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    6,7-modified paclitaxels
    2.
    发明授权
    6,7-modified paclitaxels 失效
    6,7修饰紫杉醇

    公开(公告)号：US5380751A

    公开(公告)日：1995-01-10

    申请号：US128619

    申请日：1993-09-28

    申请人： Shu-Hui Chen ,  Vittorio Farina ,  Gregory Roth ,  John Kadow

    发明人： Shu-Hui Chen ,  Vittorio Farina ,  Gregory Roth ,  John Kadow

    IPC分类号： A61K31/337 ,  A61P35/00 ,  C07D305/14 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07F7/18 ,  A61K31/335

    CPC分类号： C07D407/12 ,  C07D305/14 ,  C07D409/12 ,  C07D413/12 ,  C07F7/1856

    摘要： The present invention provides paclitaxel derivatives of formula I ##STR1## in which R.sup.1 is --COR.sup.z in which R.sup.Z is RO-- or R;R.sup.2 is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or a radical of the formula --W--R.sup.x in which W is a bond, C.sub.2-6 alkenediyl, or --(CH.sub.2).sub.t --, in which t is one to six; and R.sup.x is naphthyl, phenyl, or heteroaryl, and furthermore R.sup.x can be optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups;R.sup.a is --OCOR, H, OH, --OR, --OSO.sub.2 R, --OCONR.sup.o R, --OCONHR, --OCOO(CH.sub.2).sub.t R, or --OCOOR;R.sup.b and R.sup.c are both hydroxy or together form a bond with the carbon atoms to which they are attached; andR and R.sup.o are independently C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl, C.sub.2-6 alkynyl, or phenyl, optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups.Also provided by this invention are pharmaceutical formulations (compositions) and a method of treating mammalian tumors with a compound of formula I.

    摘要翻译： 本发明提供式I的紫杉醇衍生物，其中R 1是其中R Z是RO-或R的-CORz; R 2是C 1-6烷基，C 2-6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亚烯基或 - （CH 2）t - 其中t为1至6; 并且Rx是萘基，苯基或杂芳基，此外Rx可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 a是-OCOR，H，OH，-OR，-OSO 2 R，-OCONRoR，-OCONHR，-OCOO（CH 2）t R或-OCOOR; Rb和Rc都是羟基或与它们所连接的碳原子一起形成键; 并且R和R 4独立地是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 -CF3组。 本发明还提供了药物制剂（组合物）和用式I化合物治疗哺乳动物肿瘤的方法。

    Fluoro taxols
    3.
    发明授权
    Fluoro taxols 失效
    氟紫杉醇

    公开(公告)号：US5294637A

    公开(公告)日：1994-03-15

    申请号：US62687

    申请日：1993-05-20

    申请人： Shu-Hui Chen ,  Vittorio Farina ,  Joydeep Kant ,  Dolatrai M. Vyas

    发明人： Shu-Hui Chen ,  Vittorio Farina ,  Joydeep Kant ,  Dolatrai M. Vyas

    IPC分类号： C07D305/14 ,  C07D407/12 ,  C07D409/12 ,  C07F7/18 ,  C07F9/655 ,  C07F9/6558 ,  H01L21/48 ,  H05K1/03 ,  H05K1/09 ,  H05K1/16 ,  H05K3/40 ,  A01N43/02 ,  C07D305/00

    CPC分类号： C07D407/12 ,  C07D305/14 ,  C07D409/12 ,  C07F7/1856 ,  C07F9/65512 ,  C07F9/65586 ,  H01L21/4839 ,  H05K1/16 ,  H05K1/0306 ,  H05K1/092 ,  H05K3/403

