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    N.sup.4 -(substituted-oxycarbonyl)-5'-deoxy-5-fluorocytidine compounds, compositions and methods of using same
    1.
    发明授权
    N.sup.4 -(substituted-oxycarbonyl)-5'-deoxy-5-fluorocytidine compounds, compositions and methods of using same 失效
    N4-（取代氧羰基）-5'-脱氧-5-氟胞苷化合物，组合物及其使用方法

    公开(公告)号：US5472949A

    公开(公告)日：1995-12-05

    申请号：US167392

    申请日：1993-12-14

    申请人： Motohiro Arasaki ,  Hideo Ishitsuka ,  Isami Kuruma ,  Masanori Miwa ,  Chikako Murasaki ,  Nobuo Shimma ,  Isao Umeda

    发明人： Motohiro Arasaki ,  Hideo Ishitsuka ,  Isami Kuruma ,  Masanori Miwa ,  Chikako Murasaki ,  Nobuo Shimma ,  Isao Umeda

    IPC分类号： A61K31/70 ,  A61K31/305 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7064 ,  A61K31/7068 ,  A61P35/00 ,  C07D239/00 ,  C07H19/06

    CPC分类号： C07H19/06 ,  Y02P20/55

    摘要： The invention relates to N.sup.4 -(substituted-oxycarbonyl)-5'-deoxy-5-fluorocytidine derivatives which are useful as an agent for treating tumors, pharmaceutical compositions including the same, a method of treating tumors and a method of preparing N.sup.4 -(substituted-oxycarbonyl)-5'-deoxy-5-fluorocytidine derivatives for treating tumors.Compounds of formula (I), ##STR1## wherein R.sup.1 is a saturated or unsaturated, straight or branched hydrocarbon radical wherein the number of carbon atoms in the longest straight chain of this hydrocarbon radical ranges from three to seven, or is a radical of the formula --(CH.sub.2)n--.sup.Y wherein Y is a cyclohexyl radical, a C.sub.1 -C.sub.4 alkoxy radical or a phenyl radical and wherein when Y is a cyclohexyl radical n is an integer from 0 to 4, and when Y is C.sub.1 -C.sub.4 alkoxy radical or a phenyl radical n is an integer from 2 to 4, and R.sup.2 is a hydrogen atom or a radical easily hydrolyzable under physiological conditions,or a hydrate or solvate thereof. Compounds of formula (I) are useful in the treatment of tumors.

    摘要翻译： 本发明涉及可用作治疗肿瘤的药物的N4-（取代 - 氧代羰基）-5'-脱氧-5-氟胞苷衍生物，包含其的药物组合物，治疗肿瘤的方法和制备N4-（ 取代氧羰基）-5'-脱氧-5-氟胞苷衍生物用于治疗肿瘤。 式（I）化合物，其中R1是饱和或不饱和的直链或支链烃基，其中该烃基的最长直链中的碳原子数范围为3-7，或者是 基团 - （CH 2）n Y其中Y是环己基，C 1 -C 4烷氧基或苯基，并且其中当Y是环己基时，n是0-4的整数，当Y是C 1 -C 4 烷氧基或苯基n是2〜4的整数，R2是氢原子或在生理条件下易水解的基团，或其水合物或溶剂合物。 式（I）化合物可用于治疗肿瘤。

    Fluorocytidine derivatives
    2.
    发明授权
    Fluorocytidine derivatives 失效
    氟胞嘧啶衍生物

    公开(公告)号：US4966891A

    公开(公告)日：1990-10-30

    申请号：US268437

    申请日：1988-11-08

    申请人： Morio Fujiu ,  Hideo Ishitsuka ,  Masanori Miwa ,  Isao Umeda ,  Kazuteru Yokose

    发明人： Morio Fujiu ,  Hideo Ishitsuka ,  Masanori Miwa ,  Isao Umeda ,  Kazuteru Yokose

    IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7064 ,  A61K31/7068 ,  A61P35/00 ,  C07H19/06 ,  C07H19/067

    CPC分类号： C07H19/06

    摘要： The novel 5'-deoxy-5-fluorocytidine derivatives of formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are hydrogen or an easily hydrolyzable radical under physiological conditions, with the proviso that, at least one or R.sup.1, R.sup.2 and R.sup.3 is an easily hydrolyzable radical under physiological conditions,as well as hydrates of solvates of these compounds have antitumor properties. They can be prepared from compounds of formula I, wherein R.sup.1 is hydrogen or an amino-protecting radical and R.sup.2 and R.sup.3 are hydrogen or a hydroxy-protecting radical or taken together are a cyclic hydroxy-protecting radical.

