2', 5' -DIDEOXY-5-FLUOROURIDINE DERIVATIVES HAVING CYTOTOXIC ACTIVITY, A PROCESS FOR THE MANUFACTURE THEREOF AND APPLICATION THEREOF
    2.
    发明申请
    2', 5' -DIDEOXY-5-FLUOROURIDINE DERIVATIVES HAVING CYTOTOXIC ACTIVITY, A PROCESS FOR THE MANUFACTURE THEREOF AND APPLICATION THEREOF 有权
    具有细胞毒活性的2',5'-二氧代-5-氟尿嘧啶衍生物,其制备方法及其应用

    公开(公告)号:US20160244473A1

    公开(公告)日:2016-08-25

    申请号:US14413618

    申请日:2014-03-04

    IPC分类号: C07H19/06

    摘要: The subject matter of the invention is novel 2′,5′-dideoxy-5-fluorouridine derivatives of general formula 1. wherein R1 denotes cinchona alkaloid fragment with defined absolute configuration at C-8 and C-9 atoms.In a second aspect, the subject matter of the invention is a process for the manufacture of 2′,5′-dideoxy-5-fluorouridine derivatives of general formula 1.In a third aspect, the subject matter of the invention is an application of 2′,5′-dideoxy-5-fluorouridine derivatives of general formula 1 in the anticancer treatment of breast cancer, cervical cancer, lung cancer and nasopharynx cancer.

    摘要翻译: 本发明的主题是通式1的新的2',5'-二脱氧-5-氟尿苷衍生物。其中R1表示在C-8和C-9原子具有确定的绝对构型的cinchona生物碱片段。 在第二方面,本发明的主题是制备通式1的2',5'-二脱氧-5-氟尿苷衍生物的方法。在第三方面,本发明的主题是 2',5'-二脱氧-5-氟尿苷衍生物在乳癌,宫颈癌,肺癌和鼻咽癌的抗癌治疗中的应用。

    Monovinylgermasilsesquioxanes
    3.
    发明授权
    Monovinylgermasilsesquioxanes 有权
    单乙烯基硅氧烷倍半硅氧烷

    公开(公告)号:US09249167B1

    公开(公告)日:2016-02-02

    申请号:US14677125

    申请日:2015-04-02

    IPC分类号: C07F7/30

    CPC分类号: C07F7/30

    摘要: A new cage monovinylgermasilsesquioxanes of the general formula 1, in which R1 are the same and represent a C1 to C6 alkyl group or a cyclopentyl or cyclohexyl group or a phenyl group. The invention also relates to the method of synthesis of cage monovinylgermasilsesquioxanes of the general formula 1.

    摘要翻译: 一种通式1的新型笼型单乙烯基硅氧烷倍半硅氧烷,其中R 1相同并且表示C1-C6烷基或环戊基或环己基或苯基。 本发明还涉及通式1的笼式单乙烯基倍半硅氧烷的合成方法。

    APPLICATION OF CINCHONA ALKALOID DERIVATIVES AS CYTOTOXIC COMPOUNDS
    4.
    发明申请
    APPLICATION OF CINCHONA ALKALOID DERIVATIVES AS CYTOTOXIC COMPOUNDS 有权
    金丝雀碱衍生物作为细胞毒素化合物的应用

    公开(公告)号:US20160022668A1

    公开(公告)日:2016-01-28

    申请号:US14430168

    申请日:2014-03-04

    IPC分类号: A61K31/49

    CPC分类号: A61K31/49

    摘要: 9-O-propargyl ethers of cinchona alkaloids of general formula represented by formula 1 wherein respective ethers have the following absolute configuration at C-8 and C-9 atoms: (8R,9S)—cinchonine configuration or (8R,9R)—9-epicinchonine configuration are useful in treatments of at least one of breast cancer, cervical cancer, lung cancer and nasopharynx cancer.

