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523 条记录 (耗时 0.039 秒)

    1-SULFONYL-3-PHENYLPYRAZOLE UND IHRE VERWENDUNG ALS HERBIZIDE UND ZUR DESIKKATION/DEFOLIATION VON PFLANZEN
    156.
    发明公开
    1-SULFONYL-3-PHENYLPYRAZOLE UND IHRE VERWENDUNG ALS HERBIZIDE UND ZUR DESIKKATION/DEFOLIATION VON PFLANZEN 失效
    -1-磺酰基-3-苯基吡唑及其作为除草剂和植物的干燥/落叶

    公开(公告)号：EP0931072A1

    公开(公告)日：1999-07-28

    申请号：EP97942003.0

    申请日：1997-09-09

    申请人： BASF AKTIENGESELLSCHAFT

    发明人： ZAGAR, Cyrill ,  HAMPRECHT, Gerhard ,  MENGES, Markus ,  MENKE, Olaf ,  SCHÄFER, Peter ,  WESTPHALEN, Karl-Otto ,  MISSLITZ, Ulf ,  WALTER, Helmut

    IPC分类号： A01N43 ,  C07D231 ,  C07D401 ,  C07D403 ,  C07D405

    CPC分类号： C07D231/18 ,  A01N43/56 ,  C07D231/24

    摘要： 1-sulfonyl-3-phenylpyrazoles having the formula (I) and their salts are disclosed. In the formula, R1 is C1-C4-alkyl, C1-C4-alkyl halide; R2 is C1-C4-alkyl, C1-C4-alkyl halide; R3 is H, CN, halogen, C¿1?-C4-alkyl; R?4¿ is H, halogen; R5 is H, CN, NO¿2?, halogen, C1-C4-alkyl, C1-C4-alkyl halide, C1-C4-alkoxy, C1-C4-alkoxy halide; X is a chemical bond, an optionally substituted methylene, ethylene, propan-1,3-diyl, ethen-1,2-diyl chain or an oxymethylene or thiamethylene chain bound to the phenyl ring by the heteroatom; R?6¿ is H, NO¿2?, CN, halogen, SO2-halogen, -O-Y-R?8¿, -O-CO-Y-R8, -N(Y-R8)(Z-R9), -N(Y-R8)-SO2-Z-R9, -N(SO¿2?-Y-R?8)(SO¿2-Z-R9), -N(Y-R8)-CO-Z-R9, -N(Y-R?8)(O-Z-R9¿), -S-Y-R8, -SO-Z-R8, -SO2-Y-R8, -SO2-O-Y-R8, -SO2-N(Y-R8)(Z-R9), -CO-Y-R8, -C(=NOR?10)-Y-R8¿, -(=NOR?10)-O-Y-R8¿, -CO-O-Y-R8, -CO-S-Y-R8, -CO-N(Y-R8)(Z-R9), -CO-N(Y-R?8)(O-Z-R9¿), -PO(O-Y-R8)2; R7 is H, or R?5 + XR6 or XR6 + R7¿ form, together with the C atoms of the phenyl ring which interconnect them, an annulated, optionally substituted carbocyclic or 5-/6-membered heterocyclic ring with 1-3 heteroatoms, whereas the cycle may also contain 1 or 2 CO-, CS- or SO¿2? ring members. These compounds are useful as herbicides, and for desiccating/defoliating plants.

    Selective beta 3 adrenergic agonists
    157.
    发明公开
    Selective beta 3 adrenergic agonists 审中-公开
    Selektive Beta-3 adrenergische Agonisten

    公开(公告)号：EP0921120A1

    公开(公告)日：1999-06-09

    申请号：EP98309868.2

    申请日：1998-12-02

    申请人： ELI LILLY AND COMPANY

    发明人： Crowell, Thomas Alan ,  Jones, Charles David ,  Shuker, Anthony John

    IPC分类号： C07D231/18 ,  C07D403/12 ,  C07D401/12 ,  C07D413/12 ,  C07D405/12 ,  A61K31/415

    CPC分类号： C07D401/12 ,  C07D231/18 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12

    摘要： The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective b 3 receptor agonists useful in the treatment of Type II diabetes and obesity. The invention provides compounds and methods of treating type II diabetes and obesity, comprising administering to a mammal in need thereof compounds of the Formula I:
    wherein:

    X 1 is -OCH 2 -, -SCH 2 -, or a bond;
    R 1 is a heterocycle of the formula:

    R 2 and R 3 are independently hydrogen, C 1 -C 4 alkyl, or aryl;
    R 4 is an optionally substituted heterocycle or a moiety selected from the group consisting of:

