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    SULFONE LIVER X-RECEPTOR MODULATORS
    1.
    发明申请
    SULFONE LIVER X-RECEPTOR MODULATORS 审中-公开
    SULFONE肝脏X受体调节剂

    公开(公告)号：WO2003099775A1

    公开(公告)日：2003-12-04

    申请号：PCT/US2003/016381

    申请日：2003-05-23

    Applicant: PHARMACIA CORPORATION ,  BECKER, Daniel, P. ,  DECRESCENZO, Gary, A. ,  MALECHA, James, W. ,  MIYASHIRO, Julie, M. ,  VAN CAMP, Jennifer, Ann ,  COLLINS, Joe, T.

    Inventor： BECKER, Daniel, P. ,  DECRESCENZO, Gary, A. ,  MALECHA, James, W. ,  MIYASHIRO, Julie, M. ,  VAN CAMP, Jennifer, Ann ,  COLLINS, Joe, T.

    IPC: C07C317/22

    CPC classification number: C07C317/22 ,  C07C317/24

    Abstract: The present invention is directed to slective LXR modulators, small molecule compounds corresponding to Formula (I) wherein: R 1 and R 2 are independently hydrogen or optionally substituted alkyl, alkenyl, aryl, acyi, or alkaryl; R 3 is optionally substituted alkyl or aryl; each R 4 is independently hydrogen, alkyl, aryl,.heteroaryl, hydroxy, alkoxy, cyano, nitro, amino, alkenyl, alkynyl, amido, alkylcarbonyl, alkoxycarbonyl, aryloxycarbonyl, haloalkylcarbonyl, alkylthiocarbonyl, arylthlocarbonyl, alkyl optionally substituted with one or more substituent selected from lower alkyl, halogen, hydroxyl, haloalkyl, cyano, nitro, carboxyl, amino, alkoxy and aryl, or aryl optionally substituted with one or more substituent selected from hydrogen, halogen, haloalkyl, hydroxy, lower alkyl, alkoxy, methylene dioxy, ethylenedioxy, cyano, nitro, atkylthio, alkylsulfonyl, sulfonic acid, sulfonamide, carboxyl derivatives, amino, aryl and heteroaryl; and a is 0-4, and is further directed to a process of treating a condition in a mammal that is modulated by LXR using a therapeutically effective dose of a compound of Formula I.

    Abstract translation: 本发明涉及选择性LXR调节剂，对应于式（I）的小分子化合物，其中：R 1和R 2独立地为氢或任选取代的烷基，烯基，芳基，酰基或烷芳基; R3是任选取代的烷基或芳基; 每个R 4独立地是氢，烷基，芳基，杂芳基，羟基，烷氧基，氰基，硝基，氨基，烯基，炔基，酰氨基，烷基羰基，烷氧基羰基，芳氧基羰基，卤代烷基羰基，烷硫基羰基，芳基羰基羰基，任选地被一个或多个取代基 由低级烷基，卤素，羟基，卤代烷基，氰基，硝基，羧基，氨基，烷氧基和芳基或任选被一个或多个选自氢，卤素，卤代烷基，羟基，低级烷基，烷氧基，亚甲基二氧基，亚乙二氧基 氰基，硝基，烷硫基，烷基磺酰基，磺酸，磺酰胺，羧基衍生物，氨基，芳基和杂芳基; a为0-4，并且还涉及使用治疗有效剂量的式I化合物治疗由LXR调节的哺乳动物状况的方法。

    SUBSTITUTED PYRAZOLYL BENZENESULFONAMIDES FOR THE TREATMENT OF INFLAMMATION
    3.
    发明申请
    SUBSTITUTED PYRAZOLYL BENZENESULFONAMIDES FOR THE TREATMENT OF INFLAMMATION 审中-公开
    用于治疗炎症的取代的吡唑并苯并呋喃

    公开(公告)号：WO1995015316A1

    公开(公告)日：1995-06-08

    申请号：PCT/US1994012720

    申请日：1994-11-14

    Applicant: G. D. SEARLE & CO. ,  TALLEY, John, J. ,  PENNING, Thomas, D. ,  COLLINS, Paul, W. ,  ROGIER, Donald, J., Jr. ,  MALECHA, James, W. ,  MIYASHIRO, Julie, M. ,  BERTENSHAW, Stephen, R. ,  KHANNA, Ish, K. ,  GRANETS, Matthew, J. ,  ROGERS, Roland, S. ,  CARTER, Jeffery, S. ,  DOCTER, Stephen, H. ,  YU, Stella, S.

