Deoxy taxols
    1.
    发明公开
    Deoxy taxols 失效
    脱氧紫杉醇酯衍生物。

    公开(公告)号:EP0590267A2

    公开(公告)日:1994-04-06

    申请号:EP93112247.7

    申请日:1993-07-30

    摘要: in which

    R¹ is -COR z in which R z is RO- or R;
    R g is C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₃₋₆ cycloalkyl, or a radical of the formula -W-R x in which W is a bond, C₂₋₆ alkenediyl, or -(CH₂) t -, in which t is one to six; and R x is naphthyl, phenyl, or heteroaryl, and furthermore R x can be optionally substituted with one to three same or different C₁₋₆ alkyl, C₁₋₆ alkoxy, halogen or -CF₃ groups;
    R² is -OCOR, H, OH, -OR, -OSO₂R, -OCONR o R, -OCONHR, -OCOO(CH₂) t R, or -OCOOR; and
    R and R o are independently C₁₋₆ alkyl, C₂₋₆ alkenyl, C₃₋₆ cycloalkyl, C₂₋₆ alkynyl, or phenyl, optionally substituted with one to three same or different C₁₋₆ alkyl, C₁₋₆ alkoxy, halogen or -CF₃ groups.

    Further provided by this invention are pharmaceutical formulations and intermediates for the the preparation of deoxy taxols of formula I. A method of treating mammalian tumors using a compound of formula I is also provided.

    摘要翻译: 其中R 1为-COR z,其中R z为RO-或R; R g是C 1-6烷基,C 2-6烯基,C 2-6炔基,C 3-6环烷基或其中W是键的式-WR x基团,C 2-6亚烯基或 - (CH 2)t - ,其中t为1至6; 并且R x是萘基,苯基或杂芳基,此外R x可以任选地被一至三个相同或不同的C 1-6烷基,C 1-6烷氧基,卤素或-CF 3基团取代; R 2是-OCOR,H,OH,-OR,-OSO 2 R,-OCONR o,-OCONHR,-OCOO(CH 2)t R或-OCOOR; 并且R和R o独立地为C 1-6烷基,C 2-6烯基,C 3-6环烷基,C 2-6炔基或苯基,任选地被一至三个相同或不同的C 1-6烷基,C 1-6烷氧基 ,卤素或-CF 3基团。 本发明进一步提供了用于制备式I的脱氧紫杉醇的药物制剂和中间体。还提供了使用式I化合物治疗哺乳动物肿瘤的方法。

    Fluoro taxols with antitumor activity
    4.
    发明公开
    Fluoro taxols with antitumor activity 失效
    氟紫杉醇抗肿瘤剂Wirkung。

    公开(公告)号:EP0577082A1

    公开(公告)日:1994-01-05

    申请号:EP93110374.1

    申请日:1993-06-29

    IPC分类号: A61K31/335 C07D305/14

    摘要: This invention relates to a fluorinated taxol of formula I

    in which

    R¹ is -COR z in which R z is RO- or R;
    R g is C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₃₋₆ cycloalkyl, or a radical of the formula -W-R x in which W is a bond, C₂₋₆ alkenediyl, or -(CH₂) t -, in which t is one to six; and R x is naphthyl, furyl, thienyl or phenyl, and furthermore R x can be optionally substituted with one to three same or different C₁₋₆ alkyl, C₁₋₆ alkoxy, halogen or -CF₃ groups;
    R² is -OCOR, H, OH, -OR, -OSO₂R, -OCONR o R, -OCONHR, -OCOO(CH₂) t R, or -OCOOR; and
    R and R o are independently C₁₋₆ alkyl, C₂₋₆ alkenyl, C₃₋₆ cycloalkyl, C₂₋₆ alkynyl, or phenyl, optionally substituted with one to three same or different C₁₋₆ alkyl, C₁₋₆ alkoxy, halogen or -CF₃ groups.
    Further provided by this invention are pharmaceutical formulations and useful intermediates for the fluorinated taxols of formula I. A method of treating mammalian tumors using a compound of formula I is also provided.

    摘要翻译: 本发明涉及式Ⅰ的氟化紫杉醇,其中R 1为-COR z,其中R z为RO-或R; R g是C 1-6烷基,C 2-6烯基,C 2-6炔基,C 3-6环烷基或其中W是键的式-WR x基团,C 2-6亚烯基或 - (CH 2)t - ,其中t为1至6; 并且R x是萘基,呋喃基,噻吩基或苯基,此外R x可以任选地被一至三个相同或不同的C 1-6烷基,C 1-6烷氧基,卤素或-CF 3基团取代; R 2是-OCOR,H,OH,-OR,-OSO 2 R,-OCONR o,-OCONHR,-OCOO(CH 2)t R或-OCOOR; 并且R和R o独立地为C 1-6烷基,C 2-6烯基,C 3-6环烷基,C 2-6炔基或苯基,任选地被一至三个相同或不同的C 1-6烷基,C 1-6烷氧基 ,卤素或-CF 3基团。 本发明进一步提供了用于式I的氟化的紫杉醇的药物制剂和有用的中间体。还提供了使用式I化合物治疗哺乳动物肿瘤的方法。

    Deoxy taxols
    9.
    发明公开
    Deoxy taxols 失效
    脱氧紫杉醇

    公开(公告)号:EP0590267A3

    公开(公告)日:1994-05-18

    申请号:EP93112247.7

    申请日:1993-07-30

    摘要: in which
    R¹ is -COR z in which R z is RO- or R; R g is C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₃₋₆ cycloalkyl, or a radical of the formula -W-R x in which W is a bond, C₂₋₆ alkenediyl, or -(CH₂) t -, in which t is one to six; and R x is naphthyl, phenyl, or heteroaryl, and furthermore R x can be optionally substituted with one to three same or different C₁₋₆ alkyl, C₁₋₆ alkoxy, halogen or -CF₃ groups; R² is -OCOR, H, OH, -OR, -OSO₂R, -OCONR o R, -OCONHR, -OCOO(CH₂) t R, or -OCOOR; and R and R o are independently C₁₋₆ alkyl, C₂₋₆ alkenyl, C₃₋₆ cycloalkyl, C₂₋₆ alkynyl, or phenyl, optionally substituted with one to three same or different C₁₋₆ alkyl, C₁₋₆ alkoxy, halogen or -CF₃ groups. Further provided by this invention are pharmaceutical formulations and intermediates for the the preparation of deoxy taxols of formula I. A method of treating mammalian tumors using a compound of formula I is also provided.

    摘要翻译: 其中R 1是-CORz,其中Rz是RO-或R; Rg是C 1-6烷基,C 2-6链烯基,C 2-6炔基,C 3-6环烷基或式-W-Rx的基团,其中W是键,C 2-6链烯二基或 - (CH 2)t - ,其中t是1到6; Rx是萘基,苯基或杂芳基,而且Rx可以任选被1-3个相同或不同的C1-6烷基,C1-6烷氧基,卤素或-CF3基团取代; R 2是-OCOR,H,OH,-OR,-OSO 2 R,-OCONR 0R,-OCONHR,-OCOO(CH 2)t R或-OCOOR; R 1和R 2独立地为C 1-6烷基,C 2-6链烯基,C 3-6环烷基,C 2-6炔基或苯基,它们任选被1-3个相同或不同的C 1-6烷基,C 1-6烷氧基,卤素或 -CF 3基团。 本发明进一步提供了用于制备式I的脱氧紫杉醇的药物制剂和中间体。还提供了使用式I化合物治疗哺乳动物肿瘤的方法。