Pharmaceutical composition comprising arginine deiminase for inhibiting angiogenesis

The present invention relates to a pharmaceutical composition for inhibiting angiogenesis which comprises arginine deiminase as an active ingredient, where the arginine deiminase, obtained from Mycoplasma arginini or prepared by a genetic recombination technique, may be conjugated to an activated polymer to lower its immunogenecity and increase its life time. The pharmaceutical composition of the present invention exhibits an excellent inhibitory activity against angiogenesis.

Preparation of g-csf stoichiometrically conjugated with biocompatible polymers at cystein residue

The present invention relates to a conjugate of a biocompatible polymer and a G-CSF bonded through a thiol group of a dysteine residue in G-CSF at a 1:1 molar ratio, and methods of preparation thereof.

Pharmaceutical composition comprising arginine deiminasa for inhibiting angio-genesis

The present invention relates to a pharmaceutical composition for inhibiting angiogenesis which comprises arginine deiminase as an active ingredient, where the arginine deiminase, obtained from Mycoplasma arginini or prepared by a genetic recombination technique, may be conjugated to an activated polymer to lower its immunogenecity and increase its life time. The pharmaceutical composition of the present invention exhibits an excellent inhibitory activity against angiogenesis.

Biologically active material conjugated with biocompatible polymer with 1:1 complex, preparation method thereof and pharmaceutical composition comprising the same

The present invention relates to conjugates of biocompatible polymers and biologically active molecules wherein the activated biocompatible polymer is conjugated to a carboxyl group of biologically active material at a molar ratio of 1:1 and methods of preparation thereof and a pharmaceutical composition comprising the same.

siRNA of NF-kB p105 for inhibiting cell proliferation and migration and a composition comprising same

The present invention relates to a siRNA which targets mRNA of the NF-Kappa B p105 gene to cause its degradation by RNAi induction. In addition, the present invention provides a pharmaceutical composition for the treatment of diseases associated with aberrant cell proliferation and migration, comprising the siRNA and delivery vehicle capable of intracellular delivery of the same.

SIRNA OF NF-KB P105 FOR INHIBITING CELL PROLIFERATION AND MIGRATION AND A COMPOSITION COMPRISING SAME

The present invention relates to a siRNA which targets mRNA of the NF-Kappa B p105 gene to cause its degradation by RNAi induction. In addition, the present invention provides a pharmaceutical composition for the treatment of diseases associated with aberrant cell proliferation and migration, comprising the siRNA and delivery vehicle capable of intracellular delivery of the same.

Chitosan Based Polymer Conjugate and a Method for Producing the Same

The present invention relates to a conjugate of chitosan and polyamine polymer that is useful for transferring a desired gene medicine into cells, and a method for preparing the same. In particular, the present invention relates to a double conjugate that is prepared by 1 in king poly-L-arginine to low molecular weight chitosan or triple conjugate that is prepared by additionally linking polyethylene glycol (PEG) to the double conjugate, and a method for preparing the same. The chitosan based cationic polymer conjugate of the present invention forms a complex with negatively charged gene medicine such as plasmid DNA and small interfering RNA to efficiently transfer the desired gene medicine into cells with low cytotoxicity. Accordingly, the conjugate can be used as an effective delivery system for in vivo administration of gene medicine.

Biopolymer Conjugates Comprising an Interleukin-11 Analog

The present invention provides for biopolymer conjugates of an IL-11 analog (mIL-11) and a biocompatible polymer. The mIL-11 of the invention displays an enhanced resistance to acidolysis and shows increased stability as compared to rhIL-11. The conjugates of the present invention are characterized by a longer serum half-life and exhibit essentially no loss of activity as compared to the corresponding unconjugated mIL-11.

Biologically active material conjugated with biocompatible polymer with 1:1 complex, preparation method thereof and pharmaceutical composition comprising the same

The present invention relates to conjugates of biocompatible polymers and biologically active molecules wherein the activated biocompatible polymer is conjugated to a carboxyl group of biologically active material at a molar ratio of 1:1 and methods of preparation thereof and a pharmaceutical composition comprising the same.

Nasal transmucosal delivery of peptide conjugated with biocompatible polymers

The present invention relates to a pharmaceutical composition for the nasal transmucosal delivery of a biocompatible polymer-biologically active peptide conjugate. The pharmaceutical composition of the present invention increases the water solubility of peptide, which is sparingly soluble in water, improves its stability by protecting it from being degraded by proteases. As a result, the number of administrations of the drug and the side-effects induced by drug abuse are decreased. In addition, since the pharmaceutical composition of the present invention is delivered through the nasal cavity, it allows drug activity to be expressed in a short period of time and improves a bioavailability.

Pharmaceutical composition comprising arginine deiminase for inhibiting angiogenesis

The present invention relates to a pharmaceutical composition for inhibiting angiogenesis which comprises arginine deiminase as an active ingredient, where the arginine deiminase, obtained from Mycoplasma arginini or prepared by a genetic recombination technique, may be conjugated to an activated polymer to lower its immunogenecity and increase its life time. The pharmaceutical composition of the present invention exhibits an excellent inhibitory activity against angiogenesis.

