Patent classifications
C07H7/02
Compounds and methods for treating osteoarthritis
Disclosed herein are substrates and/or inhibitors of endo-O-sulfatase 1 (Sulf-1). According to some embodiments, the substrates and/or inhibitors of Sulf-1 are compounds of formula (I) or (II), ##STR00001##
In formula (I) or (II), n is 2 or 3; X is methylene, O, or N; R.sub.1 is —SO.sub.3M, or —SO.sub.2NH.sub.2; R.sub.2 is C.sub.1-6 alkyl or C.sub.1-6 alkylamine; and M is a monovalent cation selected from the group consisting of lithium, sodium, potassium, and ammonium. Also encompasses herein are methods of identifying and treating a subject having or suspected of having osteoarthritis. The method includes steps of (a) mixing a urine sample of the subject with 4-methylumbelliferyl sulfate (4-MUS) and a Sulf-1 inhibitor of formula (I) or (II); (b) determining a fluorescence intensity of the mixture of the step (a); and (c) treating the subject with an analgesic, a non-steroidal anti-inflammatory drug (NSAID), or a corticosteroid when the determined fluorescence intensity of the step (b) is smaller than that of a control sample, which is a mixture of the urine sample and 4-MUS.
Mannose Derivatives for Treating Bacterial Infections
The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I:
##STR00001##
The invention also provides pharmaceutically acceptable compositions containing the compounds and methods of using the compositions in the treatment of bacteria infections. Finally, the invention provides processes for making compounds of the invention.
Mannose Derivatives for Treating Bacterial Infections
The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I:
##STR00001##
The invention also provides pharmaceutically acceptable compositions containing the compounds and methods of using the compositions in the treatment of bacteria infections. Finally, the invention provides processes for making compounds of the invention.
Methods and compositions for making antibodies and antibody derivatives with reduced core fucosylation
The invention provides methods and compositions for preparing antibodies and antibody derivatives with reduced core fucosylation.
SYNTHESIS OF C-GLYCOSIDES OF INTEREST
The present invention relates to a biotechnological method for producing a C-glycoside of interest. The invention further relates to the use of a sialylated C-glycoside as a donor in an enzymatic glycosylation reaction. The present invention further relates to the following C- glycosides.
MODIFIED VIRAL COMPOSITIONS FOR VIRAL TRANSDUCTION
This disclosure provides compositions and methods for delivering a viral composition to cells, e.g., for cell surface receptor-mediated uptake, and enhanced viral transduction. Viral transduction can be achieved via a modified viral composition that includes a moiety that binds to a cell surface receptor ligand. Modified viral compositions and methods for reducing levels or titers of neutralizing antibodies in a subject in need of viral therapy, e.g., gene therapy, are provided. In some embodiments, the modified viral composition includes empty viral particles that bind and internalize neutralizing autoantibodies. Modified viral compositions including empty viral particles can be administered prior to viral therapy. Also provided are pharmaceutical compositions and kits including a modified viral composition.
MODIFIED VIRAL COMPOSITIONS FOR VIRAL TRANSDUCTION
This disclosure provides compositions and methods for delivering a viral composition to cells, e.g., for cell surface receptor-mediated uptake, and enhanced viral transduction. Viral transduction can be achieved via a modified viral composition that includes a moiety that binds to a cell surface receptor ligand. Modified viral compositions and methods for reducing levels or titers of neutralizing antibodies in a subject in need of viral therapy, e.g., gene therapy, are provided. In some embodiments, the modified viral composition includes empty viral particles that bind and internalize neutralizing autoantibodies. Modified viral compositions including empty viral particles can be administered prior to viral therapy. Also provided are pharmaceutical compositions and kits including a modified viral composition.
Method for preparing intermediate by reduced glutathione-indicated amino acid maillard reaction
A method for preparing an intermediate by a reduced glutathione-indicated amino acid Maillard reaction is provided. The method includes a two-stage reaction at an increased temperature. A reduced glutathione is added after different times of a low-temperature reaction, and a subsequent Maillard reaction is effectively inhibited on a basis wherein a substance is interacted with an intermediate degradation product to reduce a formation of colored substances. Comparing with a browning of Maillard products after a high-temperature stage, a reaction time with a best color inhibition effect is found to be the optimal preparation condition of the intermediate, and the intermediate is prepared in an aqueous medium at a low temperature under this optimal preparation condition. The method uses the water soluble reduced glutathione as a tracer to improve a tracing accuracy comparing to cysteine.
Method for preparing intermediate by reduced glutathione-indicated amino acid maillard reaction
A method for preparing an intermediate by a reduced glutathione-indicated amino acid Maillard reaction is provided. The method includes a two-stage reaction at an increased temperature. A reduced glutathione is added after different times of a low-temperature reaction, and a subsequent Maillard reaction is effectively inhibited on a basis wherein a substance is interacted with an intermediate degradation product to reduce a formation of colored substances. Comparing with a browning of Maillard products after a high-temperature stage, a reaction time with a best color inhibition effect is found to be the optimal preparation condition of the intermediate, and the intermediate is prepared in an aqueous medium at a low temperature under this optimal preparation condition. The method uses the water soluble reduced glutathione as a tracer to improve a tracing accuracy comparing to cysteine.
ASGPR-binding compounds for the degradation of extracellular proteins
Compounds and compositions that have an asialoglycoprotein receptor (ASGPR) binding ligand bound to an extracellular protein binding ligand for the selective degradation of the target extracellular protein in vivo to treat disorders mediated by the extracellular protein are described.