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1. 发明申请

US20080182855A1 Antibacterial Quinoline Derivatives 有权
标题翻译：抗菌喹啉衍生物
公开(公告)号：US20080182855A1
公开(公告)日：2008-07-31
申请号：US11996786
申请日：2006-07-26
申请人： Jerome Emile Georges Guillemont , David Francis Alain Lancois , Elisabeth Therese Jeanne Pasquier , Koenraad Jozef Lodewijk Andries , Anil Koul
发明人： Jerome Emile Georges Guillemont , David Francis Alain Lancois , Elisabeth Therese Jeanne Pasquier , Koenraad Jozef Lodewijk Andries , Anil Koul
IPC分类号： A61K31/496 , C07D215/12 , A61K31/47 , A61P31/04 , A61K31/4709 , C07D401/12
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。

2. 发明申请

US20090036466A1 AMINO-BENZIMIDAZOLES DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION 审中-公开
标题翻译：氨基苯并咪唑衍生物作为呼吸道同发病毒复制的抑制剂
公开(公告)号：US20090036466A1
公开(公告)日：2009-02-05
申请号：US10596500
申请日：2004-12-20
申请人： Jean-Francois Bonfanti , Koenraad Jozef Lodewijk Andries , Frans Eduard Janssens , Francois Maria Sommen , Jerome Emile Georges Guillemont , Jean Fernand Armand Lacrampe
发明人： Jean-Francois Bonfanti , Koenraad Jozef Lodewijk Andries , Frans Eduard Janssens , Francois Maria Sommen , Jerome Emile Georges Guillemont , Jean Fernand Armand Lacrampe
IPC分类号： A61K31/496 , C07D401/02 , A61K31/4439 , C07D401/14 , A61P31/12 , A61K31/4545 , C07D403/14
CPC分类号： C07D405/14 , C07D401/06 , C07D401/14
摘要： The present invention concerns amino-benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula their prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms wherein Q is Ar1 or C1-6alkyl substituted with one or more substituents selected from trifluoromethyl, C3-7cycloalkyl, Ar2, hydroxy, C1-4alkoxy, C1-4alkylthio, Ar2-oxy-, Ar2-thio-, Ar2(CH2)noxy, Ar2(CH2)nthio, hydroxycarbonyl, aminocarbonyl, C1-4alkylcarbonyl, Ar2-carbonyl, C1-4alkoxycarbonyl, Ar2(CH2)ncarbonyl, aminocarbonyloxy, C1-4alkylcarbonyloxy, Ar2-carbonyloxy, Ar2(CH2)ncarbonyloxy, hydroxy-C2-4-alkyloxy, C1-4alkoxycarbonyl(CH2)noxy, mono- or di(C1-4alkyl)-aminocarbonyl, mono- or di(C1-4alkyl)aminocarbonyloxy, aminosulfonyl, mono- or di(C1-4alkyl)aminosulfonyl, dioxolanyl optionally substituted with one or two C1-6alkyl radicals, and a heterocycle selected from pyrrolidinyl, pyrrolyl, dihydropyrrolyl, thiazolidinyl, imidazolyl, triazolyl, piperidinyl, homopiperidinyl, piperazinyl, pyridyl and tetrahydropyridyl, which each may optionally be substituted with oxo or C1-6alkyl; G is a direct bond or optionally substituted C1-10alkanediyl R1 is Ar1 or a monocyclic or bicyclic heterocycle; one of R2a and R3a is C1-6alkyl and the other one of R2a and R3a is hydrogen; in case R2a is different from hydrogen then R2b is hydrogen or C1-6alkyl, and R3b is hydrogen; in case R3a is different from hydrogen then R3b is hydrogen or C1-6alkyl, and R2b is hydrogen; Ar1 is phenyl or substituted phenyl and Ar2 is phenyl or substituted phenyl. It further concerns their preparation and compositions comprising them, as well as their use as a medicine.
摘要翻译：本发明涉及对呼吸道合胞病毒复制具有抑制活性的氨基苯并咪唑，其具有其前药，N-氧化物，加成盐，季胺，金属络合物和立体化学异构体形式，其中Q为Ar 1或C 1-6烷基取代具有一个或多个选自三氟甲基，C 3-7环烷基，Ar 2，羟基，C 1-4烷氧基，C 1-4烷硫基，Ar 2 - 氧基 - ，Ar 2 - 硫基 - ，Ar 2（CH 2）n羟基，Ar 2（CH 2）n硫基，羟基羰基，氨基羰基，C 1-4烷基羰基，Ar 2 - 羰基，C 1-4烷氧基羰基，Ar 2（CH 2）n羰基，氨基羰基氧基，C 1-4烷基羰基氧基，Ar 2 - 羰基氧基，Ar 2（CH 2）n - 羰基氧基，羟基-C 2-4 4-烷氧基，C 1-4烷氧基羰基（CH 2）一或二（C 1-4烷基） - 氨基羰基，一或二（C 1-4烷基）氨基羰基氧基，氨基磺酰基，一或二（C 1-4烷基）氨基磺酰基，任选被一个或两个C 1-6烷基取代的二氧戊环基，选自吡咯烷基，吡咯基，二氢吡咯基，噻唑烷基的杂环，咪唑基，三唑基，哌啶基，高哌啶基，哌嗪基，吡啶基和四氢吡啶基，其各自可以任选被氧代或C 1-6烷基取代; G是直接键或任选取代的C 1-10烷二基R 1是Ar 1或单环或双环杂环; R2a和R3a之一是C1-6烷基，R2a和R3a中的另一个是氢; 在R2a不同于氢的情况下，则R2b为氢或C1-6烷基，R3b为氢; 在R3a不同于氢的情况下，R 3b是氢或C 1-6烷基，R 2b是氢; Ar 1是苯基或取代的苯基，Ar 2是苯基或取代的苯基。它还涉及它们的制备方法和包含它们的组合物，以及它们作为药物的用途。

