Korea Research Institute of Chemical Technology

Rexahn Pharmaceuticals, Inc.

Sk Chemicals Co., Ltd.

Lsk Nrdo Co., Ltd.

Rexhan Pharmaceuticals, Inc.

Young-Dae Gong

Moon-Kook Jeon

Sung-Eun Yoo

Jae Yang Kong

Jin-Soo Seo

Young Bok Lee

Jong Yeon Hwang

Hyae-Gyeong Cheon

Dong-Su Kim

Soon-Hee Hwang

Gun-Do Kim

Eun Ju Lee

Chang Ho Ahn

Wie-Jong Kwak

Gildon Choi

Nam Kyu Lee

Heeyeong Cho

Dae Young Jeong

Chang-Ho Ahn

Yong-Baik Cho

Sukho Lee

Taeho Lee

Eun Sil Lee

Tae-Sung Koo

Jeong-Ran Kim

Na Yeon Kim

Nam-Sook Kang

Cho Young Sik

Choi Hyung Sub

Jeon Hyun Suk

Song Jin Sook

Kim Chi Hyun

Young-Sik Cho

Jong-Yeon Hwang

Ji-Yeon Park

Mi-Sook Dong

Jung Bum Lee

Soo-Youl Kim

Jun Won Lee

The present invention relates to a novel 4-(aryl)-N-(3-alkoxyfuro[2,3-b]pyrazin-2-yl)-piperazine-1-carboxamide derivative compound useful in the prevention or treatment of cancer; a preparation method thereof; and a pharmaceutical composition comprising the same. The novel 4-(aryl)-N-(3-alkoxyfuro[2,3-b]pyrazin-2-yl)-piperazine-1-carboxamide derivative compound of the present invention can effectively inhibit the growth of proliferating cells, and thus can be useful in the prevention or treatment of cancer.

4-(aryl)-N-(3-alkoxyfuro[2,3-b]pyrazin-2-yl)-piperazine-1-carboxamide derivative and antiproliferative effect thereof

The present invention relates to novel quioxaline-piperazine compounds, 1-[(6,7-substituted alkoxyquinoxalinyl)aminocarbonyl]-4-(hetero)arylpiperazine derivatives of formula (1): and their pharmaceutically acceptable salts, a process for their preparation thereof, and compositions containing such compounds. Therapeutic methods for the treatment of hyperproliferative disorders, including cancers, by administering quioxalin-piperazine compounds are also included.

1-[(6,7-substituted alkoxyquinoxalinyl)aminocarbonyl]-4-(hetero)arylpiperazine derivatives for treating tumors

The present invention related to a novel urea derivative for formula (I): which is useful as an anti-cancer agent, its pharmaceutically acceptable acid addition salt or stereoisomer, and to a process for preparing the urea derivative and an anti-cancer composition comprising the same as an active ingredient.

1-[6,7-substituted alkoxyquinoxalinyl)aminocarbonyl]-4-(hetero)arylpiperazine derivatives

The present invention relates to a novel benzopyran derivative having goodantagonistic activity on TGF-&#x3b2; receptor which can be effectively used as a prophylactic and therapeutic agent for liver disease as well as several fibroplasiadiseases such as hepatic fibrosis, liver cirrhosis, pulmonary fibrosis, dermatosclerosis, glomerular fibrosis and the like; and a pharmaceutical use thereof.

Benzopyran derivatives having inhibitory activities against liver fibrosis and cirrhosis and their pharmaceutical uses

Disclosed herein are 2,4-disubstituted-5-aminocarbonyl-1,3-thiazole derivatives, a preparation method thereof, and a therapeutic agent for treating inflammatory diseases induced by SPC, which contains the derivative as an active ingredient. The anti-inflammatory effect of the 2,4-disubstituted-5-aminocarbonyl-1,3-thiazole derivatives was analyzed through a test employing human dermal cells and an animal test using mice and, as a result, it was found that the derivatives showed excellent inhibitory activity on SPC receptor compared to thiazole derivatives known in the prior art. Thus, the 2,4-disubstituted-5-aminocarbonyl-1,3-thiazole derivatives or pharmaceutically acceptable salts thereof are useful as active ingredients in therapeutic agents for treating inflammatory diseases, such as inflammation, pruritus and skin infection, which appear in atopic dermatitis and other diseases induced by SPC activity. wherein R, R, Rand Rare as defined in the specification.

