Abstract: The present invention provides a 3?,4?,5-trimethoxy flavone derivative and a pharmaceutically acceptable salt thereof, preparation thereof, and a pharmaceutical composition for the treatment and prevention of dry eye syndrome comprising the same as an active ingredient. The 3?,4?,5-trimethoxy flavone derivative and its pharmaceutically acceptable salt inhibit corneal damage through excellent stimulatory action on mucus secretion in the conjunctiva and therefore may be effective as a prophylactic or therapeutic agent for dry eye syndrome.

Abstract: The present invention provides a novel heterocyclic compound containing a beta-amino group, a method for preparing the same, and a pharmaceutical composition comprising the same heterocyclic compound or a pharmaceutically acceptable salt thereof as an active ingredient. The heterocyclic compound of the present invention exhibits excellent DPP-IV inhibitory activity and bioavailability and therefore can be useful for the prophylaxis or treatment of DPP-IV-related diseases such as diabetes or obesity.

Abstract: The present invention provides novel crystalline forms D1 and D2 of [R—(R*,R*)]-2-(4-fluorophenyl)-?,?-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid hemicalcium salt, and hydrates thereof. The crystalline forms D1 and D2 have X-ray powder diffraction peaks described in FIGS. 1 and 3, respectively. Further, the present invention provides processes for preparing the crystalline forms and pharmaceutical compositions comprising the crystalline forms. The crystalline forms can be produced on a commercial scale and exhibit excellent stability.

Abstract: The present invention relates to three-branched PEG-G-CSF conjugate of general formula (1) in which the bonding ratio of three-branched polyethylene glycol (PEG) and G-CSF is 1:1 (mol/mol), wherein PEG has an average molecular weight of from 200 to 45,000 daltons; a pharmaceutical composition comprising the same, and a preparing method thereof.

Abstract: The present invention provides a novel benzamide derivative represented by formula 1 and an isomer, a pharmaceutically acceptable salt or hydrate thereof, and a composition for activating a 5-HT<sb>4</sb> receptor comprising the same, as an active ingredient. Benzamide derivatives of the present invention has superior affinity for 5-HT<sb>4</sb> receptors, capability to reduce the gastric evacuation time, capability to alleviate ventricular tachycardia, ventricular fibrillation, torsades de pointes and QT prolongation, and low toxicity. Therefore, benzamide derivatives of the present invention are therapeutically effective for digestive system diseases.

Abstract: The present invention relates to more improved process for preparing 2?-deoxy-2?,2?-difluoronucleoside and its intermediate. The present invention provide a process for preparing an erythro enantiomer in greater than 98% purity, comprising forming a lactone ring by hydrolyzing ethyl (3RS)-2,2-difluoro-3-hydroxy-3-(2,2-dimethyloxolan-4-yl)propionate is hydrolyzed in the presence of hydrolysis reagents selected from acetic acid or chloroacetic acid, water and a mixture of organic solvents selected from the group comprising acetonilrile, dioxane, tetrahydrofuran or toluene, introducing a substituted benzoyl protecting group at the 3-position and 5-position, and recrys- tallizing said erythro enantiomer. Further, the present invention provides a process for selectively preparing, in greater than 99% purity, a beta-anomer 2?-deoxy-2?,2?-difluoronucleoside at the 3?-position and 5?-position that are protected by a substituted benzoyl in a 2:3 alpha/beta anomeric ratio.

Abstract: The present invention relates to novel derivatives of oxazolidinone, a method thereof and pharmaceutical compositions comprising the derivatives for use in an antibiotic. The oxazolidinone derivatives of the present invention show inhibitory activity against a broad spectrum of bacteria and lower toxicity. The prodrugs, prepared by reacting the compound having hydroxyl group with amino acid or phosphate, have an excellent efficiency on solubility thereof against water. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium. Accordingly, the compositions comprising the oxazolidinone are used in an antibiotic.

Abstract: The present invention relates to three-branched polyethylene glycol-interferon alpha conjugate of general formula (1) wherein polyethylene glycol has an average molecular weight of from 400 to 45,000 daltons, and a pharmaceutical composition comprising the same. The bioactive polyethylene glycol-interferon alpha conjugate of general formula (1) has antiviral and antitumoral activities, improved yield and purity by high reactivity in the reaction, and the effects to increase the half-life in blood remarkably, and to minimize the decreases in biological activity of interferon.

Abstract: Disclosed herein is a hair growth-stimulating composition containing a non-polar solvent-soluble extract fraction of Cantharis as an active ingredient. The composition shows an excellent hair growth activity with minimal skin irritation compared to conventional ones. It can be used for hair growth in various fields, including medical and non-medical supplies and cosmetics.

