Abstract: The present invention relates to herbal extracts of Sinapis Semen, Corydalis Tuber, Pharbitidis Seed, and Strychni Ignatii Semen, and a composition containing the same for treating and preventing gastrointestinal motility disorder. The extracts of the present invention have a remarkable effect of promoting gastrointestinal motility through HT3 receptor antagonism and/or HT4 receptor antagonism.

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: Disclosed herein are novel 1,3-dihydro-5-isobenzofurancarbonitrile derivatives represented by Formula 1, or pharmaceutically acceptable salts thereof. Also disclosed is a pharmaceutical composition for treating or preventing premature ejaculation including the compound. The 1,3-dihydro-5-isobenzofurancarbonitrile derivatives have a short half-life and inhibit the ejaculation process by selectively inhibiting serotonin reuptake via a serotonin reuptake transporter present in a presynaptic neuron. Thus, the compounds are useful in the treatment and prevention of premature ejaculation.

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 an acid addition salt of Udenafil, a preparation method thereof and a pharmaceutical composition comprising the same. The acid addition salt of Udenafil in which Udenafil is bonded to an organic acid selected from the group consisting of oxalic acid, benzenesulfonic acid, camphorsulfonic acid, cinnamic acid, adipic acid and cyclamic acid, has excellent solubility in an aqueous medium, water stability and crystallinity, thereby being suitably applied for a pharmaceutical composition.

Abstract: This invention relates to a controlled-release composition for producing a sustained-release preparation containing udenafil, including (A) udenafil and a pharmaceutically acceptable salt, (B) a solubility modulator, (C) an adsorbent, and (D) a hydrophilic polymer. This controlled-release composition for producing a sustained-release preparation containing udenafil releases drugs constantly regardless of the pH level in the gastrointestinal tract, and thus freely controls the drug release time within the range of 3˜24 hours, and reduces the variability in the effect of drugs among individuals. Also, this composition can be produced into a sustained-release preparation which has an optimum condition for expressing the effect of drugs in the treatment of diseases including pulmonary arterial hypertension, hepatic portal vein hypertension, benign prostatic hyperplasia, and the like, which can be treated by udenafil and which requires the long-term drug administration.

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: This invention relates to a single-liquid pharmaceutical composition for injection containing docetaxel. The composition includes (A) docetaxel and pharmaceutically acceptable salts thereof, (B) a surfactant selected from the group consisting of polysorbate, polyoxyethylene glycol ester and polyoxyethylene castor oil derivatives, (C) a solvent comprising anhydrous ethanol in a concentration range of 100 to 800 mg/ml, in an injectable solution, and (D) a pH adjuster of an amount suitable for adjusting the pH of the liquid composition to 5 or less. The composition may be directly diluted in a perfusion liquid even without the use of an intermediary dilute solution in case the composition is used for injectable preparations since the composition is in a single liquid phase. Furthermore, the composition is suitable for effective administration of docetaxel since the pharmaceutical stability of the composition is significantly improved.

Abstract: Disclosed herein are novel 1,3-dihydro-5-isobenzofurancarbonitrile derivatives represented by Formula 1, or pharmaceutically acceptable salts thereof. Also disclosed is a pharmaceutical composition for treating or preventing premature ejaculation including the compound. The 1,3-dihydro-5-isobenzofurancarbonitrile derivatives have a short half-life and inhibit the ejaculation process by selectively inhibiting serotonin reuptake via a serotonin reuptake transporter present in a presynaptic neuron. Thus, the compounds are useful in the treatment and prevention of premature ejaculation.

Abstract: The present invention relates to a composition and a method for treating or preventing benign prostatic hyperplasia (BPH) and lower urinary tract symptoms (LUTS) without showing the side effect, by dramatically relaxing the smooth muscle in prostate and bladder.

Abstract: Disclosed herein is a therapeutic agent for chronic heart failure comprising, as an effective ingredient, 5-[2-propyloxy-5-(1-methyl-2-pyrrolidinyl-ethylamidosulfonyl)phenyl]-1-methyl-propyl-1,6-dihydro-7H-pyrazolo(4,3-d)pyrimidine-7-one. The compound inhibits phosphodiesterase-5 (PDE-5), which catalyzes the intracellular degradation of cyclic guanosine monophosphatase (cGMP), thereby mitigating several signs of chronic heart failure, that is, thereby preventing left ventricular dilatation, decreasing ventricular wall thinning, lowering elevated cardiac and circulating levels of atrial natriuretic peptide (ANP), and inhibiting ventricular fibrosis. Also, the compound has advantages in that it reaches the maximal plasma level in a short time, has an in vivo half-life longer than conventional PDE-5 inhibitors, allowing decreased administration frequency, and has fewer side effects, thus ensuring safety. Thus, the compound is useful as a therapeutic agent for chronic heart failure.

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 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 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 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 phenylpropionic acid derivative and a PPAR-? modulator comprising the same as an active ingredient. The phenylpropionic acid derivative of the present invention has modulatory action on function of PPAR-? and then exhibits hypoglycemic, hypolipidemic and insulin resistance-reducing effects on PPAR-mediated diseases or disorders. Therefore, the present invention is prophylactically or therapeutically effective for diabetes and metabolic diseases.

Abstract: The present invention relates to herbal extracts of Sinapis Semen, Corydalis Tuber, Pharbitidis Seed, and Strychni Ignatii Semen, and a composition containing the same for treating and preventing gastrointestinal motility disorder. The extracts of the present invention have a remarkable effect of promoting gastrointestinal motility through HT3 receptor antagonism and/or HT4 receptor antagonism.

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 the method for preparing pyrazolopyrimidinone derivatives and their pharmaceutically acceptable salts having efficacy on the treatment of impotence, one of male sexual dysfunctions. The method according to the present invention comprises the steps of chlorosufonation the pyrazolamide, followed by amination with amine and intramolecular cyclization. The method provides the pyrazolopyrimidinone derivatives and their pharmaceutically acceptable salts with high yield and in an economic manner.