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24 条记录 (耗时 0.045 秒)

    Pyridyl imidazole derivatives and processes for the preparation thereof
    12.
    发明授权
    Pyridyl imidazole derivatives and processes for the preparation thereof 失效
    吡啶基咪唑衍生物及其制备方法

    公开(公告)号：US5691348A

    公开(公告)日：1997-11-25

    申请号：US750460

    申请日：1996-12-08

    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： A61K31/435 ,  A61K31/44 ,  A61P9/12 ,  A61P43/00 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： Novel pyridyl 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 or alkenyl group, OR.sup.1 (wherein R.sup.1 is a hydrogen, or a straight, branched or cyclic C.sub.1 -C.sub.6 alkyl or alkenyl radical), or NR.sup.2 R.sup.3 (wherein R.sup.2 and R.sup.3 are independently a hydrogen, or a straight, branched or cyclic C.sub.1 -C.sub.6 alkyl radical); B is a group of the following formula ##STR2## D is a hydrogen; a halogen; a straight, branched or cyclic C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 alkynyl group which is optionally substituted with OH, a C.sub.1 -C.sub.4 alkoxy radical, CO.sub.2 R.sup.1, COR.sup.1, CON(R.sup.1).sub.2 or N(R.sup.1).sub.2, wherein R.sup.1 is the same as defined above; tetrazol-5-yl; a perfluoro-C.sub.1 -C.sub.4 alkyl group; or N(R.sup.1).sub.2, OR.sup.1, CO.sub.2 R.sup.1 or CON(R.sup.1).sub.2, wherein R.sup.1 is the same as defined above; E is a hydrogen; a halogen; a straight or branched C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 alkynyl group which is optionally substituted with OH, a C.sub.1 -C.sub.4 alkoxy radical, CO.sub.2 R.sup.1, COR.sup.1, CON(R.sup.1).sub.2 or N(R.sup.1).sub.2, wherein R.sup.1 is the same as defined above; a perfluoro-C.sub.1 -C.sub.4 alkyl group; NO.sub.2 ; or N(R.sup.1).sub.2 or OR.sup.1, wherein R.sup.1 is the same as defined above; and n is 0 or an integer of 1 to 4.

    摘要翻译： PCT No.PCT / KR95 / 00075 Sec。 371日期1996年12月6日第 102（e）日期1996年12月6日PCT归档1995年6月7日PCT公布。 出版物WO95 / 34564 日期：1995年12月21日新型式（I）吡啶基咪唑衍生物有效抑制血管紧张素II的作用，具有优异的抗高血压活性：d或环状C 1 -C 6烷基或链烯基，OR 1（其中R 1为氢或直链 ，支链或环状的C 1 -C 6烷基或链烯基）或NR 2 R 3（其中R 2和R 3独立地是氢或直链，支链或环状的C 1 -C 6烷基）; B是一组下列公式： D是氢; 卤素 任选被OH，C 1 -C 4烷氧基，CO 2 R 1，COR 1，CON（R 1）2或N（R 1）2取代的直链，支链或环状C 1 -C 6烷基，C 2 -C 6烯基或C 2 -C 6炔基 其中R1与上述相同; 四唑-5-基; 全氟-C 1 -C 4烷基; 或N（R1）2，OR1，CO2R1或CON（R1）2，其中R1与上述定义相同; E是氢; 卤素 任选被OH，C 1 -C 4烷氧基，CO 2 R 1，COR 1，CON（R 1）2或N（R 1）2取代的直链或支链C 1 -C 6烷基，C 2 -C 6烯基或C 2 -C 6炔基，其中 R1与上述定义相同; 全氟-C 1 -C 4烷基; NO2; 或N（R1）2或OR1，其中R1与上述定义相同; n为0或1〜4的整数。

    6-alkylamino-2,2′-disubstituted-7,8-disubstituted-2H-1-benzopyran derivatives as 5-lipoxygenase inhibitor
    17.
    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.

