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20 条记录 (耗时 0.032 秒)

    Substituted 1,2-dihydro-4h-3,1-benzoxazin-4-one derivatives inhibitors of interleukin 1
    6.
    发明授权
    Substituted 1,2-dihydro-4h-3,1-benzoxazin-4-one derivatives inhibitors of interleukin 1 失效
    取代的1,2-二氢-4h-3,1-苯并恶嗪-4-酮衍生物白细胞介素1抑制剂

    公开(公告)号：US4894374A

    公开(公告)日：1990-01-16

    申请号：US233186

    申请日：1988-08-17

    申请人： Jerauld S. Skotnicki ,  Ahmed F. Abdel-Magid

    发明人： Jerauld S. Skotnicki ,  Ahmed F. Abdel-Magid

    IPC分类号： A61K31/535 ,  C07D498/10

    CPC分类号： C07D498/10 ,  A61K31/535

    摘要： There are disclosed compounds of the formula: ##STR1## wherein X is CHR, NR.sup.1, S or O;R is hydrogen, lower alkenyl, pyridyl, quinolinyl, pyrazinyl, pyrimidinyl, quinoxalinyl or quinazolinyl, or substituted phenyl, naphthyl, pyridyl, quinolinyl, pyrazinyl, pyrimidinyl, quinoxalinyl or quinazolinyl, wherein the substituents are selected from halo, carboxy, lower alkoxycarbonyl, lower alkylsulfonyl, cyano, nitro and trifluoromethyl;R.sup.1 is lower alkenyl, pyridyl, pyrazinyl, pyrimidinyl, quinoxalinyl or quinazolinyl, or substituted phenyl, naphthyl, pyridyl, quinolinyl, pyrazinyl, pyrimidinyl, quinoxalinyl or quinazolinyl, wherein the substituents are selected from halo, carboxy, lower alkoxycarbonyl, lower alkylsulfonyl, cyano, nitro and trifluoromethyl; andR.sup.2 and R.sup.3 are each, independently, hydrogen, halo, lower alkyl, lower alkenyl, lower alkoxy, hydroxy, amino, mono- or diloweralkylamino, carboxy, lower alkoxycarbonyl, nitro or cyano;which, by virtue of their ability to inhibit interleukin 1, are of use as antiinflammatory agents and in treatment of disease states involving enzymatic tissue destruction, and there is also disclosed a method using such compounds in the treatment of immunoinflammatory, inflammatory/proliferative and enzymatic tissue destruction conditions.

    摘要翻译： 公开了下式的化合物：其中X是CHR，NR1，S或O; 吡啶基，喹喔啉基或喹唑啉基，或取代的苯基，萘基，吡啶基，喹啉基，吡嗪基，嘧啶基，喹喔啉基或喹唑啉基，其中取代基选自卤素，羧基，低级烷氧基羰基， 低级烷基磺酰基，氰基，硝基和三氟甲基; R 1是低级烯基，吡啶基，吡嗪基，嘧啶基，喹喔啉基或喹唑啉基，或取代的苯基，萘基，吡啶基，喹啉基，吡嗪基，嘧啶基，喹喔啉基或喹唑啉基，其中取代基选自卤素，羧基，低级烷氧基羰基，低级烷基磺酰基， ，硝基和三氟甲基; 卤素，低级烷基，低级烯基，低级烷氧基，羟基，氨基，单 - 或二 - 低级烷基氨基，羧基，低级烷氧羰基，硝基或氰基; 由于其抑制白细胞介素1的能力，可用作抗炎剂和治疗涉及酶组织破坏的疾病状态，并且还公开了使用这些化合物治疗免疫炎症，炎症/增殖和酶促的方法 组织破坏条件。

    Process for preparing 1, 5-diaryl-3-substituted pyrazoles
    7.
    发明授权
    Process for preparing 1, 5-diaryl-3-substituted pyrazoles 有权
    制备1,5-二芳基-3-取代的吡唑的方法

    公开(公告)号：US06613914B2

    公开(公告)日：2003-09-02

    申请号：US10086583

    申请日：2002-03-01

    申请人： Ahmed F. Abdel-Magid ,  Bruce D. Harris ,  Cynthia A. Maryanoff

    发明人： Ahmed F. Abdel-Magid ,  Bruce D. Harris ,  Cynthia A. Maryanoff

    IPC分类号： C07D23112

    CPC分类号： C07D231/12 ,  C07C51/083 ,  C07C59/88

    摘要： A process for making a compound of formula I wherein the substituents are as described in the specification comprising reacting a ketone of formula II with succinic anhydride and an alkoxide base to form a compound of formula III which is reacted with a compound of formula IV to form a compound of V and reacting with an alcohol to form the corresponding ester of formula VI and reacting the ester with N-methylhydroxylamine.

    摘要翻译： 制备式I化合物的方法，其中取代基如说明书中所述包括使式II的酮与琥珀酸酐和醇盐碱反应形成式III化合物，其与式IV化合物反应形成 钒的化合物与醇反应以形成相应的式VI的酯，并使酯与N-甲基羟胺反应。