Category: 882518-89-0

On July 22, 2021, Tu, Yalin; Sun, Yameng; Qiao, Shuang; Luo, Yao; Liu, Panpan; Jiang, Zhong-Xing; Hu, Yumin; Wang, Zifeng; Huang, Peng; Wen, Shijun published an article.Application of 882518-89-0 The title of the article was Design, Synthesis, and Evaluation of VHL-Based EZH2 Degraders to Enhance Therapeutic Activity against Lymphoma. And the article contained the following:

Traditional EZH2 inhibitors are developed to suppress the enzymic methylation activity, and they may have therapeutic limitations due to the nonenzymic functions of EZH2 in cancer development. Here, we report proteolysis-target chimera (PROTAC)-based EZH2 degraders to target the whole EZH2 in lymphoma. Two series of EZH2 degraders were designed and synthesized to hijack E3 ligase systems containing either von Hippel-Lindau (VHL) or cereblon (CRBN), and some VHL-based compounds were able to mediate EZH2 degradation Two best degraders, YM181 (I) and YM281 (II), induced robust cell viability inhibition in diffuse large B-cell lymphoma (DLBCL) and other subtypes of lymphomas, outperforming a clin. used EZH2 inhibitor EPZ6438 (tazemetostat) that was only effective against DLBCL. The EZH2 degraders displayed promising antitumor activities in lymphoma xenografts and patient-derived primary lymphoma cells. Our study demonstrates that EZH2 degraders have better therapeutic activity than EZH2 inhibitors, which may provide a potential anticancer strategy to treat lymphoma. The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).Application of 882518-89-0

The Article related to lymphoma ezh2 inhibitors degraders vhl crbn ym181 ym281 antitumor, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Application of 882518-89-0

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

On August 4, 2022, Wu, Liang; Deng, Yijun published a patent.Recommanded Product: 882518-89-0 The title of the patent was Targeting chimeric compound, pharmaceutical composition, preparation method and use. And the patent contained the following:

A targeting chimeric compound, a pharmaceutical composition comprising same, a preparation method therefor and use thereof. The targeting chimeric compound is as represented by general formula I [wherein X = CH or N; A = CH=CH, N=N, S, O, or NH; L1 = a bond; L2 = a bond or CO; R1 = OH, alkylsulfonyl, B(OH)2, CO2H, etc.; R2 = independently OH, alkylsulfonyl, CO2H, etc.; R3 and R4 = independently H, alkyl, alkoxy, haloalkyl, etc.; m = 0-5]. Compared with fulvestrant in the prior art, the targeting chimeric compound has comparable or even better proliferative inhibitory activity on estrogen receptor α in mutant drug-resistant cells, and thus is expected to show a comparable or even better therapeutic effect on therapy. 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 targeting chimeric pharmaceutical composition preparation estrogen receptor inhibitor, Amino Acids, Peptides, and Proteins: Poly(Amino Acids) and Peptides and other aspects.Recommanded Product: 882518-89-0

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

On December 15, 2020, Yang, Xiaobao; Jiang, Biao; Song, Xiaoling; Sun, Ning; Ren, Chaowei; Kong, Ying; Zhang, Jianshui; Chen, Jinju; Li, Yan; Zhou, Yuedong published a patent.Reference of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate The title of the patent was ALK protein regulator and anti-tumor application thereof. And the patent contained the following:

The invention relates a series of compounds designed and synthesized, have a wide range of pharmacol. activities,. The inventive compounds are capable of degrading specific proteins and/or inhibiting their activities, and can be applied to the treatment of tumor and cancer. The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).Reference of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate

The Article related to alk protein brigatinib alecensa phosphine oxide derivative preparation, antitumor activity brigatinib alecensa phosphine oxide derivative, Organometallic and Organometalloidal Compounds: Phosphorus Compounds and other aspects.Reference of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate

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

On August 2, 2018, Qian, Yimin; Crew, Andrew P.; Crews, Craig M.; Dong, Hanqing; Hornberger, Keith R.; Wang, Jing published a patent.Related Products of 882518-89-0 The title of the patent was Preparation of substituted benzothiophenes as modulators of estrogen receptor proteolysis and associated methods of use. And the patent contained the following:

