Category: 882518-89-0

On February 6, 2020, Crew, Andrew P.; Wang, Jing; Berlin, Michael; Dragovich, Peter; Chen, Huifen; Staben, Leanna published a patent.Application 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).Application 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.Application of 882518-89-0

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

On September 7, 2021, Huang, Huidan; Zhu, Li; Zhang, Chao; Liu, Xiaoping published a patent.COA of Formula: C17H26O7S The title of the patent was Preparation of hydroxypyranone based compound for targeting ubiquitination and degradation of tyrosinase. And the patent contained the following:

The present invention relates to the preparation of hydroxypyranone based compound for targeting ubiquitination and degradation of tyrosinase. In particular the hydroxypyranone based compound I and II (wherein, the linking chain I = triazole derivative or acetamide derivative, the linking chain II = triazole derivative) was prepared According to the inventive method, a Tyr inhibitor, kojic acid, is covalently bound to Pomalidomide or a VHL enzyme targeting ligand via a connecting chain to obtain a compound targeting a Ubiquitinated degradation tyrosinase with a specific structure; the inventive method has simple operation and mild conditions; the inventive product can significantly inhibit the activity of a vegetable, inhibit the production of melanin, have a significant anti-melanoma effect, can significantly prolong the insurance period of a tyrosinase and fruit and have broad application prospects in medicine, food and cosmetics. The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).COA of Formula: C17H26O7S

The Article related to hydroxypyranone derivative preparation tyrosinase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.COA of Formula: C17H26O7S

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

On June 25, 2019, Zhang, Xingxian published a patent.Reference of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate The title of the patent was Compound for targeted ubiquitination degradation of EGFR protein and its pharmaceutical composition and application. And the patent contained the following:

Title compounds I [wherein A = (CH2CH2O)nCH2 or (CH)n, n is 1 to 6; B = (CH2)m, m is 1 or 2], and their pharmaceutically acceptable salts thereof, were prepared as EGFR inhibitors, useful in the treatment of cancer (breast cancer, colon cancer, prostate cancer, etc.). Thus, the invention compound I [A = (CH2)3; B = CH2] was prepared and gave PC9 inhibition IC50 value of 0.8444 μM. 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 heteroaryl antitumor egfr inhibitor preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Reference of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate

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

On September 30, 2021, Choi, Si Woo; Ryu, Soo Hee; Ryu, Ji Hoon; Son, San Ha; Lee, Hwa Jin; Kim, Seong Hoon; Nam, Boas; Min, Im Suk; Ryu, Hye Guk; Kang, Keum Young published a patent.Reference of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate The title of the patent was Preparation of pyrimidodiazepine derivatives as PLK1 selective degradation inducers for the treatment and prevention of PLK1-related diseases. And the patent contained the following:

The invention relates to preparation of pyrimidodiazepines that induce selective polo-like kinase 1 (PLK1) degradation Specifically, the invention provides a bifunctional compound in which a PLK1 binding moiety and an E3 ubiquitin ligase-binding moiety are linked by a chem. linker. The example compound I was prepared via 6-steps synthesis using 4-bromobutanoic acid as starting material (procedure given). The compounds of the invention may be effectively utilized in prevention and treatment of PLK1-related diseases. 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 pyrimidodiazepine preparation plk1 degradation inducer disease treatment prophylaxis, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Reference of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate

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

On August 13, 2020, Hwang, Jong Yeon; Ha, Jae Du; Cho, Sung Yun; Kim, Pilho; Yun, Chang Soo; Kim, Hyun Jin; Park, Sung Goo; Park, Byoung Chul; Kim, Jeong Hoon; Kim, Sunhong published a patent.SDS of cas: 882518-89-0 The title of the patent was Preparation of target protein EED degradation-inducing degraducer for preventing or treating diseases related to EED, EZH2, or PRC2. And the patent contained the following:

The present invention relates to a target protein degradation-inducing Degraducer, a preparation method thereof, and a pharmaceutical composition for preventing or treating diseases related to EED, EZH2, or PRC2 comprising same as an active ingredient. A novel compound ULB-L-PTM [PTM = EED targeting mols.; L = single bond, chem. linker; ULB = cereblon, MDM2, cIAP, VHL E3 ubiquitin ligase binder] is a Degraducer compound that induces degradation of a target protein, i.e., embryonic ectoderm development (EED) or polycomb repressive complex 2 (PRC2), utilizing cereblon E3 ubiquitin ligase, von Hippel-Lindau tumor suppressor (VHL) E3 ubiquitin ligase, mouse double minute 2 homolog (MDM2) E3 ubiquitin ligase, and cellular inhibitor of apoptosis protein 1 (cIAP) E3 ubiquitin ligase, wherein the compound has an aspect of remarkably achieving target protein degradation-inducing activity through a ubiquitin proteasome system (UPS), and therefore there is a useful effect in that it is possible to provide a pharmaceutical composition for preventing or treating diseases or conditions related to a target protein, and a functional health food composition for preventing or improving same, comprising said compound as an active ingredient. 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 preparation target protein eed degradation inducing degraducer, eed ezh2 prc2 disease treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.SDS of cas: 882518-89-0

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

On August 12, 2022, Liu, Jieqing; Li, Jie; Zhang, Peixi; Xia, Yuanxi; Ma, Junjie; Zhang, Ling; Wang, Qiaolai; Zhang, Ziqing published a patent.Related Products of 882518-89-0 The title of the patent was Preparation of icaritin PROTACs as antitumor agents. And the patent contained the following:

