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    QUINOLINE DERIVATIVES AS ANTIBACTERIAL AGENTS
    2.
    发明申请
    QUINOLINE DERIVATIVES AS ANTIBACTERIAL AGENTS 审中-公开
    喹诺酮衍生物作为抗菌剂

    公开(公告)号：WO2007000435A1

    公开(公告)日：2007-01-04

    申请号：PCT/EP2006/063553

    申请日：2006-06-26

    Applicant: JANSSEN PHARMACEUTICA N.V. ,  ANDRIES, Koenraad, Jozef, Lodewijk, Marcel ,  KOUL, Anil ,  GUILLEMONT, Jérôme, Emile, Georges ,  LANÇOIS, David, Francis, Alain ,  MOTTE, Magali, Madeleine, Simone ,  DORANGE, Ismet ,  BACKX, Leo, Jacobus, Jozef ,  MEERPOEL, Lieven

    Inventor： ANDRIES, Koenraad, Jozef, Lodewijk, Marcel ,  KOUL, Anil ,  GUILLEMONT, Jérôme, Emile, Georges ,  LANÇOIS, David, Francis, Alain ,  MOTTE, Magali, Madeleine, Simone ,  DORANGE, Ismet ,  BACKX, Leo, Jacobus, Jozef ,  MEERPOEL, Lieven

    IPC: A61K31/47 ,  A61P31/04 ,  C07D215/22

    CPC classification number: A61K31/47 ,  C07D215/227

    Abstract: Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of formula (Ia) or (Ib) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, a tautomeric form thereof or a N -oxide form thereof, wherein R 1 is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1, 2, 3 or 4; R 2 is hydrogen, hydroxy, mercapto, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula ; R 3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; q is 1, 2 or 3; R 4 and R 5 are hydrogen, alkyl or benzyl; or R 4 and R 5 together and including the N to which they are attached may form a ring; R 6 is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl ; or two vicinal R 6 radicals may be taken together to form a bivalent radical of formula - CH=CH-CH=CH-; r is 1, 2, 3, 4 or 5; R 7 is hydrogen, alkyl, Ar or Het; R 8 is hydrogen or alkyl; R 9 is oxo ; or R 8 and R 9 together form the radical -CH=CH-N=.

    Abstract translation: 使用化合物制造用于治疗细菌感染的药物，只要细菌感染不是分枝杆菌感染，所述化合物是式（Ia）或（Ib）的化合物，其药学上可接受的酸或碱加成 其盐，其立体化学异构形式，其互变异构形式或其N-氧化物形式，其中R 1是氢，卤素，卤代烷基，氰基，羟基，Ar，Het，烷基，烷氧基， 烷硫基，烷氧基烷基，烷硫基烷基，芳烷基或二（Ar）烷基; p为1,2,3或4; R 2是氢，羟基，巯基，烷氧基，烷氧基烷氧基，烷硫基，一或二（烷基）氨基或式的基团; R 3是烷基，Ar，Ar-烷基，Het或Het-烷基; q为1,2或3; R 4和R 5是氢，烷基或苄基; 或R 4和R 5一起并且包括它们所连接的N可以形成环; R 6是氢，卤素，卤代烷基，羟基，Ar，烷基，烷氧基，烷硫基，烷氧基烷基，烷硫基烷基，芳烷基或二（Ar）烷基; 或两个邻位R 6个基团可以一起形成式-CH = CH-CH = CH-的二价基团; r为1,2,3,4或5; R 7是氢，烷​​基，Ar或Het; R 8是氢或烷基; R 9是氧代; 或R 8和R 9一起形成基团-CH = CH-N =。

    HIV INHIBITING PYRIMIDINES DERIVATIVES
    6.
    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。

    HIV INHIBITING 6-SUBSTITUTED PYRIMIDINES
    7.
    发明申请
    HIV INHIBITING 6-SUBSTITUTED PYRIMIDINES 审中-公开
    艾滋病毒抑制6-取代的吡咯烷酮

    公开(公告)号：WO2008080964A1

    公开(公告)日：2008-07-10

    申请号：PCT/EP2007/064605

    申请日：2007-12-28

    Applicant: TIBOTEC PHARMACEUTICALS LTD. ,  GUILLEMONT, Jérôme Emile Georges ,  MORDANT, Céline Isabelle

