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1. 发明申请

US20100063026A1 ANTIBACTERIAL QUINOLINE DERIVATIVES 审中-公开
标题翻译：抗生素喹啉衍生物
公开(公告)号：US20100063026A1
公开(公告)日：2010-03-11
申请号：US12516420
申请日：2007-12-04
申请人： Jérôme Emile Georges Guillemont , Ismet Dorange , David Francis Alain Lançois , José Manuel Villalgordo-Soto , Yvan René Ferdinand , Magali Madeleine Simone Motte , Koenraad Jozef Lodewijk Marcel Andries , Anil Koul
发明人： Jérôme Emile Georges Guillemont , Ismet Dorange , David Francis Alain Lançois , José Manuel Villalgordo-Soto , Yvan René Ferdinand , Magali Madeleine Simone Motte , Koenraad Jozef Lodewijk Marcel Andries , Anil Koul
IPC分类号： A61K31/4709 , C07D215/227 , C07D401/06 , C07D401/14 , C07D487/04 , C07D417/06 , A61K31/551 , A61K31/541 , A61P31/04
CPC分类号： C07D401/06 , C07D215/227 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/14 , C07D417/06 , C07D487/08
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。

2. 发明授权

US08841321B2 Quinoline derivatives as antibacterial agents 有权
标题翻译：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 =。

3. 发明授权

US08415475B2 Antibacterial quinoline derivatives 有权
标题翻译：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。

4. 发明授权

US07915292B2 Antibacterial quinoline derivatives 有权
标题翻译：抗菌喹啉衍生物
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。

5. 发明授权

US08017606B2 Quinoline derivatives as antibacterial agents 有权
标题翻译：喹啉衍生物作为抗菌剂
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。

6. 发明授权

US08802671B2 Quinoline derivatives as antibacterial agents 有权
标题翻译：喹啉衍生物作为抗菌剂
公开(公告)号：US08802671B2
公开(公告)日：2014-08-12
申请号：US11997173
申请日：2006-07-31
申请人： Jérôme Emile Georges Guillemont , Elisabeth Thérèse Jeanne Pasquier , David Francis Alain Lançois , Koenraad Jozef Lodewijk Marcel Andries , Anil Koul , Leo Jacobus Jozef Backx , Lieven Meerpoel
发明人： Jérôme Emile Georges Guillemont , Elisabeth Thérèse Jeanne Pasquier , David Francis Alain Lançois , Koenraad Jozef Lodewijk Marcel Andries , Anil Koul , Leo Jacobus Jozef Backx , Lieven Meerpoel
IPC分类号： A61K31/535
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.
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（I）化合物，其药学上可接受的酸或碱加成盐，季铵盐胺，立体化学异构形式，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，（Ar）烷基; p为1〜3; s为0〜4; R2是氢; 光环; 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基团可以与它们所连接的苯环一起形成萘基; r为1〜5; R7是氢，烷基，Ar或Het; R8是氢，烷基，羟基，氨基羰基，单或二（烷基）氨基羰基，Ar，Het，被一个或两个Het取代的烷基，被一个或两个Ar，Het-C（= O） - 或Ar- C（= O） - ; 条件是当将带有R3的自由基置于喹啉部分的位置3时; R7位于4位，R2位于2位，代表氢，羟基，巯基，烷氧基，烷氧基烷氧基，烷硫基，单或二（烷基）氨基或式基团，其中s为1至4。

7. 发明申请

US20140163038A1 Antibacterial piperidinyl substituted 3,4-dihydro-1H-[1,8]naphthyridinones 有权
标题翻译：抗菌哌啶基取代的3,4-二氢-1H- [1,8]萘啶酮
公开(公告)号：US20140163038A1
公开(公告)日：2014-06-12
申请号：US14237851
申请日：2012-08-10
申请人： Jerôme Emile Georges Guillemont , David Francis Alain Lançois , Magali Madeleine Simone Motte , Anil Koul , Wendy Mia Albert Balemans
发明人： Jerôme Emile Georges Guillemont , David Francis Alain Lançois , Magali Madeleine Simone Motte , Anil Koul , Wendy Mia Albert Balemans
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The present invention is related to novel compounds of formula (I) that inhibit the activity of the Fab1 enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.
摘要翻译：本发明涉及抑制Fab1酶活性的新型式（I）化合物，因此可用于治疗细菌感染。它还涉及包含这些化合物的药物组合物和用于制备这些化合物的化学方法。

8. 发明授权

US08906923B2 Antibacterial cyclopenta[c]pyrrole substituted 3,4-dihydro-1H-[1,8]naphthyridinones 有权
公开(公告)号：US08906923B2
公开(公告)日：2014-12-09
申请号：US14237862
申请日：2012-08-10
申请人： Jerôme Emile Georges Guillemont , David Francis Alain Lançois , Magali Madeleine Simone Motte , Anil Koul , Wendy Mia Albert Balemans , Eric Pierre Alexandre Arnoult
发明人： Jerôme Emile Georges Guillemont , David Francis Alain Lançois , Magali Madeleine Simone Motte , Anil Koul , Wendy Mia Albert Balemans , Eric Pierre Alexandre Arnoult
IPC分类号： C07D471/00 , C07D487/00 , C07D471/02 , A61K31/50 , A61K31/495 , A61K31/44
CPC分类号： C07D471/04 , C07D487/04 , C07D519/00
摘要： The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.

9. 发明授权

US09394295B2 Antibacterial homopiperidinyl substituted 3,4-dihydro-1H-[1,8]naphthyridinones 有权
标题翻译：抗菌高哌啶基取代的3,4-二氢-1H- [1,8]萘啶酮
公开(公告)号：US09394295B2
公开(公告)日：2016-07-19
申请号：US14237841
申请日：2012-08-10
申请人： Jerôme Emile Georges Guillemont , David Francis Alain Lançois , Magali Madeleine Simone Motte , Anil Koul , Wendy Mia Albert Balemans
发明人： Jerôme Emile Georges Guillemont , David Francis Alain Lançois , Magali Madeleine Simone Motte , Anil Koul , Wendy Mia Albert Balemans
IPC分类号： A61K31/55 , A61K31/551 , C07D471/04
CPC分类号： C07D471/04
摘要： The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.
摘要翻译：本发明涉及抑制因此可用于治疗细菌感染的FabI酶的活性的式（I）化合物。它还涉及包含这些化合物的药物组合物和用于制备这些化合物的化学方法。

10. 发明授权

US09012634B2 Antibacterial piperidinyl substituted 3,4-dihydro-1H-[1,8]naphthyridinones 有权
标题翻译：抗菌哌啶基取代的3,4-二氢-1H- [1,8]萘啶酮
公开(公告)号：US09012634B2
公开(公告)日：2015-04-21
申请号：US14237851
申请日：2012-08-10
申请人： Jerôme Emile Georges Guillemont , David Francis Alain Lançois , Magali Madeleine Simone Motte , Anil Koul , Wendy Mia Albert Balemans
发明人： Jerôme Emile Georges Guillemont , David Francis Alain Lançois , Magali Madeleine Simone Motte , Anil Koul , Wendy Mia Albert Balemans
IPC分类号： A61K31/4375 , C07D515/04 , C07D471/04
CPC分类号： C07D471/04
摘要： The present invention is related to novel compounds of formula (I) that inhibit the activity of the Fab1 enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.
摘要翻译：本发明涉及抑制Fab1酶活性的新型式（I）化合物，因此可用于治疗细菌感染。它还涉及包含这些化合物的药物组合物和用于制备这些化合物的化学方法。

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