3. 发明申请

US20110166179A1 ANTIBACTERIAL QUINOLINE DERIVATIVES 审中-公开
标题翻译：抗生素喹啉衍生物
公开(公告)号：US20110166179A1
公开(公告)日：2011-07-07
申请号：US12516396
申请日：2007-12-04
申请人： Jérôme Emile Georges Guillemont , Koenraad Jozef Lodewijk Andries , Anil Koul
发明人： Jérôme Emile Georges Guillemont , Koenraad Jozef Lodewijk Andries , Anil Koul
IPC分类号： A61K31/47 , C07D215/227 , A61K31/4709 , A61P31/04
CPC分类号： C07D401/04 , C07D215/14 , 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 solvateas 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的化合物。

4. 发明申请

US20090062278A1 5- OR 6-SUBSTITUTED BENZIMIDAZOLE DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION 有权
标题翻译： 5-或6-取代的苯并咪唑衍生物作为呼吸道同种病毒复制的抑制剂
公开(公告)号：US20090062278A1
公开(公告)日：2009-03-05
申请号：US12253450
申请日：2008-10-17
申请人： Jean-Francois Bonfanti , Koenraad Jozef Lodewijk Andries , Jerome Michel Claude Fortin , Philippe Muller , Frederic Marc Maurice Doublet , Christophe Meyer , Rudy Edmond Willebrords , Tom Valerius Josepha Gevers , Philip Maria Martha Bern Timmerman
发明人： Jean-Francois Bonfanti , Koenraad Jozef Lodewijk Andries , Jerome Michel Claude Fortin , Philippe Muller , Frederic Marc Maurice Doublet , Christophe Meyer , Rudy Edmond Willebrords , Tom Valerius Josepha Gevers , Philip Maria Martha Bern Timmerman
IPC分类号： A61K31/5377 , A61K31/4545 , C07D211/06 , C07D413/14 , A61P31/12 , A61K31/496 , C07D403/14
CPC分类号： C07D401/06 , C07D401/14 , C07D405/14
摘要： The present invention concerns 5- or 6-substituted-benzimidazole derivatives having inhibitory activity on the replication of the respiratory syncytial virus and having the formula a prodrug, N-oxide, addition salt, quaternary amine, metal complex or stereochemically isomeric form thereof wherein Q is Ar2, R6, pyrrolidinyl substituted with R6, piperidinyl substituted with R6 or homopiperidinyl substituted with R6, G is a direct bond or optionally substituted C1-10alkanediyl; R1 is Ar1 or a monocyclic or bicyclic heterocycle; one of R2a and R2b is cyanoC1-6alkyl, cyanoC2-6alkenyl, Ar3C1-6alkyl, Het1C1-6alkyl, N(R8aR8b)C1-6alkyl, Ar3C2-6alkenyl, Het1C2-6alkenyl, Ar3aminoC1-6alkyl, Het1aminoC1-6alkyl, Ar3thioC1-6alkyl, Het1thioC1-6alkyl, Ar3sulfonylC1-6alkyl, Het1sulfonylC1-6alkyl, Ar3aminocarbonyl, Het1aminocarbonyl, Ar3(CH2)naminocarbonyl, Het1(CH2)naminocarbonyl, Ar3carbonylamino, Het1carbonylamino, Ar3(CH2)ncarbonylamino, Het1(CH2)ncarbonylamino, and the other one of R2a and R2b is hydrogen; in case R2a is hydrogen, then R3 is hydrogen; in case R2b is hydrogen, the R3 is hydrogen or C1-6alkyl. It further concerns their preparation and compositions comprising them, as well as their use as a medicine.
摘要翻译：本发明涉及对呼吸道合胞病毒复制具有抑制活性的5-或6-取代苯并咪唑衍生物，其具有前药，N-氧化物，加成盐，季胺，金属络合物或其立体化学异构形式，其中Q 是Ar 2，R 6，被R 6取代的吡咯烷基，被R 6取代的哌啶基或被R 6取代的高哌啶基，G是直接键或任意取代的C 1-10烷二基; R1是Ar1或单环或双环杂环; R2a和R2b之一是氰基C 1-6烷基，氰基C 2-6烯基，Ar 3 C 1-6烷基，Het 1 C 1-6烷基，N（R 8 a R 8 b）C 1-6烷基，Ar 3 C 2-6烯基，Het 1 C 2-6烯基，Ar 3氨基C 1-6烷基，Het 1氨基C 1-6烷基，Ar 3硫代C 1-6烷基， Het 1硫基C 1-6烷基，Ar 3磺酰基C 1-6烷基，Het 1磺酰基C 1-6烷基，Ar 3氨基羰基，Het 1氨基羰基，Ar 3（CH 2）n氨基羰基，Het 1（CH 2）n氨基羰基，Ar 3羰基氨基，Het 1羰基氨基，Ar 3（CH 2）n - 羰基氨基，Het 1（CH 2）n羰基氨基，和R2b是氢; 在R2a为氢的情况下，R3为氢; 在R2b为氢的情况下，R3为氢或C1-6烷基。它还涉及它们的制备方法和包含它们的组合物，以及它们作为药物的用途。

