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    • 5. 发明授权
    • Retinoic acid mimetic anlides
    • 视黄酸模拟物
    • US06319939B1
    • 2001-11-20
    • US09555775
    • 2000-06-01
    • Dominique MabireChristophe Denis AdelinetImré Christian CsokaMarc Gaston Venet
    • Dominique MabireChristophe Denis AdelinetImré Christian CsokaMarc Gaston Venet
    • C07D22354
    • C07D231/12C07D233/56C07D233/61C07D249/08C07D401/12C07D403/12C07D405/12C07D409/12C07D413/12C07D417/12
    • 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.
    • 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。
    • 6. 发明授权
    • Retinoic acid mimetic anilides
    • 视黄酸模拟苯胺
    • US07579352B2
    • 2009-08-25
    • US11926699
    • 2007-10-29
    • Dominique MabireChristophe Denis AdelinetImré Christian CsokaMarc Gaston Venet
    • Dominique MabireChristophe Denis AdelinetImré Christian CsokaMarc Gaston Venet
    • A61K31/496A61K31/454A61K31/4439A61K31/4196C07D403/02C07D401/06C07D401/02C07D249/08
    • C07D231/12C07D233/56C07D233/61C07D249/08C07D401/12C07D403/12C07D405/12C07D409/12C07D413/12C07D417/12
    • 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.
    • 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。