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    ARYLSULFONANILIDE PHOSPHATES
    5.
    发明公开
    ARYLSULFONANILIDE PHOSPHATES 有权
    芳基磺酰胺磷酸盐

    公开(公告)号：EP1090014A1

    公开(公告)日：2001-04-11

    申请号：EP99928777.4

    申请日：1999-06-16

    申请人： Tularik Inc.

    发明人： HOUZE, Jonathan, B.

    IPC分类号： C07F9/12 ,  A61K31/66 ,  C07F9/6506 ,  C07F9/655

    CPC分类号： C07F9/65517 ,  C07F9/12 ,  C07F9/65068

    摘要： The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.

    摘要翻译： 本发明提供了涉及新型芳基磺酰苯胺衍生物的化合物，组合物和方法及其作为药理活性剂的用途。 该组合物特别用作治疗疾病，特别是癌症，牛皮癣，血管再狭窄，感染，动脉粥样硬化和高胆固醇血症的药理学试剂，或作为用于开发这些试剂的先导化合物。

    ARYLSULFONANILIDE PHOSPHATES
    7.
    发明授权
    ARYLSULFONANILIDE PHOSPHATES 有权
    ARYLSULFONANILID磷酸

    公开(公告)号：EP1090014B1

    公开(公告)日：2003-09-03

    申请号：EP99928777.4

    申请日：1999-06-16

    申请人： Tularik Inc.

    发明人： HOUZE, Jonathan, B.

    IPC分类号： C07F9/12 ,  A61K31/66 ,  C07F9/6506 ,  C07F9/655

    CPC分类号： C07F9/65517 ,  C07F9/12 ,  C07F9/65068

    摘要： The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.

    PPAR-GAMMA MODULATORS
    8.
    发明公开
    PPAR-GAMMA MODULATORS 有权
    PPAR-γ调节剂

    公开(公告)号：EP1053227A1

    公开(公告)日：2000-11-22

    申请号：EP99901492.1

    申请日：1999-01-20

    申请人： TULARIK, INC.

    发明人： DE LA BROUSE-ELWOOD, Fabienne ,  JAEN, Juan, C. ,  MCGEE, Lawrence, R. ,  MIAO, Shi-Chang ,  RUBENSTEIN, Steven, Marc ,  CHEN, Jin-Long ,  CUSHING, Timothy, D. ,  FLYGARE, John, A. ,  HOUZE, Jonathan, B. ,  KEARNEY, Patrick, C.

    IPC分类号： C07D213/65 ,  A61K31/435 ,  C07D239/34 ,  C07D213/643 ,  C07D233/70 ,  C07D413/12

    CPC分类号： C07D213/70 ,  C07C311/21 ,  C07D213/65 ,  C07D215/20 ,  C07D217/04 ,  C07D405/12

    摘要： Modulators of PPARη activity are provided having formula (I): in which the symbol Ar represents an aryl group; the letter X represents a divalent linkage selected from the group consisting of =C1-C6alkylene, -(C1-C6)alkylenoxy, -O-, -C(O)-, -N(R11)-, -N(R11)C(O)-, -S(O)¿k?- and a single bond, in which R?11¿ is a member selected from the group consisting of hydrogen, alkyl, heteroalkyl, and arylalkyl and the subscript k is an integer of from 0 to 2. The letter Y, in formula (I) represents a divalent linkage selected from the group consisting of alkylene, -O-, -C(O)-, -N(R12)-S(O)¿m?-, -N(R?13¿)-S(O)¿m-N(R?13)-, -N(R12)C(O)-, -S(O)¿n?-, a single bond, and combinations thereof in which R?12 and R13¿ are members independently selected from the group consisting of hydrogen, alkyl, heteroalkyl and arylalkyl; and the subscripts m and n independently integers of from 0 to 2. The symbol R1 represents a member selected from the group consisting of hydrogen, alkyl, heteroalkyl, aryl, arylalkyl, -CO¿2R?14, -CO(R)14, -C(O)NR15R16, -S(O)¿p-R?14, -S(O)¿q?-NR?15R16¿, -O-C(O)-OR17, -O-C(O)-R17, -O-C(O)-NR?15R16, -N(R14¿)-C(O)-NR?15R16, -N(R14¿)-C(O)-R17 and -N(R14)-C(O)-OR17, in which R14 is a member selected from the group consisting of hydrogen, alkyl, heteroalkyl, aryl and arylalkyl, and R?15 and R16¿ are members independently selected from the group consisting of hydrogen, alkyl, heteroalkyl, aryl and arylalkyl, or taken together with the nitrogen to which each is attached from a 5-, 6- or 7-membered ring. The symbol R17 represents a member selected from the group consisting of alkyl, heteroalkyl, aryl and arylalkyl. Additionally, for the R1 groups described above, the subscript p is an integer of from 0 to 3, and the subscript q is an integer of from 1 to 2. The symbol R2 represents a member selected from the group consisting of alkyl, heteroalkyl, aryl and arylalkyl. In another aspect, the present invention provides compounds of formula (I), as well as pharmaceutical compositions containing the compounds described above for the treatment of conditions such as type II diabetes and obesity.

    ARYLSULFONANILIDE UREAS
    9.
    发明公开
    ARYLSULFONANILIDE UREAS 有权

    公开(公告)号：EP1115701A1

    公开(公告)日：2001-07-18

    申请号：EP99969408.6

    申请日：1999-09-21

    申请人： Tularik Inc.

    发明人： HOUZE, Jonathan, B.

    IPC分类号： C07C311/21 ,  C07D231/38 ,  C07D307/52 ,  C07D295/20 ,  C07D277/48 ,  C07D249/14 ,  C07D257/06 ,  C07D285/12 ,  A61K31/18 ,  A61K31/33

    CPC分类号： C07D231/38 ,  C07C311/21 ,  C07D295/215 ,  C07D307/52

    摘要： The invention provides compounds, compositions and methods relating to arylsulfonanilide derivatives having the formula (I) or a pharmaceutically acceptable salt thereof, wherein Ar is a member selected from the group consisting of (a), (b), (c), and (d) and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.

    摘要翻译： 本发明提供涉及具有式（I）的芳基磺酰苯胺衍生物或其药学上可接受的盐的化合物，组合物和方法，其中Ar是选自（a），（b），（c）和（ d）及其作为药理活性剂的用途。 该组合物特别用作治疗疾病，特别是癌症，牛皮癣，血管再狭窄，感染，动脉粥样硬化和高胆固醇血症的药理学试剂，或作为用于开发这些试剂的先导化合物。