COLCHICINE DERIVATIVES, THE USE THEREOF AND FORMULATIONS CONTAINING THEM
    1.
    发明申请
    COLCHICINE DERIVATIVES, THE USE THEREOF AND FORMULATIONS CONTAINING THEM 审中-公开
    化合物衍生物,其使用和含有它们的制剂

    公开(公告)号:WO1997001570A1

    公开(公告)日:1997-01-16

    申请号:PCT/EP1996002718

    申请日:1996-06-21

    发明人: INDENA S.P.A.

    IPC分类号: C07H15/248

    摘要: The present invention relates to novel colchicine derivatives having antiproliferative, antineoplastic, anti-inflammatory and muscle relaxant activities; said derivatives include novel colchine nitrogen amides for use either as such or after derivatization of the hydroxyl at C3 of the aromatic ring and at C10 of the tropolone ring. These novel compounds have a cytotoxicity on human tumoral cell lines comparable with colchicine but, in comparison with the latter, they are much more active on cells resistant to the usual antiblastics. The compounds can be included in pharmaceutical formulations useful for the intravenous, oral and topical administrations.

    摘要翻译: 本发明涉及具有抗增殖,抗肿瘤,抗炎和肌肉松弛活性的新型秋水仙素衍生物; 所述衍生物包括用于本发明或在芳环的C 3的羟基衍生化和在氯普罗酮环的C 10之间使用的新型胆碱氮酰胺。 这些新型化合物对与秋水仙素相当的人肿瘤细胞系具有细胞毒性,但与后者相比,它们对通常抗生素耐药性的细胞活性更高。 该化合物可以包含在用于静脉内,口服和局部给药的药物制剂中。

    PROCESS FOR EXTRACTION OF NON TOXIC HIGH PURITY COLCHICOSIDE FROM GLORIOSA SUPERBA AND EXTRACT THEREOF

    公开(公告)号:WO2023031948A1

    公开(公告)日:2023-03-09

    申请号:PCT/IN2022/050151

    申请日:2022-02-21

    申请人: GOEL, Pawan Kumar

    IPC分类号: A61K36/00 C07H15/248

    摘要: Present invention discloses a novel process for extraction of non-toxic, high purity colchicoside from Gloriosa superba and extract thereof. Present invention utilizes a novel non-chromatographic, simple and less timing consuming process. The process disclosed in present invention involve extraction of G. superba seeds using methanol, isolation of colchicine using non-polar solvent chloroform, isolation of colchicoside using n-butanol, removal of N-formyl impurity from colchicoside by using acid catalyst optimally hydroxylamine hydrochloride in methanol with traces of water optimally 1% water and further NMR spectroscopic analysis to detect the presence or absence of N-formyl impurity within the extracted pure product. By employing the method of present invention colchicoside of >90% purity is obtained.

    COLCHICINE NEOGLYCOSIDES AND METHODS FOR THEIR SYNTHESIS AND USE
    3.
    发明申请
    COLCHICINE NEOGLYCOSIDES AND METHODS FOR THEIR SYNTHESIS AND USE 审中-公开
    蛇毒神经鞘苷及其合成和使用方法

    公开(公告)号:WO2008067039A2

    公开(公告)日:2008-06-05

    申请号:PCT/US2007080696

    申请日:2007-10-08

    摘要: Colchicine neoglycosides, method for their synthesis and methods for their use are disclosed. The invention provides analogs of colchicine glycosylated to include a sugar moiety on a colchicine scaffold that is generally unglycosylated in nature. The colchicine neoglycosides disclosed herein are shown to have cytotoxic effects equivalent to at least the known cytotoxins paclitaxel and doxorubicin. Further, the neoglycosides disclosed according to the invention have physiologic effects not previously recognized in the alkaloid family that includes colchicine but recognized in other cytotoxic drug families such as the taxanes which act by stabilizing tubulin formation.

    摘要翻译: 公开了秋水仙碱新糖苷,其合成方法及其使用方法。 本发明提供了糖基化的秋水仙碱类似物,其包含在秋水仙碱支架上包含糖部分,其本质上通常是非糖基化的。 显示本文公开的秋水仙碱新糖苷具有与至少已知的细胞毒素紫杉醇和多柔比星相当的细胞毒性作用。 此外,根据本发明公开的新糖苷类具有以前在生物碱家族中未曾认识到的生理作用,其包括秋水仙碱,但在其他细胞毒药物家族例如通过稳定微管蛋白形成起作用的紫杉烷类中被识别。

    COLCHICINE NEOGLYCOSIDES AND METHODS FOR THEIR SYNTHESIS AND USE

    公开(公告)号:WO2008067039A3

    公开(公告)日:2008-06-05

    申请号:PCT/US2007/080696

    申请日:2007-10-08

    摘要: Colchicine neoglycosides, method for their synthesis and methods for their use are disclosed. The invention provides analogs of colchicine glycosylated to include a sugar moiety on a colchicine scaffold that is generally unglycosylated in nature. The colchicine neoglycosides disclosed herein are shown to have cytotoxic effects equivalent to at least the known cytotoxins paclitaxel and doxorubicin. Further, the neoglycosides disclosed according to the invention have physiologic effects not previously recognized in the alkaloid family that includes colchicine but recognized in other cytotoxic drug families such as the taxanes which act by stabilizing tubulin formation.

