Chong Kun Dang Corporation

Chong Kun Dang Pharmaceutical Corporation

Chung Il Hong

Jung Woo Kim

Hee Jong Shin

Nam Hee Choi

Su Geun Yang

Jae Hyun Kim

Soon Kil Ahn

Jong Lae Lim

Hyoung Sik Chun

Seung Kee Moon

Kyung Hwan Kim

Nam Song Choi

Sang Joon Lee

Tae Won Kang

Hung Bae Chang

Ryung Kee Hong

Jong Gwan Kim

Gang Sun Choi

Won Kyu Choi

Hyeog Jin Son

Byoung Taik Choi

Su Kyung Lee

Chong Kook Kim

Nam Hyun Lyu

Cheol Kyu Han

Dong Ock Cho

Yong Rack Choi

The present invention relates to an inclusion compound of fumagillol derivative or its salt with hydroxypropyl-&#x3b2;-cyclodextrin or sulfobutylether-7-&#x3b2;-cyclodextrin, and pharmaceutical compositions comprising the same. The inclusion compound according to the present invention has superior water solubility and stability while exhibiting low toxicity, rendering it valuable as an anticancer agent or inhibitor of tumor metastasis.

Inclusion compounds of fumagillol derivative or its salt, and pharmaceutical compositions comprising the same

The present invention relates to an improved process for preparing simvastatin and more particularly, the improved process for preparing simvastatin expressed by formula 1 with high yield and high purity by performing the following sequential processes comprising: (i) hydrolysis of lovastatin as starting material with potassium t-butoxide in an organic solvent and small amount of water under a mild reaction condition, followed by lactonization of the obtained solid intermediate with preventing from formation of by-products; (ii) protection of an alcohol group with t-butyldimethylsilyl group which can be easily removed with concentrated hydrochloric acid without the formation of by-products; (iii) acylation of the obtained protected intermediate with acyloxytriphenyl phosphonium salt as an acylating agent under a mild reaction condition; and (iv) removal of the silyl protective group with a concentrated hydrochloric acid. The present invention is to provide the improved process of preparing simvastatin expressed by formula 1 environmentally sound, economically efficient, and industrially useful.

Process for preparing simvastatin

Disclosed herein is a process for preparing highly pure acarbose of formula (I) useful as medicine for the treatment of diabetes. The disclosed process comprises prepurifying an acarbose-containing solution using a synthetic adsorbent to produce a prepurified acarbose having an acarbose content of a predetermined level or more; and contacting the prepurified acarbose with a monodispersed, strongly acid cation exchanger, in one step, to absorb acarbose.

Process for preparing acarbose with high purity

The present invention relates to Streptomyces sp. producing tautomycetin which possesses an immunosuppressive or antibacterial activities, a process for preparing tautomycetin from the said microorganism, and an immunosuppressant or immunosuppressive pharmaceutical composition comprising tautomycetin as an active ingredient which suppresses interleukin-2 production, CD69 and interleukin-2 receptor(IL-2R) expression on the cell surface, and graft rejection in the organ transplantation. The present inventors isolated a soil microorganism which produces a substance possessing antibiotic and immunosuppressive activities, and identified the said microorganism and substance as a novel Streptomyces sp. and tautomycetin, respectively. Further, the present inventors developed a method of manufacturing the tautomycetin in a large scale from the culture of the said microorganism and discovered that tautomycetin suppresses mouse mixed lymphocyte reaction(MLR) and the expression of IL-2 based on a series of experiments employing cell line transfected with a recombinant gene.

Streptomyces sp producing tautomycetin and immunosuppressant comprising tautomycetin as active ingredient

A pharmaceutical composition comprising a cyclosporin solid-state microemulsion is disclosed. In a preferred embodiment, the composition comprises a cyclosporin microemulsion dispersed in an enteric carrier. The composition does not dissolve in external phases such as artificial gastric fluid, but dissolves rapidly in artificial intestinal fluid, whereby it releases the cyclosporin microemulsion, providing rapid delivery of cyclosporin. The composition effectively maintains a therapeutic blood concentration of cyclosporin with once a day dosing, providing for convenience of administration and avoiding adverse effects induced by increasing peak blood cyclosporin concentrations associated with conventional cyclosporin formulations.

Pharmaceutical composition comprising cyclosporin solid-state microemulsion

The present invention relates to a microemulsion preconcentrate composition comprising (1) cyclosporin as an active component; (2) alkyl ester of polycarboxylic acid and/or carboxylic acid ester of polyols as a lipophilic solvent; (3) oil; and (4) surfactant. The composition according to the present invention is characterized in that it dissolves in an external phase such as water, artificial gastric fluid and artificial intestinal fluid by controlling the mixing ratio of the components thereby to get the microemulsion form of inner phase diameter of 100 nm or below. The composition according to the present invention can be formulated as the dosage form of a soft capsule, a hard capsule sealed with a gelatin banding at the conjugated portion, or an oral liquid preparation for oral administration. Especially, in the case that the composition according to the present invention is formulated in a soft capsule, the resultant capsule does not show the disadvantages of the prior arts such as the reactivity of hydrophilic solvent with gelatin shell of soft capsule and the volatility of hydrophilic solvent. It is because the existing patents use a hydrophilic solvent as an essential component of their compositions but the present invention does not use any hydrophilic solvent.

Cyclosporin-containing microemulsion preconcentrate composition

Compounds useful as angiogenesis inhibiting agents and processes for their preparation are disclosed. In one embodiment, the compounds of the invention are represented by Formula 1: ##STR1## Also disclosed is a pharmaceutical composition for inhibiting angiogenesis in a mammal, said composition comprising a compound of Formula 1, or a pharmaceutically acceptable salt thereof, as an active ingredient.

Fumagillol derivatives and processes for preparing the same

The present invention relates to a microemulsion preconcentrate composition comprising (1) cyclosporin as an active component; (2) alkyl ester of polycarboxylic acid and/or carboxylic acid ester of polyols as a lipophilic solvent; (3) oil; and (4) surfactant. The composition according to the present invention is characterized in that it dissolves in an external phase such as water, artificial gastric fluid and artificial intestinal fluid by controlling the mixing ratio of the components thereby to get the microemulsion form of inner phase diameter of 100 nm or below. The composition according to the present invention can be formulated as the dosage form of a soft capsule, a hard capsule sealed with a gelatin banding at the conjugated portion, or an oral liquid preparation for oral administration. Especially, if the cyclosporin microemulsion preconcentrate comprising cyclosporin, oil, lipophilic solvent and surfactant is formulated in a soft capsule according to the present invention, the resultant capsule removes the disadvantages of the prior arts showing the reactivity of hydrophilic solvent with gelatin shell of soft capsule and the volatility of hydrophilic solvent wherein the hydrophilic solvent was essential component in the composition according to the existing patents.

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Chicago, IL, United States of America

Chung Il Hong