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    HIV INHIBITING PYRIMIDINES DERIVATIVES
    7.
    发明申请
    HIV INHIBITING PYRIMIDINES DERIVATIVES 审中-公开
    艾滋病毒抑制吡啶衍生物

    公开(公告)号：WO2003016306A1

    公开(公告)日：2003-02-27

    申请号：PCT/EP2002/008953

    申请日：2002-08-09

    Applicant: JANSSEN PHARMACEUTICA N.V. ,  GUILLEMONT, Jérôme, Emile, Georges ,  PALANDJIAN, Patrice ,  DE JONGE, Marc, René ,  KOYMANS, Lucien, Maria, Henricus ,  VINKERS, Hendrik, Maarten ,  DAEYAERT, Frederik, Frans, Desiré ,  HEERES, Jan ,  VAN AKEN, Koen, Jeanne, Alfons ,  LEWI, Paulus, Joannes ,  JANSSEN, Paul, Adriaan, Jan

    Inventor： GUILLEMONT, Jérôme, Emile, Georges ,  PALANDJIAN, Patrice ,  DE JONGE, Marc, René ,  KOYMANS, Lucien, Maria, Henricus ,  VINKERS, Hendrik, Maarten ,  DAEYAERT, Frederik, Frans, Desiré ,  HEERES, Jan ,  VAN AKEN, Koen, Jeanne, Alfons ,  LEWI, Paulus, Joannes ,  JANSSEN, Paul, Adriaan, Jan

    IPC: C07D403/12

    CPC classification number: C07D239/48 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  C07C255/42 ,  C07C257/12 ,  C07D239/47 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

    Abstract: This invention concerns HIV replication inhibitors of formula (I) the N -oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a 1 =a 2 -a 3 =a 4 - and -b 1 =b 2 -b 3 =b 4 - represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl;n is 0 to 5; m is 1 to 4; R 1 is hydrogen; aryl; formyl; C 1-6 alkylcarbonyl; C 1-6 alkyl; C 1-6 alkyloxycarbonyl, substituted C 1-6 alkyl, C 1-6 alkylcarbonyl; R 2 is hydroxy, halo, optionally substituted C 1-6 alkyl, C 3-7 cycloalkyl, optionally substituted C 2-6 alkenyl, optionally substituted C 2-6 alkynyl, C 1-6 alkyloxy, C 1-6 alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C 1-6 alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, -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 or a 5-membered heterocycle; X 1 is -NR 5 -, -NH-NH-, -N=N-, -O-, -C(=O)-, C 1-4 alkanediyl, -CHOH-, -S-, -S(=O) p -, -X 2 -C 1-4 alkanediyl- or -C 1-4 alkanediyl-X 2 -; R 3 is NHR 13 ; NR 13 R 14 ; -C(=O)-NHR 13 ; -C(=O)-NR 13 R 14 ; -C(=O)-R 15 ; -CH=N-NH-C(=O)-R 16 ; substituted C 1-6 alkyl; optionally substituted C 1-6 alkyloxyC 1-6 alkyl; substituted C 2-6 alkenyl; substituted C 2-6 alkynyl; C 1-6 alkyl substituted with hydroxy and a second substituent; -C(=N-O-R 8 )-C 1-4 alkyl; R 7 ; or -X 3 -R 7 ; R 4 is halo, hydroxy, C 1-6 alkyl, C 3-7 cycloalkyl, C 1-6 alkyloxy, cyano, nitro, polyhaloC 1-6 alkyl, polyhaloC 1-6 alkyloxy, aminocarbonyl, C 1-6 alkyloxycarbonyl, C 1-6 alkylcarbonyl, formyl, amino, mono- or di(C 1-4 alkyl)amino; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.

