cas 874302-76-8, 4-nitrophenyl 2-(2-(pyridin-2-yl)disulfanyl)ethyl carbonate

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Multifunctionalization of magnetic nanoparticles for controlled drug release: A general approach
In this study, a general approach for the multifunctionalization of magnetic nanoparticles (MNPs) with drugs (Doxorubicin and Gemcitabine) and targeting moieties (Nucant pseudopeptide) for controlled and selective release is described. The functionalizati
Latorre, Alfonso,Couleaud, Pierre,Aires, Antonio,Cortajarena, Aitziber L.,Somoza, álvaro
p. 355 - 362
(2014)
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Conjugation Chemistry-Dependent T-Cell Activation with Spherical Nucleic Acids
Spherical nucleic acids (SNAs) can be potent sequence-specific stimulators of antigen presenting cells (APCs). When loaded with peptide antigens, they can be used to activate the immune system to train T-cells to specifically kill cancer cells. Herein, th
Skakuj, Kacper,Wang, Shuya,Qin, Lei,Lee, Andrew,Zhang, Bin,Mirkin, Chad A.
p. 1227 - 1230
(2018)
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GLP1R AGONIST NMDAR ANTAGONIST CONJUGATES
The present invention relates to a conjugated molecule comprising a peptide displaying at least 0.1% activity of native glucagon-like peptide 1 (GLP-1) at the GLP-1 receptor, and an N-methyl-D-aspartate receptor (NMDAR) antagonist, the peptide being coval
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(2021/12/28)

CONJUGATED CHEMICAL INDUCERS OF DEGRADATION AND METHODS OF USE
The subject matter described herein is directed to antibody-CIDE conjugates (Ab-CIDEs), to pharmaceutical compositions containing them, and to their use in treating diseases and conditions where targeted protein degradation is beneficial.
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(2020/05/28)

ANTICANCER DRUGS AND METHODS OF MAKING AND USING SAME
The present invention provides drug modifications for improving biodistribution and/or specificity of an anticancer drug. In certain embodiments, the compound of the invention comprises a drug, a linker and a core acid. The core acid can be varied to tune
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(2020/08/13)

Amplified Self-Immolative Release of Small Molecules by Spatial Isolation of Reactive Groups on DNA-Minimal Architectures
Triggering the release of small molecules in response to unique biomarkers is important for applications in drug delivery and biodetection. Due to low quantities of biomarker, amplifying release is necessary to gain appreciable responses. Nucleic acids have been used for both their biomarker-recognition properties and as stimuli, notably in amplified small-molecule release by nucleic-acid-templated catalysis (NATC). The multiple components and reversibility of NATC, however, make it difficult to apply in vivo. Herein, we report the use of the hybridization chain reaction (HCR) for the amplified, conditional release of small molecules from standalone nanodevices. We couple HCR with a DNA-templated reaction resulting in the amplified, immolative release of small molecules. We integrate the HCR components into single nanodevices as DNA tracks and spherical nucleic acids, spatially isolating reactive groups until triggering. This could be applied to biosensing, imaging, and drug delivery.
Hennecker, Christopher,Mittermaier, Anthony,Prinzen, Alexander L.,Saliba, Daniel,Sleiman, Hanadi F.,Trinh, Tuan
p. 12900 - 12908
(2020/06/02)

POLYMERIC CONJUGATES AND USES THEREOF
The present invention relates to novel chemical entities comprising a polymeric carrier incorporating covalently linked drug(s) as well as their pharmaceutical compositions containing the said polymer-drug conjugates as pharmaceutical agents and their use
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(2020/10/18)

Reduction response type Her2-targeting polypeptide drug conjugate as well as preparation method and application thereof
The invention relates to a reduction response type Her2-targeting polypeptide drug conjugate as well as a preparation method and application thereof. The polypeptide drug conjugate has the molecular structural formula shown in a formula I, wherein Aaa1 is
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Paragraph 0047; 0057; 0058; 0065

(2020/05/30)

CONJUGATION OF PEPTIDES TO SPHERICAL NUCLEIC ACIDS (SNAS) USING TRACELESS LINKERS
The present disclosure provides compositions and methods directed to combining spherical nucleic acid (SNA) components that are required for T-cell activation and proliferation.
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(2020/12/14)

Anticancer Drugs and Methods of Making and Using Same
The present invention provides drug modifications for improving biodistribution and/or specificity of an anticancer drug. In certain embodiments, the compound of the invention comprises a drug, a linker and a core acid. The core acid can be varied to tune
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(2019/02/13)

BICYCLIC PEPTIDE LIGAND PRR-A CONJUGATES AND USES THEREOF
The present invention provides compounds, compositions thereof, and methods of using the same.
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(2019/03/05)