    摘要翻译： 式（Ⅰ）的新的5'-脱氧-5-氟胞苷衍生物，其中R 1，R 2和R 3在生理条件下为氢或易水解的基团，条件是至少一个或R 1，R 2和R 3 在生理条件下是易水解的基团，以及这些化合物的溶剂合物的水合物具有抗肿瘤性质。 它们可以由式I化合物制备，其中R 1是氢或氨基保护基，并且R 2和R 3是氢或羟基保护基或一起是环状羟基保护基。

    5'deoxycytidine derivatives
    3.
    发明授权
    5'deoxycytidine derivatives 失效
    5'-脱氧胞苷衍生物

    公开(公告)号：US6005098A

    公开(公告)日：1999-12-21

    申请号：US234200

    申请日：1999-01-20

    申请人： Kazuo Hattori ,  Tohru Ishikawa ,  Hideo Ishitsuka ,  Yasunori Kohchi ,  Nobuhiro Oikawa ,  Nobuo Shimma ,  Hitomi Suda

    发明人： Kazuo Hattori ,  Tohru Ishikawa ,  Hideo Ishitsuka ,  Yasunori Kohchi ,  Nobuhiro Oikawa ,  Nobuo Shimma ,  Hitomi Suda

    IPC分类号： C07H19/06 ,  A61K31/513 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7064 ,  A61K31/7068 ,  A61K31/7072 ,  A61P35/00 ,  A61P43/00 ,  C07H19/067 ,  C07H19/16 ,  C07H19/167

    CPC分类号： C07H19/16

    摘要： Compounds of the formula (I) ##STR1## wherein R.sup.1 is each independently hydrogen or a group easily hydrolyzable under physiological conditions;R.sup.2 is --(CH.sub.2).sub.n -cycloalkyl wherein cycloalkyl contains 3 to 5 carbon atoms and n is an integer from 0 to 4, heteroaryl-(lower-alkyl), (lower-alkoxy)-(lower-alkyl), aryloxy-(lower-alkyl), aralkyloxy-(lower-alkyl), (lower-alkylthio)-(lower-alkyl), arylthio-(lower-alkyl), aralkylthio-(lower-alkyl), oxo-(lower-alkyl), acylamino-(lower-alkyl), cyclic amino-(lower-alkyl), (2-oxocyclic amino)-(lower-alkyl) wherein the alkylene chain is unsubstituted or substituted with one or two lower-alkyl group(s); andR.sup.3 is iodo, or a vinyl or ethynyl group which group is unsubstituted or substituted by one or more substituents selected from the group consisting of halogen, C.sub.1-4 alkyl, cycloalkyl, aralkyl, carbocyclic aromatic ring and heteorcyclic aromatic ring.The compounds of formula I are useful in the treatment of malignant diseases and can also be administered together with 5-fluorouracil or derivatives thereof to enhance the antitumour activity of the latter.

    摘要翻译： 式（I）的化合物，其中R 1各自独立地为氢或在生理条件下易于水解的基团; R 2为 - （CH 2）n - 环烷基，其中环烷基含有3至5个碳原子，n为0至4的整数，杂芳基 - （低级 - 烷基），（低级 - 烷氧基） - （低级 - 烷基），芳氧基 - （ 低级烷基），芳烷氧基 - （低级烷基），（低级 - 烷硫基） - （低级 - 烷基），芳硫基 - （低级烷基），芳烷硫基 - （低级烷基），氧代（低级烷基） - （低级烷基），环状氨基 - （低级 - 烷基），（2-氧代环氨基） - （低级烷基），其中亚烷基链未被取代或被一个或两个低级烷基取代; 或R 3为碘，或乙烯基或乙炔基，该基团是未取代的或被一个或多个选自卤素，C 1-4烷基，环烷基，芳烷基，碳环芳环和杂环芳环的取代基取代。 式I化合物可用于治疗恶性疾病，也可与5-氟尿嘧啶或其衍生物一起施用以增强后者的抗肿瘤活性。

    5′-deoxy-cytidine derivative administration to treat solid tumors
    4.
    发明授权
    5′-deoxy-cytidine derivative administration to treat solid tumors 有权
    5'-脱氧胞苷衍生物给药治疗实体瘤

    公开(公告)号：US06211166B1

    公开(公告)日：2001-04-03

    申请号：US09534156

    申请日：2000-03-24

    申请人： Kazuo Hattori ,  Tohru Ishikawa ,  Hideo Ishitsuka ,  Yasunori Kohchi ,  Nobuhiro Oikawa ,  Nobuo Shimma ,  Hitomi Suda

