Anti-proliferative compounds, compositions, and methods of use thereof

    公开(公告)号:US08268802B2

    公开(公告)日:2012-09-18

    申请号:US12436004

    申请日:2009-05-05

    CPC分类号: C07F9/65616 Y02P20/55

    摘要: Compounds and compositions of Formula I are described, useful as anti-proliferative agents, and in particular anti-HPV, wherein: Y1A and Y1B are independently Y1; RX1 and RX2 are independently RX; Y1 is ═O, —O(RX), ═S, —N(RX), —N(O)(RX), —N(ORX), —N(O)(ORX), or —N(N(RX)(RX)); RX is independently R1, R2, R4, W3, or a protecting group; R1 is independently —H or alkyl of 1 to 18 carbon atoms; R2 is independently R3 or R4 wherein each R4 is independently substituted with 0 to 3 R3 groups or taken together at a carbon atom, two R2 groups form a ring of 3 to 8 carbons and the ring may be substituted with 0 to 3 R3 groups; R3 is R3a, R3b, R3c or R3d, provided that when R3 is bound to a heteroatom, then R3 is R3c or R3d; R3a is —H, —F, —Cl, —Br, —I, —CF3, —CN, N3, —NO2, or —OR4; R3b is ═O, —O(R4), ═S, —N(R4), —N(O)(R4), —N(OR4), —N(O)(OR4), or —N(N(R4)(R4)); R3c is —R4, —N(R4)(R4), —SR4, —S(O)R4, —S(O)2R4, —S(O)(OR4), —S(O)2(OR4), —OC(R3b)R4, —OC(R3b)OR4, —OC(R3b)(N(R4)(R4)), —SC(R3b)R4, —SC(R3b)OR4, —SC(R3b)(N(R4)(R4)), —N(R4)C(R3b)R4, —N(R4)C(R3b)OR4, —N(R4)C(R3b) (N(R4)(R4)), W3 or —R5W3; R3d is —C(R3b)R4, —C(R3b)OR4, —C(R3b)W3, —C(R3b)OW3 or —C(R3b)(N(R4)(R4)); R4 is —H, or an alkyl of 1 to 18 carbon atoms, alkenyl of 2 to 18 carbon atoms, or alkynyl of 2 to 18 carbon atoms; R5 is alkylene of 1 to 18 carbon atoms, alkenylene of 2 to 18 carbon atoms, or alkynylene of 2 to 18 carbon atoms; W3 is W4 or W5; W4 is R6, —C(R3b)R6, —C(R3b)W5, —SOM2R6, or —SOM2W5, wherein R6 is R4 wherein each R4 is substituted with 0 to 3 R3 groups; W5 is carbocycle or heterocycle wherein W5 is independently substituted with 0 to 3 R2 groups; and M2 is 0, 1 or 2; and pharmaceutically acceptable salts thereof.

