98168-52-6Relevant academic research and scientific papers
Triglyceride-mimetic structure-gated prodrug nanoparticles for smart cancer therapy
Tian, Chutong,Guo, Jingjing,Miao, Yifan,Zheng, Shunzhe,Sun, Bingjun,Sun, Mengchi,Ye, Qing,Liu, Wenxue,Zhou, Shuang,Kamei, Ken-Ichiro,He, Zhonggui,Sun, Jin
, p. 15936 - 15948 (2021/11/18)
Off-target drug release and insufficient drug delivery are the main obstacles for effective anticancer chemotherapy. Prodrug-based self-assembled nanoparticles bioactivated under tumor-specific conditions are one of the effective strategies to achieve on-demand drug release and effective tumor accumulation. Herein, stimuli-activable prodrugs are designed yielding smart tumor delivery by combination of the triglyceride-mimic (TG-mimetic) prodrug structure and disulfide bond. Surprisingly, these prodrugs can self-assemble into uniform nanoparticles (NPs) with a high drug loading (over 40%) and accumulate in tumor sites specifically. The super hydrophobic TG structure can act as a gate that senses lipase to selectively control over NP dissociation and affect the glutathione-triggered prodrug activation. In addition, the impacts of the double bonds in the prodrug NPs on parent drug release and the following cytotoxicity, pharmacokinetics, and antitumor efficiency are further demonstrated. Our findings highlight the promising potential of TG-mimetic structure-gated prodrug nanoparticles for tumor-specific drug delivery.
LIPID PRODRUGS OF PREGNANE NEUROSTEROIDS AND USES THEREOF
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Paragraph 00420; 00422, (2020/02/23)
The present invention provides lymphatic system-directing lipid prodrugs, pharmaceutical compositions thereof, methods of producing such prodrugs and compositions, as well as methods of improving the bioavailability or other properties of a therapeutic agent that comprises part of the lipid prodrug. The present invention also provides methods of treating a disease, disorder, or condition such as those disclosed herein, comprising administering to a patient in need thereof a disclosed lipid prodrug or a pharmaceutical composition thereof.
LIPID PRODRUGS OF JAK INHIBITORS AND USES THEREOF
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Paragraph 00587; 00589, (2020/09/12)
The present invention provides lymphatic system-directing lipid prodrugs, pharmaceutical compositions thereof, methods of producing such prodrugs and compositions, and methods of improving the bioavailability or other properties of a therapeutic agent that comprises part of the lipid prodrug. The present invention also provides methods of treating a disease, disorder, or condition such as those disclosed herein, comprising administering to a patient in need thereof a disclosed lipid prodrug or a pharmaceutical composition thereof.
LIPID PRODRUGS OF BTK INHIBITORS AND USES THEREOF
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Paragraph 00405; 00596; 00598, (2020/09/12)
The present invention provides lymphatic system-directing lipid prodrugs, pharmaceutical compositions thereof, methods of producing such prodrugs and compositions, and methods of improving the bioavailability or other properties of a therapeutic agent that comprises part of the lipid prodrug. The present invention also provides methods of treating a disease, disorder, or condition such as those disclosed herein, comprising administering to a patient in need thereof a disclosed lipid prodrug or a pharmaceutical composition thereof.
LIPID PRODRUGS OF GLUCOCORTICOIDS AND USES THEREOF
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Paragraph 00580; 00582, (2020/09/12)
The present invention provides lymphatic system-directing lipid prodrugs, pharmaceutical compositions thereof, methods of producing such prodrugs and compositions, and methods of improving the bioavailability or other properties of a therapeutic agent that comprises part of the lipid prodrug. The present invention also provides methods of treating a disease, disorder, or condition such as those disclosed herein, comprising administering to a patient in need thereof a disclosed lipid prodrug or a pharmaceutical composition thereof.
LIPID-CONTROLLED RELEASE COMPOSITIONS
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Page/Page column 52-53, (2020/12/11)
The disclosure provides a glass syringe or a glass cartridge, containing a lipid-based pre-formulation suitable for refrigerated storage.
MODIFIED AMINE LIPIDS
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Page/Page column 160-161; 288-289, (2020/07/04)
The disclosure provides ionizable amine lipids and salts thereof (e.g., pharmaceutically acceptable salts thereof) useful for the delivery of biologically active agents, for example delivering biologically active agents to cells to prepare engineered cells. The ionizable amine lipids disclosed herein are useful as ionizable lipids in the formulation of lipid nanoparticle-based compositions.
Stereospecific synthesis of phosphatidylglycerol using a cyanoethyl phosphoramidite precursor
Storch, Judith,Struzik, Zachary J.,Thompson, David H.,Weerts, Ashley N.
, (2020/07/03)
Phosphatidylglycerols (PG) are a family of naturally occurring phospholipids that are responsible for critical operations within cells. PG are characterized by an (R) configuration in the diacyl glycerol backbone and an (S) configuration in the phosphoglycerol head group. Herein, we report a synthetic route to provide control over the PG stereocenters as well as control of the acyl chain identity.
LYMPHATIC SYSTEM-DIRECTING LIPID PRODRUGS
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Paragraph 00547; 00549, (2019/03/17)
The present invention provides lymphatic system-directing lipid prodrugs, pharmaceutical compositions thereof, methods of producing such prodrugs and compositions, as well as methods of improving the bioavailability or other properties of a therapeutic agent that comprises part of the lipid prodrug. The present invention also provides methods of treating a disease, disorder, or condition such as those disclosed herein, comprising administering to a patient in need thereof a provided lipid prodrug or a pharmaceutical composition thereof.
TRIACYLGLYCEROL OLIGOMERS
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Paragraph 0049, (2015/11/27)
This application relates to triacylglycerol oligomers derived from the metathesis of natural oils. These oligomers are structure controlled dimers and quatrimers, and the effect of saturation, molecular size, and positional isomerization are also described herein.
