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7 条记录 (耗时 0.018 秒)

    Derivatives of bicyclic lactols
    1.
    发明授权
    Derivatives of bicyclic lactols 失效
    双环乳糖的衍生物

    公开(公告)号：US4257962A

    公开(公告)日：1981-03-24

    申请号：US942819

    申请日：1978-09-15

    申请人： Tibor Szabo ,  Laszlo Institoris ,  Gabor Kovacs ,  Gyula Dalmadi ,  Bela Koszegi ,  Istvan Stadler

    发明人： Tibor Szabo ,  Laszlo Institoris ,  Gabor Kovacs ,  Gyula Dalmadi ,  Bela Koszegi ,  Istvan Stadler

    IPC分类号： C07C405/00 ,  A61K31/34 ,  A61K31/343 ,  A61P7/02 ,  A61P25/02 ,  A61P35/00 ,  C07D307/935

    CPC分类号： C07D307/935

    摘要： Racemic or optically active compounds with antitumor activity of the formula: ##STR1## wherein X is oxygen or sulfur;R.sup.1 is hydrogen, C.sub.1 to C.sub.4 alkanoyl, benzoyl or phenyl-substituted benzoyl;R.sup.2 is hydrogen or C.sub.1 to C.sub.4 alkanoyl;R.sup.3 is C.sub.2 to C.sub.40 straight or branched chain alkyl substituted by hydroxy, epoxy, amino, C.sub.1 to C.sub.6 alkylamino, C.sub.1 to C.sub.6 dialkylamino, C.sub.1 to C.sub.6 alkanoyloxy or, C.sub.1 to C.sub.4 alkoxycarbonyl; cyclohexyl, phenyl unsubstituted or substituted by halogen, amino, C.sub.1 to C.sub.4 alkyl-substituted amino, C.sub.1 to C.sub.4 alkoxy, nitro, or hydroxy; C.sub.1 to C.sub.6 alkanoyl; allyl or phenyl-C.sub.1 to C.sub.4 alkyl unsubstituted or substituted by a C.sub.2 to C.sub.6 alkene group; or where X is sulfur R.sup.3 is as defined above or is C.sub.1 to C.sub.40 straight or branched chain alkyl; and.about. represents the exo- or endo-steric position in the ring and indicates an .alpha.- or .beta.-steric position in the side chain are disclosed.

    摘要翻译： 具有下式的抗肿瘤活性的外消旋或光学活性化合物：其中X是氧或硫; R1是氢，C1至C4烷酰基，苯甲酰基或苯基取代的苯甲酰基; R2是氢或C1-C4烷酰基; R3为C2至C40被羟基，环氧基，氨基，C1至C6烷基氨基，C1至C6二烷基氨基，C1至C6烷酰氧基或C1至C4烷氧基羰基取代的直链或支链烷基; 环己基，未取代或被卤素取代的苯基，氨基，C1至C4烷基取代的氨基，C1至C4烷氧基，硝基或羟基; C1至C6烷酰基; 烯丙基或未被取代或被C2至C6烯基取代的苯基-C1至C4烷基; 或其中X为硫的R 3如上所定义或为C 1至C 40直链或支链烷基; 而DIFFERENCE表示环中的外 - 或内 - 立体位置，并且表示侧链中的α或β-甾族位置。

    Cytostatic terminally bifunctional sugar alcohols process for preparing them and pharmaceutical compositions containing them
    4.
    发明授权
    Cytostatic terminally bifunctional sugar alcohols process for preparing them and pharmaceutical compositions containing them 失效
    用于制备它们的细胞静止末端双功能糖醇方法和含有它们的药物组合物

    公开(公告)号：US4337266A

    公开(公告)日：1982-06-29

    申请号：US177948

    申请日：1980-08-14

    申请人： Sandor Vidra nee Ildiko ,  Laszlo Institoris

    发明人： Sandor Vidra nee Ildiko ,  Laszlo Institoris

    IPC分类号： C07C43/13 ,  C07D303/22 ,  A61K31/335

    CPC分类号： C07D303/22 ,  C07C43/137

    摘要： The invention relates to novel anticarcinogenic compounds of formula I, ##STR1## wherein R.sup.1 is halogenR.sup.2 is hydroxy orR.sup.1 and R.sup.2 together form an oxygen bridge,R.sup.3 is methyl,R.sup.4 is hydrogen, methyl or acyl,n is 1 or zero, with the provisos, that in case n is 1 the steric positions of --R.sup.2, OR.sup.3 and --OR.sup.4 groups correspond to dulcitol, mannitol or sorbitol configurations independently of their actual meanings, in case n is zero the steric positions of --R.sup.2 and --OR.sup.3 groups correspond to xylitol configuration independently of their actual meanings.The novel compounds can be used as antitumor agents in themselves or formulated as pharmaceutical preparations.

