207850-04-2Relevant articles and documents
Dendrimer-like star polymers
Trolls?s, Mikael,Hedrick, James L.
, p. 4644 - 4651 (1998)
Dendrimer-like star polymers, a novel type of molecular architecture, have been synthesized. The architecture of the new polymers resembles that of three-dimensional spherical dendrimers as well as classical star polymers. The controlled structures, based
Synthesis and characterization of linear, homopolyester, benzoyl-protected Bis-MPA
Kareem, Oluwapelumi O.,Daymon, Samantha P.,Keller, Christopher B.,Chen, Beibei,Nazarenko, Sergei,Grayson, Scott M.
, p. 6608 - 6618 (2020)
Because of the growing interest in bis-MPA dendrimers and hyperbranched polymers, a linear, polyester equivalent is of great importance in understanding how this commercially viable family of branched polymers behaves when compared to their linear analogs
Non-nucleosidic analogues of polyaminonucleosides and their influence on thermodynamic properties of derived oligonucleotides
Brzezinska, Jolanta,Markiewicz, Wojciech T.
, p. 12652 - 12669 (2015)
The rationale for the synthesis of cationic modified nucleosides is higher expected nuclease resistance and potentially better cellular uptake due to an overall reduced negative charge based on internal charge compensation. Due to the ideal distance between cationic groups, polyamines are perfect counterions for oligodeoxyribonucleotides. We have synthesized non-nucleosidic analogues built from units that carry different diol structures instead of sugar residues and functionalized with polyamines. The non-nucleosidic analogues were attached as internal or 5′-terminal modifications in oligodeoxyribonucleotide strands. The thermodynamic studies of these polyaminooligonucleotide analogues revealed stabilizing or destabilizing effects that depend on the linker or polyamine used.
Tumor-Targeting Micelles Based on Linear-Dendritic PEG-PTX8 Conjugate for Triple Negative Breast Cancer Therapy
Zhang, Yujie,Lu, Yifei,Zhang, Yu,He, Xi,Chen, Qinjun,Liu, Lisha,Chen, Xinli,Ruan, Chunhui,Sun, Tao,Jiang, Chen
, p. 3409 - 3421 (2017)
Most small molecular chemotherapeutics have poor water solubility and unexpected pharmacokinetics and toxicity to normal tissues. A series of nano drug delivery systems have been developed to solve the problems, among which a micelle based on linear-dendritic polymer-drug conjugates (LDPDCs) is a promising strategy to deliver hydrophobic chemotherapeutics due to its small size, fine stability in blood circulation, and high drug loading capacity. In this work we synthesized a novel amphiphilic linear-dendritic PEG-PTX8 conjugate which can also encapsulate extra free PTX and self-assemble into uniform ultrasmall micelles with a hydrated diameter of 25.50 ± 0.27 nm. To realize efficient drug delivery to tumor sites, a cyclic tumor homing and penetrating peptide iNGR was linked to the PEG-PTX8 conjugate. The biological evaluation was performed on a human triple negative breast cancer model. PTX accumulation in tumor at 24 h of the TNBC-bearing mice treated with iNGR-PEG-PTX8/PTX micelles was significantly enhanced (P 8/PTX micelles. Furthermore, iNGR-PEG-PTX8/PTX micelles showed an obvious strong antitumor effect, and the median survival time of TNBC bearing mice treated with iNGR-modified micelles was significantly extended compared to Taxol. Therefore, this smart micelle system may be a favorable platform for effective TNBC therapy.
Selective monobenzylation of 2,2-bis(hydroxymethyl)propionic acid (bis-MPA) to yield an AB linear monomer and analogous linear oligomers
Giesen, Joseph A.,Grayson, Scott M.
supporting information, (2020/05/28)
The synthesis of a mono-benzylated AB monomer based on bis-MPA is explored and accomplished via a three-step synthesis without column chromatography. This optimized synthesis utilizes a generic acid-catalyzed esterification of bis-MPA to the ethyl ester.
Polymeric conjugates of active principles, their process of preparation and their polymeric intermediates
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Page/Page column 12, (2016/06/01)
The present invention relates to novel conjugates of active principles grafted to a polymer, to the nanoparticles comprising them, to their preparation and to their polymeric intermediates.
The first peripherally masked thiol dendrimers: A facile and highly efficient functionalization strategy of polyester dendrimers via one-pot xanthate deprotection/thiol-acrylate Michael addition reactions
Auty, Sam E. R.,Andrén, Oliver,Malkoch, Michael,Rannard, Steven P.
supporting information, p. 6574 - 6577 (2014/06/10)
Introducing multiple reactive functional groups at the periphery of dendrimer materials presents considerable challenges if the functionality is able to self-react. An efficient and facile approach to introducing masked thiols at the surface of polyester dendrimers is presented. One-pot, deprotection/thiol-acrylate Michael addition from the xanthate-functional dendritic substrates (generation zero to two) has been achieved for the first time, with high efficiency demonstrated using three acrylates of varying chemistry and avoiding disulfide formation. This journal is the Partner Organisations 2014.
METHOD FOR PREPARING TEMSIROLIMUS
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Paragraph 0028, (2013/11/19)
A method for preparing temsirolimus, the method including: using a substituted aromatic aldehyde to protect 2,2-dimethylol propionic acid to produce intermediate II; carrying out reaction between the intermediate II and 2,4,6-trichlorobenzoyl chloride; carrying out condensation reaction between a resulting product and rapamycin to produce intermediate III; and finally using sulfuric acid to remove a protecting group from the intermediate III to yield temsirolimus.
PROCESS FOR PREPARING TORISEL
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Paragraph 0022, (2013/12/02)
A process for preparing Torisel, which is a derivative of Rapamycin, is provided. The process comprises the following steps: acetalating 2,2-dihydroxymethylpropionic acid with substituted or unsubstituted aromatic aldehyde in the presence of p-toluenesulfonic acid as catalyst to form the intermediate II; reacting the obtained intermediate with 2,4,6-trichlorobenzoyl chloride; then esterifying the obtained chloride with Rapamycin and finally deprotecting the diol to provide the product Torisel with yield over 35.6%. The aromatic aldehyde is one selected from benzaldehyde, p-methoxybenzaldehyde, p-chlorobenzaldehyde and p-trifluoromethyl benzaldehyde.
8-Azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists
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Page/Page column 39, (2008/06/13)
The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R1, R2, R3, A, and G are defined in the specification, or a pharmaceutically-acceptable salt or solvate thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.