The disclosure relates to bifunctional compounds of formulas I and II, which find utility as modulators of estrogen receptor (target protein). In particular, the disclosure is directed to bifunctional compounds of formulas I and II, which contain on one end a cereblon, Von Hippel-Lindau ligase-binding moiety, Inhibitors of Apotosis Proteins, or mouse double-minute homolog 2 ligand, which binds to the resp. 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. Compounds of formulas I and II wherein ULM is a small mol. E3 ubiquitin ligase binding moiety that binds or targets and E3 ubiquitin ligase; L is a chem. linker; X is O and CO; X1 and X2 are independently N and HC; R1 is OH, alkanoyloxy, aroyloxy and lower alkoxy; R2 and R4 are independently H, OH, halo, CN, CF3, etc.; R3 and R5 are independently H and halo; with provisions; and pharmaceutically acceptable salts, enantiomers, stereoisomers, solvates, polymorphs and prodrugs thereof, are claimed. The disclosure exhibits a broad range of pharmacol. 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 disclosure. Example compound III was prepared by a general procedure (procedure given). The invention compounds were evaluated for their estrogen receptor proteolysis modulatory activity. From the assay, it was determined that compound III exhibited IC50 value of 12.7 nM. 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 benzothiophene preparation estrogen receptor proteolysis modulator, Heterocyclic Compounds (One Hetero Atom): Areno- and Diarenothiophenes and other aspects.Related Products of 882518-89-0

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

On April 2, 2021, Zhou, Haibing; Wu, Shuwen; Xu, Zhichao published a patent.Related Products of 882518-89-0 The title of the patent was Preparation of oseltamivir PROTAC compound and application in anti-influenza virus drugs. And the patent contained the following:

The present invention relates to the preparation of oseltamivir PROTAC compound and application in antiinfluenza virus drugs. In particular, oseltamivir PROTAC compound I and II, wherein ( E3 ligase = VHL or CRBN ligand; linker = alkylene or alkoxy) was prepared The compound provided by the invention can effectively degrade influenza virus neuraminidase so as to exert the activity of inhibiting influenza virus replication, not only has the inhibitory activity on wild strain influenza virus, but also has a good inhibitory effect on oseltamivir-resistant strains, and has low toxicity on cells, the compound of the present invention, or a pharmacol. or physiol. acceptable salt thereof, can be used for the preparation of a medicament against influenza virus. 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 oseltamivir protac compound preparation antiinfluenza virus, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Related Products of 882518-89-0

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

On June 28, 2018, Grew, Andrew P.; Zimmermann, Kurt; Wang, Jing; Berlin, Michael; Dong, Hanqing; Ishchenko, Alexey; Qian, Yimin; Crews, Craig M.; Jaime-Figueroa, Saul; Burslem, George published a patent.Name: tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate The title of the patent was Preparation of heterocyclic compounds as EGFR proteolysis targeting chimeric molecules and associated methods of use. And the patent contained the following:

The disclosure relates to bifunctional compounds of formula I, which find utility as modulators of receptor tyrosine kinase (RTK) proteins. The disclosure is directed to bifunctional compounds of formula I, which contain on one end a ligand which binds to an E3 ubiquitin ligase and on the other end a moiety which binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effectuate ubiquitination, and therefore, degradation (and inhibition) of the target protein. The disclosure exhibits a broad range of pharmacol. 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 disclosure. Compounds of formula I wherein ULM is a small mol. E3 ubiquitin ligase binding moiety; PTM is a small mol. receptor tyrosine kinase protein targeting moiety; L is a bond and a chem. linking moiety; and pharmaceutically acceptable salts, enantiomers, stereoisomers, solvates, polymorphs and prodrugs thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluate for their EGFR inhibitory activity. From the assay, it was determined that compound II exhibited IC50 values of in the range of 0.0021 μM to 12 μM. The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).Name: tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate

The Article related to heterocycle preparation egfr proteolysis targeting chimeric mol, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Name: tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate

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

On September 6, 2019, Zhang, Xingxian; He, Kailun; Wang, Wenbing; Wang, Xiaoju; Zheng, Xiaoliang published a patent.HPLC of Formula: 882518-89-0 The title of the patent was Compound targeting EGFR protein degradation useful in treatment of cancer and its preparation. And the patent contained the following:

