present disclosure relates to bifunctional compounds, which find utility as modulators of enhancer of zeste homolog 2 (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
Amide bond-containing monodisperse polyethylene glycols beyond 10000 da
Wan, Zihong,Li, Yu,Bo, Shaowei,Gao, Ming,Wang, Xuemeng,Zeng, Kai,Tao, Xin,Li, Xuefei,Yang, Zhigang,Jiang, Zhong-Xing
, p. 7912 - 7919 (2016/08/30)
Although monodisperse polyethylene glycols (M-PEGs) above 4000 Da are especially valuable in biomedical applications, their synthesis remains a long-standing challenge. To this end, a peptide-based strategy for such M-PEGs was developed. With macrocyclic sulfates as the key intermediates, a panel of oligoethylene glycol (OEG) containing ω-amino acids were prepared with high efficiency. Through solid phase peptide synthesis (SPPS), these amino acids were conveniently assembled into a series of amide bond-containing M-PEGs with high flexibility in molecular weight and amide density selection. With this strategy, an M-PEG of 10262 Da was prepared on a gram scale and its biocompatibility was assessed in a mice model.
TARGETED DRUG DELIVERY THROUGH AFFINITY BASED LINKERS
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Paragraph 00294, (2015/12/08)
The current invention discloses targeted drug delivery conjugates comprising a targeting moiety linked to a drug via a molecule having an affinity for the targeting moiety. Typically, the conjugate comprises a targeting ligand and a molecule of interest, e.g., a therapeutic agent. The targeting ligand and the molecule of interest are linked to each other via an affinity ligand. The affinity ligand is further covalently or non-covalently linked to a drug or therapeutic agent. The drug can be modified to make it more soluble and so that it cleaves from the linking molecule at the target site.
Synthesis and characterization of fluorinated conjugates of albumin
Yue, Xuyi,Feng, Yue,Yu, Y. Bruce
supporting information, p. 173 - 181 (2013/11/06)
A small fluorocarbon dendron that contains nine chemically identical fluorine atoms was covalently conjugated to albumin via a flexible linker. Two versions were made, which differ by 10% in the linker length. Both versions display split 19F signal and much shorter 19F longitudinal relaxation time than their small molecule counterparts. 10% difference in the flexible linker length has negligible impact on the 19F signal.
Antithrombotic compound
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, (2008/06/13)
The present invention relates compounds of the formula Aoligosaccharide-spacer-GpIIb/IIIa antagonist wherein the oligosaccharide is a negatively charged oligosaccharide residue comprising four to twenty five monosaccharide units, the charge being compensa