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    SUBSTITUTED 10-ARYL-11H-BENZO[B]FLUORENES AND 7-ARYL-5,6-DIHYDRO-BENZ[A]ANTHRACENES FOR SELECTIVE EFFECTS ON ESTROGEN RECEPTORS
    61.
    发明公开
    SUBSTITUTED 10-ARYL-11H-BENZO[B]FLUORENES AND 7-ARYL-5,6-DIHYDRO-BENZ[A]ANTHRACENES FOR SELECTIVE EFFECTS ON ESTROGEN RECEPTORS 有权
    替代品10-ARYL-11H-BENZO [B] FLUORENEFÜRSELEKTIVE EFFEKTE AUF ESTROGEN-RECEPTOREN

    公开(公告)号：EP1478613A2

    公开(公告)日：2004-11-24

    申请号：EP03706624.8

    申请日：2003-02-14

    申请人： Akzo Nobel N.V.

    发明人： LOOZEN, Hubert Jan Jozef,N.V. Organon ,  WAGENER, Markus,N.V. Organon ,  VEENEMAN, Gerrit Herman,N.V. Organon ,  ZWART, Eduard Willem,N.V. Organon

    IPC分类号： C07C39/17 ,  C07C39/42 ,  C07C43/23 ,  C07C323/18 ,  C07D295/08 ,  A61K31/05 ,  A61P5/30

    CPC分类号： C07D239/42 ,  C07C39/17 ,  C07C43/225 ,  C07C43/23 ,  C07C49/753 ,  C07C217/58 ,  C07C323/18 ,  C07C2603/40 ,  C07C2603/42 ,  C07D211/70 ,  C07D277/62 ,  C07D295/088 ,  C07D317/54

    摘要： This invention provides a compound, or its possible salt, having the formula, wherein: Re and 'Re are OH, optionally independently etherified or esterified; Z is -CH2CH2- or -C(R4,R5)- , wherein R4 and R5 are independently H, (1C-2C)alkyl or form together a spiro(3C-5C)cycloalkyl; R1 is H, halogen, CF3 , or (1C-4C)alkyl; R2 and R3 are independently H, halogen, -CF3, -OCF3, (1C-8C)alkyl, hydroxy, (1C-8C)alkyloxy, aryloxy, aryl(1C-8C)alkyl, halo (1C-8C)alkyl, -O(CH2)mX, wherein X is halogen or phenyl and m = 2-4; -O(CH2)mNRaRb , -S(CH2)mNRaRb or -(CH2)mNRaRb, wherein m = 2-4 and wherein Ra, Rb are independently (1C-8C)alkyl, (2C-8C)alkenyl, (2C-8C)alkynyl, or aryl, which alkyl, alkenyl and aryl can optionally be substituted with halogen, -CF3, -OCF3, -CN, -NO2, -OH, (1C-8C)alkoxy, aryloxy, carboxyl, (1C-8C)alkylthio, carboxylate, (1C-8C)alkyl, aryl, aryl(1C-8C)alkyl or halo (1C-8C) alkyl; or Ra and Rb form a 3-8 membered ring structure, optionally substituted with halogen, -CF3, -OCF3, -CN, -NO2, hydroxy, hydroxy(1C-4C)alkyl, (1C-8C)alkoxy, aryloxy, (1C-8C)alkylthio, carboxyl, carboxylate, (1C-8C)alkyl, aryl, aryl(1C-8C)alkyl, halo (1C-8C) alkyl.

    摘要翻译： 本发明提供具有下式的化合物或其可能的盐，其中：R e和R e是OH，任选地独立地醚化或酯化; Z是-CH 2 CH 2 - 或-C（R 4，R 5） - ，其中R R 4和R 5独立地为H，（1C-2C）烷基或一起形成螺（3C-5C）环烷基; R 1是H，卤素，CF 3或（1C-4C）烷基; R 2和R 3独立地是H，卤素，-CF 3，-OCF 3，（1C- 8C）烷基，羟基，（1C-8C）烷氧基，芳氧基，芳基（1C-8C）烷基，卤代（1C-8C）烷基，-O（CH 2 CH 2） SUB X，其中X是卤素或苯基，m = 2-4; -O（CH 2）2 - ， - （CH 2 CH 2）n - 或 - （CH 2 2）m - 或 - - - - - （CH 2） 其中m = 2-4，并且其中R a，R b，R b各自独立地是（1C -8C）烷基，（2C-8C）烯基，（2C-8C）炔基或芳基，其中烷基，烯基和芳基可任选被卤素取代，-CF 3，-OCF