The invention relates to compounds of formula I and II targeting EGFR protein degradation useful in treatment of cancer and its preparation Compounds I and II, wherein R is C1-6 alkyl; m is an integer of 1-7; n is an integer of 1-6; their pharmaceutically acceptable salts, are claimed. The inventive compound shows excellent EGFR-degrading action and high antitumor activity, and can be applied in cancer prevention and/or treatment. The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).HPLC of Formula: 882518-89-0

The Article related to pyrimidine derivative preparation treatment cancer egfr degrading, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.HPLC of Formula: 882518-89-0

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

On February 5, 2021, Yang, Xiaobao; Jiang, Biao; Song, Xiaoling; Sun, Ning; Ren, Chaowei; Sun, Renhong; Qu, Xiaojuan; Liu, Haixia; Qiu, Xing published a patent.Category: esters-buliding-blocks The title of the patent was Diastereoselective preparation of (aryl)amides derivatives as antitumor agents for EGFR degradation. And the patent contained the following:

The present invention relates to the diastereoselective preparation of (aryl)amides derivatives as antitumor agents for EGFR degradation In particular, (aryl)amide derivatives I [wherein, EGFR binders can bind to EGFR protein; ULM is II; wherein, A is selected from -CH2-, -(C=O)-; B, X, Y, and Z are each independently selected from CH and N; R is -S-, -SO-, -NH-, etc., or not present; D is -(C=O)-, or D does not exist; or, ULM is III, wherein, Z is selected from -(C=O)-, or Z does not exist; or, ULM is IV, wherein, A is selected from -CH2-, -NR’-, -O-, -S-, -(C=O)-, wherein R’ is selected from H, linear or branched C1-C10 alkyl or C3-C10 cycloalkyl; B is -(C=O)-, or B does not exist; D1, D2, D3, D4, D5, D6, D7, D8 are each independently selected from F, Cl, Br, etc.; LIN represents a linking group connected to EGFR binders and ULM through covalent bonds.] bifunctional compound or a pharmaceutically acceptable salt, isomer, prodrug, polymorph or solvate thereof 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 aryl amide derivative preparation antitumor agent egfr degradation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Category: esters-buliding-blocks

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

On August 25, 2020, Zhang, Xingxian; He, Kailun; Wang, Wenbing published a patent.Category: esters-buliding-blocks The title of the patent was Preparation of lenalidomide derivatives as antitumor agents. And the patent contained the following:

The invention discloses a preparation of lenalidomide derivative with general formula I as antitumor agents [wherein A = (CH2CH2X)n, n = 1 to 6; X = O or CH2]. For example, compound I (n = 2, X = O) was prepared in a multi-step synthesis. The title compounds have good antitumor activity and EGFR protein degradation level, which can be used to prepare antitumor agents. 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 substitution iodization hydrolysis amidation preparation lenalidomide pyrimidine antitumor human, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Category: esters-buliding-blocks

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

On April 8, 2021, Crew, Andrew P.; Wang, Jing; Berlin, Michael; Dragovich, Peter; Chen, Huifen; Staben, Leanna published a patent.Synthetic Route of 882518-89-0 The title of the patent was Preparation of pyridazinamine derivatives as modulators of SMARCA2 and BRM target proteins and associated methods of use. And the patent contained the following:

The disclosure relates to bifunctional compounds of formula I, which find utility as modulators of SMARCA2 or BRM (target protein). The disclosure is directed to bifunctional compounds of formula I, which contain on one end a ligand that binds to the Von Hippel-Lindau 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. Compounds of formula I wherein ULM is a small mol. E3 ubiquitin ligase binding moiety that binds a Von Hippel-Lindau E3 ubiquitin ligase; L is a bond and a chem. linker; PTM is a small mol. comprising a SMARCA2 protein targeting moiety; and pharmaceutically acceptable salts, enantiomers, stereoisomers, solvates, polymorphs and prodrugs thereof, are claimed. The disclosure exhibits a broad range of pharmacol. 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 disclosure. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their SMARCA2 and BRM modulatory activity. From the assay, it was determined that compound II exhibited DC50 value of ≥ 30 nM and Dmax value of > 75%. The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).Synthetic Route of 882518-89-0

The Article related to pyridazine preparation smarca2 brm protein modulator, Heterocyclic Compounds (More Than One Hetero Atom): Pyridazines, Cinnolines, and Phthalazines and other aspects.Synthetic Route of 882518-89-0

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