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92 条记录 (耗时 0.107 秒)

    Quinoline derivatives as antibacterial agents
    41.
    发明授权
    Quinoline derivatives as antibacterial agents 有权
    喹啉衍生物作为抗菌剂

    公开(公告)号：US08841321B2

    公开(公告)日：2014-09-23

    申请号：US11993145

    申请日：2006-06-26

    申请人： Koenraad Jozef Lodewijk Marcel Andries ,  Anil Koul ,  Jérôme Emile Georges Guillemont ,  David Francis Alain Lançois ,  Magali Madeleine Simone Motte ,  Ismet Dorange ,  Leo Jacobus Jozef Backx ,  Lieven Meerpoel

    发明人： Koenraad Jozef Lodewijk Marcel Andries ,  Anil Koul ,  Jérôme Emile Georges Guillemont ,  David Francis Alain Lançois ,  Magali Madeleine Simone Motte ,  Ismet Dorange ,  Leo Jacobus Jozef Backx ,  Lieven Meerpoel

    IPC分类号： A01N43/42 ,  A61K31/47 ,  A01N43/40 ,  A61K31/445 ,  A61K31/44 ,  C07D215/227

    CPC分类号： A61K31/47 ,  C07D215/227

    摘要： 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 R1 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; R2 is hydrogen, hydroxy, mercapto, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula; R3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; q is 1, 2 or 3; R4 and R5 are hydrogen, alkyl or benzyl; or R4 and R5 together and including the N to which they are attached may form a ring; R6 is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkythioalkyl, Ar-alkyl or di(Ar)alkyl; or two vicinal R6 radicals may be taken together to form a bivalent radical of formula —CH═CH—CH═CH—; r is 1, 2, 3, 4 or 5; R7 is hydrogen, alkyl, Ar or Het; R8 is hydrogen or alkyl; R9 is oxo; or R8 and R9 together form the radical —CH═CH—N═.

    摘要翻译： 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， 烷基或二（Ar）烷基; p为1,2,3或4; R2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; R3是烷基，Ar，Ar-烷基，Het或Het-烷基; q为1,2或3; R4和R5是氢，烷基或苄基; 或R 4和R 5一起并包括它们所连接的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，链仲烷基，芳烷基或二（Ar） 或两个连位的R6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; R7是氢，烷​​基，Ar或Het; R8是氢或烷基; R9是氧代; 或R8和R9一起形成基团-CH = CH-N =。

    Antifungal 4-substituted 5,6-dihydro-4h-pyrrolo[1,2-a][1,4] benzodiazepines
    50.
    发明授权
    Antifungal 4-substituted 5,6-dihydro-4h-pyrrolo[1,2-a][1,4] benzodiazepines 有权
    抗真菌剂4-取代的5,6-二氢-4H-吡咯并[1,2-a] [1,4]苯并二氮杂卓

    公开(公告)号：US07202240B2

    公开(公告)日：2007-04-10

    申请号：US10399596

    申请日：2001-10-17

    申请人： Terence Gilkerson ,  Roger John Nash ,  Jozel Frans Elisabetha Van Gestel ,  Lieven Meerpoel

    发明人： Terence Gilkerson ,  Roger John Nash ,  Jozel Frans Elisabetha Van Gestel ,  Lieven Meerpoel

    IPC分类号： A61K31/55 ,  A61P31/10 ,  C07D487/04

    CPC分类号： C07D487/04 ,  A61K31/55 ,  A61K31/551

    摘要： The present invention concerns compounds for use as a medicine having the formula (I), the N-oxide forms, the salts, the quaternary amines and stereochemically isomeric forms thereof, wherein R1 represents hydrogen, C1-6 alkyl, C1-4alkylthio, C1-4alkyloxy, or halo; R2 represents hydrogen or C1-6alkyl; R3 represents phenyl substituted with halo, cyano, C1-4alkyloxy, C1-4alkylthio, C1-6alkyl, haloC1-6alkyl; 2-thienyl; or 3-thienyl, R4 represents hydrogen; or R2 and R4 form an extra bond, which are active against dermatophytes, and their preparation; it further relates to compositions comprising them, as well as their use as a medicine.

    摘要翻译： 本发明涉及用作具有式（I）的药物，N-氧化物形式，其盐，季胺及其立体化学异构形式的化合物，其中R 1表示氢， C 1-4烷基，C 1-4烷基硫基，C 1-4烷基氧基或卤素; R 2表示氢或C 1-6烷基; R 3表示被卤素，氰基，C 1-4烷氧基，C 1-4烷基硫基，C 1-6烷基取代的苯基 烷基，卤代C 1-6烷基; 2-噻吩基; 或3-噻吩基，R 4表示氢; 或R 2和R 4形成对皮肤癣菌有活性的额外的结合，及其制备; 它还涉及包含它们的组合物以及它们作为药物的用途。