Etoposide analogs and methods of use thereof
    41.
    发明授权
    Etoposide analogs and methods of use thereof 失效
    依托泊苷类似物及其使用方法

    公开(公告)号:US06872841B2

    公开(公告)日:2005-03-29

    申请号:US10349351

    申请日:2003-01-22

    CPC分类号: C07D493/04 C07D497/04

    摘要: Etoposide analogs such as 4′-O-demethyl-4β-[4″-(methyl-L-tyrosine-N-carbonyl)-anilino]-4-desoxy-podophyllotoxin (12) and 4′-O-demethyl-4β-[4″-(methyl-L-tryptophan-N-carbonyl)-anilino]-4-desoxypodophyllotoxin (13) are described, along with pharmaceutical formulations containing the same, methods of use thereof, and intermediates and methods of making the same.

    摘要翻译: 依托泊苷类似物如4'-O-脱甲基-4,4a- [4“ - (甲基-L-酪氨酸-N-羰基) - 苯胺基] -4-脱氧鬼臼毒素(12)和4'-O-脱甲基-4beta - [4“ - (甲基-L-色氨酸-N-羰基) - 苯胺基] -4-脱氧鬼臼毒素(13),以及含有其的药物制剂,其使用方法和中间体以及制备 相同。

    Dibenzonaphthyrones
    42.
    发明申请
    Dibenzonaphthyrones 失效
    二苯并噻吩

    公开(公告)号:US20020095046A1

    公开(公告)日:2002-07-18

    申请号:US09880211

    申请日:2001-06-13

    IPC分类号: C07D497/04

    摘要: Dibenzonaphthyrone of formula (I) 1 wherein A1 and A2 independently of each other are unsubstituted or mono- to tetra-substituted o-C6-C18arylene, with the proviso that formula (I) does not represent a dibenzonaphthyrone of the formula 2 The invention further relates to processes for the preparation thereof, to the use thereof for colouring/pigmenting high-molecular-weight organic material and to substance compositions comprising dibenzonaphthyrones.

    摘要翻译: 式(I)的二苯并萘酮其中A1和A2彼此独立地是未取代的或一至四取代的o-C 6 -C 18亚芳基,条件是式(I)不表示下式的二苯并萘酮本发明还涉及 其制备方法,其用于着色/着色高分子量有机材料的用途以及包含二苯并噻吩的物质组合物。

    Free radicals
    46.
    发明授权
    Free radicals 失效
    自由基

    公开(公告)号:US5530140A

    公开(公告)日:1996-06-25

    申请号:US220522

    申请日:1994-03-31

    摘要: The invention provides novel persistent free radicals useful in Overhauser MRI being triarylmethyl radicals having as at least one aryl group a group of formula ##STR1## (wherein each X which may be the same or different is an oxygen or sulphur atom or a group CO or S(O).sub.n, (where n is 1 to 3) with the proviso that at least one group X is a sulphur atom or a S(O).sub.n group; R.sup.1 is a hydrogen atom or group of formula --M, --XM, --X--Ar.sup.2, or --Ar.sup.2 where M is a water solubilizing group, and Ar.sup.2 represents a 5-10 membered aromatic ring optionally substituted by a water solubilizing group M; and each of the groups R.sup.7, which may be the same or different, is a hydrogen atom, or a hydrocarbon group or a water solubilizing group M, or two groups R.sup.7 together with the atom to which they are bound represent a carbonyl group or a 5 to 8 membered cycloalkylidene, mono- or di-oxacycloalkylidene, mono- or di-azacycloalkylidene or mono- or di-thiacycloalkylidene group optionally with the ring attachment carbon replaced by a silicon atom, and R.sup.7 where it is other than hydrogen, is optionally substituted by a hydroxyl group, an optionally alkoxylated, optionally hydroxylated acyloxy or alkyl group or a water solubilizing group M)). The novel radicals have good stability, long relaxation times and good relaxivity.

    摘要翻译: 本发明提供了在Overhauser MRI中有用的新型持久性自由基,其具有作为至少一个芳基的基团为具有下式的基团的三芳基甲基(其中可以相同或不同的X是氧或硫原子或 基团CO或S(O)n,(其中n为1至3),条件是至少一个基团X为硫原子或S(O)n基团; R 1为氢原子或式-M ,-XM,-X-Ar2或-Ar2,其中M是水溶性基团,Ar2表示任选被水增溶基团M取代的5-10元芳香环;并且各基团R7可以是 相同或不同的是氢原子,或烃基或水溶性基团M,或两个R 7与它们所连接的原子一起代表羰基或5-8元环亚烷基,单 - 或二 - 单环或二氮杂环亚烷基或任选具有环连接c的单 - 或二 - 芳烃被硅原子取代,并且其中不是氢的R 7任选被羟基取代,任选烷氧基化,任选羟基化的酰氧基或烷基或水溶性基团M))。 新型自由基具有良好的稳定性,较长的松弛时间和良好的松弛性。

    Substituted 1H-indazole-3-carboxamides
    49.
    发明授权
    Substituted 1H-indazole-3-carboxamides 失效
    取代的1H-吲唑-3-甲酰胺

    公开(公告)号:US5037844A

    公开(公告)日:1991-08-06

    申请号:US554918

    申请日:1990-07-20

    摘要: The present invention is concerned with compounds of formula 1: ##STR1## wherein R.sub.1 is straight or branched alkyl having 1-4 C-atoms, halogen or cyano;n has the value 0-1;R.sub.2 is hydrogen, (1-6 C)alkyl, (3-6 C)alkenyl, (3-6 C)alkenyl, (3-6 C)cycloalkyl, (3-6 C)cycloalkyl-(1-4 C) alkyl, phenyl, phenyl-(1-3 C)alkyl, COOR.sub.6, COR.sub.6, CONR.sub.6 R.sub.7 or SO.sub.2 --R.sub.6, wherein R.sub.6 and R.sub.7 independently of each other are hydrogen, (1-6 C)alkyl, (3-6 C)cycloalkyl, phenyl or phenyl-(1-4 C)alkyl, wherein the benzene ring is optionally substituted with a methyl group or a halogen atom, with the proviso that R.sub.6 is not hydrogen when R.sub.2 is a group COOR.sub.6 or SO.sub.2 R.sub.6 ;R.sub.3 is hydrogen, straight or branched (1-6 C)alkyl or a phenyl-(1-3 C)alkyl group optionally substituted in the benzene ring; andA is a group of formula 2 or 3 ##STR2## wherein one of the groups R.sub.8, R.sub.9 and R.sub.10 is hydrogen, (1-C)alkyl, (3-6 C)cycloalkyl, (3-4 C)alkenyl or (3-4 C)alkynyl and the two other groups, independently of each other, are hydrogen or (1-4 C)alkyl, and the pharmacologically acceptable acid addition salts thereof, which are pharmaceutically useful as strong and selective antagonists of "neuronal" 5-hydroxy tryptamine (5-HT) receptors.