    摘要： This invention relates to a fluorinated taxol of formula I ##STR1## in which R.sup.1 is --COR.sup.z in which R.sup.z is RO-- or R;R.sup.g is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or a radical of the formula --W--R.sup.x in which W is a bond, C.sub.2-6 alkenediyl, or --(CH.sub.2).sub.t --, in which t is one to six; and R.sup.x is naphthyl, furyl, thienyl or phenyl, and furthermore R.sup.x can be optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups;R.sup.2 is --OCOR, H, OH, --OR, --OSO.sub.2 R, --OCONR.sup.o R, --OCONHR, --OCOO(CH.sub.2).sub.t R, or --OCOOR; andR and R.sup.o are independently C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl, C.sub.2-6 alkynyl, or phenyl, optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 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是-COR 3，其中R z是RO-或R; R 8为C 1-6烷基，C 2-6烯基，C 2-6炔基，C 3-6环烷基或W-Rx基团，W为键，C 2-6亚烯基或 - （CH 2）t - 其中t为1至6; 并且Rx是萘基，呋喃基，噻吩基或苯基，此外Rx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; R2是-OCOR，H，OH，-OR，-OSO2R，-OCONRoR，-OCONHR，-OCOO（CH2）tR或-OCOOR; 并且R和R 4独立地是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 -CF3组。 本发明进一步提供了用于式I的氟化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。

    7,8-cyclopropataxanes
    4.
    发明授权
    7,8-cyclopropataxanes 失效
    7,8-环丙烷

    公开(公告)号：US5254580A

    公开(公告)日：1993-10-19

    申请号：US29819

    申请日：1993-03-11

    申请人： Shu-Hui Chen ,  Vittorio Farina

    发明人： Shu-Hui Chen ,  Vittorio Farina

    IPC分类号： C07D305/14 ,  A01N43/02 ,  C07C305/00

    CPC分类号： C07D305/14

    摘要： An antitumor compound of formula I ##STR1## in which R.sup.1 is --COR.sup.z in which R.sup.z is t-butyloxy, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or phenyl, optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups;R.sup.2 is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or a radical of the formula --W--R.sup.x in which W is a bond, C.sub.2-6 alkenediyl, or --(CH.sub.2).sub.t --, in which t is one to six; and R.sup.x is naphthyl, furyl, thienyl or phenyl, and furthermore R.sup.x can be optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups;R.sup.3 is OCOR, --OCOOR, H, or OH; R.sup.4 is hydrogen; or R.sup.3 and R.sup.4 jointly form a carbonyl group; and R is C.sub.1-6 alkyl.Also provided by this invention are pharmaceutical formulations (compositions) and a method of treating mammalian tumors with a compound of formula I.

    摘要翻译： 式I的抗肿瘤化合物，其中R 1为-COR z，其中R z为叔丁氧基，C 1-6烷基，C 2-6烯基，C 2-6炔基，C 3-6环烷基或苯基，任选被 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; R 2是C 1-6烷基，C 2-6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亚烯基或 - （CH 2）t - 其中t为1至6; 并且Rx是萘基，呋喃基，噻吩基或苯基，此外Rx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; R3是OCOR，-OCOOR，H或OH; R4是氢; 或R3和R4共同形成羰基; 且R为C 1-6烷基。 本发明还提供了药物制剂（组合物）和用式I化合物治疗哺乳动物肿瘤的方法。

    Taxol derivatives
    5.
    发明授权
    Taxol derivatives 失效
    紫杉醇衍生物

    公开(公告)号：US5248796A

    公开(公告)日：1993-09-28

    申请号：US900365

    申请日：1992-06-18

    申请人： Shu-Hui Chen ,  Vittorio Farina

    发明人： Shu-Hui Chen ,  Vittorio Farina

    IPC分类号： C07D305/14

    CPC分类号： C07D305/14 ,  C07C2103/80

    摘要： The present invention relates to 10-desacetoxy-11,12-dihydrotaxol-10,12(18)-diene derivatives which are useful as antitumor agents and as intermediates for the preparation of 10-desacetoxytaxol. Also disclosed is a novel process for the preparation of 10-desacetoxytaxol which comprises treating hydroxy protected 10-deacetyltaxol with 1,1,2-trifluoro-2-chlorotriethylamine followed by catalytic hydrogenation.

    摘要翻译： 本发明涉及可用作抗肿瘤剂的10-脱乙酰氧基-11,12-二氢塔考醇-10,12（18） - 二烯衍生物，作为制备10-脱乙酰氧基紫杉醇的中间体。 还公开了一种用于制备10-脱乙酰氧基紫杉醇的新方法，其包括用1,1,2-三氟-2-氯三乙胺处理羟基保护的10-脱乙酰紫杉醇，然后催化氢化。

    Fluoro taxols
    6.
    发明授权
    Fluoro taxols 失效

    公开(公告)号：US5192796A

    公开(公告)日：1993-03-09

    申请号：US907261

    申请日：1992-07-01

    申请人： Shu-Hui Chen ,  Vittorio Farina

    发明人： Shu-Hui Chen ,  Vittorio Farina

    摘要： This invention relates to a fluorinated taxol of formula I ##STR1## in which R.sup.1 is benzoyl or t-butyloxycarbonyl; R.sup.2 is acetoxy, hydrogen or hydroxy; and the wavy line indicates either the .alpha.- or the .beta.-configuration.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.

