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9 条记录 (耗时 0.021 秒)

    Substituted quinolines as antitumor agents
    3.
    发明申请
    Substituted quinolines as antitumor agents 失效

    公开(公告)号：US20070021407A1

    公开(公告)日：2007-01-25

    申请号：US11374423

    申请日：2006-03-14

    申请人： Francis Boyle ,  Keith Gibson ,  Kevin Foote

    发明人： Francis Boyle ,  Keith Gibson ,  Kevin Foote

    IPC分类号： A61K31/496 ,  A61K31/4709 ,  A61K31/4704 ,  C07D403/02

    CPC分类号： C07D215/56 ,  C07D215/54 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

    摘要： The invention provides a compound of Formula (Ia), or a pharmaceutically acceptable salt, pro-drug or solvate thereof. wherein: n is 0 or 1; Y is selected from —NH—, —O—, —S—, or —NR7— where R7 is alkyl of 1-6 carbon atoms; R5 is cyano, fluoro, chloro or bromo; R6 is cycloalkyl of 3 to 7 carbon atoms, which may be optionally substituted with one or more alkyl of 1 to 6 carbon atom groups; or is a pyridinyl, pyrimidinyl, or phenyl ring; wherein the pyridinyl, pyrimidinyl, or phenyl ring may be optionally mono- di-, or tri-substituted; or R6 is a group —R8—X—R9 where R8 is a divalent cycloalkyl of 3 to 7 carbon atoms, which may be optionally further substituted with one or more alkyl of 1 to 6 carbon atom groups; or is a divalent pyridinyl, pyimidinyl, or phenyl ring; wherein the pyridinyl, pyrimidinyl, or phenyl ring may be optionally further substituted with one or more groups; and where X is selected from —NH—, —O—, —S—, CH2 or —NR7′— where R7′ is alkyl of 1-6 carbon atoms, and R9 is a group (CH2)mR10 where m is 0, or an integer of from 1-3 and R10 is an optionally substituted aryl or optionally substituted cycloalkyl ring of up to 10 carbon atoms, or R10 is a optionally substituted heterocyclic ring or an N-oxide of any nitrogen containing ring; R1, R2, R4 are independently selected from hydrogen, hydroxy, halogeno, cyano, nitro, trifluoromethyl, C1-3alkyl, —NR11R12— (wherein R11 and R12, which may be the same or different each represents hydrogen, or C1-3alkyl), or a group R13—X1—(CH2)x wherein x is 0 or an integer of from 1 to 3, X1 represents a direct bond, —O—, —CH2—, —OC(O)—, —C(O)—, —S—, —SO—, —SO2—, —NR14C(O)—, —NR14C(O)O—, —C(O)NR15—, —C(O)ONR15—, —SO2NR16—, —NR17SO2— —NR18— or —NR18NR18— (wherein R14, R15, R16, R17 and R18 each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl)), and R13 is hydrogen, optionally substituted hydrocarbyl, or optionally substituted heterocyclyl; and R3 is selected from (i) a group of formula —X1—Rx—(OH)p where X1 is as defined above, Rx is an alkylene, alkenylene or alkynylene chain, optionally interposed with a heteroatom or a heteocyclic ring and p is 1 or 2; (ii) a group of formula R13a—(CH2)y—X1—(CH2)x where R13 a is as defined for R13 above, and X1 and x are as defined above, y is 0 or an integer between 1 and 5, wherein (CH2)y is optionally interposed by an X1 group; (iii) a group of formula —X1—Ry—NRz—Ry′—S—Ry″ where X1 is as defined above, Ry, Ry′ and Ry″ are independently selected from alkyl, alkenyl or alkynyl chains, and Rz is hydrogen or alkyl, or Rz and Ry″ are joined together to form an optionally substituted nitrogen and sulphur containing ring; (iv) a group of formula —X1—Rx′—(C3-6cycloalkyl) where X1 is as defined above and Rx′ is an alkylene, alkenylene or alkynylene chain, optionally interposed with a heteroatom a group of the formula —X1—C1-5alkyl where X1 is as defined above and C1-5alkyl is substituted by one more substituents independently selected from chloro and cyano; (v) a group of the formula —X1—C1-3alkyl-CO—NR18NR18—R20 where R18 is as defined above and R20 is selected from hydrogen or C1-5alkoxycarbonyl; or (vi) a heterocyclic ring. The invention also provides a process for the preparation of a compound of Formula (Ia), pharmaceutical compositions of a compound of Formula (Ia) and methods for the treatment or prevention of cancer comprising administering an effective amount of a compound of Formula (1a).

