Benzopyran derivatives substituted with a benzimidazole derviative, pharmaceutically acceptable salts thereof, their preparations and pharmaceutical compositions containing them
    14.
    发明申请
    Benzopyran derivatives substituted with a benzimidazole derviative, pharmaceutically acceptable salts thereof, their preparations and pharmaceutical compositions containing them 失效
    被苯并咪唑衍生物取代的苯并吡喃衍生物,其药学上可接受的盐,其制剂和含有它们的药物组合物

    公开(公告)号:US20060293376A1

    公开(公告)日:2006-12-28

    申请号:US10558020

    申请日:2004-05-28

    IPC分类号: A61K31/4184 C07D405/04

    CPC分类号: C07D405/04 C07D405/14

    摘要: The present invention relates to benzopyran derivatives substituted with a benzimidazole derivative, or pharmaceutically acceptable salts thereof, a preparation method of the same and pharmarceutical compositions containing them. Benzopyran derivatives substituted with a benzimidazole derivative, represented in Formula (1), have the function of protecting heart from ischemia-reperfusion without side effect like vasodilation, so that a pharmaceutical composition containing benzopyran derivatives substituted with a benzimidazole derivative or pharmaceutically acceptable salts thereof of the present invention as an effective ingredient can be effectively used for the protection of tissues influenced by ischemia-reperfusion, for example, for the protection of heart, nervous cells, brain, retinal cells, storage organs, etc. and for the treatment of diseases caused by ischemia-reperfusion.

    摘要翻译: 本发明涉及被苯并咪唑衍生物取代的苯并吡喃衍生物或其药学上可接受的盐,其制备方法和含有它们的药物组合物。 由式(1)表示的苯并咪唑衍生物取代的苯并吡喃衍生物具有保护心脏免于缺血再灌注而无副作用如血管舒张的功能,因此含有苯并咪唑衍生物或其药学上可接受的盐取代的苯并吡喃衍生物的药物组合物 作为有效成分的本发明可以有效地用于保护受缺血再灌注影响的组织,例如用于保护心脏,神经细胞,脑,视网膜细胞,储存器官等,并用于治疗疾病 由缺血再灌注引起。

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

    公开(公告)号:US07368575B2

    公开(公告)日:2008-05-06

    申请号:US10970046

    申请日:2004-10-20

    IPC分类号: C07D311/00 C07D405/00

    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

    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

    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。