NOVEL FLUORESCENT DERIVATIVES OF POLYAMINES, METHOD FOR PREPARING SAME AND APPLICATIONS THEREOF AS DIAGNOSIS TOOLS IN THE TREATMENT OF CANCEROUS TUMORS
    22.
    发明申请
    NOVEL FLUORESCENT DERIVATIVES OF POLYAMINES, METHOD FOR PREPARING SAME AND APPLICATIONS THEREOF AS DIAGNOSIS TOOLS IN THE TREATMENT OF CANCEROUS TUMORS 审中-公开
    聚氨酯的新型荧光衍生物,其制备方法及其在治疗癌症肿瘤中的诊断工具的应用

    公开(公告)号:US20100202975A1

    公开(公告)日:2010-08-12

    申请号:US12670611

    申请日:2008-07-28

    IPC分类号: A61K49/00 C07D271/12

    CPC分类号: C07D271/12

    摘要: The invention relates to novel fluorescent derivatives of polyamines having a benzoxadiazole group, to a method for preparing the same and to the use thereof as diagnosis tools for emphasising the polyamine transport system in cancerous cells in order to adapt the treatment thereof, and thus for selecting patients carrying such tumours in order to adapt their treatment. The derivatives are of the formula (I) or a pharmaceutically acceptable salt thereof, in which: R1 is one or more NO2 groups in position 4 or 6, or a SO2Ph, SO2NMe2, SO2NH2 or SO3H group; R2 is hydrogen, C1-6 alkyl, benzyl, a perfluoroalkyl group; the values of a, b, c range from 2 to 5 independently from each other and represent alkylene chains separating the amino groups, and the values of d and e can independently be 0 or 1.

    摘要翻译: 本发明涉及具有苯并恶二唑基团的多胺的新型荧光衍生物,其制备方法及其作为诊断工具,用于强调癌细胞中的多胺转运体系以适应其治疗,从而用于选择 携带这种肿瘤的患者为了适应其治疗。 衍生物具有式(I)化合物或其药学上可接受的盐,其中:R1是位置4或6中的一个或多个NO 2基团,或SO 2 Ph,SO 2 NMe 2,SO 2 NH 2或SO 3 H基团; R2是氢,C1-6烷基,苄基,全氟烷基; a,b,c的值彼此独立地为2至5,并且表示分隔氨基的亚烷基链,d和e的值可以独立地为0或1。

    Novel 3beta-amino azabicyclooctane heteroaromatic amid derivatives preparation method and therapeutic uses thereof
    24.
    发明申请
    Novel 3beta-amino azabicyclooctane heteroaromatic amid derivatives preparation method and therapeutic uses thereof 有权
    新型3β-氨基偶氮二异辛烷杂芳族酰胺衍生物的制备方法及其治疗用途

    公开(公告)号:US20050080085A1

    公开(公告)日:2005-04-14

    申请号:US10494639

    申请日:2002-10-30

    CPC分类号: C07D491/04 C07D495/04

    摘要: The invention concerns compounds of general formula 1, wherein: A, B, D and E represent one or two nitrogen atoms, the others being carbon atoms; X represents a S or, a O, thereby forming a bicyclic fused heteroaromatic, such as thieno[2,3-b]pyridine, furo[2,3-b]pyridine, thieno[3,2-b]pyridine, furo[3,2-b]pyridine, thieno[2,3-b]pyrazine, furo[2,3-b]pyrazine, thieno[2,3-c]pyridine, furo[2,3-c]pyridine, thieno[3,2-c]pyridine and furo[3,2-c]pyridine; R1 represents a linear or branched C1-C6 alkoxy group, a linear or branched C1-C6 alkylthio group; R2 represents a linear, branched, cyclic C2-C8 group, a 2- or 3- thienylmethyl group, or a benzyl group optionally substituted by one or several halogens, F, Cl, Br, I, C1-C4 alkyl, C1-C4 alkoxy, CF3, CN, NO2, OH; and their pharmaceutically acceptable salts. Said compounds are anti-dopaminergic agents.

