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11. 发明授权

US07998979B2 Antibacterial quinoline derivatives 有权
标题翻译：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。

12. 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。

13. 发明授权

US10604523B2 1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]quinoxaline derivatives 有权
公开(公告)号：US10604523B2
公开(公告)日：2020-03-31
申请号：US14128835
申请日：2012-06-26
申请人： José Ignacio Andrés-Gil , Peter Jacobus Johannes Antonius Buijnsters , Andrés Avelino Trabanco-Suárez , Meri De Angelis , Greta Constantia Peter Vanhoof , Jérôme Emile Georges Guillemont , Frederik Jan Rita Rombouts , Maarten Vliegen , Guy Maurits R. Bormans , Sofie Jeanne Leopoldine Celen
发明人： José Ignacio Andrés-Gil , Peter Jacobus Johannes Antonius Buijnsters , Andrés Avelino Trabanco-Suárez , Meri De Angelis , Greta Constantia Peter Vanhoof , Jérôme Emile Georges Guillemont , Frederik Jan Rita Rombouts , Maarten Vliegen , Guy Maurits R. Bormans , Sofie Jeanne Leopoldine Celen
IPC分类号： A61K51/00 , A61M36/14 , C07D487/04 , A61K31/4985 , A61K45/06 , A61K51/04 , G01N33/60
摘要： The present invention relates to novel 1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]-quinoxaline derivatives as inhibitors of phosphodiesterase 2 (PDE2) and to a lesser extent of phosphodiesterase 10 (PDE10) or as inhibitors of both, phosphodiesterases 2 and 10. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which PDE2 is involved, or disorders in which both PDE2 and PDE10 are involved, such as neurological and psychiatric disorders, and endocrinological or metabolic diseases. The present invention also relates to radiolabelled compounds which may be useful for imaging and quantifying the PDE2 enzyme in tissues, using positron-emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging a tissue, cells or a host, in vitro or in vivo and to precursors of said compounds.

14. 发明授权

US07928104B2 7-phenylalkyl substituted 2-quinolinones and 2-quinoxalinones as poly(ADP-ribose) polymerase inhibitors 有权
标题翻译： 7-苯基烷基取代的2-喹啉酮和2-喹喔啉酮作为聚（ADP-核糖）聚合酶抑制剂
公开(公告)号：US07928104B2
公开(公告)日：2011-04-19
申请号：US10595882
申请日：2004-11-18
申请人： Dominique Jean-Pierre Mabire , Jérôme Emile Georges Guillemont , Jacobus Alphonsus Josephus Van Dun , Maria Victorina Francisca Somers , Walter Boudewijn Leopold Wouters
发明人： Dominique Jean-Pierre Mabire , Jérôme Emile Georges Guillemont , Jacobus Alphonsus Josephus Van Dun , Maria Victorina Francisca Somers , Walter Boudewijn Leopold Wouters
IPC分类号： A61K31/498 , C07D401/08
CPC分类号： C07D403/06 , C07D241/44 , C07D401/06
摘要： The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, R1, R2, R3, R4, R5, R6 and X have defined meanings.
摘要翻译：本发明提供式（I）化合物，其作为PARP抑制剂的用途以及包含所述式（I）化合物的药物组合物，其中n，R1，R2，R3，R4，R5，R6和X具有定义的含义。

15. 发明申请

US20100029679A1 ANTIBACTERIAL QUINOLINE DERIVATIVES 有权
公开(公告)号：US20100029679A1
公开(公告)日：2010-02-04
申请号：US12516249
申请日：2007-12-04
申请人： Jérôme Emile Georges Guillemont , Ismet Dorange , Magali Madeleine Simone Motte , Koenraad Jozef Lodewijk Marcel , Anil Koul
发明人： Jérôme Emile Georges Guillemont , Ismet Dorange , Magali Madeleine Simone Motte , Koenraad Jozef Lodewijk Marcel , Anil Koul
IPC分类号： A61K31/496 , C07D215/227 , C07D401/06 , A61K31/47 , A61P31/04
CPC分类号： C07D215/227 , C07D401/06 , C07D401/10 , C07D405/06 , C07D405/10 , C07D409/10
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.