    摘要翻译: 由式1表示的通式生物碱的9-O-炔丙基醚,其中相应的醚在C-8和C-9原子具有以下绝对构型:(8R,9S) - 嘧啶醌构型或(8R,9R)-9 至少一种乳腺癌,宫颈癌,肺癌和鼻咽癌的治疗有用。

    2,3'-ANHYDRO-2'-DEOXY-5-FLUOROURIDINE DERIVATIVES WITH CYTOTOXIC ACTIVITY, A MANUFACTURING PROCESS AND APPLICATION
    6.
    发明申请
    2,3'-ANHYDRO-2'-DEOXY-5-FLUOROURIDINE DERIVATIVES WITH CYTOTOXIC ACTIVITY, A MANUFACTURING PROCESS AND APPLICATION 有权
    具有细胞毒活性的2,3'-壬基-2'-脱氧-5-氟尿嘧啶衍生物,制造方法和应用

    公开(公告)号:US20160024133A1

    公开(公告)日:2016-01-28

    申请号:US14420487

    申请日:2014-08-22

    IPC分类号: C07H19/10

    摘要: The subject matter of the invention is novel 2,3′-anhydro-2′-deoxy-5-fluorouridine derivatives of general formula 1 where R is a trifluoromethyl, 2,2,2-trifluoroethyl, difluoromethyl, perfluoroethyl, 1-fluoroethyl, 2-fluoroethyl, 1,1 -difluoroethyl, 1,2-difluoroethyl, 2,2-difluoroethyl, 1,1,2-trifluoroethyl, 1,2,2-trifluoroethyl, 1,1,2,2-tetrafluoroethyl, 1,2,2,2-tetrafluoroethyl group. In a second aspect, the subject matter of the invention is a process for the manufacture of 2,3-anhydro-2′-deoxy-5-fluorouridine derivatives of general formula 1.In a third aspect, the subject matter of the invention is an application of 2,3′-anhydro-2′-deoxy-5-fluorouridine derivatives of general formula 1 in the anticancer treatment of breast cancer, cervical cancer, lung cancer and nasopharynx cancer.

    摘要翻译: 本发明的主题是通式1的2,3' - 脱氢-2'-脱氧-5-氟尿苷衍生物,其中R是三氟甲基,2,2,2-三氟乙基,二氟甲基,全氟乙基,1-氟乙基, 2-氟乙基,1,1-二氟乙基,1,2-二氟乙基,2,2-二氟乙基,1,1,2-三氟乙基,1,2,2-三氟乙基,1,1,2,2-四氟乙基, 2,2,2-四氟乙基。 在第二方面,本发明的主题是制备通式1的2,3-脱水-2'-脱氧-5-氟尿苷衍生物的方法。在第三方面,本发明的主题是 在抗癌治疗乳腺癌,宫颈癌,肺癌和鼻咽癌中应用通式1的2,3'-脱氢-2'-脱氧-5-氟尿苷衍生物。

    Application of cinchona alkaloid derivatives as cytotoxic compounds
    8.
    发明授权
    Application of cinchona alkaloid derivatives as cytotoxic compounds 有权
    香草素生物碱衍生物作为细胞毒性化合物的应用

    公开(公告)号:US09301956B2

    公开(公告)日:2016-04-05

    申请号:US14430168

    申请日:2014-03-04

    IPC分类号: A61K31/49

    CPC分类号: A61K31/49

    摘要: 9-O-propargyl ethers of cinchona alkaloids of general formula represented by formula 1 wherein respective ethers have the following absolute configuration at C-8 and C-9 atoms: (8R,9S)-cinchonine configuration or (8R,9R)-9-epicinchonine configuration are useful in treatments of at least one of breast cancer, cervical cancer, lung cancer and nasopharynx cancer.

