A61K47/61

PROCESS FOR THE MODIFICATION OF A GLYCOPROTEIN USING A GLYCOSYLTRANSFERASE THAT IS OR IS DERIVED FROM A ß(1,4)-N-ACETYLGALACTOSAMINYLTRANSFERASE

The present invention relates to a process for the enzymatic modification of a glycoprotein. The process comprises the step of contacting a glycoprotein comprising a glycan comprising a terminal GlcNAc-moiety, in the presence of glycosyltransferase that is, or is derived from, a β-(1,4)-N-acetylgalactosaminyltransferase, with a non-natural sugar-derivative nucleotide. The non-natural sugar-derivative nucleotide is according to formula (3):

##STR00001##

wherein A is selected from the group consisting of —N.sub.3, —C(O)R.sup.3, —(CH.sub.2).sub.iC≡C—R.sup.4, —SH, —SC(O)R.sup.8, —SC(O)OR.sup.8, —SC(S)OR.sup.8, —F, —Cl, —Br —I, —OS(O).sub.2R.sup.5, terminal C.sub.2-C.sub.24 alkenyl groups, C.sub.3-C.sub.5 cycloalkenyl groups, C.sub.4-C.sub.8 alkadienyl groups, terminal C.sub.3-C.sub.24 allenyl groups and amino groups. The invention further relates to a glycoprotein obtainable by the process according to the invention, to a bioconjugate that can be obtained by conjugating the glycoprotein with a linker-conjugate, and to β-(1,4)-N-acetylgalactosaminyltransferases that can be used in preparing the glycoprotein according to the invention.

RESPONSIVE ELASTIC POLYMERS AND METHODS OF MAKING AND USING SAME
20230098351 · 2023-03-30 ·

Disclosed herein are functionalized hyaluronic acid (HA), a responsive elastic polymer system comprising functionalized HA, and methods of fabrication and utilization of the same. This polymer system may be used for controlled local or systemic drug delivery release of analgesics, anesthetics, antibiotics and other drugs as well as tissue engineering articles

RESPONSIVE ELASTIC POLYMERS AND METHODS OF MAKING AND USING SAME
20230098351 · 2023-03-30 ·

Disclosed herein are functionalized hyaluronic acid (HA), a responsive elastic polymer system comprising functionalized HA, and methods of fabrication and utilization of the same. This polymer system may be used for controlled local or systemic drug delivery release of analgesics, anesthetics, antibiotics and other drugs as well as tissue engineering articles

NOVEL KETOGENIC COMPOUNDS, COMPOSITIONS, METHODS AND USE THEREOF

The present disclosure relates to compounds comprising as β-hydroxybutyric acid, and a weakly basic polymer. The disclosure also includes methods for inducing nutritional ketosis comprising administering the compounds or compositions to a mammal in need thereof.

NOVEL KETOGENIC COMPOUNDS, COMPOSITIONS, METHODS AND USE THEREOF

The present disclosure relates to compounds comprising as β-hydroxybutyric acid, and a weakly basic polymer. The disclosure also includes methods for inducing nutritional ketosis comprising administering the compounds or compositions to a mammal in need thereof.

TYROSINE KINASE INHIBITOR CONJUGATES
20230102309 · 2023-03-30 ·

The present invention relates to a tyrosine kinase inhibitor (“TKI”) conjugate or a pharmaceutically acceptable salt thereof, wherein said conjugate comprises a plurality of TKI moieties -D covalently conjugated via at least one moiety -L.sup.1-L.sup.2- to a polymeric moiety Z, wherein -L.sup.1- is covalently and reversibly conjugated to -D and -L.sup.2- is covalently conjugated to Z and wherein -L.sup.1- is a linker moiety and -L.sup.2- is a chemical bond or a spacer moiety; and to related aspects.

TYROSINE KINASE INHIBITOR CONJUGATES
20230102309 · 2023-03-30 ·

The present invention relates to a tyrosine kinase inhibitor (“TKI”) conjugate or a pharmaceutically acceptable salt thereof, wherein said conjugate comprises a plurality of TKI moieties -D covalently conjugated via at least one moiety -L.sup.1-L.sup.2- to a polymeric moiety Z, wherein -L.sup.1- is covalently and reversibly conjugated to -D and -L.sup.2- is covalently conjugated to Z and wherein -L.sup.1- is a linker moiety and -L.sup.2- is a chemical bond or a spacer moiety; and to related aspects.

COMPOSITIONS AND METHODS RELATING TO COMBINATORIAL HYALURONIC ACID CONJUGATES

Described herein are compositions comprising polymers conjugated to at least one immunomodulator, e.g., a) a retinoid and an imidazoquinoline, b) a retinoid and a HDAC inhibitor, or c) a HDAC inhibitor and an imidazoquinoline. Further described herein are methods of using said compositions, e.g., in modulating immune responses and/or treating a disease such as cancer.

COMPOSITIONS AND METHODS RELATING TO COMBINATORIAL HYALURONIC ACID CONJUGATES

Described herein are compositions comprising polymers conjugated to at least one immunomodulator, e.g., a) a retinoid and an imidazoquinoline, b) a retinoid and a HDAC inhibitor, or c) a HDAC inhibitor and an imidazoquinoline. Further described herein are methods of using said compositions, e.g., in modulating immune responses and/or treating a disease such as cancer.

COMPOUNDS AND METHODS FOR SUPPRESSING AN IMMUNE RESPONSE TO SUBSTANCES CONTAINING POLYETHYLENE GLYCOL

Compounds, compositions and methods for suppressing an immune response to polyethylene glycol (PEG) are provided.