    Inventor： G. D. SEARLE & CO.

    IPC: C07D231/12

    CPC classification number: C07D495/04 ,  C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D231/54 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04

    Abstract: A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by formula (II), whrein R is selected from hydrido, alkyl, haloalkyl, alkoxycarbonyl, cyano, cyanoalkyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, cycloalkylaminocarbonyl, arylaminocarbonyl, carboxyalkylaminocarbonyl, carboxyalkyl, aralkoxycarbonylalkylaminocarbonyl, aminocarbonylalkyl, alkoxycarbonylcyanoalkenyl and hydroxyalkyl; wherein R is selected from hydrido, alkyl, cyano, hydroxyalkyl, cycloalkyl, alkylsulfonyl and halo; and wherein R is selected from aralkenyl, aryl, cycloalkyl, cycloalkenyl and heterocyclic; wherein R is optionally substituted at a substitutable position with one or more radicals selected from halo, alkylthio, alkylsulfonyl, cyano, nitro, haloalkyl, alkyl, hydroxyl, alkenyl, hydroxyalkyl, carboxyl, cycloalkyl, alkylamino, dialkylamino, alkoxycarbonyl, aminocarbonyl, alkoxy, haloalkoxy, sulfamyl, heterocyclic and amino; provided R and R are not both hydrido; further provided that R is not carboxyl or methyl when R is hydrido and when R is phenyl; further provided that R is not triazolyl when R is methyl; further provided that R is not aralkenyl when R is carboxyl, aminocarbonyl or ethoxycarbonyl; further provided that R is not phenyl when R is methyl and R is carboxyl; and further provided that R is not unsubstituted thienyl when R is trifluoromethyl; or a pharmaceutically acceptable salt thereof.

    Abstract translation: 描述了一类吡唑基苯磺酰胺化合物用于治疗炎症和炎症相关疾病。 特别感兴趣的化合物由式（II）定义，R 2选自氢，烷基，卤代烷基，烷氧基羰基，氰基，氰基烷基，羧基，氨基羰基，烷基氨基羰基，环烷基氨基羰基，芳基氨基羰基，羧基烷基氨基羰基，羧基烷基，芳烷氧基羰基烷基氨基羰基，氨基羰基烷基， 烷氧羰基氰基烯基和羟烷基; 其中R 3选自氢化，烷基，氰基，羟基烷基，环烷基，烷基磺酰基和卤素; 其中R 4选自芳烯基，芳基，环烷基，环烯基和杂环; 其中R 4在可取代位置任选被一个或多个选自卤素，烷硫基，烷基磺酰基，氰基，硝基，卤代烷基，烷基，羟基，烯基，羟基烷基，羧基，环烷基，烷基氨基，二烷基氨基，烷氧基羰基，氨基羰基 ，烷氧基，卤代烷氧基，氨磺酰基，杂环和氨基; 条件是R 2和R 3都不是氢的; 进一步提供当R 3是氢的时，当R 4是苯基时，R 2不是羧基或甲基; 进一步提供当R 2是甲基时，R 4不是三唑基; 进一步提供当R 2是羧基时，R 4不是芳烯基，氨基羰基或乙氧基羰基; 进一步提供当R 2是甲基且R 3是羧基时，R 4不是苯基; 并且进一步提供当R 2为三氟甲基时R 4为未取代的噻吩基; 或其药学上可接受的盐。

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