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    Hiv Inhibiting 1,2,4-Triazin-6-One Derivatives
    1.
    发明申请
    Hiv Inhibiting 1,2,4-Triazin-6-One Derivatives 有权
    HIF抑制1,2,4-三嗪-6-酮衍生物

    公开(公告)号：US20090012092A1

    公开(公告)日：2009-01-08

    申请号：US11573224

    申请日：2005-08-10

    申请人： Georges Joseph Cornelius Hoornaert ,  Amuri Kilonda ,  Jan Heeres ,  Paulus Joannes Lewi ,  Marc Rene de Jonge ,  Frederik Frans Desire Daeyaert ,  Hendrik Maarten Vinkers ,  Lucien Maria Henricus Koymans ,  Paul Adriaan Jan Janssen ,  Frank Xavier Jozef Herwig Arts

    发明人： Georges Joseph Cornelius Hoornaert ,  Amuri Kilonda ,  Jan Heeres ,  Paulus Joannes Lewi ,  Marc Rene de Jonge ,  Frederik Frans Desire Daeyaert ,  Hendrik Maarten Vinkers ,  Lucien Maria Henricus Koymans ,  Paul Adriaan Jan Janssen ,  Frank Xavier Jozef Herwig Arts

    IPC分类号： A61K31/53 ,  C07D253/06 ,  A61P31/18

    CPC分类号： C07D253/075

    摘要： The present invention relates to HIV replication inhibitors of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein ring A and ring B represent phenyl, pyridyl, pyridazinyl, pyrimidinyl or pyrazinyl; n and m are 1 to 4; R1 represents hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxyC1-6alkylcarbonyl substituted with C1-6alkyloxycarbonyl; R2 or R4 represents hydrogen; hydroxy; halo; optionally substituted C1-6alkyl; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-4alkyl; polyhaloC1-4alkyloxy; polyhaloC1-4alkylthio; —S(═O)pR6; —NH—S(═O)pR6; —C(═O)R6; —NHC(═O)H; —C(═O)NHNH2; NHC(═O)R6; C(═NH)R6; or R7; R2a or R3 represents cyano; aminocarbonyl; amino; halo; NHR13; NR13R14 —C(═O)—NHR13; —C(═O)—NR13 R14; —C(═O)—R15; —CH═N—NH—C(═O)—R16; optionally substituted C1-6alkyl; optionally substituted C1-6alkyloxy; optionally substituted C1-6alkyloxyC1-6alkyl; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7 or —X3—R7; X1 or X2 represents —NR1—; —NH—NH—; —N═N—; —O—; —C(═O)—; —C1-4alkanediyl-; —CHOH—; —S—; —S(═O)p—; —X4—C1-4alkanediyl-; —C1-4alkanediyl-X4—; or —C1-4alkanediyl-X4—C1-4alkanediyl-; their use as a medicine, their use for the manufacture of a medicament for the treatment or the prevention of HIV infection; their processes for preparation and pharmaceutical compositions comprising them.

    摘要翻译： 本发明涉及式N-氧化物的HIV复制抑制剂，其药学上可接受的加成盐，季胺或其立体化学异构形式，其中环A和环B表示苯基，吡啶基，哒嗪基，嘧啶基或吡嗪基; n和m为1〜4; R1表示氢; 芳基; 甲酰基 C 1-6烷基羰基; C 1-6烷氧基羰基; 任选取代的C 1-6烷基; 被C 1-6烷氧基羰基取代的C 1-6烷氧基C 1-6烷基羰基; R2或R4代表氢; 羟基; 光环; 任选取代的C 1-6烷基; 任选取代的C 2-6烯基; 任选取代的C 2-6炔基; C 3-7环烷基; C 1-6烷氧基; C 1-6烷氧基羰基; C 1-6烷基羰基氧基; 羧基; 氰基; 硝基 氨基; 单或二（C 1-6烷基）氨基; 多卤代C 1-4烷基; 多卤代1-4烷基氧基; 多卤代 -S（-O）p R 6; -NH-S（-O）p R 6; -C（-O）R 6; -NHC（-O）H; -C（-O）NHNH 2; NHC（-O）R 6; C（-NH）R 6; 或R7; R2a或R3表示氰基; 氨基羰基; 氨基; 光环; NHR13; NR 13 R 14 -C（-O）-NHR 13; -C（ - ） - NR 13 R 14; -C（-O）-R 15; -CH-N-NH-C（-O）-R16; 任选取代的C 1-6烷基; 任选取代的C 1-6烷氧基; 任选取代的C 1-6烷氧基C 1-6烷基; 任选取代的C 2-6烯基; 任选取代的C 2-6炔基; -C（-N-O-R 8）-C 1-4烷基; R7或-X3-R7; X1或X2表示-NR1-; -NH-NH-; -N-N- -O-; -C（-O） - ; -C 1-4烷二基 -CHOH-; -S-; -S（-O）p - ; -X4-C1-4烷二基 -C 1-4烷二基-X4-; 或-C1-4烷二基-X4-C1-4烷二基; 它们作为药物的用途，它们用于制备用于治疗或预防HIV感染的药物的用途; 其制备方法和包含它们的药物组合物。

    Compounds for the treatment of neurodegenerative diseases
    9.
    发明授权
    Compounds for the treatment of neurodegenerative diseases 有权
    用于治疗神经变性疾病的化合物

    公开(公告)号：US09284271B2

    公开(公告)日：2016-03-15

    申请号：US13993756

    申请日：2011-12-13

    申请人： Gerard Griffioen ,  Tom Van Dooren ,  Verónica Rojas De La Parra ,  Arnaud Marchand ,  Sara Alassia ,  Amuri Kilonda ,  Patrick Chaltin

    发明人： Gerard Griffioen ,  Tom Van Dooren ,  Verónica Rojas De La Parra ,  Arnaud Marchand ,  Sara Alassia ,  Amuri Kilonda ,  Patrick Chaltin

    IPC分类号： C07D209/14 ,  C07D209/18 ,  C07D401/12 ,  C07D409/12 ,  C07D471/04

    CPC分类号： C07D209/18 ,  C07D209/14 ,  C07D401/12 ,  C07D409/12 ,  C07D471/04

    摘要： This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterized by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds. The compounds have the formula (A1), wherein R1, R2, R4, R5, R6, E, n, Y1, Y2, Y3, Y4, Y5, B, R8, and m are as defined in the claims.

    摘要翻译： 本发明提供了新的化合物和用作药物的新化合物，更特别是用于预防或治疗神经变性疾病，更具体地，某些神经系统疾病，例如统称为tau蛋白病的病症，以及细胞毒性α-突触核蛋白淀粉样变性特征的病症 。 本发明还涉及所述新化合物在制备可用于治疗这种神经变性疾病的药物中的用途。 本发明还涉及包含所述新化合物的药物组合物和制备所述新化合物的方法。 化合物具有式（A1），其中R1，R2，R4，R5，R6，E，n，Y1，Y2，Y3，Y4，Y5，B，R8和m如权利要求中所定义。