Silica‐Supported Sodium Hydrogen Sulfate Catalyzed Facile Transformation ofp‐Hydroxybenzyl Alcohols top‐Hydroxybenzyl Ethers and Thioethers
摘要:
The heterogeneous catalyst, silica-supported sodium hydrogen sulfate (NaHSO4 - SiO2) has been found to be highly efficient in carrying out the transformation of p-hydroxybenzyl alcohols at room temperature to p-hydroxybenzyl ethers and thioethers in very high yields.
Non-chromatographic purification of macrocyclic peptides by a resin catch and release
申请人:BRISTOL-MYERS SQUIBB COMPANY
公开号:US11479581B2
公开(公告)日:2022-10-25
The disclosure is directed to compounds and methods for preparing purified macrocyclic peptide using “catch-release” methods. These methods comprise reacting a free amino group of a resin-bound linear peptide with an azide- or alkyne-functionalized cap to form a resin-bound capped linear peptide having an azide- or alkyne-functionalized cap; cleaving the capped linear peptide from the resin to form a free capped linear peptide having an azide- or alkyne-functionalized cap; reacting the free capped linear peptide having an azide-functionalized cap with an alkyne-functionalized catch resin, or reacting the free capped linear peptide having an akynyl-functionalized cap with an azide functionalized catch resin, to form a catch-resin bound capped linear peptide; reacting the catch-resin bound capped linear peptide under conditions sufficient to effect macrocyclization of the linear peptide and release of the macrocyclic peptide from the catch resin.
PROBES FOR RAPID AND SPECIFIC DETECTION OF MYCOBACTERIA
申请人:The Board of Trustees of the Leland Stanford Junior University
公开号:US20170044593A1
公开(公告)日:2017-02-16
The compositions of the present disclosure provide novel fluorogenic probes for use in the specific imaging and detection of mycobacteria species, and in particular β-lactam-antibiotic resistant. Specificity for mycobacteria is conferred on these probes by incorporating a moiety that specifically targets the unique trapping mechanism of the DprE1 found in in mycobacteria. Accordingly, only Mycobacteria species that express both a β-lactamase and DprE1 enable both the activation of the caged fluorescent probe, and the affixing of the released fluorescent probes to the bacteria cells through the functioning reduction-covalent binding mechanism. Advantageously, such a probe is able, at its most sensitive, to allow single
mycobacterium
detection.
LIPID PRODRUGS OF MYCOPHENOLIC ACID AND USES THEREOF
申请人:PureTech LYT, Inc.
公开号:US20200390777A1
公开(公告)日:2020-12-17
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.
NON-CHROMATOGRAPHIC PURIFICATION OF MACROCYCLIC PEPTIDES BY A RESIN CATCH AND RELEASE
申请人:BRISTOL-MYERS SQUIBB COMPANY
公开号:US20210079046A1
公开(公告)日:2021-03-18
The disclosure is directed to compounds and methods for preparing purified macrocyclic peptide using “catch-release” methods. These methods comprise reacting a free amino group of a resin-bound linear peptide with an azide- or alkyne-functionalized cap to form a resin-bound capped linear peptide having an azide- or alkyne-functionalized cap; cleaving said capped linear peptide from the resin to form a free capped linear peptide having an azide- or alkyne-functionalized cap; reacting the free capped linear peptide having an azide-functionalized cap with an alkyne-functionalized catch resin, or reacting the free capped linear peptide having an akynyl-functionalized cap with an azide functionalized catch resin, to form a catch-resin bound capped linear peptide; reacting the catch-resin bound capped linear peptide under conditions sufficient to effect macrocyclization of the linear peptide and release of the macrocyclic peptide from the catch resin.
LIPID PRODRUGS OF NEUROSTEROIDS
申请人:PureTech LYT, Inc.
公开号:US20220395513A1
公开(公告)日:2022-12-15
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.