    Inventor： GUILLEMONT, Jérôme Emile Georges ,  MORDANT, Céline Isabelle

    IPC: C07D239/48 ,  C07D401/04 ,  C07D401/12 ,  C07D403/06 ,  C07D405/12 ,  C07D409/12 ,  C07D417/06 ,  A61K31/505 ,  A61K31/506 ,  A61P31/18

    CPC classification number: C07D239/48 ,  C07D401/04 ,  C07D401/12 ,  C07D403/06 ,  C07D405/12 ,  C07D409/12 ,  C07D417/06

    Abstract: HIV replication inhibitors of formula (I). R 1 is hydrogen; aryl; formyl; C 1-6 alkylcarbonyl; C 1-6 alkyl; C 1-6 alkyloxycarbonyl; R 2 , R 3 , R 6 and R 7 are hydrogen; hydroxy; halo; C 3-7 cycloalkyl; C 1-6 alkyloxy; carboxyl; C 1-6 alkyloxycarbonyl; cyano; nitro; amino; mono- or di(C 1-6 alkyl)amino; polyhaloC 1-6 alkyl; polyhaloC 1-6 alkyloxy; -C(=O)R 9 ; optionally substituted C 1-6 alkyl, C 2-6 alkenyl or C 2-6 alkynyl; R 4 and R 8 are hydroxy; halo; C 3-7 cycloalkyl; C 1-6 alkyloxy; carboxyl; C 1-6 alkyloxy- carbonyl; formyl; cyano; nitro; amino; mono- or di(C 1-6 alkyl)amino; polyhaloC 1-6 alkyl; polyhaloC 1-6 alkyloxy; -C(=O)R 9 ; cyano; -S(=O) r R 9 ; -NH-S(=O) 2 R 9 ; -NHC(=O)H; -C(=O)NHNH 2 ; -NHC(=O)R 9 ; Het; -Y-Het; optionally substituted C 1-6 alkyl, C 2-6 alkenyl or C 2-6 alkynyl; R 5 is pyridyl, -C(=O)NR 5a R 5b ; -CH(OR 5c )R 5d ; -CH 2 -NR 5e R 5f ; -CH=NOR 5a ; -CH 2 -O-C 2-6 alkenyl; -CH 2 -O-P(=O)(OR 5g ) 2 ; -CH 2 -O-C(=O)-NH 2 ; -C(=O)-R 5d ; X is -NR 1 -, -O-, -CH 2 -, -S-; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds and compositions.

    Abstract translation: 式（I）的HIV复制抑制剂。 R 1是氢; 芳基; 甲酰基; ç 1-6 烷基羰基; ç 1-6 烷基; ç 1-6 烷氧基羰基; R 2，R 3，R 6和R 7是氢; 羟基; 光环; ç 3-7 环烷基; ç 1-6 烷氧基; 羧基; ç 1-6 烷氧基羰基; 氰基; 硝基; 氨基; 单或二（C 1-6烷基）氨基; 多卤代 1-6 烷基; 多卤代 1-6 烷氧基; -C（= O）R 9 ; 任选取代的C 1-6烷基，C 2-6 - 烯基或C 2-6 - 亚炔基; R 4和R 8是羟基; 光环; ç 3-7 环烷基; ç 1-6 烷氧基; 羧基; C 1-6烷基氧基 - 羰基; 甲酰基; 氰基; 硝基; 氨基; 单或二（C 1-6烷基）氨基; 多卤代 1-6 烷基; 多卤代 1-6 烷氧基; -C（= O）R 9 ; 氰基; -S（= O） - [R - [R 9 ; -NH-S（= O） 2 - [R 9 ; -NHC（= O）H; -C（= O）NHNH 2 ; -NHC（= O）R 9 ; HET; -Y-HET; 任选取代的C 1-6烷基，C 2-6 - 烯基或C 2-6 - 亚炔基; R 5是吡啶基，-C（= O）NR 5a R 5b; -CH（OR 图5c ）R 5D ; -CH 2 -NR 5E - [R 5F ; -CH = NOR 图5a ; -CH 2 -O-C 2-6 烯基; -CH 2 -O-P（= O）（OR 5克） 2 ; -CH 2 -O-C（= O）-NH 2 ; -C（= O）-R 5D ; X是-NR 1 - ， - O - ， - CH 2 - ， - S - ; 含有这些化合物作为活性成分的药物组合物和制备所述化合物和组合物的方法。

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