2,4-disubstituted-5-aminocarbonyl-1,3-thiazole derivatives for therapeutic agent of antiinflammatory disease, method thereof for preparation, therapeutic agent for antiinflammatory disease induced by SPC activity containing the same

The present invention relates to a noble 6-alkylamino-2-methyl-2'-(N-methyl substituted sulfonamido)methyl-2H-1-benzopyran derivative, a method for preparing the same with high efficiency using a parallel synthetic method, one of combinatorial chemical synthetic techniques, and a use of the novel compound showing a high inhibitory effect to 5-lipoxygenase (5-LO) activity for preventing and treating leukotriene (LTA4, B4, C4, D4) activation-related diseases such as inflammatory diseases, rheumatoid arthritis, colitis, asthma and psoriasis.

6-Alkylamino-2-methyl-2'-(N-methyl substituted sulfonamido)methyl-2H-1-benzopyran derivative as anti-inflammatory inhibitor

When a multi-step process reaction is carried out in a solution, it generally requires several treatments and purification procedures to go through with after the reaction, however, the inventive method for preparing 2,2'-disubstituted-3,4-dihydro-7,8-disubstituted-6-amino benzopyran derivative using a solid-phased synthetic method simplifies the treatment and purification procedures after the reaction, which makes possible to efficiently construct numerous drug-like libraries. In particular, since the inventive method of the present invention comprises the steps of introducing a carbonate linker of formula 2 into Wang resin used as a common solid support (Step 1); synthesizing various benzopyran in a carbamate form of formula 3 as a key intermediate by reacting various amino benzopyran derivatives with the carbamate resin of formula 2 (Step 2); synthesizing 2,2&#x2032;-disubstituted-3,4-2H-6-substituted benzopyran resin of formula 4 (Step 3); and synthesizing 2,2&#x2032;-disubstituted-3,4-2H-6-alkylamino benzopyran derivative of formula 1 using a dichloromethane solution containing TFA or an organic solvent containing an organic acid, the inventive method is capable of efficiently synthesizing various 2,2&#x2032;-disubstituted-3,4-2H-6-alkylamino benzopyran derivatives. Consequently, the present invention has developed a new technique for constructing 2,2&#x2032;-disubstituted-3,4-2H-6-alkylamino benzopyran library using a solid-phase parallel synthetic method and makes increased the applicability of combinatorial chemical synthetic method. Further, 2,2&#x2032;-disubstituted-3,4-2H-6-alkylamino benzopyran derivative prepared by the inventive method has a high inhibitory effect to 5-lipoxygenase (5-LO) activity, and therefore, can be effectively used for developing a new propylactic or therapeutic drug for leukotriene activation-related diseases such as chronic inflammation, rheumatic arthritis, colitis, asthma and psoriasis.

6-alkylamino-2,2'-disubstituted-7,8-disubstituted-2H-1-benzopyran derivatives as 5-lipoxygenase inhibitor

The present invention provides (i) 6-amino-2,2-dimethyl-3,4,6-trisubstituted benzopyran derivatives; (ii) a process for synthesizing benzopyran derivatives with high efficiency by parallel synthesis on a solid-phase as one of combinatorial chemical synthesis technologies; and (iii) a use of the benzopyran derivatives for preventing and treating diseases or disorders induced by promotion of lipid peroxidation or accumulation of oxidized products.

6-amino-2,2-dimethyl-3,4,6-trisubstituted benzopyran derivatives and their construction by parallel synthesis on solid-phase

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Daejeon, South Korea

Young-Dae Gong