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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。

    5'deoxycytidine derivatives
    4.
    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
    5.
    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
    6.
    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。