    Colchinol derivatives as vascular damaging agents
    6.
    发明申请
    Colchinol derivatives as vascular damaging agents 审中-公开

    公开(公告)号：US20060128633A1

    公开(公告)日：2006-06-15

    申请号：US11256018

    申请日：2005-10-24

    申请人： Peter Davis ,  Jean-Claude Arnould ,  Francis Boyle

    发明人： Peter Davis ,  Jean-Claude Arnould ,  Francis Boyle

    IPC分类号： A61K38/05 ,  A61K31/445 ,  A61K31/40 ,  A61K31/22 ,  A61K31/663

    CPC分类号： A61K31/165

    摘要： The invention relates to the use of compounds of formula (I): wherein X is —C(O)—, —C(S)—, —C═NOH, or —CH(R7)— wherein R7 is hydrogen, hydroxy, C1-7alkoxy, —OR8 or —NR8R9 (wherein R8 is a group —Y1R10 (wherein Y1 is a direct bond, —C(O)—, —C(S)—, —S—, —C(O)O—, —C(O)NR11—, —SO2— or —SO2NR12— (wherein R11 and R12, which may be the same or different, each independently represents hydrogen; C1-3alkyl or C1-3alkoxyC2-3alkyl) and R10 is as defined herein, R9 includes hydrogen; R11, R12 and R13 are as defined herein and are preferably methyl; R4, R5 and R6 are as defined herein with the proviso that R5 is not hydroxy, alkoxy, substituted alkoxy, —OPO3H2, —O—C1-7alkanoyl or benzyloxy; and salts thereof in the manufacture of a medicament for use in the production of a vascular damaging effect in warm-blooded animals such as humans. The present invention further relates to compounds of the formula (I), pharmaceutical compositions containing them, processes for their preparation and to a method of treatment using the compounds to produce a vascular damaging effect in a warm-blooded animal such as a human. The compounds of formula (I) and the pharmaceutically acceptable salts thereof may be useful in the treatment of a number of disease states including cancer and rheumatoid arthritis.

    3-Mercaptopyrrolidines as farnesyl protein transferase inhibitors
    9.
    发明申请
    3-Mercaptopyrrolidines as farnesyl protein transferase inhibitors 审中-公开
    3-巯基吡咯烷酮作为法呢基蛋白转移酶抑制剂

    公开(公告)号：US20050209217A1

    公开(公告)日：2005-09-22

    申请号：US11124278

    申请日：2005-05-09

    申请人： Francis Boyle ,  James Wardleworth

    发明人： Francis Boyle ,  James Wardleworth

    IPC分类号： A61K31/40 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/496 ,  A61P25/00 ,  A61P35/00 ,  A61P43/00 ,  C07D207/12 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D417/12 ,  A61K31/551 ,  C07D43/02

    CPC分类号： C07D401/12 ,  C07D207/12 ,  C07D403/06 ,  C07D417/12

    摘要： The present invention relats to inhibitors of ras farnesylation of Formula (I) wherein: R1 is for example H and further values as defined in the specification; R2 is for example H and further values as defined in the specification; R3 is for example H or a substituent having values as defined in the specification; p is 0-3 in which R3 values can be the same or different; L is a linking moiety for example —CH2—NH— and further values as defined in the specification; A is selected from phenyl; naphthyl; a 5-10 membered monocyclic or bicyclic heteroaryl ring containing up to 5 heteroatoms where the heteroatoms are independently selected from O, N and S; or a —S—S— dimer thereof when R2=H; or a N-oxide or a pharmaceutically-acceptable salt, prodrug or solvate thereof. Processes for their preparation, their use as therapeutic agents and pharmaceutical compositions containing them. A particular use is in cancer therapy.

    摘要翻译： 本发明相对于式（I）的ras法呢基化抑制剂：其中：R 1为例如H和本说明书中定义的其它值; R 2是例如H和说明书中定义的其它值; R 3是例如H或具有本说明书中定义的值的取代基; p为0-3，其中R 3 3可以相同或不同; L是例如-CH 2 -NH-的连接部分和如说明书中定义的进一步的值; A选自苯基; 萘基; 含有多达5个杂原子的5-10元单环或双环杂芳基环，其中杂原子独立地选自O，N和S; 或其-S-S-二聚体时，R 2 = H; 或N-氧化物或其药学上可接受的盐，前药或溶剂化物。 其制备方法，用作治疗剂和含有它们的药物组合物。 一个特别的用途是癌症治疗。