    X 2 is a bond, or a 1 to 5 carbon straight or branched alkylene;
    R 5 is hydrogen or C 1 -C 4 alkyl;
    R 6 is hydrogen or C 1 -C 4 alkyl;
    or R 5 and R 6 combine with the carbon to which each is attached to form a C 3 -C 6 cycloalkyl;
    or R 6 combines with X 2 and the carbon to which each is attached to form a C 3 -C 8 cycloalkyl;
    or R 6 combines with X 2 , R 4 , and the carbon to which each is attached to form:
    provided that R 5 is hydrogen;
    R 7 is hydrogen, hydroxy, cyano, oxo, CO n R 2 , CONHR 2 , C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkyl, C 1 -C 4 optionally substituted alkyl, (CH 2 ) n aryl, (CH 2 ) n heterocycle, (CH 2 ) n optionally substituted aryl, or (CH 2 ) n optionally substituted heterocycle;
    R 8 is independently hydrogen, halo, or C 1 -C 4 alkyl;
    R 9 is halo, CN, OR 10 , C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, CO 2 R 2 , CONR 11 R 12 , CONH(C 1 -C 4 alkyl or C 1 -C 4 alkoxy), SR 2 , CSNHR 2 , CSNR 11 R 12 , SO 2 R 2 , SOR 2 , NR 11 R 12 , optionally substituted aryl, optionally substituted heterocycle, or C 2 -C 4 alkenyl substituted with CN, CO 2 R 2 , or CONR 11 R 12 ;
    R 10 is C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, (CH 2 ) n C 3 -C 8 cycloalkyl, (CH 2 ) n aryl, (CH 2 ) n heterocycle, (CH 2 ) n C 3 -C 8 optionally substituted cycloalkyl, (CH 2 ) n optionally substituted aryl, or (CH 2 ) n optionally substituted heterocycle;
    R 11 and R 12 are independently hydrogen, C 1 -C 4 alkyl, aryl, (CH 2 ) n aryl, or combine with the nitrogen to which each is bound to form morpholinyl, piperidinyl, pyrrolidinyl, or piperazinyl;
    R 13 is hydrogen, halo, aryl, or C 1 -C 4 alkyl;
    m is 0 or 1;
    n is 0, 1, 2, or 3;
    or a pharmaceutically acceptable salt thereof.

    摘要翻译： 本发明在医药领域，特别是在治疗II型糖尿病和肥胖症方面。 更具体地，本发明涉及可用于治疗II型糖尿病和肥胖症的选择性b3受体激动剂。 本发明提供了治疗II型糖尿病和肥胖症的化合物和方法，包括向有需要的哺乳动物施用式I化合物：其中：X 1是-OCH 2 - ， - CH 2 - 或键; R 1是下式的杂环：R 2和R 3独立地是氢，C 1 -C 4烷基或芳基; R4是任选取代的杂环或选自下列的部分：CH 2 X 2是一个键，或一个到五碳直链或支链亚烷基; R5是氢或C1-C4烷基; R6是氢或C1-C4烷基; 或R 5和R 6与各自连接的碳结合形成C 3 -C 6环烷基; 或R6与X 2和各自连接的碳结合形成C 3 -C 8环烷基; 或R6与X2，R4和各自连接的碳结合形成：，条件是R 5为氢; R 2是氢，羟基，氰基，氧代，COnR 2，CONHR 2，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4任选取代的烷基，（CH 2）n芳基，（CH 2）n杂环，（CH 2） n任选取代的芳基或（CH 2）n任选取代的杂环; R8独立地是氢，卤素或C1-C4烷基; R9是卤素，CN，OR10，C1-C4烷基，C1-C4卤代烷基，CO2R2，CONR11R12，CONH（C1-C4烷基或C1-C4烷氧基），SR2，CSNHR2，CSNR11R12，SO2R2，SOR2，NR11R12，任选取代的芳基 ，任选取代的杂环，或被CN，CO 2 R 2或CONR 11 R 12取代的C 2 -C 4烯基; R 10是C 1 -C 4烷基，C 1 -C 4卤代烷基，（CH 2）n C 3 -C 8环烷基，（CH 2）n芳基，（CH 2）n杂环，（CH 2）n C 3 -C 8任选取代的环烷基，（CH 2）n任选取代的芳基或（ CH2）n任选取代的杂环; R 11和R 12独立地为氢，C 1 -C 4烷基，芳基，（CH 2）n芳基，或与各自键合的氮键合形成吗啉基，哌啶基，吡咯烷基或哌嗪基; R 13是氢，卤素，芳基或C 1 -C 4烷基; m为0或1; n为0,1,2或3; 或其药学上可接受的盐