5. 发明授权

US08044073B2 Aminobenzimidazoles and benzimidazoles as inhibitors of respiratory syncytial virus replication 有权
标题翻译：氨基苯并咪唑和苯并咪唑作为呼吸道合胞病毒复制的抑制剂
公开(公告)号：US08044073B2
公开(公告)日：2011-10-25
申请号：US10596514
申请日：2004-12-20
申请人： Jean-François Bonfanti , Koenraad Jozef Lodewijk Andries , Jér{hacek over (o)}me Michel Claude Fortin , Philippe Muller , Frédéric Marc Maurice Doublet , Christophe Meyer , Rudy Edmond Willebrords , Tom Valerius Josepha Gevers , Philip Maria Martha Bern Timmerman
发明人： Jean-François Bonfanti , Koenraad Jozef Lodewijk Andries , Jér{hacek over (o)}me Michel Claude Fortin , Philippe Muller , Frédéric Marc Maurice Doublet , Christophe Meyer , Rudy Edmond Willebrords , Tom Valerius Josepha Gevers , Philip Maria Martha Bern Timmerman
IPC分类号： A61K31/4439 , C07D401/04 , C07D401/06
CPC分类号： C07D401/06 , C07D235/20 , C07D235/30 , C07D401/12 , C07D401/14 , C07D403/02 , C07D405/14 , C07D471/04 , C07F9/65583
摘要： Aminobenzimidazoles and benzimidazoles having inhibitory activity on RSV replication and having the formula the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof; wherein G is a direct bond or C1-10alkanediyl optionally substituted with one or more hydroxy, C1-6alkyloxy, Ar1C1-6alkyloxy, C1-6alkylthio, Ar1C1-6alkylthio, HO(—CH2—CH2—O)n—, C1-6alkyloxy(—CH2—CH2—O)n— or Ar1C1-6alkyloxy(—CH2—CH2—O)n—; R1 is Ar1 or a monocyclic or bicyclic heterocycle; Q is hydrogen, amino or mono- or di(C1-4alkyl)amino; one of R2a and R3a is selected from halo, optionally mono- or polysubstituted C1-6alkyl, optionally mono- or polysubstituted C2-6alkenyl, nitro, hydroxy, Ar2, N(R4aR4b), N(R4aR4b)sulfonyl, N(R4aR4b)carbonyl, C1-6alkyloxy, Ar2oxy, Ar2C1-6alkyloxy, carboxyl, C1-6alkyloxycarbonyl, or —C(═Z)Ar2; and the other one of R2a and R3a is hydrogen; in case R2a is different from hydrogen then R2b is hydrogen, C1-6alkyl or halogen and R3b is hydrogen; in case R3a is different from hydrogen then R3b is hydrogen, C1-6alkyl or halogen and R2b is hydrogen. Compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.
摘要翻译：对RSV复制具有抑制活性的氨基苯并咪唑和苯并咪唑，具有前药，N-氧化物，加成盐，季胺，金属络合物及其立体化学异构形式; 其中G是直接键或任选被一个或多个羟基，C 1-6烷氧基，Ar 1 C 1-6烷氧基，C 1-6烷硫基，Ar 1 C 1-6烷硫基，HO（-CH 2 -CH 2 -O）n - ，C 1-6烷氧基（ -CH 2 -CH 2 -O）n - 或Ar 1 C 1-6烷氧基（-CH 2 -CH 2 -O）n - R1是Ar1或单环或双环杂环; Q是氢，氨基或单或二（C 1-4烷基）氨基; R 2a和R 3a中的一个选自卤素，任选的单取代或多取代的C 1-6烷基，任选单取代或多取代的C 2-6烯基，硝基，羟基，Ar 2，N（R 4aR 4 b），N（R 4 R 4 b）磺酰基，N（R 4 R 4 b），C 1-6烷氧基，Ar 2氧基，Ar 2 C 1-6烷氧基，羧基，C 1-6烷氧基羰基或-C（= Z）Ar 2; R2a和R3a中的另一个是氢; 在R2a不同于氢的情况下，R2b为氢，C1-6烷基或卤素，R3b为氢; 在R3a不同于氢的情况下，R 3b是氢，C 1-6烷基或卤素，R 2b是氢。含有这些化合物作为活性成分的组合物和制备这些化合物和组合物的方法。

