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    Retinoic acid mimetic anlides
    5.
    发明授权
    Retinoic acid mimetic anlides 有权
    视黄酸模拟物

    公开(公告)号：US06319939B1

    公开(公告)日：2001-11-20

    申请号：US09555775

    申请日：2000-06-01

    申请人： Dominique Mabire ,  Christophe Denis Adelinet ,  Imré Christian Csoka ,  Marc Gaston Venet

    发明人： Dominique Mabire ,  Christophe Denis Adelinet ,  Imré Christian Csoka ,  Marc Gaston Venet

    IPC分类号： C07D22354

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D233/61 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

    摘要： The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents O, S or NR3; R1 represents hydrogen, hydroxy, C1-6alkyl or aryl; R2 represents hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl; aryl; Het1; or R1 and R2 taken together may form a bivalent radical of formula —(CH2)n— wherein n is 2, 3, 4, 5 or 6; R3 represents hydrogen, optionally substituted C1-6alkyl, aryl, Het1; R4 represents hydrogen; hydroxy; mercapto; C1-6alkyloxy; C1-6alkylthio; aryloxy; arylthio; Het1-oxy; Het1-thio; optionally substituted C1-12alkyl; optionally substituted C2-8alkenyl; optionally substituted C2-8alkynyl; optionally substituted C3-7cycloalkyl; optionally substituted C5-7cycloalkenyl; aryl; Het1; or -Alk-NR3R5 (i) or —NR3R5 (ii) wherein Alk represents C1-6alkanediyl; and R5 represents hydrogen, C1-6alkyl, aryl, Het1, (aryl or Het1)C1-6alkyl, (aryl or Het1)carbonyl or (aryl or Het1)C1-6alkyloxycarbonyl; aryl represents optionally substituted indanyl, indenyl, naphtyl, 5,6,7,8-tetrahydro-2-naphtalenyl or phenyl; Het represents an optionally substituted unsaturated heterocycle; and Het1 represents an optionally substituted monocyclic or bicyclic heterocycle; having retinoic mimetic activity; their preparation, compositions containing them and their use as a medicine.

    摘要翻译： 本发明涉及配制N-氧化物的化合物，其药学上可接受的加成盐和立体化学异构形式，其中X表示O，S或NR 3; R 1表示氢，羟基，C 1-6烷基或芳基; R2表示氢; 任选取代的C 1-12烷基; C 3-7环烷基; C2-8烯基; 芳基; Het1; 或者R 1和R 2一起形成式 - （CH 2）n - 的二价基团，其中n为2,3,4,5或6; R 3表示氢，任选取代的C 1-6烷基，芳基，Het 1; R4代表氢; 羟基; 巯基 C 1-6烷氧基; C 1-6烷硫基; 芳氧基 芳硫基 Het1-oxy; Het1-硫代 任选取代的C 1-12烷基; 任选取代的C 2-8烯基; 任选取代的C 2-8炔基; 任选取代的C 3-7环烷基; 任选取代的C 5-7环烯基; 芳基; Het1; 或-Alk-NR 3 R 5（i）或-NR 3 R 5（ii）其中Alk表示C 1-6烷二基; 并且R 5表示氢，C 1-6烷基，芳基，Het 1，（芳基或Het 1）C 1-6烷基，（芳基或Het 1）羰基或（芳基或Het 1）C 1-6烷氧基羰基; 芳基表示任选取代的茚满基，茚基，萘基，5,6,7,8-四氢-2-萘基或苯基; Het表示任选取代的不饱和杂环; 且Het1表示任选取代的单环或双环杂环; 具有视黄酸模拟活性; 其制剂，含有它们的组合物及其作为药物的用途。

    Retinoic acid mimetic anilides
    7.
    发明授权
    Retinoic acid mimetic anilides 有权
    视黄酸模拟苯胺

    公开(公告)号：US07579352B2

    公开(公告)日：2009-08-25

    申请号：US11926699

    申请日：2007-10-29

    申请人： Dominique Mabire ,  Christophe Denis Adelinet ,  Imré Christian Csoka ,  Marc Gaston Venet

    发明人： Dominique Mabire ,  Christophe Denis Adelinet ,  Imré Christian Csoka ,  Marc Gaston Venet

    IPC分类号： A61K31/496 ,  A61K31/454 ,  A61K31/4439 ,  A61K31/4196 ,  C07D403/02 ,  C07D401/06 ,  C07D401/02 ,  C07D249/08

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D233/61 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

