cas 518044-32-1, Hydroxy-PEG-5-t-butyl ester

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A new route for the synthesis of 1-amino-3,6,9,12-tetraoxapentadecan-15-oic acid
1-Amino-3,6,9,12-tetraoxapentadecan-15-oic acid 8 was synthesised from tetraethylene glycol through a 7 step sequence including esterification, mesylation, azide substitution with subsequent reduction followed by hydrolysis. The structure of product 8 was
Wu, Xuan,Zong, Xi,Ji, Min
p. 368 - 370
(2016)
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PROTAC small molecular compound and application thereof
The invention discloses a compound with a general formula I, or a pharmaceutically acceptable salt, a stereoisomer, an ester, a prodrug, a solvate and a deuterated compound thereof, a composition containing the compound with the general formula I, and application of the compound with the general formula I or the pharmaceutically acceptable salt, stereoisomer, ester, prodrug, solvate and deuteratedcompound thereof in preparation of medicines for treating diseases related to serine/threonine kinase family (MAP4Ks), preferably medicines for treating diseases related to hematopoietic stem cell kinase 1 (HPK1).
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Paragraph 0251-0253

(2021/03/30)

USES OF ANTI-CD3 ANTIBODY FOLATE BIOCONJUGATES
Described herein are anti-CD3 antibody folate bioconjugates and uses thereof in the treatment of diseases, conditions, and cancers.
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Paragraph 00357; 00358

(2021/09/03)

COMPOUNDS AND METHODS FOR THE TREATMENT OF OCULAR DISORDERS
Described herein are compositions and methods for the treatment of ocular surface disorders including meibomian gland dysfunction, blepharitis, dry eye disease and other inflammatory/ infections disease of the anterior surface of the eye. Said compositions and methods comprise keratolytic conjugate which demonstrate keratolytic activity, and anti-inflammatory or other desirable activities. Topical administration of said compositions to the eye, ocular surface or surrounding areas provides therapeutic benefit to patients suffering from ocular surface disorders.
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Paragraph 00212-00213

(2020/10/27)

Optimization of IEDDA bioorthogonal system: Efficient process to improve trans-cyclooctene/tetrazine interaction
The antibody pretargeting approach for radioimmunotherapy (RIT) using inverse electron demand Diels-Alder cycloaddition (IEDDA) constitutes an emerging theranostic approach for solid cancers. However, IEDDA pretargeting has not reached clinical trial. The major limitation of the IEDDA strategy depends largely on trans-cyclooctene (TCO) stability. Indeed, TCO may isomerize into the more stable but unreactive cis-cyclooctene (CCO), leading to a drastic decrease of IEDDA efficiency. We have thus developed both efficient and reproducible synthetic pathways and analytical follow up for (PEGylated) TCO derivatives, providing high TCO isomeric purity for antibody modification. We have set up an original process to limit the isomerization of TCO to CCO before the mAbs’ functionalization to allow high TCO/tetrazine cycloaddition.
Béquignat, Jean-Baptiste,Boucheix, Claude,Canitrot, Damien,Chezal, Jean-Michel,Degoul, Fran?oise,Miot-Noirault, Elisabeth,Moreau, Emmanuel,Navarro-Teulon, Isabelle,Quintana, Mercedes,Rondon, Aurélie,Taiariol, Ludivine,Ty, Nancy
supporting information

(2020/07/21)

ANTI-CD3 ANTIBODY FOLATE BIOCONJUGATES AND THEIR USES
Described herein are novel anti-CD3 Folate antibodies and uses thereof in the treatment of diseases or conditions that would benefit from such.
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Paragraph 00338; 00349; 00350

(2020/03/23)

BIFUNCTIONAL SUBSTITUED PYRIMIDINES AS MODULATORS OF FAK PROTEOLYSE
The present disclosure relates to bifunctional compounds, which find utility as modulators of focal adhesion kinase (FAK) or protein tyrosine kinase 2 (PTK2). 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.
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Paragraph 00399; 00413; 00415

(2020/02/16)

Preparation method, raw material, product and application of photo-crosslinking hydrogel material
The invention provides a preparation method, a raw material, a product and an application of a photo-crosslinking hydrogel material. The preparation method comprises the steps of dissolving a component A, namely a photosensitive high polymer derivative, i
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Paragraph 0668; 0669; 0676

(2019/06/07)

STEROIDS AND PROTEIN-CONJUGATES THEREOF
Described herein protein steroid conjugates that are useful, for example, for the target-specific delivery of glucocorticoids (GCs) to cells.
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Paragraph 0638-0639

(2018/05/27)

