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。

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.

公开(公告)号：US20080227775A1

公开(公告)日：2008-09-18

申请号：US11997015

申请日：2006-07-31

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

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

IPC分类号： A61K31/5355 ,  C07D413/08 ,  A61P31/04

CPC分类号： C07D413/06 ,  A61K31/4709 ,  C07D413/14 ,  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, 3 or 4; R2 is hydrogen, hydroxy, thio, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula R3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; R4 is hydrogen, alkyl or benzyl; R5 is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; or two vicinal R5 radicals may be taken together to form together with the phenyl ring to which they are attached a naphthyl; r is 1, 2, 3, 4 or 5; R6 is hydrogen, alkyl, Ar or Het; R7 is hydrogen or alkyl; R5 is oxo; or R7 and R5 together form the radical —CH═CH—N═; Z is CH2 or C(═O).

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1,2,3或4; R 2是氢，羟基，硫代，烷氧基，烷氧基烷氧基，烷硫基，一或二（烷基）氨基或式R 3的基团是烷基，Ar，Ar- 烷基，Het或Het-烷基; R 4是氢，烷基或苄基; R 5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 5个基团可以与它们所连接的苯环一起形成萘基; r为1,2,3,4或5; R 6是氢，烷基，Ar或Het; R 7是氢或烷基; R 5是氧代; 或R 7和R 5一起形成基团-CH-CH-N-; Z是CH 2或C（-O）。

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。

公开(公告)号：US07915292B2

公开(公告)日：2011-03-29

申请号：US11996786

申请日：2006-07-26

申请人： Jérôme Emile Georges Guillemont ,  David Francis Alain Lançois ,  Elisabeth Thérèse Jeanne Pasquier ,  Koenraad Jozef Lodewijk Marcel Andries ,  Anil Koul

发明人： Jérôme Emile Georges Guillemont ,  David Francis Alain Lançois ,  Elisabeth Thérèse Jeanne Pasquier ,  Koenraad Jozef Lodewijk Marcel Andries ,  Anil Koul

IPC分类号： C07D215/00 ,  A61K31/472

CPC分类号： C07D215/227 ,  C07D215/12 ,  C07D215/48 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/06 ,  C07D405/12 ,  C07D413/06 ,  C07D417/06

摘要： The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or 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 a bacterial disease including a mycobacterial disease, particularly those diseases caused by pathogenic mycobacteria such as Mycobacterium tuberculosis, M. bovis, M. avium and M. marinum. 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 bacterial diseases 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：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 N-氧化物形式。 所要求保护的化合物可用于治疗细菌性疾病，包括分枝杆菌病，特别是由致病性分枝杆菌引起的疾病，例如结核分枝杆菌，牛分枝杆菌，鸟分枝杆菌和马氏海绵体。 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性疾病的药物中的用途以及制备方法 要求保护的化合物。

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-;

公开(公告)号：US20100204270A1

公开(公告)日：2010-08-12

申请号：US11917923

申请日：2006-06-26

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

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

IPC分类号： A61K31/47 ,  C07D215/16 ,  A61P31/04

CPC分类号： C07D215/227 ,  A61K31/4353 ,  A61K45/06 ,  C07D215/36 ,  A61K2300/00

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. Several of these compounds are also claimed as such. Further the combination of the above compounds with other antibacterial agents is described

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。 这些化合物中的几种也是这样声称的。 此外，还描述了上述化合物与其它抗菌剂的组合

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 =。

公开(公告)号：US08017606B2

公开(公告)日：2011-09-13

申请号：US11997182

申请日：2006-07-31

申请人： Koenraad Jozef Lodewijk Marcel Andries ,  Anil Koul ,  Jérôme Emile Georges Guillemont ,  Elisabeth Thérèse Jeanne ,  David Francis Alain Lançois

发明人： Koenraad Jozef Lodewijk Marcel Andries ,  Anil Koul ,  Jérôme Emile Georges Guillemont ,  Elisabeth Thérèse Jeanne ,  David Francis Alain Lançois

IPC分类号： A61K31/535 ,  A61K31/497 ,  A61K31/47

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═; and R11 is as defined in the claims.

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; R2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R3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CH2; 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; R6是氢或式R7的基团是氢，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 =; 和R 11如权利要求中所定义。

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。