    摘要： The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents O, S or NR3; R1 represents hydrogen, hydroxy, C1-6alkyl or aryl; R2 represents hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl; aryl; Het1; R3 represents hydrogen, optionally substituted C1-6alkyl, aryl, Het1; R4 represents hydrogen; hydroxy; mercapto; C1-6alkyloxy; C1-6alkylthio; aryloxy; arylthio; Het1-oxy; Het1-thio; optionally substituted C1-12alkyl; optionally substituted C2-8alkenyl; optionally substituted C2-8alkynyl; optionally substituted C3-7cycloalkyl; optionally substituted C5-7cycloalkenyl; aryl; Het1; or -Alk-NR3R5 (i) or —NR3R5 (ii) wherein Alk represents C1-6alkanediyl; and R5 represents hydrogen, C1-6alkyl, aryl, Het1, (aryl or Het1)C1-6alkyl, (aryl or Het1)carbonyl or (aryl or Het1)C1-6alkyloxycarbonyl; aryl represents optionally substituted indanyl, indenyl, naphtyl, 5,6,7,8-tetrahydro-2-naphtalenyl or phenyl; Het is triazolyl; and Het1 represents an optionally substituted monocyclic or bicyclic heterocycle; having retinoic mimetic activity; their preparation, compositions containing them and their use as a medicine.

    摘要翻译： 本发明涉及式I化合物的N-氧化物，其药学上可接受的加成盐和立体化学异构形式，其中X代表O，S或NR 3; R 1表示氢，羟基，C 1-6烷基或芳基; R2表示氢; 任选取代的C 1-12烷基; C 3-7环烷基; C2-8烯基; 芳基; Het1; R 3表示氢，任选取代的C 1-6烷基，芳基，Het 1; R4代表氢; 羟基; 巯基 C 1-6烷氧基; C 1-6烷硫基; 芳氧基 芳硫基; Het1-oxy; Het1-硫代 任选取代的C 1-12烷基; 任选取代的C 2-8烯基; 任选取代的C 2-8炔基; 任选取代的C 3-7环烷基; 任选取代的C 5-7环烯基; 芳基; Het1; 或-Alk-NR 3 R 5（i）或-NR 3 R 5（ii）其中Alk表示C 1-6烷二基; 并且R 5表示氢，C 1-6烷基，芳基，Het 1，（芳基或Het 1）C 1-6烷基，（芳基或Het 1）羰基或（芳基或Het 1）C 1-6烷氧基羰基; 芳基表示任选取代的茚满基，茚基，萘基，5,6,7,8-四氢-2-萘基或苯基; Het是三唑基; 且Het1表示任选取代的单环或双环杂环; 具有视黄酸模拟活性; 其制剂，含有它们的组合物及其作为药物的用途。

    Retinoic acid mimetic anilides
    8.
    发明授权
    Retinoic acid mimetic anilides 有权

    公开(公告)号：US07179825B2

    公开(公告)日：2007-02-20

    申请号：US11081393

    申请日：2005-03-16

    申请人： Dominique Mabire ,  Christophe Denis Adelinet ,  Imré Christian Csoka ,  Marc Gaston Venet

    发明人： Dominique Mabire ,  Christophe Denis Adelinet ,  Imré Christian Csoka ,  Marc Gaston Venet

    IPC分类号： C07D213/02 ,  A61K31/44

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D233/61 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

    摘要： The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents O, S or NR3; R1 represents hydrogen, hydroxy, C1-6alkyl or aryl; R2 represents hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl; aryl; Het1; or R1 and R2 taken together may form a bivalent radical of formula —(CH2)n— wherein n is 2, 3, 4, 5 or 6; R3 represents hydrogen, optionally substituted C1-6alkyl, aryl, Het1; R4 represents hydrogen; hydroxy; mercapto; C1-6alkyloxy; C1-6alkylthio; aryloxy; arylthio; Het1-oxy; Het1-thio; optionally substituted C1-12alkyl; optionally substituted C2-8alkenyl; optionally substituted C2-8alkynyl; optionally substituted C3-7cycloalkyl; optionally substituted C5-7cycloalkenyl; aryl; Het1; or -Alk-NR3R5 (i) or —NR3R5 (ii) wherein Alk represents C1-6alkanediyl; and R5 represents hydrogen, C1-6alkyl, aryl, Het1, (aryl or Het1)C1-6alkyl, (aryl or Het1)carbonyl or (aryl or Het1)C1-6alkyloxycarbonyl; aryl represents optionally substituted indanyl, indenyl, naphtyl, 5,6,7,8-tetrahydro-2-naphtalenyl or phenyl; Het represents an optionally substituted unsaturated heterocycle; and Het1 represents an optionally substituted monocyclic or bicyclic heterocycle; having retinoic mimetic activity; their preparation, compositions containing them and their use as a medicine.