    摘要翻译: 本发明涉及通式1的化合物,其中:A,B,D和E代表一个或两个氮原子,其余是碳原子; X表示S或O,由此形成双环稠合杂芳族化合物,例如噻吩并[2,3-b]吡啶,呋喃并[2,3-b]吡啶,噻吩并[3,2-b]吡啶,呋喃并[ 3,2-b]吡啶,噻吩并[2,3-b]吡嗪,呋喃并[2,3-b]吡嗪,噻吩并[2,3-c]吡啶,呋喃并[2,3-c]吡啶,噻吩并[ 3,2-c]吡啶和呋喃并[3,2-c]吡啶; R1表示直链或支链C1-C6烷氧基,直链或支链C1-C6烷硫基; R 2表示直链,支链,环状的C 2 -C 8基团,2-或3-噻吩基甲基或任选被一个或多个卤素F,Cl,Br,I,C 1 -C 4烷基,C 1 -C 4 烷氧基,CF 3,CN,NO 2,OH; 及其药学上可接受的盐。 所述化合物是抗多巴胺能药。

    FLUORESCENT DERIVATIVES OF POLYAMINES, METHOD FOR PREPARING SAME AND APPLICATIONS THEREOF AS DIAGNOSIS TOOLS IN THE TREATMENT OF CANCEROUS TUMORS
    28.
    发明申请
    FLUORESCENT DERIVATIVES OF POLYAMINES, METHOD FOR PREPARING SAME AND APPLICATIONS THEREOF AS DIAGNOSIS TOOLS IN THE TREATMENT OF CANCEROUS TUMORS 有权
    聚氨酯的荧光衍生物,其制备方法及其应用于诊断癌症肿瘤中的诊断工具

    公开(公告)号:US20120252059A1

    公开(公告)日:2012-10-04

    申请号:US13493556

    申请日:2012-06-11

    IPC分类号: G01N21/64

    CPC分类号: C07D271/12

    摘要: The invention relates to novel fluorescent derivatives of polyamines having a benzoxadiazole group, to a method for preparing the same and to the use thereof as diagnosis tools for emphasising the polyamine transport system in cancerous cells in order to adapt the treatment thereof, and thus for selecting patients carrying such tumours in order to adapt their treatment. The derivatives are of the formula (I) or a pharmaceutically acceptable salt thereof, in which: R1 is one or more NO2 groups in position 4 or 6, or a SO2Ph, SO2NMe2, SO2NH2 or SO3H group; R2 is hydrogen, C1-6 alkyl, benzyl, a perfluoroalkyl group; the values of a, b, c range from 2 to 5 independently from each other and represent alkylene chains separating the amino groups, and the values of d and e can independently be 0 or 1.

    摘要翻译: 本发明涉及具有苯并恶二唑基团的多胺的新型荧光衍生物,其制备方法及其作为诊断工具,用于强调癌细胞中的多胺转运体系以适应其治疗,从而用于选择 携带这种肿瘤的患者为了适应其治疗。 衍生物具有式(I)化合物或其药学上可接受的盐,其中:R1是位置4或6中的一个或多个NO 2基团,或SO 2 Ph,SO 2 NMe 2,SO 2 NH 2或SO 3 H基团; R2是氢,C1-6烷基,苄基,全氟烷基; a,b,c的值彼此独立地为2至5,并且表示分隔氨基的亚烷基链,d和e的值可以独立地为0或1。

    Method for preparing 4B-amino-4'-demethyl-4-desoxypodophyllotoxin
    30.
    发明申请
    Method for preparing 4B-amino-4'-demethyl-4-desoxypodophyllotoxin 有权
    制备4B-氨基-4'-去甲基-4-脱氧鬼臼毒素的方法

    公开(公告)号:US20110021791A1

    公开(公告)日:2011-01-27

    申请号:US12894684

    申请日:2010-09-30

    IPC分类号: C07D407/10

    CPC分类号: C07D493/04

    摘要: The invention relates to a method for synthesizing 4β-amino-4′-demethyl-4-desoxypodophyllotoxin of formula (1), characterized by comprising the following successive steps: a) reacting, in a pure weak acid or in a mixture consisting of acid, water and of organic solvent, without another solvent, at a temperature higher than the ambient temperature, thiourea with 4β-halogenoacetamido-4′-demethyl-4-desoxypodophyllotoxin, and; b) recovering the 4β-amino-4′-demethyl-4-desoxypodophyllotoxin.

    摘要翻译: 本发明涉及一种合成式(1)的4​​'-二氨基-4'-脱甲基-4-脱氧鬼臼毒素的方法,其特征在于包括以下连续步骤:a)在纯的弱酸或由 酸,水和有机溶剂,没有另一种溶剂,在高于环境温度的温度下,硫脲与4'-卤代乙酰氨基-4'-去甲基-4-脱氧鬼臼毒素,和 b)回收4'-二 - 氨基-4'-去甲基-4-脱氧鬼臼毒素。