The invention relates to the chitosan polymer derivatives of formula I: and pharmaceutically acceptable salts and esters thereof, wherein Y, X.sup.1, X.sup.4, R.sup.1, R.sup.2, and n are defined in the detailed description and claims. The chitosan polymer derivatives of formula I bind to or associate with alpha-4-beta-1 (α4β1) and alpha-V-beta-3 (α Vβ3) integrin dimers and can be used in delivery formulations to deliver drugs, nucleic acids, or other therapeutic compounds to tissues or cells expressing such integrins. ##STR00001##

The invention relates to the chitosan polymer derivatives of formula I: and pharmaceutically acceptable salts and esters thereof, wherein Y, X.sup.1, X.sup.4, R.sup.1, R.sup.2, and n are defined in the detailed description and claims. The chitosan polymer derivatives of formula I bind to or associate with alpha-4-beta-1 (α4β1) and alpha-V-beta-3 (α Vβ3) integrin dimers and can be used in delivery formulations to deliver drugs, nucleic acids, or other therapeutic compounds to tissues or cells expressing such integrins. ##STR00001##

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.

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.

New aminooxylipids of general formula I, wherein n.sub.1=5-30 and X is polymethylene linker of the general formula II where n.sub.2=2-10, or X is polyethylene glycol linker of the general formula III, wherein n.sub.3=1-14 are provided. A method of preparation of the aminooxylipids of general formula I characterized in that the acylation of N-tert-butoxycarbonyl-polymethylenediamine {(CH.sub.3).sub.3C—O—(C═O)—HN—(CH.sub.2).sub.n—NH.sub.2, n=2-13}, or N-tert-butoxycarbonyl-polyethyleglycoldiamine {(CH.sub.3).sub.3C—O—(C═O)—HN—(CH.sub.2).sub.2—[O—(CH.sub.2)].sub.n—O—(CH.sub.2).sub.2NH.sub.2, n=1-14} with in position C(2) symmetrically branched fatty acids of general formula IV, wherein n.sub.1=5-30, in the presence of condensation reagent, or from acid of general formula IV derived acylchloride of general formula V wherein n.sub.1=5-30, produces N-Boc-aminolipids of general formula VI, wherein n.sub.1=5-30 a X is polymethylene linker of the general formula II or X is polyethylene glycol linker of the general formula III.

New aminooxylipids of general formula I, wherein n.sub.1=5-30 and X is polymethylene linker of the general formula II where n.sub.2=2-10, or X is polyethylene glycol linker of the general formula III, wherein n.sub.3=1-14 are provided. A method of preparation of the aminooxylipids of general formula I characterized in that the acylation of N-tert-butoxycarbonyl-polymethylenediamine {(CH.sub.3).sub.3C—O—(C═O)—HN—(CH.sub.2).sub.n—NH.sub.2, n=2-13}, or N-tert-butoxycarbonyl-polyethyleglycoldiamine {(CH.sub.3).sub.3C—O—(C═O)—HN—(CH.sub.2).sub.2—[O—(CH.sub.2)].sub.n—O—(CH.sub.2).sub.2NH.sub.2, n=1-14} with in position C(2) symmetrically branched fatty acids of general formula IV, wherein n.sub.1=5-30, in the presence of condensation reagent, or from acid of general formula IV derived acylchloride of general formula V wherein n.sub.1=5-30, produces N-Boc-aminolipids of general formula VI, wherein n.sub.1=5-30 a X is polymethylene linker of the general formula II or X is polyethylene glycol linker of the general formula III.

Provided herein are compounds, compositions, conjugates and methods for the treatment of diseases, and/or conditions such as, but not limited to, proliferative diseases. In certain embodiments, compounds, compositions, and conjugates are provided, which include cyclodextrin-based linker-payloads and protein conjugates thereof, and/or in combination with other agents. By administering these compounds, compositions, and conjugates as described herein to specific target cells, side-effects due to non-specific binding phenomena, for example, to non-target cells are reduced.

Provided herein are compounds, compositions, conjugates and methods for the treatment of diseases, and/or conditions such as, but not limited to, proliferative diseases. In certain embodiments, compounds, compositions, and conjugates are provided, which include cyclodextrin-based linker-payloads and protein conjugates thereof, and/or in combination with other agents. By administering these compounds, compositions, and conjugates as described herein to specific target cells, side-effects due to non-specific binding phenomena, for example, to non-target cells are reduced.

A method of inhibiting inflammation with milk oligosaccharides or glycoconjugates containing the oligosaccharides.

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.