Category: 882518-89-0

On July 17, 2014, Campos, Sebastien Andre; Harling, John David; Miah, Afjal Hussain; Smith, Ian Edward David published a patent.Recommanded Product: 882518-89-0 The title of the patent was Proteolysis targeting chimeras (protacs) directed to the modulation of the estrogen receptor. And the patent contained the following:

The invention relates to compounds I [wherein L is a linking group comprising a length of 6-16 atoms in shortest length having the formula (CH2)n(R1CH2CH2)m(OCH2)qCONH; n = 0-6; m = 2-10; q = 0 or 1; each R1 is independently O, NH, N(C1-3-alkyl), or a 4-6 membered heterocyclyl group containing 2 N atoms linked to the carbons in the chain via the ring N atoms (optionally substituted by oxo).; R2 is straight or branched C1-6-alkyl or C3-6-cycloalkyl; X is oxazol-5-yl or 2-R4-4-R3-thiazol-5-yl; R3 is H or CH3; R4 is H or CH3; and R5 is OH or O-(C1-3-alkyl)], or a pharmaceutically acceptable salt thereof. The invention also relates to processes for the preparation of said compounds, compositions, combinations and medicaments containing said compounds and the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of the estrogen receptor, including degrading the estrogen receptor, the treatment of diseases and conditions mediated by the estrogen receptor. Thus, protac II was prepared from 16-((7R,8R,9S,13S,14S,17S)-3,17-dihydroxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-7-yl)-3,6,9,12-tetraoxahexadecan-1-oic acid (III) via amidation with (2S,4R)-1-((S)-2-amino-3-methylbutanoyl)- 4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide hydrochloride (IV.HCl); the preparations of III and IV are also presented. All compounds showed evidence of ERα degradation in this assay relative to the DMSO control at 1 uM. The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).Recommanded Product: 882518-89-0

The Article related to estrane steroids amino acid conjugate preparation modulation estrogen receptor, proteolysis targeting chimera estratriene preparation modulation estrogen receptor, Steroids: Estranes and other aspects.Recommanded Product: 882518-89-0

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On April 13, 2006, Robillard, Marc S.; Gruell, Holger published a patent.Application In Synthesis of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate The title of the patent was Targeted imaging and/or therapy using the Staudinger ligation. And the patent contained the following:

The use of a selective chem. and bioorthogonal reaction providing a covalent ligation such as the Staudinger ligation (reaction between an azide and a phosphine), in targeted mol. imaging and therapy is presented, more specifically with interesting applications for pre-targeted imaging or therapy. Current pre-targeted imaging is hampered by the fact that it relies solely on natural/biol. targeting constructs (i.e. biotin/streptavidin). Size considerations and limitations associated with their endogenous nature severely limit the number of applications. The present invention describes how the use of an abiotic, bio-orthogonal reaction which forms a stable adduct under physiol. conditions, by way of a small or undetectable bond, can overcome these limitations. As an example of pre-targeted imaging, injection of a targeting probe comprising a somatostatin receptor-binding peptide linked to an azide is followed by a secondary radiolabeled probe linked to a Staudinger phosphine group. Following in vivo Staudinger ligation, the radiolabel enables detection of the presence of somatostatin receptor-pos. tissue such as neuroendocrine tumor. The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).Application In Synthesis of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate

The Article related to staudinger ligation targeted imaging therapy, azide phosphine reaction targeted contrast agent delivery, Pharmaceuticals: Pharmaceutics and other aspects.Application In Synthesis of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On January 25, 2018, Crew, Andrew P.; Raina, Kanak; Dong, Hanqing; Qian, Yimin; Wang, Jing; Vigil, Dominico; Serebrenik, Yevgeniy V.; Hamman, Brian D.; Morgan, Alicia; Ferraro, Caterina; Siu, Kam; Neklesa, Taavi K.; Winkler, James D.; Coleman, Kevin G.; Crews, Craig M. published an article.SDS of cas: 882518-89-0 The title of the article was Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1. And the article contained the following:

Proteolysis Targeting Chimeras (PROTACs) are bifunctional mols. that recruit an E3 ligase to a target protein to facilitate ubiquitination and subsequent degradation of that protein. While the field of targeted degraders is still relatively young, the potential for this modality to become a differentiated and therapeutic reality is strong, such that both academic and pharmaceutical institutions are now entering this interesting area of research. In this paper, the authors describe a broadly applicable process for identifying degrader hits based around the serine/threonine kinase TANK-binding kinase 1 (TBK1), and have generalized the key structural elements associated with degradation activities. Compound I is a potent hit (TBK1 DC50 = 12 nM, Dmax = 96%) with excellent selectivity against a related kinase IKKε, which was further used as a chem. tool to assess TBK1 as a target in mutant K-Ras cancer cells. The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).SDS of cas: 882518-89-0

The Article related to von hippel lindau protac tank binding kinase 1, Pharmacology: Structure-Activity and other aspects.SDS of cas: 882518-89-0

