Patent classifications
C07H13/12
Cell-permeable probes for identification and imaging of sialidases
Provided herein are compounds for use as sialidase inhibitors, including alkynyl-3-fluorosialyl fluoride. The compounds, which include the compound DFSA, function by trapping a 3-fluorosialylenzyme intermediate (reporter-inhibitor-enzyme conjugate). These compounds can be conjugated with a detectable tagging moiety for isolation and identification of sialidases.
GLUCURONIDE PRODRUGS OF JANUS KINASE INHIBITORS
The invention relates to glucuronide prodrug compounds of Janus kinase (JAK) inhibitors having formula I:
##STR00001##
where W.sup.1, R.sup.1 and A.sup.1 are as defined. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds to treat gastrointestinal inflammatory diseases; and processes and intermediates for preparing such compounds.
Methods and compounds for identifying glycosyltransferase inhibitors
The present invention provides moenomycin-based probe compounds of Formula (I) for use in screening inhibitors of bacterial glycosyltransferases. The present invention also provides bacterial glycosyltransferase screening assays using compounds of Formula (I).
Methods and compounds for identifying glycosyltransferase inhibitors
The present invention provides moenomycin-based probe compounds of Formula (I) for use in screening inhibitors of bacterial glycosyltransferases. The present invention also provides bacterial glycosyltransferase screening assays using compounds of Formula (I).
Neuraminidase Inhibitor Compounds, Compositions and Methods for the Use Thereof in Anti-Viral Treatments
Compounds having a structure of Formula I and compositions comprising these compounds are provided. Uses of such compounds and compositions are provided for treatment or prophylaxis of viral infection. In particular, compounds and compositions may be for use in the treatment or prophylaxis of viral influenza.
Neuraminidase Inhibitor Compounds, Compositions and Methods for the Use Thereof in Anti-Viral Treatments
Compounds having a structure of Formula I and compositions comprising these compounds are provided. Uses of such compounds and compositions are provided for treatment or prophylaxis of viral infection. In particular, compounds and compositions may be for use in the treatment or prophylaxis of viral influenza.
DEUTERATED NUCLEOSIDE COMPOUNDS AND USE THEREOF
A series of deuterated nucleoside compounds are compounds represented by formula (IV), and stereoisomers or pharmaceutically acceptable salts thereof.
##STR00001##
DEUTERATED NUCLEOSIDE COMPOUNDS AND USE THEREOF
A series of deuterated nucleoside compounds are compounds represented by formula (IV), and stereoisomers or pharmaceutically acceptable salts thereof.
##STR00001##
PRODRUGS WITH 1-(DISULFANYL)ALKYLOXY-CARBONYL UNITS
The invention is in the field of medical sciences. It provides new pharmaceutical methods and preparations. The invention relates to methods for improving the pharmacokinetic, physicochemical or pharmaceutical properties of drugs by converting the drug into a promoiety-containing 1-substituted disulfanylalkyl carbonate, thiocarbamate or carbamate prodrug. In particular, the invention relates to methods for improving the solubility, permeability, stability and/or oral bioavailability of a drug by converting the drug into a promoiety-containing 1-(disulfanylalkyl) carbonate, thiocarbonate or carbamate prodrug. The invention also provides new compositions comprising a drug covalently attached to a promoiety-containing 1-(disulfanylalkyl) carbonate, thiocarbonate or carbamate. More in particular, the invention relates to a method for increasing the oral bioavailability of a drug by covalently attaching a promoiety-containing 1-disulfanylalkyloxycarbonyl unit to a hydroxyl or amine containing drug in which the promoiety contains a 1-O, 1-S, 6-O or 6-S-linked monosaccharide.
CD206 TARGETED DRUG DELIVERY VEHICLES CARRYING NOVEL BISPHOSPHONATE DRUG PAYLOADS VIA A DEGRADABLE LINKER
Provided are novel compounds containing a polymeric carbohydrate backbone, one or more mannose-binding C-type lectin receptor targeting moieties, and a nitrogenous bisphosphonate compound coupled to the backbone via a thiol-maleimide conjugation, in addition to pharmaceutical compositions, methods of synthesizing, and methods of use. The thiol-maleimide conjugation of a bisphosphonate to a polymeric carbohydrate backbone provides for methods of using the compounds and compositions thereof for releasing the therapeutic payload when internalized into a mannose-binding C-type lectin receptor-expressing cell, such as tumor associated macrophages (TAMs) for the treatment of various diseases, including, cancer, autoimmune diseases, and inflammatory disorders.