    发明人： Kazuo Hattori ,  Tohru Ishikawa ,  Hideo Ishitsuka ,  Yasunori Kohchi ,  Nobuhiro Oikawa ,  Nobuo Shimma ,  Hitomi Suda

    IPC分类号： A01N4304

    CPC分类号： C07H19/06 ,  Y02P20/55

    摘要： Novel 5′-deoxy-cytidine derivatives represented by the general formula (I) wherein R1 is a hydrogen atom or a group easily hydrolyzable under physiological conditions; R2 is a hydrogen atom, or —CO—OR4 group [wherein R4 is a saturated or unsaturated, straight or branched hydrocarbon group consisting of one to fifteen carbon atoms, or a group of the formula —(CH2)n—Y (in which Y is cyclohexyl or phenyl; n is an integer from 0 to 4)]; R3 is a hydrogen atom, bromo, iodo, cyano, a C1-4 alkyl group [which may be substituted with halogen atom(s)], a vinyl or ethynyl group [which may be substituted with halogen atom(s), C1-4 alkyl, cycloalkyl, aralkyl, or aromatic ring which may have one or more hetero atom(s)], or an aralkyl group which may be substituted for use in medical therapy, especially tumor therapy.

    摘要翻译： 由通式（I）表示的新型5'-脱氧胞苷衍生物，其中R1是氢原子或在生理条件下容易水解的基团; R2是氢原子或-CO-OR4基团[其中R4是由1-15个碳原子组成的饱和或不饱和的直链或支链烃基，或式 - （CH2）nY（其中Y是 环己基或苯基; n为0至4的整数）]; R3是氢原子，溴，碘，氰基，C1-4烷基[可以被卤素原子取代]，乙烯基或乙炔基[可以被卤原子取代，C1- 4烷基，环烷基，芳烷基或可能具有一个或多个杂原子的芳环]或可用于药物治疗，特别是肿瘤治疗的芳烷基。

    5'-deoxy-cytidine derivatives
    5.
    发明授权
    5'-deoxy-cytidine derivatives 有权
    5'-脱氧胞苷衍生物

    公开(公告)号：US6114520A

    公开(公告)日：2000-09-05

    申请号：US484174

    申请日：2000-01-14

    申请人： Kazuo Hattori ,  Tohru Ishikawa ,  Hideo Ishitsuka ,  Yasunori Kohchi ,  Nobuhiro Oikawa ,  Nobuo Shimma ,  Hitomi Suda

    发明人： Kazuo Hattori ,  Tohru Ishikawa ,  Hideo Ishitsuka ,  Yasunori Kohchi ,  Nobuhiro Oikawa ,  Nobuo Shimma ,  Hitomi Suda

    IPC分类号： C07H19/067 ,  A01N43/04 ,  A61K31/505 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7064 ,  A61K31/7068 ,  A61K31/7072 ,  A61P35/00 ,  A61P43/00 ,  C07D239/553 ,  C07H19/06

    CPC分类号： C07H19/06 ,  Y02P20/55

    摘要： Novel 5'-deoxy-cytidine derivatives represented by the general formula (I) ##STR1## wherein R.sup.1 is a hydrogen atom or a group easily hydrolyzable under physiological conditions; R.sup.2 is a hydrogen atom, or --CO--OR.sup.4 group [wherein R.sup.4 is a saturated or unsaturated, straight or branched hydrocarbon group consisting of one to fifteen carbon atoms, or a group of the formula --(CH.sub.2).sub.n --Y (in which Y is cyclohexyl or phenyl; n is an integer from 0 to 4)]; R.sup.3 is a hydrogen atom, bromo, iodo, cyano, a C.sub.1-4 alkyl group [which may be substituted with halogen atom(s)], a vinyl or ethynyl group [which may be substituted with halogen atom(s), C.sub.1-4 alkyl, cycloalkyl, aralkyl, or aromatic ring which may have one or more hetero atom(s)], or an aralkyl group which may be substituted for use in medical therapy, especially tumor therapy.

    摘要翻译： 由通式（I）表示的新型5'-脱氧胞苷衍生物，其中R1是氢原子或在生理条件下容易水解的基团; R2是氢原子或-CO-OR4基团[其中R4是由1-15个碳原子组成的饱和或不饱和的直链或支链烃基，或式 - （CH2）nY（其中Y是 环己基或苯基; n为0至4的整数）]; R3是氢原子，溴，碘，氰基，C1-4烷基[可以被卤素原子取代]，乙烯基或乙炔基[可以被卤原子取代，C1- 4烷基，环烷基，芳烷基或可能具有一个或多个杂原子的芳环]或可用于药物治疗，特别是肿瘤治疗的芳烷基。