    COLCHICOSIDE ANALOGUES
    7.
    发明申请
    COLCHICOSIDE ANALOGUES 审中-公开
    化合物类似物

    公开(公告)号:WO2004111068A1

    公开(公告)日:2004-12-23

    申请号:PCT/EP2004/005645

    申请日:2004-05-26

    IPC分类号: C07H15/248

    CPC分类号: C07H15/248

    摘要: The present invention relates to colchicine derivatives, in particular to the 3-demethyl and 3-demethylthio-colchicine of the general formula (I) in which X is oxygen or sulfur, a method for the preparation thereof and pharmaceutical compositions containing them. The compounds of formula (I) have muscle relaxing, anti-inflammatory and anti-gout activity.

    摘要翻译: 本发明涉及秋水仙素衍生物,特别涉及其中X为氧或硫的通式(I)的3-去甲基和3-脱甲基硫代秋水仙碱,其制备方法和含有它们的药物组合物。 式(I)化合物具有肌肉松弛,抗炎和抗痛风活性。

    COLCHINOL DERIVATIVES AS VASCULAR DAMAGING AGENTS
    8.
    发明申请
    COLCHINOL DERIVATIVES AS VASCULAR DAMAGING AGENTS 审中-公开
    COLCHINOL衍生物作为血管破坏剂

    公开(公告)号:WO00040529A1

    公开(公告)日:2000-07-13

    申请号:PCT/GB1999/004436

    申请日:1999-12-24

    CPC分类号: A61K31/165

    摘要: The invention relates to the use of compounds of formula (I): wherein X is -C(O)-, -C(S)-, -C=NOH, or -CH(R )- wherein R is hydrogen, hydroxy, C1-7alkoxy, -OR or -NR R (wherein R is a group -Y R (wherein Y is a direct bond, -C(O)-, -C(S)-, -S-, -C(O)O, -C(O)NR -, -SO2- or -SO2NR - (wherein R and R , which may be the same or different, each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl) and R is as defined herein, and R includes hydrogen; R , R and R are as defined herein and are preferably methyl; R , R and R are as defined herein with the proviso that R is not hydroxy, alkoxy, substituted alkoxy, -OPO3H2, -O-C1-7alkanoyl or benzyloxy; and salts thereof in the manufacture of a medicament for use in the production of a vascular damaging effect in warm-blooded animals such as humans. The present invention further relates to compounds of the formula (I), pharmaceutical compositions containing them, processes for their preparation and to a method of treatment using the compounds to produce a vascular damaging effect in a warm-blooded animal such as a human. The compounds of formula (I) and the pharmaceutically acceptable salts thereof may be useful in the treatment of a number of disease states including cancer and rheumatoid arthritis.

    摘要翻译: 本发明涉及式(I)化合物的用途:其中X是-C(O) - , - C(S) - , - C = NOH或-CH(R 7) - ,其中R 7 >是氢,羟基,C 1-7烷氧基,-OR 8或-NR 8 R 9(其中R 8是基团-Y 1 R 10(其中Y 1是 -C(O) - , - C(O)O,-C(O)NR 11 - , - SO 2 - 或-SO 2 NR 12 - (其中R 11和R 12可以相同或不同,各自独立地表示氢,C 1-3烷基或C 1-3烷氧基C 2-3 - 烷基),R 10如本文所定义,R 9, 包括氢; R 1,R 2和R 3如本文所定义,并且优选为甲基; R 4,R 5和R 6如本文所定义,条件是R“ 5>不是羟基,烷氧基,取代的烷氧基,-OPO 3 H 2,-O-C 1-7烷酰基或苄氧基;及其盐在制备用于在温血动物如人中产生血管损伤作用的药物 本发明还涉及式(I)的化合物,含有它们的药物组合物, 以及使用该化合物在温血动物如人中产生血管损伤作用的治疗方法。 式(I)化合物及其药学上可接受的盐可用于治疗许多疾病状态,包括癌症和类风湿性关节炎。