    摘要翻译: 由式1表示的通式生物碱的9-O-炔丙基醚,其中相应的醚在C-8和C-9原子具有以下绝对构型:(8R,9S) - 嘧啶醌构型或(8R,9R)-9 至少一种乳腺癌,宫颈癌,肺癌和鼻咽癌的治疗有用。

    2,3′-anhydro-2′-deoxy-5-fluorouridine derivatives with cytotoxic activity, a manufacturing process and application
    9.
    发明授权
    2,3′-anhydro-2′-deoxy-5-fluorouridine derivatives with cytotoxic activity, a manufacturing process and application 有权
    具有细胞毒活性的2,3'-脱水-2'-脱氧-5-氟尿苷衍生物,制备方法和应用

    公开(公告)号:US09260468B1

    公开(公告)日:2016-02-16

    申请号:US14420487

    申请日:2014-08-22

    IPC分类号: C07H19/10

    摘要: The subject matter of the invention is novel 2,3′-anhydro-2′-deoxy-5-fluorouridine derivatives of general formula 1 where R is a trifluoromethyl, 2,2,2-trifluoroethyl, difluoromethyl, perfluoroethyl, 1-fluoroethyl, 2-fluoroethyl, 1,1-difluoroethyl, 1,2-difluoroethyl, 2,2-difluoroethyl, 1,1,2-trifluoroethyl, 1,2,2-trifluoroethyl, 1,1,2,2-tetrafluoroethyl, 1,2,2,2-tetrafluoroethyl group. In a second aspect, the subject matter of the invention is a process for the manufacture of 2,3′-anhydro-2′-deoxy-5-fluorouridine derivatives of general formula 1.In a third aspect, the subject matter of the invention is an application of 2,3′-anhydro-2′-deoxy-5-fluorouridine derivatives of general formula 1 in the anticancer treatment of breast cancer, cervical cancer, lung cancer and nasopharynx cancer.

    摘要翻译: 本发明的主题是通式1的2,3' - 脱氢-2'-脱氧-5-氟尿苷衍生物,其中R是三氟甲基,2,2,2-三氟乙基,二氟甲基,全氟乙基,1-氟乙基, 2-氟乙基,1,1-二氟乙基,1,2-二氟乙基,2,2-二氟乙基,1,1,2-三氟乙基,1,2,2-三氟乙基,1,1,2,2-四氟乙基, 2,2,2-四氟乙基。 在第二方面,本发明的主题是制备通式1的2,3'-脱氢-2'-脱氧-5-氟尿苷衍生物的方法。在第三方面,本发明的主题 是在乳癌,宫颈癌,肺癌和鼻咽癌的抗癌治疗中应用通式1的2,3'-脱氢-2'-脱氧-5-氟尿苷衍生物。

    Functionalized unsaturated double-decker derivatives of divinylsilsesquioxanes
    10.
    发明授权
    Functionalized unsaturated double-decker derivatives of divinylsilsesquioxanes 有权
    二乙烯基倍半硅氧烷的官能化不饱和双层衍生物

    公开(公告)号:US09150596B2

    公开(公告)日:2015-10-06

    申请号:US14640618

    申请日:2015-03-06

    IPC分类号: C07F7/21

    CPC分类号: C07F7/21

    摘要: The subject of the invention are new functionalized unsaturated double-decker derivatives of divinylsilsesquioxanes of the general formula 1. In the formula, R1 are the same and stand for an aryl group containing from 1 to 2 rings, R2 are the same and stand for an alkyl group containing carbon atoms from C1 to C2, substituted or unsubstituted aryl group containing from 1 to 2 rings, R3 are the same and stand for a substituted or unsubstituted aryl group containing from 1 to 2 rings or a group of the formula —R4-R5—, where R4 stands for an alkyl group containing carbon atoms from C1 to C3, while R5 stands for aryl group containing from 1 to 2 rings.

    摘要翻译: 本发明的主题是通式1的二乙烯基倍半硅氧烷的新的官能化不饱和双层甲基衍生物。在该式中,R 1相同,代表含有1至2个环的芳基,R 2相同并代表 含C1至C2的碳原子的烷基,含有1-2个环的取代或未取代的芳基,R3相同,代表含有1至2个环的取代或未取代的芳基或式-R4- R5-,其中R4代表含有C1至C3的碳原子的烷基,R5代表含有1至2个环的芳基。