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    QUINOLINE DERIVATIVES AS ANTIBACTERIAL AGENTS
    1.
    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
    2.
    发明申请
    Quinoline Derivatives as Antibacterial Agents 有权

    公开(公告)号：US20080207687A1

    公开(公告)日：2008-08-28

    申请号：US11997173

    申请日：2006-07-31

    申请人： Jerome Emile Georges Guillemont ,  Elisabeth Therese Jeanne Pasquier ,  David Francis Alain Lancois ,  Koenraad Jozef Lodewijk Marcel Andries ,  Anil Koul ,  Leo Jacobus Jozef Backx ,  Lieven Meerpoel

    发明人： Jerome Emile Georges Guillemont ,  Elisabeth Therese Jeanne Pasquier ,  David Francis Alain Lancois ,  Koenraad Jozef Lodewijk Marcel Andries ,  Anil Koul ,  Leo Jacobus Jozef Backx ,  Lieven Meerpoel

    IPC分类号： A61K31/47 ,  A61P31/04 ,  C07D215/227

    CPC分类号： C07D215/227 ,  A61K31/47

    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 (I) a pharmaceutically acceptable acid or base addition salt, a quaternary amine, a stereochemically isomeric form, a tautomeric form 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 to 3; s is 0 to 4; R2 is hydrogen; halo; alkyl; hydroxy; mercapto; optionally substituted alkyloxy; alkyloxyalkyloxy; alkylthio; mono or di(alkyl)amino wherein alkyl may optionally be substituted; Ar; Het or a radical of formula 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 together with the phenyl ring to which they are attached a naphthyl; r is 1 to 5; R7 is hydrogen, alkyl, Ar or Het; R8 is hydrogen, alkyl, hydroxyl, aminocarbonyl, mono- or di(alkyl)aminocarbonyl, Ar, Het, alkyl substituted with one or two Het, alkyl substituted with one or two Ar, Het-C(═O)— or Ar—C(═O)—; provided that when the R3 bearing radical is placed in position 3 of the quinoline moiety; R7 is placed in position 4 and R2 is placed in position 2 and represents hydrogen, hydroxy, mercapto, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula then s is 1 to 4.

    Quinoline Derivatives as Antibacterial Agents
    3.
    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。

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

    公开(公告)号：US20080255116A1

    公开(公告)日：2008-10-16

    申请号：US11997182

    申请日：2006-07-31

    申请人： Koenraad Jozef Lodewijk Marcel Andries ,  Anil Koul ,  Jerome Emile Georges Guillemont ,  Elisabeth Therese Jeanne Pasquier ,  David Francis Alain Lancois

    发明人： Koenraad Jozef Lodewijk Marcel Andries ,  Anil Koul ,  Jerome Emile Georges Guillemont ,  Elisabeth Therese Jeanne Pasquier ,  David Francis Alain Lancois

    IPC分类号： A61K31/4709 ,  C07D215/20 ,  C07D405/02 ,  C07D401/04 ,  C07D413/04 ,  A61P31/04 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/4704

    CPC分类号： C07D215/227 ,  A61K31/47 ,  Y02A50/473

    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 quaternary amine 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 or 3; R2 is hydrogen; alkyl; hydroxy; mercapto; optionally substituted alkyloxy; alkyloxyalkyloxy; alkylthio; mono or di(alkyl)amino wherein alkyl may optionally be substituted; Ar; Het or a radical of formula R3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; q is zero, 1, 2, 3 or 4; X is a direct bond or CH2; 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 or a radical of formula 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，其季胺，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或3; R 2是氢; 烷基; 羟基; 巯基 任选取代的烷氧基; 烷氧基烷氧基; 烷硫基 单或二（烷基）氨基，其中烷基可任选被取代; Ar; Het或式R 3的基团是烷基，Ar，Ar-烷基，Het或Het-烷基; q为零，1,2,3或4; X是直接键或CH 2 N 2; R 4和R 5各自独立地是氢，烷基或苄基; 或R 4和R 5可以一起包括它们所连接的N; R 6是氢或式R 7的基团是氢，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-;

