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    Antibacterial quinoline derivatives
    1.
    发明授权
    Antibacterial quinoline derivatives 有权
    抗菌喹啉衍生物

    公开(公告)号：US07998979B2

    公开(公告)日：2011-08-16

    申请号：US12516370

    申请日：2007-12-04

    申请人： Jérôme Emile Georges Guillemont ,  Magali Madeleine Simone Motte ,  Koenraad Jozef Lodewijk Marcel Andries ,  Anil Koul

    发明人： Jérôme Emile Georges Guillemont ,  Magali Madeleine Simone Motte ,  Koenraad Jozef Lodewijk Marcel Andries ,  Anil Koul

    IPC分类号： A61K31/47 ,  A61P31/04 ,  C07D215/00 ,  C07D401/02

    CPC分类号： C07D215/227

    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 pharmaceutically acceptable salt thereof, a N-oxide form 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，其药学上可接受的盐，其N-氧化物形式或其溶剂化物。 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
    3.
    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 =。

    Quinoline Derivatives as Antibacterial Agents
    4.
    发明申请
    Quinoline Derivatives as Antibacterial Agents 审中-公开
    喹啉衍生物作为抗菌剂

    公开(公告)号：US20100197727A1

    公开(公告)日：2010-08-05

    申请号：US11917091

    申请日：2006-06-26

    申请人： Koenraad Jozef Lodewijk Marcel Andries ,  Anil Koul ,  David Francis Alain Lancois ,  Magali Madeleine Simone Motte ,  Jérôme Emile Georges Guillemont

    发明人： Koenraad Jozef Lodewijk Marcel Andries ,  Anil Koul ,  David Francis Alain Lancois ,  Magali Madeleine Simone Motte ,  Jérôme Emile Georges Guillemont

    IPC分类号： A61K31/47 ,  C07D215/227 ,  C07D409/06 ,  A61K31/4709 ,  C07D401/06 ,  C07D215/36 ,  A61P31/04

    CPC分类号： C07D409/06 ,  A61K31/47 ,  A61K31/4709 ,  C07D215/227 ,  C07D215/36 ,  C07D401/06

    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 N-oxide, a tautomeric form or a stereochemically isomeric form thereof wherein A− is a counter ion; R1 is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1 to 4; R2 is hydrogen, hydroxy, mercapto, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or wherein Y is CH2, O, S, NH or N-alkyl; R3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; q is 0 to 4; R4 and R5 each independently are hydrogen, alkyl or benzyl; or R4 and R5 may be taken together including the N to which they are attached; R6 is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; or two vicinal R6 radicals may be taken together to form —CH═CH—CH═CH—; r is 1 to 5; R7 is hydrogen, alkyl, Ar or Het; R8 is hydrogen or alkyl; R9 is oxo; or R8 and R9 taken together form —CH═CH—N═; R10 is alkyl, alkylcarbonyl, Ar, Ar-alkyl, Ar-carbonyl, Het1-alkyl or Het1-carbonyl.

    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，N-氧化物，互变异构体 形式或其立体化学异构体形式，其中A-是抗衡离子; 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） p为1〜4; R2是氢，羟基，巯基，烷氧基，烷氧基烷氧基，烷硫基，一或二（烷基）氨基或其中Y是CH2，O，S，NH或N-烷基; R3是烷基，Ar，Ar-烷基，Het或Het-烷基; q为0〜4; R4和R5各自独立地为氢，烷基或苄基; 或R4和R5可以一起包括它们所连接的N; 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） 或两个连位的R6基团可以一起形成-CH = CH-CH = CH-; r为1〜5; 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-CH = CH-N =; R10是烷基，烷基羰基，Ar，Ar-烷基，Ar-羰基，Het1-烷基或Het1-羰基。

    ANTIBACTERIAL QUINOLINE DERIVATIVES
    7.
    发明申请
    ANTIBACTERIAL QUINOLINE DERIVATIVES 有权
    抗生素喹啉衍生物

    公开(公告)号：US20100063061A1

    公开(公告)日：2010-03-11

    申请号：US12516370

    申请日：2007-12-04

    申请人： Jérôme Emile Georges Guillemont ,  Magali Madeleine Simone Motte ,  Koenraad Jozef Lodewijk Marcel Andries ,  Anil Koul

    发明人： Jérôme Emile Georges Guillemont ,  Magali Madeleine Simone Motte ,  Koenraad Jozef Lodewijk Marcel Andries ,  Anil Koul