    Anti-proliferative compounds, compositions, and methods of use thereof

    公开(公告)号:US20050222090A1

    公开(公告)日:2005-10-06

    申请号:US11026303

    申请日:2004-12-29

    CPC分类号: C07F9/65616 Y02P20/55

    摘要: Compounds and compositions of Formula I are described, useful as anti-proliferative agents, and in particular anti-HPV, wherein: Y1A and Y1B are independently Y1; RX1 and RX2 are independently RX; Y1 is ═O, —O(RX), ═S, —N(RX), —N(O)(RX), —N(ORX), —N(O)(ORX), or —N(N(RX)(RX)); RX is independently R1, R2, R4, W3, or a protecting group; R1 is independently —H or alkyl of 1 to 18 carbon atoms; R2 is independently R3 or R4 wherein each R4 is independently substituted with 0 to 3 R3 groups or taken together at a carbon atom, two R2 groups form a ring of 3 to 8 carbons and the ring may be substituted with 0 to 3 R3 groups; R3 is R3a, R3b, R3c or R3d, provided that when R3 is bound to a heteroatom, then R3 is R3c or R3d; R3a is —H, —F, —Cl, —Br, —I, —CF3, —CN, N3, —NO2, or —OR4; R3b is ═O, —O(R4), ═S, —N(R4), —N(O)(R4), —N(OR4), —N(O)(OR4), or —N(N(R4)(R4)); R3c is —R4, —N(R4)(R4), —SR4, —S(O)R4, —S(O)2R4, —S(O)(OR4), —S(O)2(OR4), —OC(R3b)R4, —OC(R3b)OR4, —OC(R3b)(N(R4)(R4)), —SC(R3b)R4, —SC(R3b)OR4, —SC(R3b)(N(R4)(R4)), —N(R4)C(R3b)R4, —N(R4)C(R3b)OR4, N(R4)C(R3b)(N(R4)(R4)), W3 or —R5W3; R3d is —C(R3b)R4, —C(R3b)OR4, —C(R3b)W3, —C(R3b)OW3 or —C(R3b)(N(R4)(R4)); R4 is —H, or an alkyl of 1 to 18 carbon atoms, alkenyl of 2 to 18 carbon atoms, or alkynyl of 2 to 18 carbon atoms; R5 is alkylene of 1 to 18 carbon atoms, alkenylene of 2 to 18 carbon atoms, or alkynylene of 2 to 18 carbon atoms; W3 is W4 or W5; W4 is R6, —C(R3b)R6, —C(R3b)W5, —SOM2R6, or —SOM2W5, wherein R6 is R4 wherein each R4 is substituted with 0 to 3 R3 groups; W5 is carbocycle or heterocycle wherein W5 is independently substituted with 0 to 3 R2 groups; and M2 is 0, 1 or 2; and pharmaceutically acceptable salts thereof.

    Flavone acetic acid analogs and methods of use thereof
    6.
    发明授权
    Flavone acetic acid analogs and methods of use thereof 失效
    黄酮乙酸类似物及其使用方法

    公开(公告)号:US06916831B2

    公开(公告)日:2005-07-12

    申请号:US10373399

    申请日:2003-02-24

    CPC分类号: C07D215/233

    摘要: Compounds are described having a structure according to Formula I or Formula II: wherein: X is selected from the group consisting of O, NH, and S; Y is selected from the group consisting of O and S; m is from 1 to 3; n is from 1 to 5; R1 and R3 are each independently selected from the group consisting of H, hydroxy, lower alky, lower alkoxy, halo, amino, aminoalkyl, nitro, heteroaryl, —OC(═O)R6, —O(C═O)OR6; and —O(C═O)N(R6)2; and R2 is side chain such as an acetic acid side chain, where p is O to 4, R5 is hydroxy, alkoxy or amino, and R6 is H or lower alkyl, or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of cancer.

    摘要翻译: 描述具有根据式I或式II的结构的化合物:其中:X选自O,NH和S; Y选自O和S; m为1〜3; n为1〜5; R 1和R 3各自独立地选自H,羟基,低级烷基,低级烷氧基,卤素,氨基,氨基烷基,硝基,杂芳基,-OC (-O)R 6,-O(CO)OR 6; 和-O(C-O)N(R 6)2。 并且R 2是侧链,例如乙酸侧链,其中p为0至4,R 5为羟基,烷氧基或氨基,R 6 或其低级烷基或其药学上可接受的盐。 该化合物可用于治疗癌症。

    Fluorinated quinolones as antimitotic and antitumor agents
    7.
    发明授权
    Fluorinated quinolones as antimitotic and antitumor agents 失效
    氟化喹诺酮作为抗生素和抗肿瘤剂

    公开(公告)号:US06569870B1

    公开(公告)日:2003-05-27

    申请号:US09669155

    申请日:2000-09-25

    IPC分类号: A61K3147

    CPC分类号: C07D491/04 C07D215/38

    摘要: The present invention provides fluorinated quinolones which are fluorinated on the phenyl group thereof, along with pharmaceutical formulations containing the same, methods of treating tumors or cancer by the administration of such compounds, and methods of inhibiting cellular mitosis by the administration of such compounds.

    摘要翻译: 本发明提供了在其苯基上氟化的氟化喹诺酮以及含有其的药物制剂,通过施用这些化合物治疗肿瘤或癌症的方法,以及通过施用这些化合物抑制细胞有丝分裂的方法。