Abstract: The present invention relates to an N-terminal amino acid-modified insulinotropic peptide having a high activity, and to a pharmaceutical composition comprising the same. The insulinotropic peptide derivatives according to the present invention exhibit therapeutic effects, which are not observed in native and other insulinotropic peptide analogs. Therefore, the insulinotropic peptide derivatives and the pharmaceutical composition comprising the same according to the present invention can be effectively provided for the treatment of the diseases.

Abstract: Optically pure voriconazole can be prepared in a high yield by a) subjecting 1-(2,4-difluorophenyl)-2(1H-1,2,4-triazol-1-yl)ethanone to Reformatsky-type coupling reaction with a substituted thiopyrimidine derivative to obtain a desired (2R,3S)/(2S,3R)-enantiomeric pair; b) removing the thiol derivative from the enantiomer to obtain racemic voriconazole; and c) isolating the racemic voriconazole by way of optical resolution using an optically active acid.

Abstract: The present invention provides a novel amide derivative and a pharmaceutically acceptable salt thereof which selectively and effectively inhibits the growth of cancer cells induced by the overexpression of an epidermal growth factor receptor and also prevents the development of drug resistance caused by the mutation of EGFR tyrosine kinase, and a pharmaceutical composition comprising same as an active ingredient.

Abstract: Disclosed is a novel use of an immunoglobulin Fc fragment, and more particularly, a pharmaceutical composition comprising an immunoglobulin Fc fragment as a carrier. The pharmaceutical composition comprising an immunoglobulin Fc fragment as a carrier remarkably extends the serum half-life of a drug while maintaining the in vivo activity of the drug at relatively high levels. Also, when the drug is a polypeptide drug, the pharmaceutical composition has less risk of inducing immune responses compared to a fusion protein of the immunoglobulin Fc fragment and a target protein, and is thus useful for developing long-acting formulations of various polypeptide drugs.

Abstract: Disclosed are a protein conjugate with improved in vivo duration and stability and the use thereof. The protein conjugate includes a physiologically active polypeptide, a non-peptide polymer and an immunoglobulin Fc fragment. Since the three components are covalently linked, the protein conjugate has extended in vivo duration and enhanced stability for the physiologically active polypeptide. The protein conjugate maintains the in vivo activity at relatively high levels and remarkably increases the serum half-life for the physiologically active polypeptide, with less risk of inducing undesirable immune responses. Thus, the protein conjugate is useful for developing long-acting formulations of various polypeptide drugs.

Abstract: The present invention discloses a non-hygroscopic crystalline bepotastine metal salt hydrate, a method for preparing same, and a pharmaceutical composition comprising same for treating or preventing a histamine-mediated disease or an allergic disease.

Abstract: A recombinant expression vector capable of expressing and secreting an antibody fragment fused with E. coli thermostable enterotoxin signal sequence derivative or E. coli outer membrane protein A (Omp A) signal sequence in the form of a soluble heterozygote protein is used to mass-produce the antibody fragment by culturing a microorganism transformed with the expression vector in a medium and collecting the antibody fragment secreted from the transformed microorganism into the medium.

Abstract: Disclosed herein is an inducible high-expression cassette comprising a dihydrofolate reductase (DHFR) promoter from which GC-rich repeat sequences are partially or entirely removed, the cassette capable of more effectively improving a gene amplification system. Also disclosed are an expression vector comprising the inducible expression cassette and optionally a gene encoding a recombinant protein of interest, an animal cell line transformed with the expression vector, and a method of mass producing and purifying a recombinant protein by culturing the transformant. The present invention enables the shortening of the time required to establish a cell line producing a recombinant protein of interest at high levels using a low concentration of a DHFR inhibitor, thereby allowing more effective production of the recombinant protein.

Abstract: This invention provides atorvastatin strontium salt or its hydrates or polymorphs having improved water solubility, which is useful for the prevention or treatment of hyperlipidemia and hypercholesterolemia, and a pharmaceutical composition comprising same.

Abstract: A protein conjugate having a prolonged in vivo half-life of a physiological activity, comprising i) a physiologically active polypeptide, ii) a non-peptidic polymer, and iii) an immunoglobulin, is useful for the development of a polypeptide drug due to the enhanced in vivo stability and prolonged half-life in blood, while reducing the possibility of inducing an immune response.

Abstract: The present invention relates to an insulinotropic peptide conjugate having improved in-vivo duration of efficacy and stability, comprising an insulinotropic peptide, a non-peptide polymer and an immunoglobulin Fc region, which are covalently linked to each other, and a use of the same. The insulinotropic peptide conjugate of the present invention has the in-vivo activity which is maintained relatively high, and has remarkably increased blood half-life, and thus it can be desirably employed in the development of long acting formulations of various peptide drugs.

Abstract: A modified human granulocyte-colony stimulating factor (hG-CSF) is produced by culturing a microorganism transformed with an expression vector comprising a gene encoding a modified hG-CSF to produce and secrete the modified hG-CSF to periplasm, said modified hG-CSF being obtained by replacing at least one of the 1st, 2nd, 3rd and 17th amino acids of wild-type hG-CSF (SEQ ID NO: 2) with other amino acid.

Abstract: The present invention provides a stable anhydrous crystalline docetaxel which has anti-tumor and anti-leukemia activity, and method for the preparation thereof.

Abstract: The present invention relates to a novel method for preparing docetaxel having anti-tumor and anti-leukemia activity, and intermediates useful for preparing docetaxel.

Abstract: The present invention relates to a method for preparing montelukast, an inhibitor against leukotrienes, and an intermediate used therein. According to the inventive method, high-purity montelukast or its sodium salt can be prepared in a high yield.

Abstract: 3R-carboxylate enantiomer derivative of formula (III) can be prepared easily and selectively by the method of the present invention, and a highly pure D-erythro-2,2-difluoro-2-deoxy-1-oxoribose derivative can be prepared efficiently from the compound of formula (III) as an intermediate.

Abstract: The bioavailability of an anticancer agent is enhanced when the anticancer agent is administered together with a pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to a method for preparing clopidogrel 1,5-naphthalenedisulfonate or a hydrate thereof, which comprises reacting a clopidogrel-acid addition salt with disodium 1,5-naphthalenedisulfonate or its hydrate in water, or a mixture of water and an organic solvent. High quality clopidogrel 1,5-naphthalenedisulfonate can be prepared by the inventive method by way of using non-corrosive disodium 1,5-naphthalenedisulfonate.

Abstract: This invention provides a crystalline S-omeprazole strontium hydrate for the prevention or treatment of gastric acid-related diseases, which has high optical purity, theremostability, solubility and nonhygroscopicity, a method for preparing same, and a pharmaceutical composition containing same.

Abstract: The present invention relates to an insulinotropic peptide conjugate having improved in-vivo duration of efficacy and stability, comprising an insulinotropic peptide, a non-peptide polymer and a carrier substance, which are covalently linked to each other, and a use of the same. The insulinotropic peptide conjugate of the present invention has the in-vivo activity which is maintained relatively high, and has remarkably increased blood half-life, and thus it can be desirably employed in the development of long acting formulations of various peptide drugs.