Stabilizing p-Dithiobenzyl Urethane Linkers without Rate-Limiting Self-Immolation for Traceless Drug Release
Exploiting the redox sensitivity of disulfide bonds is a prevalent strategy in targeted prodrug designs. In contrast to aliphatic disulfides, p-thiobenzyl-based disulfides have rarely been used for prodrug designs, given their intrinsic instability caused by the low pKa of aromatic thiols. Here, we examined the interplay between steric hindrance and the low-pKa effect on thiol–disulfide exchange reactions and uncovered a new thiol–disulfide exchange process for the self-immolation of p-thiobenzyl-based disulfides. We observed a central leaving group shifting effect in the α,α-dimethyl-substituted p-dithiobenzyl urethane linkers (DMTB linkers), which leads to increased disulfide stability by more than two orders of magnitude, an extent that is significantly greater than that observed with typical aliphatic disulfides. In particular, the DMTB linkers display not only high stability, but also rapid self-immolation kinetics due to the low pKa of the aromatic thiol, which can be used as a general and robust linkage between targeting reagents and cytotoxic drugs for targeted prodrug designs. The unique and promising stability characteristics of the present DMTB linker will likely inspire the development of novel targeted prodrugs to achieve traceless release of drugs into cells.
Zheng, Yiwu,Shen, Yang,Meng, Xiaoting,Wu, Yaqi,Zhao, Yibing,Wu, Chuanliu
p. 1196 - 1203
(2019/05/28)

Water-soluble anti-tumor compounds
The invention relates to a water-soluble antitumor compound represented by the formula (I), and further relates to a preparation method of the compound and an application of the compound in preparation of antitumor drugs. Stable prodrug with a good water
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(2019/05/04)

COMPOUNDS, COMPOSITIONS, AND METHODS FOR TREATMENT OF DISEASES INVOLVING ACIDIC OR HYPOXIC DISEASED TISSUES
Compounds for treatment of diseases having acidic or hypoxic diseased tissues and pharmaceutical compositions comprising the compounds, as well as methods for making and using the compounds and compositions.
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(2019/07/20)

Reduced response-type amphiphilic polymer prodrug and preparation method and application thereof
The invention relates to a reduced response-type amphiphilic polymer prodrug and a preparation method and an application thereof. The prodrug has a molecular structure as a formula I, wherein X is O or NH, ROH is a hydrophobic antitumor drug, n is from 5
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(2019/07/31)

Amphiphilic polymer drug precursor of reduced response type kazeptine and preparation method and application thereof (by machine translation)
The invention relates to an amphiphilic polymer drug precursor of reduced response type kazeptine and a preparation method and application, and the amphipathic polymer drug precursor has the molecular structure shown below: Wherein, the degree of polymeri
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(2019/08/01)

Reduction-responsive tumor-targeting polypeptide pharmic conjugate and preparation method and application thereof
The invention relates to a reduction-responsive tumor-targeting polypeptide pharmic conjugate and a preparation method and application thereof. The reduction-responsive tumor-targeting polypeptide pharmic conjugate has a molecular structural formula shown
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(2019/10/23)

PYRROLOBENZODIAZEPINE ANTIBODY DRUG CONJUGATES AND METHODS OF USE
The invention provides antibody-drug conjugates comprising an antibody conjugated to a pyrrolobenzodiazepine drug moiety via a disulfide linker, pyrrolobenzodiazepine linker-drug intermediates, and methods of using the antibody-drug conjugates.
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Paragraph 0593; 0594

(2017/04/23)

Modulated Fragmentation of Proapoptotic Peptide Nanoparticles Regulates Cytotoxicity
Peptides perform a diverse range of physiologically important functions. The formulation of nanoparticles directly from functional peptides would therefore offer a versatile and robust platform to produce highly functional therapeutics. Herein, we engineered proapoptotic peptide nanoparticles from mitochondria-disrupting KLAK peptides using a template-assisted approach. The nanoparticles were designed to disassemble into free native peptides via the traceless cleavage of disulfide-based cross-linkers. Furthermore, the cytotoxicity of the nanoparticles was tuned by controlling the kinetics of disulfide bond cleavage, and the rate of regeneration of the native peptide from the precursor species. In addition, a small molecule drug (i.e., doxorubicin hydrochloride) was loaded into the nanoparticles to confer synergistic cytotoxic activity, further highlighting the potential application of KLAK particles in therapeutic delivery.
Suma, Tomoya,Cui, Jiwei,Müllner, Markus,Fu, Shiwei,Tran, Jenny,Noi, Ka Fung,Ju, Yi,Caruso, Frank
p. 4009 - 4018
(2017/03/31)

PROTAC ANTIBODY CONJUGATES AND METHODS OF USE
The subject matter described herein is directed to antibody-PROTAC conjugates (PACs), to pharmaceutical compositions containing them, and to their use in treating diseases and conditions where targeted protein degradation is beneficial.
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(2017/12/18)

Design, synthesis, and evaluation of water-soluble morpholino-decorated paclitaxel prodrugs with remarkably decreased toxicity
Novel water-soluble paclitaxel prodrugs were designed and synthesized by introducing morpholino groups through different linkers. These derivatives showed 400–20,000-times greater water solubility than paclitaxel as well as comparable activity in MCF-7 an
Feng, Siliang,Chen, Kuncheng,Wang, Chenhong,Jiang, Xifeng,Dong, Huajin,Gong, Zehui,Liu, Keliang
p. 3598 - 3602
(2016/07/21)