6. 发明授权

US07355051B2 Piperdine-amino-benzimidazole derivatives as inhibitors of respiratory syncytial virus replication 有权
公开(公告)号：US07355051B2
公开(公告)日：2008-04-08
申请号：US10596519
申请日：2004-12-20
申请人： Jean-François Bonfanti , Koenraad Jozef Lodewijk Andries , Frans Eduard Janssens , François Maria Sommen , Jerôme Emile Georges Guillemont , Jean Fernand Armand Lacrampe
发明人： Jean-François Bonfanti , Koenraad Jozef Lodewijk Andries , Frans Eduard Janssens , François Maria Sommen , Jerôme Emile Georges Guillemont , Jean Fernand Armand Lacrampe
IPC分类号： C07D401/106
CPC分类号： C07D401/14 , C07D417/14
摘要： The present invention concerns piperidine-amino-benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula their prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms wherein Q is C1−6alkyl optionally substituted with trifluoromethyl, C3-7cycloalkyl, Ar2, hydroxy, C1−4alkoxy, C1−4alkylthio, Ar2-oxy-, Ar2-thio-, Ar2(CH2)noxy, Ar2(CH2)nthio, hydroxycarbonyl, aminocarbonyl, C1−4alkyl-carbonyl, Ar2carbonyl, C1−4alkoxycarbonyl, Ar2(CH2)ncarbonyl, aminocarbonyloxy, C1−4alkylcarbonyloxy, Ar2carbonyloxy, Ar2(CH2)ncarbonyloxy, C1−4alkoxy-carbonyl(CH2)noxy, mono- or di(C1−4alkyl)aminocarbonyl, mono- or di(C1−4alkyl)-aminocarbonyloxy, aminosulfonyl, mono- or di(C1−4alkyl)aminosulfonyl or a heterocycles selected from the group consisting of pyrrolidinyl, pyrrolyl, dihydropyrrolyl, imidazolyl, triazolyl, piperidinyl, homopiperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, 1-oxo-thiomorpholinyl, 1,1-dioxothiomorpholinyl, pyridyl and tetrahydropyridyl, wherein each of said heterocycle may optionally be substituted with oxo or C1−6alkyl; G is a direct bond or optionally substituted C1-10alkanediyl; R1 is Ar1 or a monocyclic or bicyclic heterocycle; one of R2a and R3a is C1−6alkyl and the other one of R2a and R3a is hydrogen; in case R2a is different from hydrogen then R2b is hydrogen or C1−6alkyl, and R3b is hydrogen; in case R3a is different from hydrogen then R3b is hydrogen or C1−6alkyl, and R2b is hydrogen; t is 1, 2 or 3; Ar1 is phenyl or substituted phenyl; and Ar2 is phenyl or substituted phenyl. It further concerns their preparation and compositions comprising them, as well as their use as a medicine.

