Self-reactive arms and prodrugs comprising same
    4.
    发明授权
    Self-reactive arms and prodrugs comprising same 有权
    包含它们的自反应性臂和前体药物

    公开(公告)号:US09000135B2

    公开(公告)日:2015-04-07

    申请号:US13699173

    申请日:2011-05-18

    摘要: The present invention relates to a compound of general formula (I): in which: X is OH, NH2, NHOH or RNH, where R may be a linear or branched, saturated or unsaturated, C1-C10 alkyl radical, Y is H, or an electron-withdrawing group, in particular selected from NO2, CF3 or a halogen, R1 and R2 are H or a linear or branched, saturated or unsaturated, C1-C10 alkyl radical, F is a reactive functional group that can be activated by click chemistry.

    摘要翻译: 本发明涉及通式(I)的化合物:其中:X是OH,NH2,NHOH或RNH,其中R可以是直链或支链饱和或不饱和的C1-C10烷基,Y是H, 或吸电子基团,特别是选自NO 2,CF 3或卤素,R 1和R 2是H或直链或支链,饱和或不饱和的C 1 -C 10烷基,F是可以被 点击化学。

    Process for preparation of a nitrophenol
    6.
    发明申请
    Process for preparation of a nitrophenol 审中-公开
    硝基苯酚的制备方法

    公开(公告)号:US20050256343A1

    公开(公告)日:2005-11-17

    申请号:US10520725

    申请日:2003-07-09

    CPC分类号: C07C201/16 C07C205/22

    摘要: The invention relates to a method of preparing a high-purity nitrophenol and, more specifically, p-nitrophenol from a nitrohalobenzene. The inventive method comprises the following steps: (a) hydrolysis of a nitrohalobenzene compound by reacting said compound with a base; (b) acidification in order to produce the nitrophenol compound from the salt thereof by means of an acid treatment; (c) crystallisation of the nitrophenol compound obtained; and (d) separation of the product obtained. The invention is characterised in that it also comprises at least the following steps: (e) concentration of the reaction medium after hydrolysis (a) and before acidification (b); and (f) liquid/liquid decantation after acidification (b) and before crystallisation (c), which is intended to eliminate the water phase obtained after acidification (b).

    摘要翻译: 本发明涉及一种从硝基卤苯制备高纯度硝基苯酚,更具体地说是对硝基苯酚的方法。 本发明的方法包括以下步骤:(a)通过使所述化合物与碱反应来水解硝基卤苯化合物; (b)酸化以通过酸处理从其盐生产硝基苯酚化合物; (c)获得的硝基苯酚化合物的结晶; 和(d)所得产物的分离。 本发明的特征在于其还包括至少以下步骤:(e)水解(a)和酸化(b)之前浓缩反应介质; 和(f)在酸化(b)和结晶(c)之前的液体/液体倾析,其旨在消除酸化后获得的水相(b)。

    Use of natural products and related synthetic compounds for the
treatment of cardiovascular disease
    9.
    发明授权
    Use of natural products and related synthetic compounds for the treatment of cardiovascular disease 失效
    使用天然产物和相关合成化合物治疗心血管疾病

    公开(公告)号:US5859067A

    公开(公告)日:1999-01-12

    申请号:US969145

    申请日:1997-11-12

    摘要: Use of a compound of formula (I), wherein Ar is an aromatic ring system comprising one or more optionally substituted phenyl rings optionally linked to or fused with one or more other optionally substituted phenyl rings or one or more 5 or 6-membered, optionally substituted heterocyclic rings wherein the heteroatom is oxygen; and wherein the ring system comprises 1-4 phenyl rings and wherein Ar can be linked to another Ar via a group X wherein the Ar is independently selected; where X is optionally substituted C.sub.1-20 alkylene, C.sub.2-20 alkenylene or C.sub.2-20 alkynylene; R is hydrogen; C.sub.1-20 alkenyl, C.sub.2-20 alkynyl, C.sub.2-20 alkanoyl, C.sub.2-20 alkynoyl, each of which can be optionally substituted; R.sub.1 is independently selected and is hydrogen; optionally substituted C.sub.1-12 alkyl, C.sub.2-12 alkenyl, C.sub.2-12 alkynyl; --COOR'--NR'R', halogen, --OR', --COR', --CONR'R', .dbd.O, --SR', --SO.sub.3 R', --SO.sub.2 NR'R', --SOR', --SO.sub.2 R', --NO.sub.2, --CN, glycoside, silyl; where R' is independently hyrogen; alkyl, alkenyl or akynyl each optionally substituted; and where two groups R.sub.1 can be joined; wherein the optional substituents are one or more independently selected from C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl; --COOR"--NR"R", halogen, OR", --COR", --CONR"R", --SR", .dbd.O, --SO.sub.3 R", --SO.sub.2 NR"R", --SOR", --SO.sub.2 ", --NO.sub.2, --CN; wherein R" is independently hydrogen, alkyl, alkenyl, or alkynyl; n=1, 2 or 3; m=1, 2, 3 or 4; or a pharmaceutically acceptable derivative thereof in the manufacture of a medicament for inhibiting the action of Ca.sup.2+ -ATPase enzymes. Certain compounds of formula (I) and 8-lavandulyl flavone pharmaceutical formulations are new.

    摘要翻译: 使用式(I)化合物,其中Ar是包含一个或多个任选取代的苯环的芳环体系,其任选地与一个或多个其它任选取代的苯环或一个或多个5或6元任意连接或稠合,任选地 取代的杂环,其中杂原子是氧; 并且其中所述环系统包含1-4个苯环,并且其中Ar可以经由独立选择Ar的基团X连接到另一个Ar; 其中X是任选取代的C 1-20亚烷基,C 2-20亚烯基或C 2-20炔基; R是氢; C 1-20烯基,C 2-20炔基,C 2-20烷酰基,C 2-20炔酰基,其各自可以任选被取代; R1独立地选择并且是氢; 任选取代的C 1-12烷基,C 2-12烯基,C 2-12炔基; -COOR'-NR'R',卤素-OR',-COR',-CONR'R',= O,-SR',-SO3R',-SO2NR'R',-SOR',-SO2R' -NO 2,-CN,糖苷,甲硅烷基; 其中R'独立地是氢; 烷基,烯基或炔基,各自任选取代; 并且可以连接两个基团R1; 其中任选的取代基是一个或多个独立地选自C 1-10烷基,C 2-10烯基,C 2-10炔基; -COOR“ - NR''R”,卤素,OR“,-COR”,-CONR''R“,-SR”,= O,-SO3R“,-SO2NR''R' ,-SOR“,-SO 2”,-NO 2,-CN; 其中R“独立地是氢,烷基,烯基或炔基; n = 1,2或3; m = 1,2,3或4; 或其药学上可接受的衍生物在制备用于抑制Ca2 + -ATP酶的作用的药物中的用途。 某些式(I)化合物和8-大茴香黄酮药物制剂是新的。