Stoichiometric conjugates of biocompatible polymers at the unpaired cysteine residue of the wild-type G-CSF

The present invention relates to a conjugate of a biocompatible polymer and a G-CSF bonded through a thiol group of a dysteine residue in G-CSF at a 1:1 molar ratio, and methods of preparation thereof.

Biocompatible polymers including peptide spacer

The present invention relates to new biocompatible polymer derivatives including peptide spacers of formula (I) and their methods of preparation. The present invention also relates to the conjugates formed by covalent or non-covalent bonding and their methods of preparation. These biocompatible polymers with peptide spacers providing regions of hydrophobicity and positive charge can enhance their interaction with cell membrane to increase the cell trafficking, endosomal disruption, the circulation half-life in blood, and the stability of conjugated therapeutic drug.

CATIONIC LIPIDS, METHODS FOR PREPARING THE SAME, AND DELIVERY SYSTEMS HAVING ABILITY TO TRANSITION INTO CELLS COMPRISING THE SAME

The present invention provides cationic lipids, methods for preparing the same, and delivery systems comprising the same. The present invention can provide cationic lipids which enhance the efficiency of intracellular or in vivo delivery of multiple-anionic target compounds such as drugs, anticancer agents, nucleic acids, etc., have no intracellular toxicity, but show increased stability, methods for preparing the same, and delivery systems comprising the same. 2. The cationic lipid according to claim 1 , wherein each of Rand Ris independently saturated or unsaturated hydrocarbon chain derived from stearate claim 1 , laurate claim 1 , myristate claim 1 , palmitate claim 1 , or oleate.3. The cationic lipid according to claim 1 , wherein Ris methyl claim 1 , ethyl claim 1 , propyl claim 1 , isopropyl claim 1 , n-butyl claim 1 , or benzyl.4. The cationic lipid of claim 1 , wherein the ligand is mPEG (methoxy end-capped polyethylene glycol) claim 1 , polypropylene glycol claim 1 , or polyoxyethylene.5. The cationic lipid of claim 1 , wherein the ligand is at least one sugar selected from the group consisting of mannitol claim 1 , sorbitol claim 1 , xylitol claim 1 , glucitol claim 1 , dulcitol claim 1 , inositol claim 1 , arabinitol claim 1 , arabitol claim 1 , galactitol claim 1 , iditol claim 1 , alitol claim 1 , fructose claim 1 , sorbose claim 1 , glucose claim 1 , mannose claim 1 , xylose claim 1 , trehalose claim 1 , allose claim 1 , dextrose claim 1 , altrose claim 1 , gulose claim 1 , idose claim 1 , galactose claim 1 , talose claim 1 , ribose claim 1 , arabinose claim 1 , lyxose claim 1 , sucrose claim 1 , maltose claim 1 , lactose claim 1 , lactulose claim 1 , fucose claim 1 , rhamnose claim 1 , melezitose claim 1 , maltotriose claim 1 , and raffinose.7. The delivery system according to claim 6 , wherein each of Rand Ris independently saturated or unsaturated hydrocarbon chain derived from stearate claim 6 , laurate claim 6 , myristate claim 6 , palmitate ...

Human growth hormone conjugated with biocompatible polymer

The present invention relates to conjugates of biocompatible polymers and hGH, particularly PEG-hGH, where the activated biocompatible polymer is conjugated to a carboxyl group of hGH at a molar ratio of 2:1 or less, preferably 1:1, methods of preparation, and related pharmaceutical compositions. The PEG-hGH conjugates have up to 20% of the activity of the native hGH while the in vivo half life is increased 10 fold. The PEG-hGH conjugates may be used therapeutically to treat growth retardation or growth failure, especially short stature in children, and conditions related to aging.

Biocompatible polymers including peptide spacer

The present invention relates to new biocompatible polymer derivatives including peptide spacers of formula (1) and their methods of preparation. The present invention also relates to the conjugates formed by covalent or non-covalent bonding and their methods of preparation. These biocompatible polymers with peptide spacers providing regions of hydrophobicity and positive charge can enhance their interaction with cell membrane to increase the cell trafficking, endosomal disruption, the circulation half-life in blood, and the stability of conjugated therapeutic drug.

Biologically active non-antigenic copolymer and conjugates thereof and methods for producing the same

The present invention relates to activated biocompatible non-antigenic copolymers formed by copolymerizing polyethyleneimine with biocompatible polymer other than polyethyleneimine, biologically active non-antigenic conjugates formed by binding said copolymers to biologically active materials such as drugs or proteins. A biologically active non-antigenic conjugate of the present invention has a characteristic feature in that its constitutive copolymer essentially consists of hydrophilic polymer, which plays a role to provide high stability and long in vivo half-life of the hydrophobic drugs or proteins, and positively charged polymer which functions to increase the cellular uptake of the drugs or proteins.

Biopolymer conjugates comprising an interleukin-11 analog

The present invention provides for biopolymer conjugates of an IL-11 analog (mIL-11) and a biocompatible polymer. The mIL-11 of the invention displays an enhanced resistance to acidolysis and shows increased stability as compared to rhIL-11. The conjugates of the present invention are characterized by a longer serum half-life and exhibit essentially no loss of activity as compared to the corresponding unconjugated mIL-11.

