PEDERIN AND PSYMBERIN AGENTS
    5.
    发明申请
    PEDERIN AND PSYMBERIN AGENTS 有权
    佩德琳和PSYMBERIN代理

    公开(公告)号:US20140161877A1

    公开(公告)日:2014-06-12

    申请号:US14234133

    申请日:2012-07-19

    IPC分类号: A61K47/48

    摘要: Compounds that include a pederin, psymberin or pederin/psymberin chimera scaffold. The pederin scaffold includes a substituent at the C10 and/or C13 position that may include a linker that may be conjugated to a targeting moiety. The psymberin scaffold includes a substituent at the C8 and/or C11 positions that may include a linker that may be conjugated to a targeting moiety. The pederin/psymberin chimera scaffold includes a substituent at the C10 and/or C13 position that may include a linker that may be conjugated to a targeting moiety. The pederin, psymberin or pederin/psymberin chimera scaffold may be modified to include substituents at positions other than the C10 or C13 of pederin, or the C8 and C11 of psymberin.

    摘要翻译: 化合物包括pederin,psymberin或pederin / psymberin嵌合体支架。 er脚骨架在C10和/或C13位置包含可以与可能与靶向部分缀合的接头的取代基。 精神分裂素支架在C8和/或C11位置包括可以包含可以与靶向部分缀合的接头的取代基。 pederin / psymberin嵌合体支架包括在C10和/或C13位置的取代基,其可以包括可以与靶向部分缀合的连接体。 可以修饰pederin,psymberin或pederin / psymberin嵌合体支架,以在除Pederin的C10或C13之外的位置或psymberin的C8和C11中包含取代基。

    Analogs of discodermolide and dictyostatin-1, intermediates therefor and methods of synthesis thereof
    8.
    发明授权
    Analogs of discodermolide and dictyostatin-1, intermediates therefor and methods of synthesis thereof 有权
    discodermolide和dictyostatin-1的类似物,其中间体及其合成方法

    公开(公告)号:US07968736B2

    公开(公告)日:2011-06-28

    申请号:US12235720

    申请日:2008-09-23

    IPC分类号: C07D313/00

    摘要: A compound of the following structure: wherein R1 is H, an alkyl group, an aryl group, an alkenyl group, an alkynyl group, or a halogen atom; R2 is H, an alkyl group, an aryl group, a benzyl group, a trityl group, —SiRaRbRc, CH2ORd, or CORe; Ra, Rb and Rc are independently an alkyl group or an aryl group; Rd is an alkyl group, an aryl group, an alkoxylalkyl group, —RiSiRaRbRc or a benzyl group, wherein Ri is an alkylene group; Re is an alkyl group, an allyl group, a benzyl group, an aryl group, an alkoxy group, or —NRgRh, wherein Rg and Rh are independently H, an alkyl group or an aryl group; R3 is (CH2)n where n is and integer in the range of 0 to 5, —CH2CH(CH3)—, —CH═CH—, —CH═C(CH3)—, or —C≡C—; R4  wherein y1 and y2 are 1 and y3, y4 and y5 are independently 0 or 1, Rk1, Rk2, Rk3, Rk4 and Rk5 are independently H, CH3, or OR2a, and Rs1, Rs2, Rs3, and Rs4 are independently H or CH3, wherein R2a is H, an alkyl group, an aryl group, a benzyl group, a trityl group, —SiRaRbRc, CH2ORd, or CORe; and R5 is H or OR2b, wherein R2b is H, an alkyl group, an aryl group, an aryl group, a benzyl group, a trityl group, —SiRaRbRc, CH2ORd, or CORe.

    摘要翻译: 下列结构的化合物:其中R1是H,烷基,芳基,烯基,炔基或卤素原子; R2是H,烷基,芳基,苄基,三苯甲基,-SiRaRbRc,CH2ORd或CORe; Ra,Rb和Rc独立地为烷基或芳基; Rd是烷基,芳基,烷氧基烷基,-RiSiRaRbRc或苄基,其中R 1是亚烷基; Re为烷基,烯丙基,苄基,芳基,烷氧基或-NRgRh,其中Rg和Rh独立地为H,烷基或芳基; R 3为(CH 2)n,其中n为0至5的整数,-CH 2 CH(CH 3) - , - CH = CH - , - CH = C(CH 3) - 或-C≡C-; R4其中y1和y2是1,y3,y4和y5独立地是0或1,Rk1,Rk2,Rk3,Rk4和Rk5独立地是H,CH3或OR2a,Rs1,Rs2,Rs3和Rs4独立地是H或 CH3,其中R2a是H,烷基,芳基,苄基,三苯甲基,-SiRaRbRc,CH2ORd或CORe; R5是H或OR2b,其中R2b是H,烷基,芳基,芳基,苄基,三苯甲基,-SiRaRbRc,CH2ORd或CORe。