Abstract: Provided is a method for treating a symptom of vibrio infection by using an RTX toxin production inhibitor comprising N-(4-oxo-4H-thieno[3,4-c]chromen-3-yl)-3-phenylprop-2-ynamide having derivatives thereof which can repress (prevent or treat) a symptom of vibrio infection by inhibiting RTX toxin production, other than directly killing vibrio bacteria, to not allow vibrio bacteria to have pathogenicity, and thereby can be an alternative to antibiotics that aim to kill bacteria themselves and thus fundamentally retain the problem of resistance incurrence.

Abstract: Provided is a method for treating a symptom of vibrio infection by using an RTX toxin production inhibitor comprising N-(4-oxo-4H-thieno[3,4-c]chromen-3-yl)-3-phenylprop-2-ynamide having derivatives thereof which can repress (prevent or treat) a symptom of vibrio infection by inhibiting RTX toxin production, other than directly killing vibrio bacteria, to not allow vibrio bacteria to have pathogenicity, and thereby can be an alternative to antibiotics that aim to kill bacteria themselves and thus fundamentally retain the problem of resistance incurrence.

Abstract: The present invention relates to a novel pentadienoyl piperidine derivative, a pharmaceutical composition containing the same for prevention or treatment of metabolic diseases, and a functional food composition using the same for improvement or relief of metabolic diseases. The pentadienoyl piperidine derivative of the present invention inhibits the differentiation of preadipocytes, reduces body weight, visceral fat, blood lipid levels, and blood glucose levels, improves a blood liver function index, and suppresses metabolic inflammation responses. Thus, ultimately, the derivative can be usefully used as a medicine or a functional food composition, which exhibits the preventive or therapeutic activity for metabolic diseases selected from the group consisting of obesity, diabetes, dyslipidemia, fatty liver and insulin resistance syndrome.

Abstract: The present invention relates to a novel pentadienoyl piperidine derivative, a pharmaceutical composition containing the same for prevention or treatment of metabolic diseases, and a functional food composition using the same for improvement or relief of metabolic diseases. The pentadienoyl piperidine derivative of the present invention inhibits the differentiation of preadipocytes, reduces body weight, visceral fat, blood lipid levels, and blood glucose levels, improves a blood liver function index, and suppresses metabolic inflammation responses. Thus, ultimately, the derivative can be usefully used as a medicine or a functional food composition, which exhibits the preventive or therapeutic activity for metabolic diseases selected from the group consisting of obesity, diabetes, dyslipidemia, fatty liver and insulin resistance syndrome.

Abstract: The present invention relates to a fluoro-homoneplanocin A, its nucleoside derivative, and synthetic methods. The novel fluoro-homoneplanocin A and its nucleoside derivative in the present invention have an effect on cancer prevention or treatment, and therefore can be used as anticancer drugs.

Abstract: Disclosed are adenosine derivatives, methods for the synthesis thereof, and pharmaceutical compositions for the prevention and treatment of inflammatory diseases, comprising the same as an active ingredient. The adenosine derivatives have high binding affinity and selectivity for adenosine receptors, especially for A3 adenosine receptors and act as A3 adenosine receptor antagonists, and exhibit anti-inflammatory activity. Thus, the adenosine derivatives are useful in the prevention and treatment of inflammatory diseases.

Abstract: The present invention relates to a method by use of a pharmaceutical composition for preventing or treating inflammatory disease, colorectal cancer and prostate cancer, which contains an A3 adenosine receptor agonist, 2-chloro-N6-(3-iodobenzyl)-4?-thioadenosine-5?-N-methyluronamide (thio-Cl-IB-MECA), N6-(3-iodobenzyl)-4?-thioadenosine-5?-N-methyluronamide (thio-IB-MECA), or a pharmaceutically acceptable salt thereof. The pharmaceutical composition of the invention is significantly less toxic than conventional A3 adenosine agonists, and thus is useful for prevention or treatment of inflammatory disease. In addition, it more selectively inhibits the growth of androgen receptor-dependent or independent prostate cancer cells than other A3 adenosine receptor agonists and thus is useful for prevention or treatment of colorectal cancer or prostate cancer.

