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    Quinoline derivatives as antibacterial agents
    2.
    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 =。

    Antibacterial quinoline derivatives
    4.
    发明授权
    Antibacterial quinoline derivatives 有权
    抗菌喹啉衍生物

    公开(公告)号：US08415475B2

    公开(公告)日：2013-04-09

    申请号：US12516065

    申请日：2007-12-04

    申请人： Jérôme Emile Georges Guillemont ,  David Francis Alain Lançois ,  Ismet Dorange ,  Koenraad Jozef Lodewijk Marcel Andries ,  Anil Koul

    发明人： Jérôme Emile Georges Guillemont ,  David Francis Alain Lançois ,  Ismet Dorange ,  Koenraad Jozef Lodewijk Marcel Andries ,  Anil Koul

    IPC分类号： C07D215/38

    CPC分类号： C07D215/14 ,  C07D401/04 ,  C07D413/04 ,  C07D417/04

    摘要： The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): including any stereochemically isomeric form thereof, a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.

    摘要翻译： 本发明涉及根据通式（Ia）或式（Ib）的新的取代喹啉衍生物：包括其任何立体化学异构形式，其N-氧化物，其药学上可接受的盐或其溶剂合物。 所要求保护的化合物可用于治疗细菌感染。 还要求保护的是包含药学上可接受的载体和作为活性成分的治疗有效量的要求保护的化合物的组合物，所要求保护的化合物或组合物在制备用于治疗细菌感染的药物中的用途和 制备所要求保护的化合物。

    QUINOLINE DERIVATIVES AS ANTIBACTERIAL AGENTS
    5.
    发明申请
    QUINOLINE DERIVATIVES AS ANTIBACTERIAL AGENTS 有权
    喹诺酮衍生物作为抗菌剂

    公开(公告)号：US20100048585A1

    公开(公告)日：2010-02-25

    申请号：US11993145

    申请日：2006-06-26

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

    IPC分类号： A61K31/497 ,  C07D215/20 ,  C07D401/10 ,  C07D405/10 ,  C07D213/02 ,  A61K31/47 ,  A61K31/4439 ,  A61K31/443 ,  A61K31/4545 ,  A61P31/04

    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 =。

    1,3-dihydro-benzimidazol-2-ylidene amines as inhibitors of respiratory syncytial virus replication
    9.
    发明授权
    1,3-dihydro-benzimidazol-2-ylidene amines as inhibitors of respiratory syncytial virus replication 有权
    1,3-二氢 - 苯并咪唑-2-亚基胺作为呼吸道合胞病毒复制的抑制剂

    公开(公告)号：US07956196B2

    公开(公告)日：2011-06-07

    申请号：US11908538

    申请日：2006-03-17

    申请人： Jean-François Bonfanti ,  Jérôme Michel Claude Fortin ,  Ismet Dorange

    发明人： Jean-François Bonfanti ,  Jérôme Michel Claude Fortin ,  Ismet Dorange

    IPC分类号： A61K31/4184 ,  A61K31/5377 ,  C07D235/30 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14

    CPC分类号： C07D401/06 ,  C07D235/30 ,  C07D401/14

    摘要： Novel 1,3-dihydro-benzimidazol-2-ylidene amine derivatives of formula the addition salts and stereochemically isomeric forms wherein each Alk is C1-6alkanediyl; Q is hydrogen; C1-6alkyl substituted with one or two Ar2 radicals; C1-6alkyl substituted with quinolinyl, oxazolidinyl, thiazolidinyl, morpholinyl, thiomorpholinyl, or with pyrrolidinonyl; —CO—Ar2; or Q is a radical of formula wherein t is 1, 2 or 3; R4 is amino, mono-or di(C1-6alkyl)amino; R1 is Ar2, —CO—Ar2 or a monocyclic or bicyclic heterocycle which may optionally be substituted; R2 is as R1 and additionally can be hydrogen; where Q is other than hydrogen, R3 is hydrogen; and where Q is other than hydrogen, R3 is a radical: wherein R6 is hydrogen, C1-6alkyl, substituted C1-6alkyl; R7, R8, R9 are halo, cyano, C1-6alkyl, substituted C1-6alkyl, C2-6alkenyl, cyanoC2-6alkenyl, C2-6alkynyl, cyanoC2 6alkynyl, Ar1, R10a—0—, R10a—S—, —N(R5aR5b), R10a—O—C(═O)—, N(R5aR5b)—C(═O)—, R10a—C(═O)—NR5b—, R10b—C(═O)—O—; and R8 and/or R9 may also be hydrogen; which are RSV inhibitors. Compositions containing these compounds and processes for preparing these compounds and compositions.

    摘要翻译： 新的1,3-二氢 - 苯并咪唑-2-亚基胺衍生物，其加成盐和立体化学异构形式，其中每个Alk是C 1-6烷二基; Q是氢; 被一个或两个Ar 2基团取代的C 1-6烷基; 用喹啉基，恶唑烷基，噻唑烷基，吗啉基，硫代吗啉基或吡咯烷基取代的C 1-6烷基; -CO-Ar2; 或Q是式的基团，其中t是1,2或3; R4是氨基，单或二（C1-6烷基）氨基; R 1是Ar 2，-CO-Ar 2或可任选被取代的单环或双环杂环; R2是R1，另外可以是氢; 其中Q不是氢，R3是氢; 并且其中Q不是氢，R 3是基团：其中R 6是氢，C 1-6烷基，取代的C 1-6烷基; R 7，R 8，R 9为卤素，氰基，C 1-6烷基，取代的C 1-6烷基，C 2-6烯基，氰基C 2-6烯基，C 2-6炔基，氰基C 2-6炔基，Ar 1，R 10a-O-，R 10a-S， ），R 10a-O-C（= O） - ，N（R 5a，R b）-C（= O） - ，R 10 a -C（= O）-NR 5 b - ，R 10 b -C（= O） 并且R 8和/或R 9也可以是氢; 其为RSV抑制剂。 含有这些化合物的组合物和制备这些化合物和组合物的方法。