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2. 发明申请

WO2006006933A2 NEW COMPOSITIONS 审中-公开
标题翻译：新组合
公开(公告)号：WO2006006933A2
公开(公告)日：2006-01-19
申请号：PCT/SE2005/001152
申请日：2005-07-14
申请人： GLUCOGENE MEDICAL HFM AB , ELLERVIK, Ulf , FRANSSON, Lars-Åke , BELTING, Mattias, Nils, Henry , MANI, Katrin
发明人： ELLERVIK, Ulf , FRANSSON, Lars-Åke , BELTING, Mattias, Nils, Henry , MANI, Katrin
IPC分类号： A61K31/7028 , A61K45/06 , C07H20060101
CPC分类号： A61K45/06 , A61K31/7028 , A61K2300/00
摘要： The invention relates to the use of compounds for the preparation of a pharmaceutical composition comprising a) at least one compound having the general formula I: wherein R1 groups are same or different and independently selected from N-Y1Y2 or O-Y; Y, Y1 and Y2 are independently selected from H, alkyl, C(O)aryl, CH2aryl, C(O)alkyl, C(O)Oalkyl, C(O)Oalkenyl, where the alkyl and alkenyl groups have 1-100 carbon atoms and the aryl group has 6-100 carbon atoms; the C(O)Oalkyl and C(O)Oalkenyl includes preferentially all acyls from acetyl (2 carbon atoms) to eicosatetranoyl (20 carbon atoms) with or without single or multiple double bonds in all positions, or R2 is or R2 is A is O, S, NH or CH2; B is selected from naphthyl, naphthylalkyl, anthracenyl, antracenylalkyl or biphenyl, substituted with one or more substituents that are independently selected from F, Cl, Br, I, NO2, CF3, COOH, N-Y1Y2 or O-Y; Y, Y1 and Y2 are independently selected from H, alkyl, C(O)aryl, CH2aryl, C(O)alkyl, C(O)Oalkyl, where the alkyl group has 1-100 carbon atoms and the aryl group has 6-100 carbon atoms; and pharmaceutically acceptable salts thereof, in combination with b) non-xylose compounds chosen from at least one polyamine synthesis inhibitor; and at least one nitric oxide donor or stimulator of nitric oxide synthesis or inducer of nitric oxide release from S-nitrosothiols; and optionally also at least at least one anti-tumor agent selected from the group consisting growth factor-receptor interaction inhibitor or heparanase inhibitor and/or cholesterol traffic inhibitors and/or from the group of inducer of epoxygenase and/or inhibitor of topoisomerase and/or cyanide-donor and/or selene-containing compounds; said combinations of compound(s) a) and agents b) being selected such that a synergistic cytotoxisk proliferative effect is accomplished. Some of the compounds with formula (I) are new and the invention also relates to the new compounds as such and compositions comprising them.
摘要翻译：本发明涉及化合物用于制备药物组合物的用途，其包含a）至少一种具有通式I的化合物：其中R1基团相同或不同并且独立地选自N-Y1Y2或O-Y; Y，Y 1和Y 2独立地选自H，烷基，C（O）芳基，CH 2芳基，C（O）烷基，C（O）O烷基，C（O）O链烯基，其中烷基和烯基具有1-100碳原子和芳基具有6-100个碳原子; C（O）O烷基和C（O）O链烯基优先包括在所有位置具有或不具有单个或多个双键的乙酰基（2个碳原子）至二十碳四烯酰基（20个碳原子）的所有酰基，或者R2是或R2是A是 O，S，NH或CH 2; B选自由一个或多个独立地选自F，Cl，Br，I，NO 2，CF 3，COOH，N-Y 1 Y 2或O-Y的取代基取代的萘基，萘基烷基，蒽基，蒽基烷基或联苯基; Y，Y 1和Y 2独立地选自H，烷基，C（O）芳基，CH 2芳基，C（O）烷基，C（O）O烷基，其中烷基具有1-100个碳原子， 100个碳原子; 和b）非木糖化合物的组合，所述非木糖化合物选自至少一种多胺合成抑制剂; 和至少一种一氧化氮供体或一氧化氮合成的刺激剂或一氧化氮从S-亚硝基硫醇中释放的诱导剂; 和任选地至少一种选自生长因子 - 受体相互作用抑制剂或乙酰肝素酶抑制剂和/或胆固醇交通抑制剂和/或来自环氧化酶诱导剂和/或拓扑异构酶抑制剂的组的至少一种抗肿瘤剂和/ 或氰化物供体和/或含烯内酯的化合物; 化合物a）和试剂b）的组合被选择为使得可以实现协同细胞毒素增殖作用。一些具有式（I）的化合物是新的，本发明还涉及新的化合物，以及包含它们的组合物。

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