Addressing Kinase-Independent Functions of Fak via PROTAC-Mediated Degradation
Enzymatic inhibition has proven to be a successful modality for the development of many small-molecule drugs. In recent years, small-molecule-induced protein degradation has emerged as an orthogonal therapeutic strategy that has the potential to expand the druggable target space. Focal adhesion kinase (Fak) is a key player in tumor invasion and metastasis, acting simultaneously as a kinase and a scaffold for several signaling proteins. While previous efforts to modulate Fak activity were limited to kinase inhibitors with low success in clinical studies, protein degradation offers a possibility to simultaneously block Fak's kinase signaling and scaffolding capabilities. Here, we report the development of a selective and potent Fak degrader, PROTAC-3, which outperforms a clinical candidate, defactinib, with respect to Fak activation as well as Fak-mediated cell migration and invasion. These results underline the potential that PROTACs offer in expanding the druggable space and controlling protein functions that are not easily addressed by traditional small-molecule therapeutics.
Cromm, Philipp M.,Samarasinghe, Kusal T. G.,Hines, John,Crews, Craig M.
supporting information
p. 17019 - 17026
(2019/01/04)

OPTIMIZED TRANSGLUTAMINASE SITE-SPECIFIC ANTIBODY CONJUGATION
Provided herein are methods and compositions for site-specific conjugation of antibodies.
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Paragraph 00162

(2017/09/15)

A-amido glycol propionic acid preparation method (by machine translation)
The invention discloses a-amido glycol propionic acid (NH2 - PEGn - CH2 CH2 C00H, n=1 - 24) of the preparation method, the preparation method in order to mono-disperse small molecular double-hydroxy polyethylene
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Paragraph 0021

(2017/10/22)

CRYPTOPHYCIN-BASED ANTIBODY-DRUG CONJUGATES WITH NOVEL SELF-IMMOLATIVE LINKERS
The present invention relates to antibody- or peptide-drug conjugate compounds where one or more cryptophycin derivatives (macrocyclic depsipeptide) are covalently attached by a self-immolative linker which binds to one or more tumor-associated antigens or cell-surface receptors. The linker contains a cleavage site for proteases and a dipeptide unit able to form a diketopiperazine. These compounds may be useful in methods of diagnosis or treatment of cancer, and other diseases and disorders, such as immune or infective diseases.
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Page/Page column 20

(2016/10/04)

ANTIBODY-DRUG CONJUGATES
Disclosed are anti-5T4 antibody drug conjugates with an improved pharmacokinetic profile and methods for preparing and using the same. In one embodiment, the antibody-drug conjugate has the formula Ab-(D)p, wherein Ab is an anti-5T4 antibody comprising a non- natural amino acid; D is a dolastatin linker derivative; and p is from about 1 to about 8.
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Page/Page column 20

(2013/05/23)

ANTI-CD70 ANTIBODY DRUG CONJUGATES
This invention relates to anti-CD70 antibodies and antibody drug conjugates comprising at least one non-naturally-encoded amino acid. Disclosed herein are αCD70 antibodies with one or more non-naturally encoded amino acids and further disclosed are antibody drug conjugates wherein the αCD70 antibodies of the invention are conjugated to one or more toxins. Further disclosed are methods for using such non-natural amino acid antibody drug conjugates, including therapeutic, diagnostic, and other biotechnology uses.
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Paragraph 00458; 00479

(2014/01/09)

PROSTATE-SPECIFIC MEMBRANE ANTIGEN ANTIBODY DRUG CONJUGATES
This invention relates to prostate-specific membrane antigen (PSMA) antibodies and antibody drug conjugates comprising at least one non-naturally-encoded amino acid. Disclosed herein are αPSMA antibodies with one or more non-naturally encoded amino acids and further disclosed are antibody drug conjugates wherein the αPSMA antibodies of the invention are conjugated to one or more toxins. Also disclosed herein are non-natural amino acid dolastatin analogs that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such dolastatin analogs. Typically, the modified dolastatin analogs include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid antibody drug conjugates, dolastatin analogs, and modified non-natural amino acid dolastatin analogs, including therapeutic, diagnostic, and other biotechnology uses.
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Paragraph 00444

(2014/01/08)

Proline-functionalized magnetic core-shell nanoparticles as efficient and recyclable organocatalysts for aldol reactions
Novel magnetically tagged organocatalysts have been developed based on core-shell nanoparticles consisting of magnetite cores and polyacrylate shells containing 4-hydroxyproline moieties. These catalysts allow the performance of direct asymmetric aldol re
Yacob, Zekarias,Nan, Alexandrina,Liebscher, Juergen
supporting information
p. 3259 - 3264
(2013/01/15)

COMPOSITIONS CONTAINING, METHODS INVOLVING, AND USES OF NON-NATURAL AMINO ACID LINKED DOLASTATIN DERIVATIVES
Disclosed herein are non-natural amino acids and dolastatin analogs that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The dolastatin analogs can include a wide range of possible functionalities, but typically have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid dolastatin analogs that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such dolastatin analogs. Typically, the modified dolastatin analogs include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid dolastatin analogs and modified non-natural amino acid dolastatin analogs, including therapeutic, diagnostic, and other biotechnology use.
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Page/Page column 163; 168

