13853-23-1Relevant academic research and scientific papers
LIPID PRODRUGS OF JAK INHIBITORS AND USES THEREOF
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Paragraph 00404-00405, (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 00288; 00289, (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 BTK INHIBITORS AND USES THEREOF
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Paragraph 00405; 00413; 00414, (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 00397; 00398, (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 00423; 00424, (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.
Expanding the utility of proteases in synthesis: Broadening the substrate acceptance in non-coded amide bond formation using chemically modified mutants of subtilisin
Khumtaveeporn, Kanjai,Ullmann, Astrid,Matsumoto, Kazutsugu,Davis, Benjamin G.,Jones
, p. 249 - 261 (2007/10/03)
The strategy of combined site directed mutagenesis and chemical modification creates chemically modified mutants (CMMs) with greatly broadened substrate specificities. We have previously reported that the CMMs of subtilisin Bacillus lentus (SBL) are efficient catalysts for the coupling of both L- and D-amino acids. We now report that these powerful catalysts also allow amide bond formation between a variety of non-coded carboxylic acids, including β-alanine and β-amino homologues of phenylalanine, with both L- and D-amino acid nucleophiles. As a guide to enzyme efficiency, a hydrolysis assay indicating pH change has been employed. CMMs selected by this screen furnished higher yields of coupling products compared to the wild-type enzyme (WT). Furthermore, both WT and CMM enzymes allow highly stereoselective aminolysis of a meso diester with an amino acid amine. These results highlight the utility of CMMs in the efficient formation of non-coded amides as potential peptide isosteres.
Preferential hydrogenolysis of NAP esters provides a new orthogonal protecting group strategy for carboxylic acids
Gaunt, Matthew J.,Boschetti, Carlos E.,Yu, Jinquan,Spencer, Jonathan B.
, p. 1803 - 1806 (2007/10/03)
Selective hydrogenolysis of 2-naphthylmethyl (NAP) esters in the presence of a benzyl ester has been observed with a wide range of dicarboxylic acids. Orthogonal deprotection of NAP esters with challenging substrates can be achieved if the other carboxylic acids in the molecule are protected with 4-trifluoromethyl benzyl group instead of benzyl groups.