The invention relates to preparation of icaritin PROTACs as antitumor agents. In particular, icaritin protacs I [wherein E3 ligand is at least one in lenalidomide or VHL type ligand (V0), linker is at least one of aliphatic chain or PEG chain, described aliphatic chain is -(CH2)n1CO-NH(CH2)n2-, where n1 represents a natural number from 1 to 6, and n2 represents a natural number 4 or 5; described PEG chain is -(CH2CH2O)n1-CH2CO-NH(CH-R1)-, -(CH2CH2O)n1-CH2CO-NH(CH2)n2-, where n1 represents the natural number 2 or 3, R1 is a C5-alkyl group, and n2 represents the natural number 4 or 5] were prepared The present invention also relates to a process for the preparation of the above-mentioned icarisin PROTACs and the use thereof based on the antitumor activity of the target GRIA3. 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 icaritin protac preparation antitumor agent, Heterocyclic Compounds (One Hetero Atom): Benzopyrans (Including Coumarins, Isocoumarins, Chromones, Benzopyrones, Dibenzopyrans, and Other Arenopyrans) and other aspects.Related Products of 882518-89-0

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

On May 17, 2019, Qiu, Xing; Sun, Ning; Kong, Ying; Li, Yan; Yang, Xiaobao; Jiang, Biao published an article.Recommanded Product: 882518-89-0 The title of the article was Chemoselective Synthesis of Lenalidomide-Based PROTAC Library Using Alkylation Reaction. And the article contained the following:

Using DIPEA as base in N-methyl-2-pyrrolidinone (NMP), lenalidomide underwent regioselective alkylation with bromoesters and Boc-protected bromoamines followed by deprotection to yield lenalidomide derivatives as a library of potential PROTAC reagents. One of the products was coupled to the known BET binding agent JQ1 to yield I; I degraded BET protein in cells and effectively inhibited cancer cell proliferation. 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 protac library lenalidomide regioselective preparation, regioselective alkylation lenalidomide bromoamine bromoester, bet degradation antitumor activity jq1 lenalidomide conjugate and other aspects.Recommanded Product: 882518-89-0

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

On October 3, 2019, Crew, Andrew P.; Wang, Jing; Berlin, Michael; Dragovich, Peter; Chen, Huifen; Staben, Leanna published a patent.Formula: C17H26O7S The title of the patent was Preparation of bifunctional PROTAC compounds and methods for degradation of targeted BRM proteins. And the patent contained the following:

The present disclosure relates to bifunctional compounds, e.g., I, their pharmaceutically acceptable salts, enantiomers, stereoisomers, solvates, polymorphs and prodrugs which find utility as modulators of switch/sucrose non fermentable-related, matrix-associated, actin-dependent regulator of chromatin subfamily a member 2 (SMARCA2) or Brahma (BRM) (target protein), particularly to bifunctional compounds, 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. The invention 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 such as SMARCA4-related/deficient cancer, such as lung cancer or non-small cell lung cancer, are treated or prevented with compounds and compositions of the present disclosure. Thus, I was prepared by coupling of 2-[2-[2-[4-[3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl]-1H-pyrazol-1-yl]ethoxy]eth oxy]acetic acid (preparation given) with (2S,4R)-1-((S)-2-amino-3,3-dimethylbutanoyl)-4-hydroxy-N-[4-(4-methylthiazol-5-yl )benzyl]pyrrolidine-2-carboxamide. A Western blot assay was used to assess the BRM degradation (Dmax and DC50) in SW 1573 cells; I displayed a DC50 ≥ 30 nM and DC50 > 75. 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 chimeric mol preparation targeted brm smarca2 degradation ubiquitination, protac modulator preparation targeted ubiquitination brm degradation inhibition antitumor, von hippel lindau dipeptide ligand preparation brm protac inhibition and other aspects.Formula: C17H26O7S

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

On February 27, 2020, Crew, Andrew P.; Dong, Hanqing; Berlin, Michael; Sparks, Steven M. published a patent.Category: esters-buliding-blocks The title of the patent was Preparation of proteolysis targeting chimeric (PROTAC) compounds with E3 ubiquitin ligase binding activity and targeting α-synuclein protein for treating neurodegenerative diseases. And the patent contained the following:

The present disclosure relates to bifunctional compounds, which find utility as modulators of α-synuclein (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, inhibitors of apoptosis 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. A bifunctional compounds I [ULM-L-PTM; wherein the ULM = a small mol. E3 ubiquitin ligase binding moiety; the PTM = a small mol. comprising a α-synuclein protein targeting moiety; and the L = a bond or a chem. linking moiety connecting the ULM and the PTM] or pharmaceutically acceptable salts, enantiomers, stereoisomers, solvates, polymorphs or prodrugs thereof, were disclosed. E.g., a multi-step synthesis of II, starting from 2-(2-benzyloxyethoxy)ethanol and tert-Bu 2-bromoacetate, was described. Targeted degradation of sarkosyl insoluble (SI) α-synuclein via exemplary bifunctional compounds I was assessed by MJFF-14-6-4-2 conformation specific ELISA following treatment of PFF-induced A53T α-synuclein overexpressing HEK293 cells with 1μM exemplary compound compared to DMSO vehicle control (data given for representative compounds I). Diseases or disorders that result from aggregation or accumulation of the target protein are α-synucleinopathies or neurodegenerative diseases associated with α-synuclein accumulation and aggregation, such as e.g., Parkinson disease, Alzheimer’s disease, dementia, dementia with Lewy bodies or multiple system atrophy, in particular Parkinson’s disease. 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 proteolysis targeting chimeric protac bifunctional compound preparation protein degradation, sarkosyl insoluble alpha synuclein targeted degradation bifunctional compound preparation, alpha synucleinopathy neurodegenerative disease treatment bifunctional compound preparation and other aspects.Category: esters-buliding-blocks

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