7. 发明授权

US07449463B2 Morpholinyl containing benzimidazoles as inhibitors of respiratory syncytial virus replication 有权
公开(公告)号：US07449463B2
公开(公告)日：2008-11-11
申请号：US10563691
申请日：2004-12-20
申请人： Jean-François Bonfanti , Koenraad Jozef Lodewijk Andries , Jérôme Michel Claude Fortin , Philippe Muller , Frédéric Marc Maurice Doublet , Christophe Meyer , Rudy Edmond Willebrords , Tom Valerius Josepha Gevers , Philip Maria Martha Bern Timmerman
发明人： Jean-François Bonfanti , Koenraad Jozef Lodewijk Andries , Jérôme Michel Claude Fortin , Philippe Muller , Frédéric Marc Maurice Doublet , Christophe Meyer , Rudy Edmond Willebrords , Tom Valerius Josepha Gevers , Philip Maria Martha Bern Timmerman
IPC分类号： A61K31/535 , C07D413/00
CPC分类号： C07D413/12 , C07D401/06 , C07D401/14 , C07D413/14
摘要： The present invention concerns morpholinyl containing benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula a prodrug, N-oxide, addition salt, quaternary amine, metal complex or stereochemically isomeric form thereof wherein G is a direct bond or optionally substituted C1-10alkanediyl; R1 is Ar1 or a monocyclic or bicyclic heterocycle Q is R7, pyrrolidinyl substituted with R7, piperidinyl substituted with R7 or homopiperidinyl substituted with R7; one of R2a and R3a is selected from halo, optionally mono- or polysubstituted C1-6alkyl, optionally mono- or polysubstituted C2-6alkenyl, nitro, hydroxy, Ar2, N(R4aR4b), N(R4aR4b)sulfonyl, N(R4aR4b)carbonyl, C1-6alkyloxy, Ar2oxy, Ar2C1-6alkyloxy, carboxyl, C1-6alkyloxycarbonyl, or —C(=Z)Ar2; and the other one of R2a and R3a is hydrogen; in case R2a is different from hydrogen then R2b is hydrogen, C1-6alkyl or halogen and R3b is hydrogen; in case R3a is different from hydrogen then R3b is hydrogen, C1-6alkyl or halogen and R2b is hydrogen. It further concerns the preparation thereof and compositions comprising these compounds, as well as the use thereof as a medicine.