    Abstract translation: 本发明涉及式（I）的N，N-氧化物的HIV复制抑制剂，其药学上可接受的加成盐，季胺及其立体化学异构形式，其中含-a 1 = a 2 -a 3 = a 4 - 和-b 1 = b 2 -b 3 = b 4 - 表示苯基，吡啶基，嘧啶基，吡嗪基，哒嗪基; n为0 至5; m为1〜4; R 1是氢; 芳基; 甲酰基; C1-6烷基; ç<1-6>烷基; C 1-6烷氧基羰基，取代的C 1-6烷基，C 1-6烷基羰基; R 2是羟基，卤素，任选取代的C 1-6烷基，C 3-7环烷基，任选取代的C 2-6烯基，任选取代的C 2-6炔基，C 1-6烷氧基，C 1-6烷氧基羰基，羧基，氰基，硝基，氨基，单或 二（C 1-6烷基）氨基，多卤代甲基，多卤代甲氧基，多卤甲硫基，-S（= O）pR 6，-NH-S（= O）pR 6，-C（= O）R 6， NHC（= O）H，-C（= O）NHNH 2，-NHC（= O）R 6，-C（= NH）R 6或5-元杂环; X1是-NR5 - ， - NH-NH-，-N = N-，-O - ， - C（= O） - ，C1-4烷二基，-CHOH-，-S-，-S（= O ）p-，-X2-C1-4烷二基或-C1-4烷二基X2-; R 3是NHR 13; NR <13> - [R <14>; -C（= O）-NHR <13>; -C（= O）-NR <13> - [R <14>; -C（= O）-R <15>; -CH = N-NH-C（= O）-R <16>; 取代的C 1-6烷基; 任选取代的C 1-6烷氧基C 1-6烷基; 取代的C 2-6烯基; 取代的C 2-6炔基; 被羟基和第二取代基取代的C 1-6烷基; -C（= N-O-R <8>） - C 1-4烷基; [R <7>; 或-X3-R7; R 4是卤素，羟基，C 1-6烷基，C 3-7环烷基，C 1-6烷氧基，氰基，硝基，多卤代C 1-6烷基，多卤代C 1-6烷氧基，氨基羰基，C 1-6烷氧基羰基，C 1-6烷基羰基，甲酰基，氨基，单或 二（C 1-4烷基）氨基; 它们作为药物的用途，其制备方法和包含它们的药物组合物。

    METHOD FOR HYDROLYZING ALPHA - CHLORINATED TOLUENE COMPOUNDS
    9.
    发明申请
    METHOD FOR HYDROLYZING ALPHA - CHLORINATED TOLUENE COMPOUNDS 审中-公开
    用于水解ALPHA-氯化堇青石化合物的方法

    公开(公告)号：WO2013013709A1

    公开(公告)日：2013-01-31

    申请号：PCT/EP2011/062850

    申请日：2011-07-26

    Applicant: INEOS CHLORVINYLS BELGIUM NV ,  VAN DEYNSE, Dirk ,  VAN AKEN, Koen ,  VAN HECKE, Wouter

    Inventor： VAN DEYNSE, Dirk ,  VAN AKEN, Koen ,  VAN HECKE, Wouter

    IPC: C07C29/124 ,  C07C33/22 ,  C07C45/43 ,  C07C47/54 ,  C07C51/093 ,  C07C63/06

    CPC classification number: C07C37/02 ,  C07C29/124 ,  C07C33/22

    Abstract: The current invention provides and improved method for hydrolyzing alpha- chlorinated toluene compounds comprising the steps of: -providing an alpha-chlorinated toluene compound of formula (I) wherein at least one of R 1 , R 2 and R 3 is CI and wherein (R a ) n designates that the benzene nucleus may have one or more substituents which may be same or different and are selected from the group consisting of H, CI, Br and - C m H 2m+1 , n being 0 or an integer from 1 to 5, and m being an integer, preferably from 1 to 6, -hydrolyzing said compound with water in the presence of a metal oxide.

    Abstract translation: 本发明提供了用于水解α-氯化甲苯化合物的改进方法，其包括以下步骤： - 提供式（I）的α-氯化甲苯化合物，其中R 1，R 2和R 3中的至少一个为Cl并且其中（Ra）n 表示苯核可以具有一个或多个可以相同或不同并且选自H，Cl，Br和-CmH 2 m + 1，n为0或1至5的整数的取代基，m为 一个整数，优选1到6个，在金属氧化物的存在下，用水水解所述化合物。

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