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    Imidazolidinonyl aminopyrimidine compounds for the treatment of cancer
    1.
    发明授权
    Imidazolidinonyl aminopyrimidine compounds for the treatment of cancer 失效
    咪唑烷酰氨基嘧啶化合物治疗癌症

    公开(公告)号：US08101628B2

    公开(公告)日：2012-01-24

    申请号：US12516514

    申请日：2007-12-11

    Applicant: Harold Burns Brooks ,  Joyce Z. Crich ,  James Robert Henry ,  Hong-Yu Li ,  Melissa Kate Slater ,  Yan Wang

    Inventor： Harold Burns Brooks ,  Joyce Z. Crich ,  James Robert Henry ,  Hong-Yu Li ,  Melissa Kate Slater ,  Yan Wang

    IPC: C07D401/00

    CPC classification number: C07D409/14

    Abstract: The present invention provides novel imidazolidinonyl aminopyrimidine compounds believed to have clinical use for treatment of cancer through inhibiting Plk1. wherein: R1 hydrogen, hydroxy, halo, methyl, C1-C2 alkoxy, amino, or methylamino; R2 is hydrogen, halo, or cyano; R3 is hydrogen or halo; R4 is hydrogen, halo, or methyl; provided that at least two of R1, R2, R3, and R4 are hydrogen; R5 is hydrogen, halo, or methyl; or a pharmaceutically acceptable salt thereof.

    Abstract translation: 本发明提供了被认为具有通过抑制Plk1治疗癌症的临床用途的新型咪唑烷基氨基嘧啶化合物。 其中：R 1氢，羟基，卤素，甲基，C 1 -C 2烷氧基，氨基或甲基氨基; R2是氢，卤素或氰基; R3是氢或卤素; R4是氢，卤素或甲基; 条件是R 1，R 2，R 3和R 4中的至少两个为氢; R5是氢，卤素或甲基; 或其药学上可接受的盐。

    IMIDAZOLIDINONYL AMINOPYRIMIDINE COMPOUNDS FOR THE TREATMENT OF CANCER
    7.
    发明申请
    IMIDAZOLIDINONYL AMINOPYRIMIDINE COMPOUNDS FOR THE TREATMENT OF CANCER 失效
    用于治疗癌症的咪达唑仑胺氨基嘧啶化合物

    公开(公告)号：US20100081641A1

    公开(公告)日：2010-04-01

    申请号：US12516251

    申请日：2007-12-11

    Applicant: Harold Burns Brooks ,  Joyce Z. Crich ,  James Robert Henry ,  Hong-Yu Li ,  Jason Scott Sawyer ,  Yan Wang

    Inventor： Harold Burns Brooks ,  Joyce Z. Crich ,  James Robert Henry ,  Hong-Yu Li ,  Jason Scott Sawyer ,  Yan Wang

    IPC: A61K31/397 ,  C07D403/14 ,  A61K31/506 ,  C07D413/14 ,  A61K31/5377 ,  A61P35/00

    CPC classification number: C07D409/14

    Abstract: The present invention provides novel imidazolidinonyl aminopyrimidine compounds believed to have clinical use for treatment of cancer through inhibiting Plk1. Formula I wherein: R1 is aminomethyl, (C1-C3 alkyl)aminomethyl, di(C1-C2 alkyl)aminomethyl, N-ethyl-N-methyl-aminomethyl, 1-aminoethyl, 1-((C1-C2 alkyl)amino)-ethyl, 3,3,3-trifluoro-propylaminomethyl, ethynyl, 2-hydroxy-ethoxy, 2-hydroxyethylaminomethyl, 2-cyanoethylaminomethyl, mopholin-4-ylmethyl, methoxymethoxymethyl, cyclopropyl, 1-azetidinylmethyl, 1-pyrrolidinylmethyl, or 1,3-dioxolan-2-yl; R2 is hydrogen or halo; R3 is hydrogen or halo; provided that at least one of R2 and R3 is hydrogen; R4 is hydrogen, methyl, or halo; and is a single bond that is either present or absent, or pharmaceutically acceptable salt thereof.

    Abstract translation: 本发明提供了被认为具有通过抑制Plk1治疗癌症的临床用途的新型咪唑烷基氨基嘧啶化合物。 式（I）其中：R1是氨基甲基，（C1-C3烷基）氨基甲基，二（C1-C2烷基）氨基甲基，N-乙基-N-甲基 - 氨基甲基，1-氨基乙基，1-（（C1-C2烷基） 乙基，3,3,3-三氟 - 丙基氨基甲基，乙炔基，2-羟基 - 乙氧基，2-羟乙基氨基甲基，2-氰基乙基氨基甲基，吗啉-4-基甲基，甲氧基甲氧基甲基，环丙基，1-氮杂环丁基甲基，1-吡咯烷基甲基， 3-二氧戊环-2-基; R2为氢或卤素; R3是氢或卤素; R2和R3中的至少一个是氢; R4是氢，甲基或卤素; 并且是存在或不存在的单键或其药学上可接受的盐。