8. 发明申请

US20070099924A1 Aminobenzimidazoles and benzimidazoles as inhibitors of respiratory syncytial virus replication 有权
公开(公告)号：US20070099924A1
公开(公告)日：2007-05-03
申请号：US10596514
申请日：2004-12-20
申请人： Jean-Francois Bonfanti , Koenraad Jozef Lodewijk Andries , Jerome Michel Claude Fortin , Philippe Muller , Frederic Marc Maurice Doublet , Chirstophe Meyer , Rudy Edmond Willebrods , Tom Valerius Josepha Gevers , Philip Maria Martha Bern Timmerman
发明人： Jean-Francois Bonfanti , Koenraad Jozef Lodewijk Andries , Jerome Michel Claude Fortin , Philippe Muller , Frederic Marc Maurice Doublet , Chirstophe Meyer , Rudy Edmond Willebrods , Tom Valerius Josepha Gevers , Philip Maria Martha Bern Timmerman
IPC分类号： A61K31/498 , A61K31/497 , A61K31/4709 , A61K31/4439 , A61K31/4184 , C07D403/02
CPC分类号： C07D401/06 , C07D235/20 , C07D235/30 , C07D401/12 , C07D401/14 , C07D403/02 , C07D405/14 , C07D471/04 , C07F9/65583
摘要： Aminobenzimidazoles and benzimidazoles having inhibitory activity on RSV replication and having the formula the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof, wherein G is a direct bond or C1-10alkanediyl optionally substituted with one or more hydroxy, C1-6alkyloxy, Ar1C1-6alkyloxy, C1-6alkylthio, Ar1C1-6alkylthio, HO(—CH2—CH2—O)n—, C1-6alkyloxy(—CH2—CH2—O)n— or Ar1C1-6alkyloxy(—CH2—CH2—O)n—; R1 is Ar1 or a monocyclic or bicyclic heterocycle; Q is hydrogen, amino or mono- or di(C1-4alkyl)amino; one of R2a and R3a is selected from halo, optionally mono- or polysubstituted C1-6alkyl, optionally mono- or polysubstituted C2-6alkenyl, nitro, hydroxy, Ar2, N(R4aR4b), N(R4aR4b)sulfonyl, N(R4aR4b)carbonyl, C1-6alkyloxy, Ar2oxy, Ar2C1-6alkyloxy, carboxyl, C1-6alkyloxycarbonyl, or —C(═Z)Ar2; and the other one of R2a and R3a is hydrogen; in case R2a is different from hydrogen then R2b is hydrogen, C1-6alkyl or halogen and R3b is hydrogen; in case R3a is different from hydrogen then R3b is hydrogen, C1-6alkyl or halogen and R2b is hydrogen. Compositions containg these compounds as active ingredient and processes for preparing these compounds and compositions.

9. 发明授权

US08883837B2 Morpholinyl containing benzimidazoles as inhibitors of respiratory syncytial virus replication 有权
标题翻译：含有吗啉基的苯并咪唑作为呼吸道合胞病毒复制的抑制剂
公开(公告)号：US08883837B2
公开(公告)日：2014-11-11
申请号：US12140686
申请日：2008-06-17
申请人： Jean-Francois Bonfanti , Koenraad Jozef Lodewijk Andries , Jérôme Michel Claude Fortin , Philippe Muller , Frédéric Marc Maurice Doublet , Christophe Meyer , Rudy Edmond Willebrords , Tom Valerius Josepha Gevers , Philip Maria Martha Bern Timmerman
发明人： Jean-Francois Bonfanti , Koenraad Jozef Lodewijk Andries , Jérôme Michel Claude Fortin , Philippe Muller , Frédéric Marc Maurice Doublet , Christophe Meyer , Rudy Edmond Willebrords , Tom Valerius Josepha Gevers , Philip Maria Martha Bern Timmerman
IPC分类号： A01N43/52 , A61K31/415 , C07D233/00 , C07D235/02 , C07D487/04 , C07D487/06 , C07D413/12
CPC分类号： C07D413/12 , C07D401/06 , C07D401/14 , C07D413/14
摘要： The present invention concerns morpholinyl containing benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula a prodrug, N-oxide, addition salt, quaternary amine, metal complex or stereochemically isomeric form thereof. It further concerns the preparation thereof and compositions comprising these compounds, as well as the use thereof as a medicine.
摘要翻译：本发明涉及对具有对呼吸道合胞病毒复制具有抑制活性的含有吗啉基的苯并咪唑，其具有前药，N-氧化物，加成盐，季胺，金属络合物或其立体化学异构形式。还涉及其制备方法和包含这些化合物的组合物，以及作为药物的用途。

