37 results about "Chemical conjugate" patented technology

Novel chemical conjugates of psychotropic drugs and organic acids, uses thereof in the treatment of psychotic and / or proliferative disorders and diseases and as chemosensitizing agents, and their syntheses are disclosed. The organic acids are selected to reduce side effects induced by the psychotropic drugs and / or to exert an anti-proliferative activity.

Novel chemical conjugates of psychotropic drugs and organic acids, uses thereof in the treatment of psychotic and / or proliferative disorders and diseases and as chemosensitizing agents, and their syntheses are disclosed. The organic acids are selected to reduce side effects induced by the psychotropic drugs and / or to exert an anti-proliferative activity.

A compound of Formula (I) or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester amide or salt. Definitions of R1-R13 and L1-L4 are provided in the disclosure, and R14 is a group capable of binding to prostate-specific membrane antigen (PSMA).

An oxygen sensitive probe comprises a monofunctional derivative of an oxygen-sensitive photoluminescent dye covalently attached to a water soluble and / or hydrophilic macromolecular carrier. The probe may be a chemical conjugate of a monofunctional phosphorescent porphyrin dye and a poly(ethyleneglycol), polypeptide or polysaccharide.

The invention provides chemical conjugates between an immunoglobulin Fab fragment and molecular entities imparting diagnostic or therapeutic utility, whereby the only sites of conjugation on the Fab fragment are one or both of the sulfhydryl groups deriving from the selective and quantitative reduction of the inter-chain disulfide bond of said Fab fragment and whereby said molecular entities imparting diagnostic or therapeutic utility have at least one free sulfhydryl-reactive group, characterized in that the conjugation stoichiometric molar ratio molecular entity to Fab fragment is in the range from 0.95 to 1.05 or in the range from 1.95 to 2.05. The invention also provides a process for preparing said conjugates and pharmaceutical compositions thereof.

The current invention relates to: procoagulant proteins which may, for example, be fusion proteins or chemical conjugates; methods of producing said procoagulant proteins; polynucleotides that encode said fusion proteins and cells that expresses them. Furthermore, the current invention relates to procoagulant proteins for use as a medicament. Individuals that have a coagulopathy, such as haemophilia A and B with or without inhibitors, may be treated with the procoagulant proteins of the current invention.

The invention relates to a meningococcus vaccine comprising a chemical conjugate of meningococcus capsular polysaccharide and carrier protein, and a first adjuvant, wherein the first adjuvant is oligodeoxynucleotide comprising at least one non-methylation CpG dinucleotide, and the length of the oligodeoxynucleotide is 15-35 ribonucleotides. The adjuvant used for increasing the immunization effectof the meningococcus vaccine is a novel human vaccine adjuvant with favorable potential application prospect, and the chemical essence of the adjuvant is the oligodeoxynucleotide which is synthesizedmanually and contains the CpG dinucleotide. By a receptor TLR9 activated immune system on immune cells, the adjuvant reinforces specific immune response aiming at vaccine antigens. The immunization effect of a vaccine can be increased by adding the vaccine adjuvant into the vaccine, so that the dosage of the vaccine antigen can be reduced, the immunization injection times can be reduced and the vaccine cost can be reduced.

Novel chemical conjugates derived from unsaturated fatty acids and therapeutically active agents, are disclosed. The chemical conjugates are designed and characterized as COX-2 and / or 5-LOX inhibitors and are useful in the treatment of inflammatory diseases, dermatitis and disorders such as Alzheimer's disease, Parkinson's disease, asthma, osteoarthritis, rheumatoid arthritis, pain, primary dysmenorrhea, Crohn's disease and ulcerative colitis.

The present invention is directed to a compound of Formula I or Formula II or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester amide or salt: Formula I Formula II The compounds of Formula I may be covalently bonded to a therapeutic compound or fragment thereof to provide a compound of Formula II and thereby extend the half-life of the therapeutic compound. The invention is also directed to pharmaceutical compositions of the disclosed compounds, as well as their use in the diagnosis or treatment of diseases.

The present invention is directed to a compound of Formula I or Formula III or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester amide or salt: wherein the definitions R1-R13 and L1-L4 are provided in the disclosure, and wherein R14 is a peptide. The compounds of Formula I may be covalently bonded to a peptide via a linker to provide a compound of Formula III and thereby extend the half-life of the therapeutic compound. The invention is also directed to pharmaceutical compositions of the disclosed compounds, as well as their use in the diagnosis or treatment of diseases.

Provided are mutants of human granulocyte-colony stimulating factor (G-CSF) designed for specific chemical conjugation, and chemical conjugates thereof for use as an adjuvant in the treatment of cancer. The present invention provides a mutant of a G-CSF in which a threonine (Thr) residue at position 133 of G-CSF comprising the amino acid sequence identified in SEQ ID NO: 1 is substituted with a cysteine (Cys) residue. In addition, the invention provides a mutant of a G-CSF in which a cysteine (Cys) residue is inserted between a glycine (GIy) residue at position 135 and an alanine (Ala) residue at position 136 of G-CSF. Further, the invention provides a chemically conjugated mutant G-CSF to which biocompatible polymer such as polyethylene glycol (PEG) was attached at the cysteine residue, which was introduced by the substitution or insertion mutation, increasing its in vivo retention time without reducing in vivo biological activity due to the conjugation with the biocompatible polymer, thereby ultimately extending the in vivo biological activity.

The present disclosure concerns chemical conjugates having structures satisfying Formula I and methods of making and using these chemical conjugates.Also described are immunomodulatory compositions comprising the chemical conjugates and methods of using the chemical conjugates and / or immunomodulatory compositions thereof to induce an immune response in a subject.

The present invention relates to a conjugated psychotropic drugs and uses thereof. The present invention discloses novel chemical conjugates of psychotropic drugs and organic acids, uses thereof in the treatment of psychotic and / or proliferative disorders and diseases and as chemosensitizing agents, and their syntheses. The organic acids are selected to reduce side effects induced by the psychotropic drugs and / or to exert an anti-proliferative activity.

The invention relates to a polysaccharide conjugate vaccine, which comprises a chemical conjugate consisting of a bacterial polysaccharide and a vector protein, wherein the vector protein is a bacterial slime invasion-associated protein, such as a bacillus coli heat-labile toxin B subunit, a campylobacter jejuni flagellum secretion protein A1, a campylobacter jejuni flagellum secretion protein A2, a pneumococcus surface protein and a pneumococcus surface adhesin. The invention further relates to a preparation method for the polysaccharide conjugate vaccine. According to the invention, the mucosa delivery of the polysaccharide conjugate vaccine can be realized on the premise of not adding any other extrinsic protein; and due to the adoption of an immune route, the vaccine is more efficient, convenient and safe to use.

The present invention is directed to a compound of Formula III or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester amide or salt: Formula III wherein the definitions of R1-R12 and L1-L4 are provided in the disclosure, wherein R13 is a chelating group comprising 177Lu, and wherein R14 is a peptide. The compounds of Formula I may be covalently bonded to a peptide via a linker to provide a compound of Formula III and thereby extend the half-life of the therapeutic compound. The invention is also directed to pharmaceutical compositions of the disclosed compounds, as well as their use in the diagnosis or treatment of diseases.