    Deoxy taxols
    7.
    发明授权
    Deoxy taxols 失效
    脱氧紫杉醇

    公开(公告)号：US5478854A

    公开(公告)日：1995-12-26

    申请号：US212447

    申请日：1994-03-10

    申请人： Vittorio Farina ,  Shu-Hui Chen ,  David Langley ,  Mark D. Wittman ,  Joydeep Kant ,  Dolatrai M. Vyas

    发明人： Vittorio Farina ,  Shu-Hui Chen ,  David Langley ,  Mark D. Wittman ,  Joydeep Kant ,  Dolatrai M. Vyas

    IPC分类号： C07D305/14 ,  C07D407/12 ,  C07D409/12 ,  C07F7/18 ,  C07F9/655 ,  C07F9/6558 ,  H01L21/48 ,  A61K31/33 ,  A61K31/34 ,  A61K31/38

    CPC分类号： C07D407/12 ,  C07D305/14 ,  C07D409/12 ,  C07F7/1856 ,  C07F9/65512 ,  C07F9/65586 ,  H01L21/4839

    摘要： R.sup.g is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or a radical of the formula --W--R.sup.x in which W is a bond, C.sub.2-6 alkenediyl, or --(CH.sub.2).sub.t --, in which t is one to six; and R.sup.x is naphthyl, phenyl, or heteroaryl, and furthermore R.sup.x can be optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups;R.sup.2 is --OCOR, H, OH, --OR, --OSO.sub.2 R, --OCONR.sup.o R, --OCONHR, --OCOO(CH.sub.2).sub.t R, or --OCOOR; andR and R.sup.o are independently C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl, C.sub.2-6 alkynyl, or phenyl, optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 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-COR z，其中R z是RO-或R; R 8为C 1-6烷基，C 2-6烯基，C 2-6炔基，C 3-6环烷基或W-Rx基团，W为键，C 2-6亚烯基或 - （CH 2）t - 其中t为1至6; 并且Rx是萘基，苯基或杂芳基，此外Rx可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; R2是-OCOR，H，OH，-OR，-OSO2R，-OCONRoR，-OCONHR，-OCOO（CH2）tR或-OCOOR; 并且R和R 4独立地是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 -CF3组。 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。

    SPLITTER
    10.
    发明申请
    SPLITTER 有权
    分机

    公开(公告)号：US20090267719A1

    公开(公告)日：2009-10-29

    申请号：US12191778

    申请日：2008-08-14

    申请人： Hung-Chieh Tseng ,  Ying-Chian Kang ,  Tsung-Hsien Lee ,  Shu-Hui Chen ,  Hua-Sheng Shih

    发明人： Hung-Chieh Tseng ,  Ying-Chian Kang ,  Tsung-Hsien Lee ,  Shu-Hui Chen ,  Hua-Sheng Shih

    IPC分类号： H01F27/02

    CPC分类号： H01F17/043 ,  H01F3/12 ,  H01F5/02 ,  H01F27/266 ,  H01F2005/043

    摘要： The present invention provides a splitter including a seat, a first inner core, a second inner core, a first coil, an outer core and a second coil. The seat has a bobbin, and the first coil is wound on the bobbin. The first inner core and the second inner core, disposed on the bobbin, are assembled with each other to cover the bobbin. The outer core and the first inner core are assembled with each other. The second coil is disposed between the outer core and the first inner core.

    摘要翻译： 本发明提供了一种分离器，包括座，第一内芯，第二内芯，第一线圈，外芯和第二线圈。 座椅具有线轴，第一线圈缠绕在线轴上。 设置在线轴上的第一内芯和第二内芯彼此组装以覆盖线轴。 外芯和第一内芯彼此组装。 第二线圈设置在外芯和第一内芯之间。