10. 发明授权

US08278455B2 5- or 6-substituted benzimidazole derivatives as inhibitors of respiratory syncytial virus replication 有权
标题翻译： 5-或6-取代的苯并咪唑衍生物作为呼吸道合胞病毒复制的抑制剂
公开(公告)号：US08278455B2
公开(公告)日：2012-10-02
申请号：US12253450
申请日：2008-10-17
申请人： Jean-François Bonfanti , Koenraad Jozef Lodewijk Andries , Jérôme Michel Claude Fortin , Philippe Muller , Frédéric Marc Maurice Doublet , Christophe Meyer , Rudy Edmond Willebrords , Tom Valerius Josepha Gevers , Philip Maria Martha Bern Timmerman
发明人： Jean-François Bonfanti , Koenraad Jozef Lodewijk Andries , Jérôme Michel Claude Fortin , Philippe Muller , Frédéric Marc Maurice Doublet , Christophe Meyer , Rudy Edmond Willebrords , Tom Valerius Josepha Gevers , Philip Maria Martha Bern Timmerman
IPC分类号： A61K31/4439 , C07D401/06
CPC分类号： C07D401/06 , C07D401/14 , C07D405/14
摘要： The present invention concerns 5- or 6-substituted-benzimidazole derivatives having inhibitory activity on the replication of the respiratory syncytial virus and having the formula a prodrug, N-oxide, addition salt, quaternary amine, metal complex or stereochemically isomeric form thereof wherein Q is Ar2, R6, pyrrolidinyl substituted with R6, piperidinyl substituted with R6 or homopiperidinyl substituted with R6, G is a direct bond or optionally substituted C1-10alkanediyl; R1 is Ar1 or a monocyclic or bicyclic heterocycle; one of R2a and R2b is cyanoC1-6alkyl, cyanoC2-6alkenyl, Ar3C1-6alkyl, Het1C1-6alkyl, N(R8aR8b)C1-6alkyl, Ar3C2-6alkenyl, Het1C2-6alkenyl, Ar3aminoC1-6alkyl, Het1aminoC1-6alkyl, Ar3thioC1-6alkyl, Het1thioC1-6alkyl, Ar3sulfonylC1-6alkyl, Het1sulfonylC1-6alkyl, Ar3aminocarbonyl, Het1aminocarbonyl, Ar3(CH2)namino-carbonyl, Het1(CH2)naminocarbonyl, Ar3carbonylamino, Het1carbonylamino, Ar3(CH2)ncarbonylamino, Het1(CH2)ncarbonylamino, and the other one of R2a and R2b is hydrogen; in case R2a is hydrogen, then R3 is hydrogen; in case R2b is hydrogen, the R3 is hydrogen or C1-6alkyl. It further concerns their preparation and compositions comprising them, as well as their use as a medicine.
摘要翻译：本发明涉及对呼吸道合胞病毒复制具有抑制活性的5-或6-取代苯并咪唑衍生物，其具有前药，N-氧化物，加成盐，季胺，金属络合物或其立体化学异构形式，其中Q 是Ar 2，R 6，被R 6取代的吡咯烷基，被R 6取代的哌啶基或被R 6取代的高哌啶基，G是直接键或任意取代的C 1-10烷二基; R1是Ar1或单环或双环杂环; R2a和R2b之一是氰基C 1-6烷基，氰基C 2-6烯基，Ar 3 C 1-6烷基，Het 1 C 1-6烷基，N（R 8 a R 8 b）C 1-6烷基，Ar 3 C 2-6烯基，Het 1 C 2-6烯基，Ar 3氨基C 1-6烷基，Het 1氨基C 1-6烷基，Ar 3硫代C 1-6烷基，（CH 2）n氨基 - 羰基，Het 1（CH 2）n氨基羰基，Ar 3羰基氨基，Het 1羰基氨基，Ar 3（CH 2）n - 羰基氨基，Het 1（CH 2）n - 羰基氨基，和另一个（CH 2）n C 1 -C 6烷基， R2a和R2b是氢; 在R2a为氢的情况下，R3为氢; 在R2b为氢的情况下，R3为氢或C1-6烷基。它还涉及它们的制备方法和包含它们的组合物，以及它们作为药物的用途。

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