    Spiro-benzopyran derivatives and useful for treating asthma and hypertension
    18.
    发明授权
    Spiro-benzopyran derivatives and useful for treating asthma and hypertension 失效
    螺 - 苯并吡喃衍生物，可用于治疗哮喘和高血压

    公开(公告)号：US5300511A

    公开(公告)日：1994-04-05

    申请号：US887189

    申请日：1992-05-21

    申请人： Sung-Eun Yoo ,  Kyu Y. Yi ,  Nak C. Jeong ,  Jee H. Suh ,  Seon-Ju Kim ,  Hwa-Sup Shin ,  Byung H. Lee ,  Kyu S. Jung

    发明人： Sung-Eun Yoo ,  Kyu Y. Yi ,  Nak C. Jeong ,  Jee H. Suh ,  Seon-Ju Kim ,  Hwa-Sup Shin ,  Byung H. Lee ,  Kyu S. Jung

    IPC分类号： A61K31/35 ,  A61K31/44 ,  A61K31/443 ,  A61K31/4433 ,  A61P9/12 ,  A61P11/00 ,  A61P11/06 ,  A61P11/08 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D471/10

    CPC分类号： C07D405/04 ,  C07D405/14

    摘要： The present invention relates to novel benzopyran derivatives of formula(I) which have exellent effectiveness in the treatment of asthma as well as hypertension. ##STR1## wherein R.sub.1 is --CN, --NO.sub.2, --OCX.sub.1 X.sub.2 X.sub.3, --NH.sub.2, --NHSO.sub.2 R.sup.A, ##STR2## --SO.sub.2 R.sup.C or --SO.sub.2 NR.sup.C R.sup.D wherein X.sub.1, X.sub.2 and X.sub.3 are, each independently, F, Cl or H, except for that X.sub.1, X.sub.2 and X.sub.3 may not be hydrogen atom simulaneously; R.sup.A and R.sup.B are, each independently, a hydrogen atom, or a C.sub.1-6 alkyl group or an optionally substituted phenyl group with a halogen atom, or a straight or branched C.sub.1-3 alkyl group; and R.sup.C and R.sup.D are, each independently, a hydrogen atom or a C.sub.1-6 alkyl group or an optionally substituted phenyl group with a halogen atom, or a straight or branched C.sub.1-3 alkyl group;R.sub.2 is a C.sub.1-4 straight or branched alkyl group;R.sub.3 is a C.sub.1-4 straight or branched alkyl group, ##STR3## wherein R.sup.G and R.sup.H are, each independently, a C.sub.1-6 alkyl group or optionally substituted phenyl group with a halogen atom, or a straight or branched C.sub.1-3 alkyl group, A and B are, each independently, S or O; and Z is a C.sub.1-3 straight or branched alkyl group;X is N or N.fwdarw.O.

    摘要翻译： 本发明涉及式（I）的新型苯并吡喃衍生物，其在治疗哮喘以及高血压方面具有显着的效果。 （*化学结构*）（I）其中R1是-CN，-NO2，-OCX1X2X3，-NH2，-NHSO2RA，（*化学结构*）-SO 2RC或-SO 2 NRCRD，其中X1，X2和X3各自独立地为F ，Cl或H，除了X1，X2和X3可能不是氢原子同时; RA和RB各自独立地为氢原子或具有卤素原子的C 1-6烷基或任选取代的苯基，或直链或支链C 1-3烷基; 和RC和RD各自独立地为氢原子或C 1-6烷基或任选取代的具有卤素原子的苯基，或直链或支链C 1-3烷基; R2是C1-4直链或支链烷基; R3是C1-4直链或支链烷基，（*化学结构*）其中RG和RH各自独立地为C1-6烷基或任选取代的具有卤素原子的苯基，或直链或支链C1- 3个烷基，A和B各自独立地为S或O; Z为直链或支链的C1-3烷基; X是N或N-> O。