(2013/02/28)

Syntheses and characterizations of novel pyrrolocoumarin probes for SNAP-tag labeling technology
SNAP-tag technology is a revolutionary protein labeling technology employing in various biological studies. Since low signal/noise ratio and severe overlap between the FRET donors/acceptors often occurred in applying present fluorescent probes and thus limited the further applications, development of new fluorescent probes with excellent fluorescent properties is still of request by today's SNAP-tag technology. In this paper, a number of SNAP-tag protein probes have been developed by incorporating a novel pyrrolocoumarin fluorophore recently developed by our group. Examination of these novel synthetic compounds shows all these materials possess satisfactory fluorescent properties. Among these, probe 7 exhibits the most excellent characters, and its quantum yield, maximum emission wavelength and Stocks shift reach to 0.44, 534 nm and 112 nm, respectively. Further analysis of structure-property relationship indicates that the probes with a longer C3-substituted alkyl (such as pentyl) give stronger fluorescence.
Mei, De-Sheng,Qu, Yi,He, Jin-Xiang,Chen, Lei,Yao, Zhu-Jun
experimental part
p. 2251 - 2259
(2011/04/22)

Spacer-separated sialyl LewisX cyclopeptide conjugates as potential E-selectin ligands
Completely protected sialyl LewisX azide was synthesized from a neolactosamine azide precursor carrying a 3-O-allyloxycarbonyl group as the temporary protecting group. After its Pd(0)-catalyzed deprotection and stereoselective α-fucosylation, the obtained
Herzner, Holger,Kunz, Horst
p. 541 - 557
(2008/03/13)

Synthesis of novel heterobifunctional isocyanato cross-linkers and their applications for the preparation of 10-hydroxycamptothecin and SN-38 conjugates with melanotransferrin p97
Novel heterobifunctional cross-linkers with an isocyanato group, a protected carboxylic group, and a linear chain spacer are synthesized in high yield by coupling monofunctionalized PEG with 1,6-diisocyanatohexane. The isocyanato groups of those linkers are highly reactive and are efficient reagents to couple with the hydroxy groups of 10-hydroxycamptothecin and SN-38 under mild conditions to give a useful precursor for the synthesis of their bioconjugates with proteins such as melanotransferrin p97. Copyright Taylor & Francis Group, LLC.
Li, Zhong,Yang, Dingqiao,Gabathuler, Reinhard,Chen, Qingqi
p. 1899 - 1915
(2008/02/03)

CHEMICAL LINKERS AND CONJUGATES THEREOF
The present disclosure provides drug-ligand conjugates that are potent cytotoxins, wherein the drug is linked to the ligand through either a peptidyl, hydrazine, or disulfide linker. The disclosure is also directed to compositions containing the drug-liga
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Page/Page column 150

(2008/06/13)

CYTOTOXIC AGENTS BEARING A REACTIVE POLYETHYLENE GLYCOL MOIETY, CYTOTOXIC CONJUGATES COMPRISING POLYETHYLENE GLYCOL LINKING GROUPS, AND METHODS OF MAKING AND USING THE SAME
Cytotoxic agents bearing a polyethylene glycol (PEG) linking group having a terminal active ester, cytotoxic conjugates comprising one or more cytotoxic agents linked to a cell-binding agent via PEG linking groups, and methods for producing both are disclosed. A therapeutic composition comprising a therapeutically-effective amount of one of the cytotoxic conjugates of the present invention, and a method of killing selected cell populations comprising contacting target cells, or tissue containing target cells, with an effective amount of one of the cytotoxic conjugates, are also disclosed.
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(2008/06/13)

Efficient synthesis of polyethylene glycol mono-carboxylate via Michael conjugate addition
Poly(ethylene glycol) (PEG) with one carboxylate group, the very useful precursors for the synthesis of the PEG derived heterobifunctional linkers, are synthesized in high yield in one-pot via Michael conjugate addition of acrylate esters with PEG and catalyst amount of sodium in THF.
Chen, Qingqi,Gabathuler, Reinhard
p. 2425 - 2432
(2007/10/03)

Synthesis of taxoids with improved cytotoxicity and solubility for use in tumor-specific delivery
To develop effective taxane-antibody immunoconjugates, we have prepared a series of modified taxanes that have both improved toxicity and solubility in aqueous systems as compared to paclitaxel (1a). These taxanes have been modified at either the C-10 or
Miller, Michael L.,Roller, Elizabeth E.,Zhao, Robert Y.,Leece, Barbara A.,Ab, Olga,Baloglu, Erkan,Goldmacher, Victor S.,Chari, Ravi V. J.
p. 4802 - 4805
(2007/10/03)