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24 条记录 (耗时 0.025 秒)

    Imidazole derivatives and processes for the preparation thereof
    7.
    发明授权
    Imidazole derivatives and processes for the preparation thereof 失效
    咪唑衍生物及其制备方法

    公开(公告)号：US5665738A

    公开(公告)日：1997-09-09

    申请号：US737563

    申请日：1996-11-13

    申请人： Sung-Eun Yoo ,  Kyu-Yang Yi ,  Sang-Hee Lee ,  Hye-Ryung Kim ,  Jee-Hee Suh ,  Nak-Jeong Kim ,  Seon-Ju Kim ,  Ok-Ja Cha ,  Young-Ah Shin ,  Wha-Sup Shin ,  Sung-Hou Lee ,  Yi-Sook Jung ,  Byung-Ho Lee ,  Ho-Won Seo ,  Hye-Suk Lee

    发明人： Sung-Eun Yoo ,  Kyu-Yang Yi ,  Sang-Hee Lee ,  Hye-Ryung Kim ,  Jee-Hee Suh ,  Nak-Jeong Kim ,  Seon-Ju Kim ,  Ok-Ja Cha ,  Young-Ah Shin ,  Wha-Sup Shin ,  Sung-Hou Lee ,  Yi-Sook Jung ,  Byung-Ho Lee ,  Ho-Won Seo ,  Hye-Suk Lee

    IPC分类号： A61K31/44 ,  A61K31/4427 ,  A61P9/12 ,  A61P43/00 ,  C07D401/14 ,  A61K31/415 ,  C07D403/14

    CPC分类号： C07D401/14

    摘要： Novel imidazole derivatives of formula(I) inhibit effectively the action of angiotensin II and have a superior antihypertensive activity: ##STR1## wherein: A is a straight, branched or cyclic C.sub.1 -C.sub.6 alkyl group, or OR.sub.1 wherein R.sub.1 is a hydrogen, or a straight, branched or cyclic C.sub.1 -C.sub.6 alkyl radical; B is a halogen, CF.sub.3 or CF.sub.2 CF.sub.3 ; X is N or N-oxide; Y is --CH.sub.2 --, --CH(OR.sub.1)-- wherein R.sub.1 is the same as defined above, or --C(.dbd.O)--; n is 0 or an integer of 1 to 4; Z is a halogen, --OH, --OR.sub.1, --NR.sub.1 R.sub.2, --N(.dbd.O)R.sub.3 R.sub.4, --C(.dbd.O)R.sub.1, --C(.dbd.O)OR.sub.1, --CH(OR.sub.1).sub.2 or --C(.dbd.O)N.sub.1 N.sub.2 wherein R.sub.1 is the same as defined above, R.sub.2 is, independently of R.sub.1, a hydrogen, or a straight, branched or cyclic C.sub.1 -C.sub.6 alkyl radical, and R.sub.3 and R.sub.4 are independently a straight, branched or cyclic C.sub.1 -C.sub.6 alkyl radical; and D is a hydrogen, or a straight, branched or cyclic C.sub.1 -C.sub.6 alkyl radical.

    摘要翻译： PCT No.PCT / KR95 / 00058 Sec。 371日期：1996年11月13日 102（e）1996年11月13日PCT PCT 1995年5月19日PCT公布。 公开号WO95 / 32198 日期：1995年11月30日公式（I）的新型咪唑衍生物有效抑制血管紧张素II的作用并具有优异的抗高血压活性：其中：A是直链，支链或环状的C 1 -C 6烷基，或 OR1，其中R1是氢或直链，支链或环状的C1-C6烷基; B是卤素，CF 3或CF 2 CF 3; X是N或N-氧化物; Y是-CH 2 - ， - CH（OR 1） - ，其中R 1与上述定义相同，或-C（= O） - ; n为0或1〜4的整数， Z是卤素，-OH，-OR1，-NR1R2，-N（= O）R3R4，-C（= O）R1，-C（= O）OR1，-CH（OR1）2或-C ）N1N2其中R1与上述定义相同，R2独立地为R1，氢或直链，支链或环状的C1-C6烷基，R3和R4独立地为直链，支链或环状的C 1 -C 6烷基 激进; 并且D是氢或直链，支链或环状的C 1 -C 6烷基。

    6-alkylamino-2,2′-disubstituted-7,8-disubstituted-2H-1-benzopyran derivatives as 5-lipoxygenase inhibitor
    9.
    发明授权
    6-alkylamino-2,2′-disubstituted-7,8-disubstituted-2H-1-benzopyran derivatives as 5-lipoxygenase inhibitor 失效

    公开(公告)号：US07368575B2

    公开(公告)日：2008-05-06

    申请号：US10970046

    申请日：2004-10-20

    申请人： Young-Dae Gong ,  Hyae-Gyeong Cheon ,  Young-Sik Cho ,  Jin-Soo Seo ,  Jong-Yeon Hwang ,  Ji-Yeon Park ,  Sung-Eun Yoo

    发明人： Young-Dae Gong ,  Hyae-Gyeong Cheon ,  Young-Sik Cho ,  Jin-Soo Seo ,  Jong-Yeon Hwang ,  Ji-Yeon Park ,  Sung-Eun Yoo

    IPC分类号： C07D311/00 ,  C07D405/00

    CPC分类号： C07D311/70 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12

    摘要： 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′-disubstituted-3,4-2H-6-substituted benzopyran resin of formula 4 (Step 3); and synthesizing 2,2′-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′-disubstituted-3,4-2H-6-alkylamino benzopyran derivatives.Consequently, the present invention has developed a new technique for constructing 2,2′-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′-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.