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On June 19, 2020, Roberts, Brett L.; Ma, Zhi-Xiong; Gao, Ang; Leisten, Eric D.; Yin, Dan; Xu, Wei; Tang, Weiping published an article.Application In Synthesis of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate The title of the article was Two-Stage Strategy for Development of Proteolysis Targeting Chimeras and its Application for Estrogen Receptor Degraders. And the article contained the following:

Proteolysis targeting chimeras (PROTACs) have emerged as useful chem. probes and potential therapeutics by taking advantage of the ubiquitin-proteasome system to degrade intracellular disease-associated proteins. PROTACs are heterobifunctional mols. composed of a target protein ligand, E3 ubiquitin ligase ligand, and a linker between them. The generation of efficient PROTACs requires screening of many parameters, especially the lengths and types of the linkers. The authors report the proof-of-concept study using a two-stage strategy to facilitate the development of PROTACs against the estrogen receptor (ER). In stage one, a library of close to 100 PROTACs was synthesized by simply mixing a library of ERα ligands containing a hydrazide functional group at different positions with a preassembled library of E3 ligase ligands bearing different types and lengths of linkers with a terminal aldehyde group in a 1:1 ratio. Cell-based screening occurred without further purification, because the formation of the acylhydrazone linkage is highly efficient and produces water as the only byproduct. Compound A3 was the most potent ER degrader in two ER+ cell lines (DC50= ~10 nM, Dmax= â‰?95%). Stage two involved transformation to a more stable amide linker to generate a more drug-like mol. The new compound, AM-A3, showed comparable biol. activity (DC50 = 1.1 nM, Dmax = 98%) and induced potent antiproliferation (IC50= 13.2 nM, Imax= 69%) in MCF-7. This proof-of -concept study demonstrates that the two-stage strategy can significantly facilitate the development of PROTACs against ER without the tedious process of making large numbers of PROTACs one by one. It has the potential to be expanded to many other targets. The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).Application In Synthesis of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate

The Article related to proteolysis targeting chimera estrogen receptor degrader, Pharmacology: Structure-Activity and other aspects.Application In Synthesis of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On October 1, 2021, Yang, Chao; Ma, Dejun; Lu, Liqing; Yang, Xing; Xi, Zhen published an article.SDS of cas: 882518-89-0 The title of the article was Synthesis of KUE-siRNA Conjugates for Prostate Cancer Cell-Targeted Gene Silencing. And the article contained the following:

The delivery of siRNAs to selectively target cells poses a great challenge in RNAi-based cancer therapy. The lack of suitable cell-targeting methods seriously restricts the advance in delivering siRNAs to extrahepatic tissues. Based on prostate-specific membrane antigen (PSMA)-targeting ligands, we have synthesized a series of lysine-urea-glutamate (KUE)-siRNA conjugates and verified their effective cell uptake and gene silencing properties in prostate cancers. The results indicated that the KUE-siRNA conjugates could selectively enter PSMA+ LNCaP cells, eventually down-regulating STAT3 expression. Based on post-synthesis modification and receptor-mediated endocytosis, this strategy of constructing ligand-siRNA conjugates might provide a general method of siRNA delivery for cell-targeted gene silencing. The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).SDS of cas: 882518-89-0

The Article related to lysine urea glutamate sirna prostate cancer cell gene silencing, kue-sirna conjugates, psma-targeted, rna interference, propargyl analog, prostate cancer, Placeholder for records without volume info and other aspects.SDS of cas: 882518-89-0

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On December 26, 2019, Yang, Xiaobao; Jiang, Biao; Sun, Ning; Qiu, Xing published a patent.Recommanded Product: tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate The title of the patent was Method for preparation of lenalidomide derivatives. And the patent contained the following:

Provided is a method for preparing a compound of formula I [wherein X = O, CONH, NHCO, NH, alkynylene, alkylidene, cycloalkylene, arylene, heterocylidene, or heteroarylene; Y = optionally protected COOH, -SO3H, NH2, N3, alkenyl, alkynyl, cyclofluorenyl, aryl, heterocyclyl, heteroaryl or hydrogen]. The preparation method comprises: a lenalidomide derivative undergoes an aminoalkylation reaction with a compound of formula R-X-Y [wherein R = a leaving group] in the presence of an organic alkali. For example, nalidamine, n-propylbromide, and N,N-diisopropylethylamine were added to a reaction tube, and then NMP was added, and the reaction was carried out at 110 °C for 6 h to give 1-oxo-4-propylamino-2-(2,6-dioxopiperidin-3-yl)isoindole as a final product. The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).Recommanded Product: tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate

The Article related to preparation lenalidomide derivative, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Recommanded Product: tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On August 6, 2021, Wen, Shijun; Huang, Peng; Tu, Yalin; Sun, Yameng; Hu, Yumin published a patent.Related Products of 882518-89-0 The title of the patent was Preparation of small molecule compounds based on degradation of EZH2 protein and their applications. And the patent contained the following:

