Korea Research Institute of Chemical Technology

Hyae-Gyeong Cheon

Sung-Eun Yoo

Young-Dae Gong

Jong Yeon Hwang

Moon-Kook Jeon

Jin-Soo Seo

Soon-Hee Hwang

Joong-Kwon Choi

Eul-Kyun Yum

Jeon Hyun Suk

Yea-Kang Yoo

Song Jin Sook

Hyo-Jung Kim

Kim Chi Hyun

Sung-Soo Kim

Choi Hyung Sub

Seung-Kyu Kang

Young-Sik Cho

Jong-Yeon Hwang

Cho Young Sik

Ji-Yeon Park

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 relates to a novel pyrrolo[3,2-c]quinoline derivatives containing haloalkoxy group, represented by Formula I, their pharmaceutically acceptable salts; process for preparation thereof; and pharmaceutical composition thereof for treating gastric ulcer. ##STR1## in which R.sub.1 is haloalkoxy group of C.sub.1 -C.sub.6 including trifluoromethoxy, difluoromethoxy and trifluoroethoxy group.

Pyrrolo [3,2-c] quinoline derivatives containing haloalkoxy group and

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Daejeon, South Korea

Hyae-Gyeong Cheon