    Urea linker derivatives for use as PPAR modulators
    8.
    发明授权
    Urea linker derivatives for use as PPAR modulators 失效
    用作PPAR调节剂的尿素接头衍生物

    公开(公告)号：US06984661B2

    公开(公告)日：2006-01-10

    申请号：US10500489

    申请日：2003-01-21

    Applicant: James Robert Henry ,  YiHong Li

    Inventor： James Robert Henry ,  YiHong Li

    IPC: A61K31/36 ,  A61K31/195 ,  C07D317/44 ,  C07C323/63 ,  C07C275/28

    CPC classification number: C07C275/36 ,  C07C275/10 ,  C07C275/24 ,  C07C275/28 ,  C07C275/30 ,  C07C275/34 ,  C07C275/38 ,  C07C2601/14 ,  C07C2602/08 ,  C07D317/66

    Abstract: The present invention is directed to compounds of the structural formula (I), and pharmaceutically acceptable salts, solvates and hydrates thereof: Formula I (a) R1, R2 and R6 are each independently selected from the group consisting of hydrogen, C1-C8 alkyl substituted C1-C8 alkyl, aryl-C0-4-alkyl, substituted aryl-C0-4-alkyl, heteroaryl-C0-4-alkyl, substituted heteroaryl-C0-4-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl, and substituted C3-C6 cycloalkylaryl-C0-2-alkyl; (b) X is an optionally substituted C1-C5 alkylene linker wherein one carbon atom of the linker may be replaced with O, NH or S; (c) Y is C, O, S, NH or a single bond; and (d) E is selected from the group consisting of hydrogen, C(R3)(R4)A, A, (CH2)n COOR19 and substituted (CH2)n COOR19.

    Abstract translation: 本发明涉及结构式（I）的化合物及其药学上可接受的盐，溶剂合物和水合物：式I（a）R 1，R 2和R 6各自独立地选自氢，C 1 -C 6烷基， 1个C 1 -C 8烷基取代的C 1 -C 8烷基，芳基-C 0-4

    Imidazolidinonyl aminopyrimidine compounds for the treatment of cancer
    9.
    发明授权
    Imidazolidinonyl aminopyrimidine compounds for the treatment of cancer 失效
    咪唑烷酰氨基嘧啶化合物治疗癌症

    公开(公告)号：US08063212B2

    公开(公告)日：2011-11-22

    申请号：US12516251

    申请日：2007-12-11

    Applicant: Harold Burns Brooks ,  Joyce Z. Crich ,  James Robert Henry ,  Hong-Yu Li ,  Jason Scott Sawyer ,  Yan Wang

    Inventor： Harold Burns Brooks ,  Joyce Z. Crich ,  James Robert Henry ,  Hong-Yu Li ,  Jason Scott Sawyer ,  Yan Wang

    IPC: C07D401/00

    CPC classification number: C07D409/14

    Abstract: The present invention provides novel imidazolidinonyl aminopyrimidine compounds believed to have clinical use for treatment of cancer through inhibiting Plk1. Formula I wherein: R1 is aminomethyl, (C1-C3 alkyl)aminomethyl, di(C1-C2 alkyl)aminomethyl, N-ethyl-N-methyl-aminomethyl, 1-aminoethyl, 1-((C1-C2 alkyl)amino)-ethyl, 3,3,3-trifluoro-propylaminomethyl, ethynyl, 2-hydroxy-ethoxy, 2-hydroxyethylaminomethyl, 2-cyanoethylaminomethyl, morpholin-4-ylmethyl, methoxymethoxymethyl, cyclopropyl, 1-azetidinylmethyl, 1-pyrrolidinylmethyl, or 1,3-dioxolan-2-yl; R2 is hydrogen or halo; R3 is hydrogen or halo; provided that at least one of R2 and R3 is hydrogen; R4 is hydrogen, methyl, or halo; and is a single bond that is either present or absent, or pharmaceutically acceptable salt thereof.

    Abstract translation: 本发明提供了被认为具有通过抑制Plk1治疗癌症的临床用途的新型咪唑烷基氨基嘧啶化合物。 式（I）其中：R1是氨基甲基，（C1-C3烷基）氨基甲基，二（C1-C2烷基）氨基甲基，N-乙基-N-甲基 - 氨基甲基，1-氨基乙基，1-（（C1-C2烷基）氨基） 乙基，3,3,3-三氟 - 丙氨基甲基，乙炔基，2-羟基 - 乙氧基，2-羟乙基氨基甲基，2-氰乙基氨基甲基，吗啉-4-基甲基，甲氧基甲氧基甲基，环丙基，1-氮杂环丁基甲基，1-吡咯烷基甲基， 3-二氧戊环-2-基; R2是氢或卤素; R3是氢或卤素; R2和R3中的至少一个是氢; R4是氢，甲基或卤素; 并且是存在或不存在的单键或其药学上可接受的盐。

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