The present invention relates to the preparation of small mol. compounds based on degradation of EZH2 protein and their applications. In particular, the small mol. compound I (wherein, X = a linker including acyclic or cyclic saturated or unsaturated carbon, ethylene glycol, amide, amino, ether, or carbonyl-containing group; Y = can be a group of affinity E3 ligase VHL or Cereblon (CRBN)) was prepared The inventive EZH2 degrading agents that can specifically degrade EZH2 protein, and these small mol. compounds has a stronger anti-tumor effect compared with EZH2 inhibitors. The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).Related Products of 882518-89-0

The Article related to heterocyclic small mol compound preparation ezh2 protein antitumor agent, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Related Products of 882518-89-0

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On January 8, 2015, Campos, Sebastien Andre; Harling, John David; Miah, Afjal Hussain; Smith, Ian Edward David published a patent.Computed Properties of 882518-89-0 The title of the patent was Benzothiophene derivatives as estrogen receptor inhibitors and their preparation and use for the treatment of diseases. And the patent contained the following:

The invention relates to benzothiophene derivatives of formula I, which are estrogen receptor inhibitors and which are useful in the treatment of diseases mediated by the estrogen receptor. Compounds of formula I wherein R1 is H, OH, C1-3 alkoxy and halo; R2 is OH and C1-3 alkoxy; X is O and CO; L is a linker; R3 is (un)branched C1-6 alkyl and C3-6 cycloalkyl; R4 is 4-methylthiazol-5-yl, oxazol-5-yl and halo; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). All the invention compounds were evaluated for their estrogen receptor alpha (ERa) degradation (data not given). The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).Computed Properties of 882518-89-0

The Article related to benzothiophene preparation estrogen receptor inhibitor treatment disease, Heterocyclic Compounds (One Hetero Atom): Thiophenes and other aspects.Computed Properties of 882518-89-0

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On April 27, 2021, Yang, Xiaobao; Jiang, Biao; Tan, Wenfu; Xu, Zhongli; Luo, Jia; Wang, Juan; Yang, Jun; Zhang, Shaoqing published a patent.Category: esters-buliding-blocks The title of the patent was Preparation of (aminonitrophenyl)sulfonylpiperazinylbenzamides as protein degradation agents. And the patent contained the following:

The present invention relates to the preparation of (aminonitrophenyl)sulfonylpiperazinylbenzamides, R1-A1-LIN-A2-R2, as protein degradation agents. In particular, R1-A1-LIN-A2-R2, wherein, R1 is 4-[[4-[[4-[4-[[2-(4-chlorophenyl)-4,4-dimethyl-cyclohexen-1-yl]methyl]piperazin-1-yl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]sulfamoyl]-2-nitro-anilino]methyl]-1-piperidyl, 3-[[4-[[4-[4-[[2-(4-chlorophenyl)-4,4-dimethyl-cyclohexen-1-yl]methyl]piperazin-1-yl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]sulfamoyl]-2-nitro-anilino]methyl]-1-piperidyl, 3-(4-chlorophenyl)-2-[[4-[4-[[3-nitro-4-(tetrahydropyran-4-ylmethylamino)phenyl]sulfonylcarbamoyl]-3-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)phenyl]piperazin-1-yl]methyl]phenoxy, etc.; A1 does not exist or represents a carbonyl group; A2 does not exist or represents a carbonyl group. Further LIN does not exist or represents a (un)substituted linear or branched alkylene group, wherein the alkylene group is optionally selected from oxygen, the group consisting of an optionally substituted heterocyclyl or any combination thereof is interrupted, when LIN does not exist, one of A1 and A2 does not exist and the other represents a carbonyl group, and R2 is I and II, wherein the R3 group represents an ethylene group or a vinylene group or salt, enantiomer, stereoisomer, solvate, polymorph thereof, and application thereof for treating diseases, were prepared The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).Category: esters-buliding-blocks

The Article related to aminonitrophenyl sulfonylpiperazinylbenzamide protein degradation agent preparation, Heterocyclic Compounds (More Than One Hetero Atom): Thiazines and other aspects.Category: esters-buliding-blocks

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On October 17, 2019, Yang, Xiaobao; Jiang, Biao; Sun, Renhong; Ren, Chaowei; Sun, Ning; Kong, Ying; Li, Yan; Chen, Jinju; Yin, Qianqian; Song, Xiaoling; Zhao, Quanju; Qiu, Xing published a patent.Formula: C17H26O7S The title of the patent was Protein degradation targeting compound, anti-tumor application, intermediate thereof and use of intermediate. And the patent contained the following:

The compound (e.g., I) has a degrading effect on a specific target protein, and is mainly composed of three parts: the first part is Small Mols. Binding Protein (SMBP); the second part is a linker unit (LIN); and the third part is a Ubiquitin Ligase Binding Moiety (ULM), wherein SMBP and LIN are covalently bound, and LIN is covalently bound to ULM. The compounds designed and synthesized by the present disclosure have a wide pharmacol. activities, have a function of degrading specific proteins and/or inhibiting activities, and can be used for the treatment of associated tumor. The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).Formula: C17H26O7S

The Article related to protein degradation targeting heteroaryl preparation antitumor smbp lin ulm, small mol binding protein smbp linker lin ulm, Heterocyclic Compounds (More Than One Hetero Atom): Diazepines and other aspects.Formula: C17H26O7S

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics