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233 条记录 (耗时 0.032 秒)

    5-AROYLNAPHTHALENE DERIVATIVES
    67.
    发明授权
    5-AROYLNAPHTHALENE DERIVATIVES 失效
    5-AROYLPHPHALALIN DERIVATE

    公开(公告)号：EP0966437B1

    公开(公告)日：2002-06-12

    申请号：EP98905325.1

    申请日：1998-01-21

    申请人： F.HOFFMANN-LA ROCHE AG

    发明人： ROTSTEIN, David, Mark ,  SJOGREN, Eric, Brian

    IPC分类号： C07C311/29 ,  C07C317/24 ,  C07C317/22 ,  C07C311/51 ,  C07D295/12 ,  C07D213/42 ,  A61K31/18 ,  A61K31/10 ,  A61K31/275 ,  A61K31/235 ,  A61K31/435

    CPC分类号： C07D207/26 ,  C07C311/16 ,  C07C311/29 ,  C07C311/51 ,  C07C317/22 ,  C07C317/24 ,  C07C317/44 ,  C07C323/22 ,  C07C323/67 ,  C07C2601/04 ,  C07C2601/14 ,  C07D211/58 ,  C07D213/42 ,  C07D295/13 ,  C07D295/26 ,  C07D307/46 ,  C07D307/52 ,  C07D333/22 ,  C07D405/06

    摘要： The present invention relates to certain 5-aroylnaphthalene derivatives of formula (I), wherein A is a bond, -CH2-, -CH(OH)-, -C=NOR4-, -C(O)-, -NR5-, -O-, or -S(O)¿n?- where n is an integer from 0 to 2, R?4¿ is hydrogen or alkyl, and R5 is hydrogen, alkyl, or acyl; Z is a group represented by formula (B), (C), (D), or (E), where n1 is 0 to 3; X is O or S; R?6 and R7¿ are independently selected from hydrogen, alkyl, halogenalkyl, cycloalkyl, cycloalkylalkyl, acyl, alkylthio, cycloalkylthio, cycloalkylalkylthio, alkoxy, cycloalkyloxy, cycloalkylalkyloxy, halogenalkyloxy, alkenyl, halogen, cyano, nitro, hydroxy, or -NR9R10 where R?9 and R10¿ are independently hydrogen, alkyl, or acyl; or R?6 and R7¿ when they are adjacent to each other form methylenedioxy or ethylenedioxy; R8 is hydrogen, alkyl, halogenalkyl, alkoxy, cycloalkyloxy, halogenalkyloxy, alkylthio, cycloalkylthio, nitro, cyano, hydroxy, or halogen; R1 is hydrogen, alkyl, alkenyl, alkynyl, halogenalkyl, cycloalkyl, cycloalkylalkyl, alkoxy, alkenyloxy, cycloalkyloxy, cycloalkylalkyloxy, halogenalkyloxy, hydroxyalkyloxy, alkoxyalkyloxy, alkylthio, cycloalkylthio, cycloalkylalkylthio, hydroxy, halogen, cyano, carboxy, alkoxycarbonyl, acyl, -C=NOR?4, -NR9R10, -CONR9R10¿, -OCONR9R10, or -OSO¿2R?11 where R?4, R9, and R10¿ are as previously defined and R11 is alkyl, cycloalkyl, or halogenalkyl; R2 is hydrogen, alkyl, alkoxy, halogen, nitro, or -NR?9R10; and R3¿ is -SO¿2R?12 or -SO¿2?NR?13R14¿ where R12 is alkyl, hydroxyalkyl, alkoxyalkyl, carboxyalkyl, or alkoxycarbonylalkyl; R13 is hydrogen, alkyl, or acyl; and R14 is hydrogen, alkyl, halogenalkyl, cycloalkyl, cycloalkylalkyl, alkenyl, hydroxyalkyl, alkoxyalkyl, alkoxycarbonylalkyl, amino, aminoalkyl, aryl, aralkyl, heteroaralkyl, heterocyclo, heterocycloalkyl, acyl, hydroxy, or alkoxy; or R?13 and R14¿ together with the nitrogen atom to which they are attached optionally form a heterocycloamino group; that are inhibitors of prostaglandin G/H synthase, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.

    摘要翻译： 本发明涉及式（I）的某些5-芳酰基萘衍生物：其为前列腺素G / H合成酶的抑制剂，含有它们的药物组合物，其使用方法和制备这些化合物的方法。

    SUBSTITUTED $g(b)-DIKETONES AND THEIR USE
    68.
    发明公开
    SUBSTITUTED $g(b)-DIKETONES AND THEIR USE 有权
    取代的β-二酮及其应用

    公开(公告)号：EP1091933A1

    公开(公告)日：2001-04-18

    申请号：EP99934722.2

    申请日：1999-06-30

    申请人： ORION CORPORATION

    发明人： AHO, Päivi ,  BÄCKSTRÖM, Reijo ,  KOPONEN, Anita ,  LINDEN, Inge-Britt ,  LOTTA, Timo ,  LÖNNBERG, Kari ,  PIPPURI, Aino ,  POHTO, Pentti

    IPC分类号： C07C317/24 ,  A61K31/12

    CPC分类号： C07C317/24

    摘要： The invention relates to the compounds of formula (I) wherein one of X1 and X2 is MeSO2 and the other one is hydrogen or halogen and X3 is hydrogen or halogen. These compounds have been found to be useful in the prevention and the treatment of respiratory diseases, especially asthma, ARDS (Acute Respiratory Distress Syndrome), COPD (chronic obstructive pulmonary diseases), allergic rhinitis and related inflammatory conditions. More specifically, the invention relates to the use of said compound in the prevention and the treatment of asthma in steroid-resistant patients. The invention also relates to pharmaceutical formulations used in the treatment of said diseases.