FUNCTIONALISED MAGNETIC NANOPARTICLE
The present invention relates to functionalised magnetic nanoparticles and the process for preparing said functionalised magnetic nanoparticles. The invention also relates to the pharmaceutical composition comprising the functionalised magnetic nanopartic
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(2016/10/11)

ANTHRACYCLINE DISULFIDE INTERMEDIATES, ANTIBODY-DRUG CONJUGATES AND METHODS
The invention provides antibody-drug conjugates comprising an antibody conjugated to an anthracycline drug moiety via a disulfide linker, anthracycline disulfide intermediates, and methods of using the antibody-drug conjugates.
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(2016/04/09)

A new delivery system for auristatin in STxB-drug conjugate therapy
A key challenge in anticancer therapy is to gain control over the biodistribution of cytotoxic drugs. The most promising strategy consists in conjugating drugs to tumor-targeting carriers, thereby combining high cytotoxic activity and specific delivery. To target Gb3-positive cancer cells, we exploit the non-toxic B-subunit of Shiga toxin (STxB). Here, we have conjugated STxB to highly potent auristatin derivatives (MMA). A former linker was optimized to ensure proper drug-release upon reaching reducing environments in target cells, followed by a self-immolation step. Two conjugates were successfully obtained, and in vitro assays demonstrated the potential of this targeting system for the selective elimination of Gb3-positive tumors.
Batisse, Cornélie,Dransart, Estelle,Ait Sarkouh, Rafik,Brulle, Laura,Bai, Siau-Kun,Godefroy, Sylvie,Johannes, Ludger,Schmidt, Frédéric
p. 483 - 491
(2015/04/14)

CONJUGATES OF THE B-SUBUNIT OF SHIGA TOXIN FOR ANTICANCER THERAPIES
Conjugates or pharmaceutical compositions comprising conjugates of the B-subunit of Shiga toxin that are useful for cancer therapies are disclosed. More specifically, the pharmaceutical compositions comprise STxB conjugated to at least one antimitotic age
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(2014/06/24)

CYCLODEXTRIN-BASED POLYMERS FOR THERAPEUTIC DELIVERY
Methods and compositions relating to CDP-taxane conjugates are described herein.
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(2013/08/14)

METHODS OF TREATING A SUBJECT AND RELATED PARTICLES, POLYMERS AND COMPOSITIONS
Described herein are methods for treating a subject with combinations of polymer-agent particles and cyclodextrin polymer agent conjugates. The methods herein may be used to treat subjects identified with cancer, cardiovascular disorders, autoimmune disorders, or inflammatory disorders. Also described herein are compositions, dosage forms, and kits comprising polymer-agent particles and cyclodextrin polymer agent conjugates.
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(2012/04/17)

CYCLODEXTRIN-BASED POLYMERS FOR THERAPEUTIC DELIVERY
Methods and compositions relating to CDP-taxane conjugates are described herein.
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(2011/06/19)

A reduction sensitive cascade biodegradable linear polymer
Cascade degradable linear polymers offer the potential for a high degree of control over the degradation process. They comprise a backbone that is stable in the presence of an end cap, but upon removal of the end cap a cascade of intramolecular reactions
Dewit, Matthew A.,Beaton, Annelise,Gillies, Elizabeth R.
experimental part
p. 3977 - 3985
(2011/11/01)

COMPOSITIONS AND METHODS FOR TRANSPORT OF MOLECULES WITH ENHANCED RELEASE PROPERTIES ACROSS BIOLOGICAL BARRIERS
Conjugates of a cargo molecule with a transporter molecule are disclosed, where the cargo molecule and the transporter molecule are linked covalently by a releasable linker. The cargo of the conjugate can be a biologically active agent or a reporter molec
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Page/Page column 76; 78

(2008/12/06)

Aryldithioethyloxycarbonyl (Ardec): A new family of amine protecting groups removable under Mild reducing conditions and their applications to peptide synthesis
The development of phenyl-dithioethyloxycarbonyl (Phdec) and 2-pyridyldithioethyloxycarbonyl (Pydec) protecting groups, which are thiollabile urethanes, is described. These new disulfide-based protecting groups were introduced onto the ε-amino group of L-
Lapeyre, Milaine,Leprince, Jerome,Massonneau, Marc,Oulyadi, Hassan,Renard, Pierre-Yves,Romieu, Anthony,Turcatti, Gerardo,Vaudry, Hubert
p. 3655 - 3671
(2008/02/05)

BIVALENT LINKERS AND CONJUGATES THEREOF
Bivalent linkers derived from compounds of formulae (V), (VI) and (VII), where X1 and X2 are leaving groups and the other variables are as defined in the claims, to be included in or for preparing vitamin, drug, diagnostic agent, and
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Page/Page column 20-21

(2008/06/13)