    IPC分类号： A61K31/496 ,  C07D215/00 ,  A61K31/47 ,  C07D401/02 ,  A61P31/04

    CPC分类号： C07D215/227

    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 pharmaceutically acceptable salt thereof, a N-oxide form 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，其药学上可接受的盐，其N-氧化物形式或其溶剂合物。 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
    8.
    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 =。

    Quinoline derivatives as antibacterial agents
    10.
    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：US07709498B2

    公开(公告)日：2010-05-04

    申请号：US11296918

    申请日：2005-12-08

    申请人： Koenraad Jozef Lodewijk Marcel Andries ,  Anil Koul ,  Jérôme Emile Georges Guillemont ,  Elisabeth Therese Jeanne Pasquier

    发明人： Koenraad Jozef Lodewijk Marcel Andries ,  Anil Koul ,  Jérôme Emile Georges Guillemont ,  Elisabeth Therese Jeanne Pasquier

    IPC分类号： C07D215/38

    CPC分类号： C07D215/227 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/541 ,  C07D215/36 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04 ,  C07D405/06 ,  C07D409/06 ,  Y02A50/473

    摘要： The present invention relates to a method for the treatment of a bacterial infection comprising administering a therapeutically effective amount of a compound of formula or a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof or a N-oxide form thereof, wherein R1 is hydrogen, halo, polyhaloC1-6alkyl, C1-6alkyl, Ar or Het; p is an integer equal to 1 or 2; R2 is C1-6alkyloxy, C1-6alkyloxyC1-6alkyloxy or C1-6alkylthio; R3 is Ar, Het or Het1; R4 and R5 each independently are hydrogen, C1-6alkyl or benzyl; or R4 and R5 together and including the N to which they are attached may form a radical selected from the group of pyrrolidinyl, 2-pyrrolinyl, 3-pyrrolinyl, pyrrolyl, imidazolidinyl, pyrazolidinyl, 2-imidazolinyl, 2-pyrazolinyl, imidazolyl, pyrazolyl, triazolyl, piperidinyl, pyridinyl, piperazinyl, pyridazinyl, pyrimidinyl, pyrazinyl, triazinyl, morpholinyl and thiomorpholinyl, each of said rings may optionally be substituted with C1-6alkyl, halo, polyhaloC1-6alkyl, hydroxy, hydroxyC1-6alkyl, C1-6alkyloxy, amino, mono- or di(C1-6alkyl)amino, C1-6alkylthio, C1-6alkyloxyC1-6alkyl, C1-6alkylthioC1-6alkyl or pyrimidinyl; R6 is hydrogen, halo, polyhaloC1-6alkyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio; or two vicinal R6 radicals may be taken together to form a bivalent radical of formula —CH═CH—CH═CH—; r is an integer equal to 1 or 2; R7 is hydrogen, C1-6alkyl, Ar, Het or Het1; provided that to bacterial infection is other than a Mycobacterial infection.

    摘要翻译： 本发明涉及一种治疗细菌感染的方法，包括给予治疗有效量的式的化合物或其药学上可接受的酸或碱加成盐，其立体化学异构形式或其N-氧化物形式，其中 R 1是氢，卤素，多卤代C 1-6烷基，C 1-6烷基，Ar或Het; p是等于1或2的整数; R2是C1-6烷氧基，C1-6烷氧基C1-6烷氧基或C1-6烷硫基; R3是Ar，Het或Het1; R 4和R 5各自独立地为氢，C 1-6烷基或苄基; 或R4和R5一起并且包括它们所连接的N可以形成选自吡咯烷基，2-吡咯啉基，3-吡咯啉基，吡咯基，咪唑烷基，吡唑烷基，2-咪唑啉基，2-吡唑啉基，咪唑基，吡唑基 三唑基，哌啶基，吡啶基，哌嗪基，哒嗪基，嘧啶基，吡嗪基，三嗪基，吗啉基和硫代吗啉基，每个所述环可任选被C 1-6烷基，卤素，多卤代C 1-6烷基，羟基，羟基C 1-6烷基，C 1-6烷氧基， 氨基，单或二（C 1-6烷基）氨基，C 1-6烷硫基，C 1-6烷氧基C 1-6烷基，C 1-6烷硫基C 1-6烷基或嘧啶基; R 6是氢，卤素，多卤代C 1-6烷基，C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基; 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是等于1或2的整数; R7是氢，C1-6烷基，Ar，Het或Het1; 只要细菌感染不是分枝杆菌感染。