    NOVEL MYCOBACTERIAL INHIBITORS
    7.
    发明申请
    NOVEL MYCOBACTERIAL INHIBITORS 审中-公开
    新型MYCOBACTERIAL INHIBITORS

    公开(公告)号：US20110124870A1

    公开(公告)日：2011-05-26

    申请号：US13020079

    申请日：2011-02-03

    申请人： Jérôme Emile Georges GUILLEMONT ,  Elisabeth Therese Jeanne Pasquier ,  David Francis Alain Lancois

    发明人： Jérôme Emile Georges GUILLEMONT ,  Elisabeth Therese Jeanne Pasquier ,  David Francis Alain Lancois

    IPC分类号： C07D405/04 ,  C07D409/04 ,  C07D215/14

    CPC分类号： C07D215/14 ,  C07D215/227 ,  C07D215/38 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14

    摘要： The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or the general Formula (Ib) the pharmaceutically acceptable acid or base addition salts thereof, the quaternary amines thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof and the N-oxide forms thereof. The claimed compounds are useful for the treatment of mycobacterial diseases. In particular, compounds are claimed in which, independently from each other, R1 is halo; p=1; R2 is optionally substituted alkyloxy, alkyl, Ar, Het, or a radical of formula R3 is optionally substituted Ar or Het; q=1, R4 and R5 each independently are alkyl; R6 is hydrogen or a radical of formula r is equal to 0 or 1 and R7 is hydrogen or Ar. 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 mycobacterial diseases and a process for preparing the claimed compounds.

    摘要翻译： 本发明涉及根据通式（Ia）或通式（Ib）的新的取代喹啉衍生物，其药学上可接受的酸或碱加成盐，其季胺，其立体化学异构形式，其互变异构形式和 其N-氧化物形式。 所要求保护的化合物可用于治疗分枝杆菌病。 特别地，要求保护的化合物，其中R1彼此独立地为卤素; p = 1; R 2是任选取代的烷氧基，烷基，Ar，Het或式R3的基团是任选取代的Ar或Het; q = 1，R4和R5各自独立地为烷基; R6是氢或式r的基团等于0或1，而R7是氢或Ar。 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分枝杆菌疾病的药物中的用途以及制备方法 要求保护的化合物。

    Mycobacterial inhibitors
    8.
    发明授权
    Mycobacterial inhibitors 有权
    分枝杆菌抑制剂

    公开(公告)号：US07902225B2

    公开(公告)日：2011-03-08

    申请号：US10596270

    申请日：2005-01-21

    申请人： Jérôme Emile Georges Guillemont ,  Elisabeth Therese Jeanne Pasquier ,  David Francis Alain Lancois

    发明人： Jérôme Emile Georges Guillemont ,  Elisabeth Therese Jeanne Pasquier ,  David Francis Alain Lancois

    IPC分类号： C07D215/38 ,  A61K31/04

    CPC分类号： C07D215/14 ,  C07D215/227 ,  C07D215/38 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14

    摘要： The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or the general Formula (Ib) the pharmaceutically acceptable acid or base addition salts thereof, the quaternary amines thereof, the stereochemically isomeric forms thereof the tautomeric forms thereof and the N-oxide forms thereof. The claimed compounds are useful for the treatment of mycobacterial diseases. In particular, compounds are claimed in which, independently from each other, R1 is halo; p=1; R2 is optionally substituted alkyloxy, alkyl, Ar, Het, or a radical of formula R3 is optionally substituted Ar or Het; q=1, R4 and R5 each independently are alkyl; R6 is hydrogen or a radical of formula r is equal to 0 or 1 and R7 is hydrogen or Ar. 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 mycobacterial diseases and a process for preparing the claimed compounds.

    摘要翻译： 本发明涉及根据通式（Ia）或通式（Ib）的新的取代喹啉衍生物，其药学上可接受的酸或碱加成盐，其季胺，其互变异构形式的立体化学异构形式和 N-氧化物形式。 所要求保护的化合物可用于治疗分枝杆菌病。 特别地，要求保护的化合物，其中R1彼此独立地为卤素; p = 1; R 2是任选取代的烷氧基，烷基，Ar，Het或式R3的基团是任选取代的Ar或Het; q = 1，R4和R5各自独立地为烷基; R6是氢或式r的基团等于0或1，而R7是氢或Ar。 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分枝杆菌疾病的药物中的用途以及制备方法 要求保护的化合物。