    NOVEL COMPOUNDS
    63.
    发明公开
    NOVEL COMPOUNDS 审中-公开
    新化合物

    公开(公告)号：EP1434756A1

    公开(公告)日：2004-07-07

    申请号：EP02775639.4

    申请日：2002-10-02

    申请人： AstraZeneca AB

    发明人： CONNOLLY, Stephen ,  ERNST, Glen

    IPC分类号： C07C217/56 ,  C07C323/32 ,  C07C255/54 ,  C07D213/62 ,  C07D213/84 ,  C07D295/08 ,  A61K31/135 ,  A61K31/4412 ,  A61P29/00 ,  A61P25/00 ,  A61P19/02

    CPC分类号： C07C323/32 ,  C07C217/58 ,  C07C217/90 ,  C07C255/54 ,  C07C2602/08 ,  C07C2602/10 ,  C07D213/85

    摘要： There are provided novel compounds of formula (I) wherein A, R?1, R3, R4, R5¿, T, U, V, W, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory diseases, pain and CNS diseases.

    摘要翻译： 提供了式（I）的新化合物及其药学上可接受的盐，其中A，R 1，R 3，R 4，R 5，T，U，V，W，X和Y如说明书中所定义。 以及它们的制备方法，含有它们的组合物以及它们在治疗中的用途。 这些化合物是一氧化氮合酶的抑制剂，因此特别适用于治疗或预防炎性疾病，疼痛和中枢神经系统疾病。

    HYDRAZINE DERIVATIVES
    68.
    发明授权
    HYDRAZINE DERIVATIVES 有权
    肼衍生物

    公开(公告)号：EP1133471B1

    公开(公告)日：2003-09-17

    申请号：EP99959293.4

    申请日：1999-11-20

    申请人： F. HOFFMANN-LA ROCHE AG

    发明人： BROADHURST, Michael, John ,  JOHNSON, William, Henry ,  WALTER, Daryl, Simon

    IPC分类号： C07C311/49 ,  C07D213/34 ,  C07D295/08 ,  A61K31/18 ,  A61K31/44 ,  A61K31/535

    CPC分类号： C07D295/088 ,  C07C311/49 ,  C07D213/34 ,  Y10S514/824 ,  Y10S514/863

    摘要： Hydrazine derivatives of formula (I) wherein R1 represents lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R2 represents heterocyclyl or NR5R6, R3 represents hydrogen, lower alkyl, halo-lower alkyl, cyano-lower alkyl, hydroxy-lower alkyl, amino-lower alkyl, lower alkoxy-lower alkyl, lower alkoxycarbonyl-lower alkyl, lower cycloalkyl-lower alkyl, aryl-lower alkyl, heterocyclyl-lower alkyl, heterocyclylcarbonyl-lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, aryl, heteroaryl or aryl-lower alkyl, R4 represents lower alkyl, lower alkenyl, lower cycloalkyl-lower alkyl or a grouping of the formula-Z-aryl, -Z-heterocyclyl or-(CH¿2?)n-CH=CR?7R8, R5 and R6¿ each independently represent hydrogen or lower alkyl, R?7 and R8¿ each independently represent hydrogen or lower alkyl or R?7 and R8¿ together represent lower alkylene in which one CH¿2? group is optionally replaced by a hetero atom, X and Z each represent a spacer group, and n stands for 0, 1 or 2, and their pharmaceutically acceptable salts thereof, inhibit the release of tumour necrosis factor alpha (TNF-α) from cells. They can be used as medicaments, especially in the treatment of inflammatory and autoimmune diseases, osteoarthritis, respiratory diseases, tumours, cachexia, cardiovascular diseases, fever, haemorrhage and spesis.