Abstract: The present invention relates to a method for preparation of MLN4924 as an E1 activating inhibitor, and more specifically, to a method for efficient and stereoselective preparation of MLN4924 by means of key steps involving stereoselective reduction of cyclopentenone with isopropylidene, regioselective cleavage of isopropylidene moiety, and synthesis of cyclic sulfate.

Abstract: The present invention relates to a method for preparation of MLN4924 as an E1 activating inhibitor, and more specifically, to a method for efficient and stereoselective preparation of MLN4924 by means of key steps involving stereoselective reduction of cyclopentenone with isopropylidene, regioselective cleavage of isopropylidene moiety, and synthesis of cyclic sulfate.

Abstract: The present invention relates to a pharmaceutical composition for preventing or treating inflammatory disease, colorectal cancer and prostate cancer, which contains an A3 adenosine receptor agonist, 2-chloro-N6-(3-iodobenzyl)-4?-thioadenosine-5?-N-methyluronamide (thio-Cl-IB-MECA), N6-(3-iodobenzyl)-4?-thioadenosine-5?-N-methyluronamide (thio-IB-MECA), or a pharmaceutically acceptable salt thereof. The pharmaceutical composition of the invention is significantly less toxic than conventional A3 adenosine agonists, and thus is useful for prevention or treatment of inflammatory disease. In addition, it more selectively inhibits the growth of androgen receptor-dependent or independent prostate cancer cells than other A3 adenosine receptor agonists and thus is useful for prevention or treatment of colorectal cancer or prostate cancer.

Abstract: Disclosed are adenosine derivatives, methods for the synthesis thereof, and pharmaceutical compositions for the prevention and treatment of inflammatory diseases, comprising the same as an active ingredient. The adenosine derivatives have high binding affinity and selectivity for adenosine receptors, especially for A3 adenosine receptors and act as A3 adenosine receptor antagonists, and exhibit anti-inflammatory activity. Thus, the adenosine derivatives are useful in the prevention and treatment of inflammatory diseases.

Abstract: The present invention relates to nucleoside derivatives represented by general formulas I and II, their synthetic methods and their pharmacologically acceptable salts thereof, and compositions containing such compounds. Methods for treating hyperproliferative disorders by administering the compounds are also included.

Abstract: Disclosed are purine nucleoside compounds that are selective to A3 adenosine receptors and are useful for the treatment of cancer and inflammatory diseases. The compounds are shown by the following general formula (I), including isomers thereof: wherein X is sulfur or oxygen; R1 is hydrogen, alkyl, benzyl, halobenzyl, or phenylalkyl; R2 is hydrogen, halogen, alkoxy, alkenyl, alkynyl, alkylthio, or thio; R3 and R3? are hydrogen, hydroxyalkyl, alkoxycarbonyl, or alkylaminocarbonyl, whereas R3 and R3? do not have identical substituents simultaneously; and R4 is hydrogen or alkyl. Also disclosed are a pharmaceutical composition comprising a compound of formula (I), an isomer, or its pharmacologically acceptable salt as an active ingredient and a method for preventing or treating various diseases, state, or condition, including asthma, inflammation, cerebral ischemia, heart diseases, and cancer.

Abstract: An asymmetric process for the preparation of enantiomerically pure .beta.-L-(-)-1,3-oxathiolane-nucleosides that includes the initial preparation of the key chiral intermediates (2R,5R) and (2R,5S)-5-(O-protected)-2-(protected-oxymethyl)-1,3-oxathiolane from 1,6-thioanhydro-L-gulose. The 2R,5(R,S)-5-(O-protected)-2-(protected-oxymethyl)-1,3-oxathiolane is condensed with a desired heterocyclic base, typically a purine or pyrimidine base, to provide the product nucleoside. The synthesis can be used to prepare the pharmaceutically important compound, .beta.-L-(-)-1-[(2.beta.,4.beta.)-2-(hydroxymethyl)-4-(1,3-thioxolane)]cyt osine (.beta.-L-(-)BCH-189).