Abstract: The present invention relates to a vaccine enhancing the protective immunity to Hepatitis C virus using plasmid DNA and recombinant adenovirus, more particularly to a vaccine consisting of ?core-E1-E2 expressing DNA vaccine, nonstructural protein NS3 and NS4 expressing DNA vaccine, nonstructural protein NS5 expressing DNA vaccine and recombinant adenovirus vaccine, and method for administration of the vaccine by priming with the DNA vaccines described above and boosting with the recombinant adenovirus vaccine thereby enhancing the protective immunity to Hepatitis C virus.

Abstract: A method for preparing pyrazolopyrimidinone derivatives and their pharmaceutically acceptable salts having efficacy on the treatment of impotence, one of male sexual dysfunctions. The method comprises the steps of: a) chlorosulfonating a pyrazolamide compound to obtain a chlorosulfonated compound; b) reacting the chlorosulfonated compound of step (a) with a primary amine to obtain a sulfonamide compound and c) performing an intramolecular cyclization of the sulfonamide compound of step (b) to produce the compound of formula below 1, wherein the steps b) and c) are performed in situ in alcohol by adding a base to the reaction mixture without workup after the step b) is completed.

Abstract: The present invention relates to novel oxazolidinone derivatives, their pharmaceutically acceptable salts and a process for the preparation thereof. More particularly, the present invention relates to oxazolidinone derivatives having pyridine or pyrimidine moeity substituted by heterocycle and heteroaromaticcycle at 4-position of phenyl ring. The compounds of the present invention have wide antibacterial spectrum, superior antibacterial activity and low toxicity, such that the compound of this invention can be used as an antibacterial agent.

Abstract: The invention relates to a novel method for preparing 2-(4-chlorobenzoylamino)-3-[2(1H)-quinolinon-4-yl]propionic acid, also known as Rebamipide represented by the formula I and useful for treatment of peptic ulcer from alkyl 2-(4-chlorobenzoylamino)-2-alkoxycarbonyl-3-[2(1H)-quinolinon-4-yl]propionate represented by the formula II in the presence of a base solution for hydrolysis and decarboxylation to remove a carboxyl group.

Abstract: The present invention relates to pyrazolopyrimidinone derivatives of formula 1, their preparation method and pharmaceutical compositions containing the said derivatives. The compounds have efficacy on the treatment of impotence, one of male sexual dysfunctions with the side effects reduced.

Abstract: The invention provides novel cephalosporin derivatives of the formula (I) ##STR1## and salts thereof for use in pharmaceutical compositions. Also novel precursors for synthesis of the cephalosporins are disclosed.

Abstract: The present invention relates to new cephalosporin compounds of the formula (I), particularly 3-position of cephem rings thereof substituted with new thione compounds and pharmaceutically acceptable salts thereof, which have broad antibacterial activities against both Gram-positive and Gram-negative bacteria, and the said compounds can be prepared by reacting the compounds of the formula (II) with the new thione compounds of the formula (III). ##STR1## wherein R.sub.1 is a C.sub.1-4 alkyl(preferably methyl or ethyl), C.sub.3-4 alkenyl(preferably allyl), C.sub.3-4 alkynyl (preferably propargyl) group or --C(R.sup.a) (R.sup.b)CO.sub.2 H(preferably --C(CH.sub.3).sub.2 CO.sub.2 H or --CH.sub.2 CO.sub.2 H), wherein R.sup.1 and R.sup.b, same or different, are a hydrogen atom or a C.sub.1-4 alkyl group;R.sub.2 is a C.sub.1-4 alkyl(preferably methyl or ethyl), C.sub.3-4 alkenyl(preferably allyl), C.sub.3-4 cycloalkyl(preferably cyclopropyl) group or carboxyalkyl(preferably --CH.sub.2 CO.sub.2 H) group;R.sub.

Abstract: Transdermal gels comprising (1) ketoprofen as an effective component, (2) poloxamer, (3) one or more agents selected from ethyl alcohol, isopropyl alcohol, propylene glycol, polyethylene glycol and glycerin, (4) one or more agents selected from the group consisting of lauric acid, oleic acid, capric acid, myristic acid, lauryl alcohol, oleyl alcohol and menthol, (5) water or a buffer solution. The gels form thin and pliable films, which are easily washable with water. They possess prolonged antiinflammatory and analgesic activities and physicochemical stability with less systemic side effects and gastric irritation.

Abstract: A benzoxazine or benzothiazine derivative of the formula (A), ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are the same or different and represent a hydrogen atom or a C.sub.1-4 alkyl group; or R.sub.1 and R.sub.2 can be joined together along with the imidazole ring to form a benzimidazole; X and Y are the same or different and represent an oxygen or sulfur atom; or a pharmaceutically acceptable salt thereof, exhibits an excellent inotropic effect and can be used as a cardiac stimulant.