Human growth hormone conjugated with biocompatible polymer

The present invention relates to conjugates of biocompatible polymers and hGH, particularly PEG-hGH, where the activated biocompatible polymer is conjugated to a carboxyl group of hGH at a molar ratio of 1:1, methods of preparation, and related pharmaceutical compositions. The PEG-hGH conjugates have up to 20% of the activity of the native hGH while the in vivo half life is increased 10 fold. The PEG-hGH conjugates may be used therapeutically to treat growth retardation or growth failure, especially short stature in children, and conditions related to aging.

Chitosan based polymer conjugate and a method for producing the same

The present invention relates to a conjugate of chitosan and polyamine polymer that is useful for transferring a desired gene medicine into cells, and a method for preparing the same. In particular, the present invention relates to a double conjugate that is prepared by 1 in king poly-L-arginine to low molecular weight chitosan or triple conjugate that is prepared by additionally linking polyethylene glycol (PEG) to the double conjugate, and a method for preparing the same. The chitosan based cationic polymer conjugate of the present invention forms a complex with negatively charged gene medicine such as plasmid DNA and small interfering RNA to efficiently transfer the desired gene medicine into cells with low cytotoxicity. Accordingly, the conjugate can be used as an effective delivery system for in vivo administration of gene medicine.

Biopolymer conjugates comprising an interleukin-11 analog

The present invention provides for biopolymer conjugates of an IL-11 analog (mIL-11) and a biocompatible polymer. The mIL-11 of the invention displays an enhanced resistance to acidolysis and shows increased stability as compared to rhIL-11. The conjugates of the present invention are characterized by a longer serum half-life and exhibit essentially no loss of activity as compared to the corresponding unconjugated mIL-11.

Improved interferon polymer conjugates

Compositions containing alpha interferon conjugated to a substantially non-antigenic polymer are disclosed in which at least about 30% o of the conjugates include covalent attachment of the alpha interferon to the substantially non-antigenic polymer at a histidine Also disclosed is a process for preparing the conjugates. The process includes contacting an alpha interferon with a succinimidyl carbonate-activated substantially non-antigenic polymer at a pH which is sufficient to facilitate covalent attachment of the polymer on a histidine of the alpha interferon.

Biologically active material conjugated with biocompatible polymer with 1:1 complex, preparation method thereof and pharmaceutical composition comprising the same

Highly reactive branched polymer and proteins or peptides conjugated with the polymer

The present invention relates to new biocompatible polymer derivatives, and a protein-polymer or a peptide-polymer which is produced by conjugation of biologically active protein and peptide with the biocompatible polymer derivatives. More particularly, the present invention relates to a highly reactive branched biocompatible polymer derivative containing a long linker between polymer derivatives and protein or peptide molecules, which is minimized in decrease the biological activity of proteins by conjugating the less number of polymer derivatives to the active sites of proteins, improved in water solubility, and protected from being degraded by protease. In hence, the highly reactive branched biocompatible polymer-proteins or peptides conjugates with long linker retain the biological activity in a long period of time and improve a bioavailability of bioactive proteins and peptides.

Biopolymer conjugates comprising an interleukin-11 analog

Biologically active material conjugated with biocompatible polymer with 1:1 complex, preparation method thereof and pharmaceutical composition comprising the same

Human growth hormone conjugated with biocompatible polymer

The present invention relates to conjugates of biocompatible polymers and hGH, particularly PEG-hGH, where the activated biocompatible polymer is conjugated to a carboxyl group of hGH at a molar ratio of 2:1 or less, preferably 1:1, methods of preparation, and related pharmaceutical compositions. The PEG-hGH conjugates have up to 20% of the activity of the native hGH while the in vivo half life is increased 10 fold. The PEG-hGH conjugates may be used therapeutically to treat growth retardation or growth failure, especially short stature in children, and conditions related to aging.

Improved interferon polymer conjugates

32 Compositions containing alpha interferon conjugated to a substantially no n- antigenic polymer are disclosed in which at least about 30% o of the conjugates include covalent attachment of the alpha interferon to the substantially non-antigen ic polymer at a histidine Also disclosed is a process for preparing the conjugates. The process includes contacting an alpha interferon with a succinimidyl carbonate- activated substantially non-antigenic polymer at a pH which is sufficient to facilitat e covalent attachment of the polymer on a histidine of the alpha interferon.

Verbesserte interferon-polymer konjugate

Human growth hormone conjugated with biocompatible polymer

The present invention relates to conjugates of biocompatible polymers and hGH, particularly PEG-hGH, where the activated biocompatible polymer is conjugated to a carboxyl group of hGH at a molar ratio of 2:1 or less, preferably 1:1, methods of preparation, and related pharmaceutical compositions. The PEG-hGH conjugates have up to 20% of the activity of the native hGH while the in vivo half life is increased 10 fold. The PEG-hGH conjugates may be used therapeutically to treat growth retardation or growth failure, especially short stature in children, and conditions related to aging.