565473-04-3Relevant academic research and scientific papers
Enhancing polo-like kinase 1 selectivity of polo-box domain-binding peptides
Zhao, Xue Zhi,Hymel, David,Burke, Terrence R.
, p. 5041 - 5049 (2017)
An important goal in the development of polo-like kinase 1 (Plk1) polo-box domain (PBD) binding inhibitors is selectivity for Plk1 relative to Plk2 and Plk3. In our current work we show that Plk1 PBD selectivity can be significantly enhanced by modulating
LIPID PRODRUGS OF NEUROSTEROIDS
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Paragraph 00347; 00350-00351, (2021/08/13)
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 GLUCOCORTICOIDS AND USES THEREOF
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Paragraph 00413; 00416, (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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, (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 PREGNANE NEUROSTEROIDS AND USES THEREOF
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Paragraph 00301; 00304; 00305, (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 00420; 00423-00424, (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.
LYMPHATIC SYSTEM-DIRECTING LIPID PRODRUGS
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Paragraph 00436; 00439; 00440, (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.
Organic chemistry: A general alkyl-alkyl cross-coupling enabled by redox-active esters and alkylzinc reagents
Qin, Tian,Cornella, Josep,Li, Chao,Malins, Lara R.,Edwards, Jacob T.,Kawamura, Shuhei,Maxwell, Brad D.,Eastgate, Martin D.,Baran, Phil S.
, p. 801 - 805 (2016/06/01)
Alkyl carboxylic acids are ubiquitous in all facets of chemical science, from natural products to polymers, and represent an ideal starting material with which to forge new connections. This study demonstrates how the same activating principles used for decades to make simple C-N (amide) bonds from carboxylic acids with loss of water can be used to make C-C bonds through coupling with dialkylzinc reagents and loss of carbon dioxide. This disconnection strategy benefits from the use of a simple, inexpensive nickel catalyst and exhibits a remarkably broad scope across a range of substrates (>70 examples).
LYMPH DIRECTING PRODRUGS
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Page/Page column 53; 54, (2016/02/29)
H:\dar\Interwoven\NRPortbl\DCC\DAR\8230712_1.doc-12/08/2015 Abstract The present invention relates to compounds and their uses, in particular, compounds in the form of prodrugs that promote transport of a pharmaceutical agent to the lymphatic system and subsequently enhance release of the parent drug.
De novo formal synthesis of (-)-apicularen A via an iterative asymmetric hydration sequence
Li, Miaosheng,O'Doherty, George A.
, p. 6087 - 6090 (2007/10/03)
(Chemical Equation Presented) A de novo approach to the formal total synthesis of the macrolide natural product (-)-apicularen A has been achieved in 18 steps'from achiral starting materials. Both the absolute and relative stereochemistries of apicularen A were introduced by a Sharpless asymmetric dihydroxylation, a π-allyl-palladium catalyzed reduction, a stereoselective reduction, and a base-promoted transannulation to install the C-9 stereocenter.