    摘要翻译： 本发明涉及式I的新型抗致癌化合物，其中R1是卤素，R2是羟基或R1和R2一起形成氧桥，R3是甲基，R4是氢，甲基或酰基，n是1或 零，条件是，在n为1的情况下，-R2，OR3和-OR4基团的空间位置对应于其实际意义上独立于曲古醇，甘露糖醇或山梨糖醇构型，n为零时-R2的空间位置和 -OR3组对应于木糖醇构型，独立于其实际含义。 该化合物本身可用作抗肿瘤剂或配制成药物制剂。

    Hexitols containing free carboxy groups and a process for the preparation thereof
    7.
    发明授权
    Hexitols containing free carboxy groups and a process for the preparation thereof 失效
    含有游离羧基的己糖醇及其制备方法

    公开(公告)号：US4419522A

    公开(公告)日：1983-12-06

    申请号：US315182

    申请日：1981-10-26

    申请人： Ilona Elekes ,  Laszlo Institoris ,  Kalman Medzihradsz ,  Laszlo tvos ,  Hedvig Medzihradszky-Schweiger ,  Katalin De Gleria ,  Janos Sugar ,  Somfai Relle ,  Sandor Eckhardt ,  Ivan Hidy ,  Sandor Kerpel-Fronius

    发明人： Ilona Elekes ,  Laszlo Institoris ,  Kalman Medzihradsz ,  Laszlo tvos ,  Hedvig Medzihradszky-Schweiger ,  Katalin De Gleria ,  Janos Sugar ,  Somfai Relle ,  Sandor Eckhardt ,  Ivan Hidy ,  Sandor Kerpel-Fronius

    IPC分类号： C07C69/003 ,  A61K31/22 ,  A61K31/225 ,  A61K31/335 ,  A61K31/336 ,  A61P35/00 ,  A61P35/02 ,  C07D303/16 ,  C07D407/12 ,  C07C69/63 ,  C07C69/635 ,  C07C69/65 ,  C07C69/653 ,  C07C69/657

    CPC分类号： C07D303/16

    摘要： The invention relates to new hexitols having the general formula (I) and (II), ##STR1## wherein the hexitol skeleton is dulcitol, mannitol or iditol,X represents halogen, preferably bromine,R is a saturated or unsaturated C.sub.4-10 alkylcarbonyl group which also contains a free carboxy group, andR.sup.1 is hydrogen, a saturated or unsaturated C.sub.4-10 alkylcarbonyl group which also contains a free carboxy group, a saturated or unsaturated C.sub.2-10 alkylcarbonyl group, a saturated or unsaturated C.sub.4-10 alkylcarbonyl group which also contains an alkoxycarbonyl group, or a saturated or unsaturated C.sub.8-10 aralkylcarbonyl group,and salts of these compounds. The new compounds according to the invention have tumor-inhibiting affects.The above compounds are prepared according to the invention so that(a) a compound of the general formula (IX), whereinthe hexitol skeleton is dulcitol, mannitol or iditol,Q is a saturated or unsaturated C.sub.11-17 alkylcarbonyl group which also contains a benzyloxycarbonyl group, andQ.sup.1 is hydrogen, a saturated or unsaturated C.sub.2-10 alkylcarbonyl group, a saturated or unsaturated C.sub.4-10 alkylcarbonyl group which also contains an alkoxycarbonyl group, a saturated or unsaturated C.sub.11-17 alkylcarbonyl group which also contains a benzyloxycarbonyl group, or a saturated or unsaturated C.sub.8-10 aralkylcarbonyl group, is hydrogenated in an anhydrous solvent in the presence of a weakly active catalyst which does not affect the epoxide ring, or(b) a 1,2-5,6-dianhydrohexitol of the general formula (X), wherein the hexitol skeleton is dulcitol, mannitol or iditol, is reacted with a dicarboxylic acid anhydride of the general formula (XI), wherein A is a C.sub.2-10 alkyl, aralkyl or aryl group, or(c) a compound of the general formula (I) is reacted with an alkali halide and/or hydrogen halide. ##STR2##

    摘要翻译： 本发明涉及具有通式（I）和（II）的新己二醇，其中己糖醇骨架是杜尔醇醇，甘露糖醇或甘油，X代表卤素，优选溴，R是饱和或不饱和的C 4-10烷基羰基 其还含有游离的羧基，并且R 1是氢，也含有游离羧基，饱和或不饱和的C 2-10烷基羰基的饱和或不饱和C 4-10烷基羰基，饱和或不饱和的C 4-10烷基羰基， 还含有烷氧基羰基，或饱和或不饱和的C 8-10芳烷基羰基，以及这些化合物的盐。 根据本发明的新化合物具有肿瘤抑制作用。 根据本发明制备上述化合物，使得（a）通式（Ⅸ）的化合物，其中己糖醇骨架是二糖醇，甘露糖醇或甘露糖醇，Q是饱和或不饱和的C 11-17烷基羰基，其还含有 苄氧基羰基，Q 1为氢，饱和或不饱和的C 2-10烷基羰基，饱和或不饱和的还含有烷氧基羰基的C 4-10烷基羰基，也含有苄氧基羰基的饱和或不饱和C 11-17烷基羰基， 或饱和或不饱和的C 8-10芳烷基羰基在无影响环氧化物环的弱活性催化剂的存在下，在无水溶剂中氢化，或（b）一般的1,2-5,6-二脱水己糖醇 式（X）其中己糖醇骨架是杜尔醇醇，甘露糖醇或甘油，与通式（XI）的二羧酸酐反应，其中A是C 2-10烷基，芳烷基或芳基，或（c） 组合 和通式（I）的化合物与碱金属卤化物和/或卤化氢反应。