    Certain pyridyl-benzopyran derivatives
    20.
    发明授权
    Certain pyridyl-benzopyran derivatives 失效
    某些吡啶基 - 苯并吡喃衍生物

    公开(公告)号：US5493029A

    公开(公告)日：1996-02-20

    申请号：US164392

    申请日：1993-12-09

    申请人： Sung-Eun Yoo ,  Kyu Y. Yi ,  Nak C. Jeong ,  Jee H. Suh ,  Seon-Ju Kim ,  Hwa-Sup Shin ,  Byung H. Lee ,  Kyu S. Jung

    发明人： Sung-Eun Yoo ,  Kyu Y. Yi ,  Nak C. Jeong ,  Jee H. Suh ,  Seon-Ju Kim ,  Hwa-Sup Shin ,  Byung H. Lee ,  Kyu S. Jung

    IPC分类号： A61K31/35 ,  A61K31/44 ,  A61K31/443 ,  A61K31/4433 ,  A61P9/12 ,  A61P11/00 ,  A61P11/06 ,  A61P11/08 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04

    CPC分类号： C07D405/04 ,  C07D405/14

    摘要： The present invention relates to novel benzopyran derivatives of formula (I) which have exellent effectiveness in the treatment of asthma as well as hypertension. ##STR1## wherein: R.sub.1 is --CN, --NO.sub.2, --OCX.sub.1 X.sub.2 X.sub.3, --NH.sub.2, --NHSO.sub.2 R.sup.A, ##STR2## --SO.sub.2 R.sup.C or --SO.sub.2 NR.sup.C R.sup.D wherein X.sub.1, X.sub.2 and X.sub.3 are, each independently, F, Cl or H, except for that X.sub.1, X.sub.2 and X.sub.3 may not be hydrogen atom simulaneously; R.sup.A and R.sup.B are, each independently, a hydrogen atom, or a C.sub.1-6 alkyl group or an optionally substituted phenyl group with a halogen atom, or a straight or branched C.sub.1-3 alkyl group; and R.sup.C and R.sup.D are, each independently, a hydrogen atom or a C.sub.1-6 alkyl group or an optionally substituted phenyl group with a halogen atom, or a straight or branched C.sub.1-3 alkyl group;R.sub.2 is a C.sub.1-4 straight or branched alkyl group;R.sub.3 is a C.sub.1-4 straight or branched alkyl group, ##STR3## wherein R.sup.G and R.sup.H are, each independently, a C.sub.1-6 alkyl group or optionally substituted phenyl group with a halogen atom, or a straight or branched C.sub.1-3 alkyl group, A and B are, each independently, S or O;X is N or N.fwdarw.O;Y is a hydrogen or halogen atom, or an amino, hydroxy, a lower alkoxy or lower alkyl group.

    摘要翻译： 本发明涉及式（I）的新型苯并吡喃衍生物，其在治疗哮喘以及高血压方面具有显着的效果。 （I）其中：R1是-CN，-NO2，-OCX1X2X3，-NH2，-NHSO2RA，-SO2RC或-SO2NRCRD，其中X1，X2和X3各自独立地是F，Cl或H， 除了X1，X2和X3可能不是同时是氢原子; RA和RB各自独立地为氢原子或具有卤素原子的C 1-6烷基或任选取代的苯基，或直链或支链C 1-3烷基; 和RC和RD各自独立地为氢原子或C 1-6烷基或任选取代的具有卤素原子的苯基，或直链或支链C 1-3烷基; R2是C1-4直链或支链烷基; R3是C1-4直链或支链烷基，其中RG和RH各自独立地是C1-6烷基或任选取代的具有卤素原子的苯基，或直链或支链C 1-3烷基 A和B各自独立地为S或O; X是N或N-> O; Y是氢或卤素原子，或氨基，羟基，低级烷氧基或低级烷基。