16. 发明授权

US07563922B2 Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile 有权
标题翻译：制备4 - [[4 - [[4-（2-氰基乙烯基）-2,6-二甲基苯基]氨基] -2-嘧啶基]氨基]苄腈的方法
公开(公告)号：US07563922B2
公开(公告)日：2009-07-21
申请号：US11738688
申请日：2007-04-23
申请人： Didier Philippe Robert Schils , Joannes Josephus Maria Willems , Bart Petrus Anna Maria Jozef Medaer , Elisabeth Therese Jeanne Pasquier , Paul Adriaan Jan Janssen , Jan Heeres , Ruben Gerardus George Leenders , Jérôme Emile Georges Guillemont
发明人： Didier Philippe Robert Schils , Joannes Josephus Maria Willems , Bart Petrus Anna Maria Jozef Medaer , Elisabeth Therese Jeanne Pasquier , Paul Adriaan Jan Janssen , Jan Heeres , Ruben Gerardus George Leenders , Jérôme Emile Georges Guillemont
IPC分类号： C07C255/42 , C07C253/30 , C07C253/20 , C07D239/48 , A61K31/505 , A61P31/18
CPC分类号： C07D239/48 , C07C253/20 , C07C253/30 , C07C255/42
摘要： Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]amino]benzonitrile of formula (I), a N-oxide, a pharmaceutically acceptable acid addition salt, a quaternary amine or a stereochemically isomeric form thereof are provided, said processes comprise: a) reacting 4-(2-cyanoethenyl)-2,6-dimethylbenzenamine with an intermediate of formula (III) in the presence of a suitable solvent; b) reacting an intermediate of formula (IV) with acrylonitrile in the presence of a suitable palladium catalyst, a suitable base and a suitable solvent; c) dehydrating the corresponding amide of the compound of formula (I).
摘要翻译：用于制备式（I）的4 - [[4 - [[4-（2-氰基乙烯基）-2,6-二甲基苯基] - 氨基] -2-嘧啶基]氨基]苄腈的方法，N-氧化物，提供药学上可接受的酸加成盐，季胺或其立体化学异构形式，所述方法包括：a）使4-（2-氰基乙烯基）-2,6-二甲基苯胺与式（III）的中间体在合适的溶剂; b）在合适的钯催化剂，合适的碱和合适的溶剂的存在下使式（Ⅳ）的中间体与丙烯腈反应; c）使相应的式（I）化合物的酰胺脱水。

17. 发明授权

US07498343B2 Mycobacterial inhibitors 有权
标题翻译：分枝杆菌抑制剂
公开(公告)号：US07498343B2
公开(公告)日：2009-03-03
申请号：US11007026
申请日：2004-12-08
申请人： Jozef Frans Elisabetha Van Gestel , Jérôme Emile Georges Guillemont , Marc Gaston Venet , Hervé Jean Joseph Poignet , Laurence Françoise Bernadette Decrane , Daniel F. J. Vernier , Frank Christopher Odds
发明人： Jozef Frans Elisabetha Van Gestel , Jérôme Emile Georges Guillemont , Marc Gaston Venet , Hervé Jean Joseph Poignet , Laurence Françoise Bernadette Decrane , Daniel F. J. Vernier , Frank Christopher Odds
IPC分类号： A61K31/44 , C07D215/38
CPC分类号： C07D215/227 , C07D215/36 , C07D215/48 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/06 , C07D409/04 , C07D409/06 , C07D471/04
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 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, particularly those diseases caused by pathogenic mycobacteria such as Mycobacterium tuberculosis, M. bovis, M. avium and M. marinum. In particular, compounds are claimed in which, independently from each other, R1 is bromo, p=1, R2 is alkyloxy, R3 is optionally substituted naphthyl or phenyl, q=1, R4 and R5 each independently are hydrogen, methyl or ethyl, R6 is hydrogen, r is equal to 0 or 1 and R7 is hydrogen. 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）的药学上可接受的酸或碱加成盐，其立体化学异构形式，其互变异构形式和N-氧化物形式的新的取代喹啉衍生物其中。所要求保护的化合物可用于治疗分枝杆菌疾病，特别是由致病性分枝杆菌引起的疾病如结核分枝杆菌，牛分枝杆菌，鸟分枝杆菌和马氏海马。特别是要求保护的化合物，其中R 1为溴，p = 1，R 2为烷氧基，R 3为任选取代的萘基或苯基，q为1，R 4和R 5各自独立地为氢，甲基或乙基， R6是氢，r等于0或1，而R7是氢。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。

18. 发明授权

US07399856B2 Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-2pyrimidinyl]amino]benzonitrile 有权
标题翻译：制备4 - [[4 - [[4-（2-氰基乙烯基）-2,6-二甲基苯基]氨基] -2-2嘧啶基]氨基]苄腈的方法
公开(公告)号：US07399856B2
公开(公告)日：2008-07-15
申请号：US10523753
申请日：2003-08-07
申请人： Didier Philippe Robert Schils , Joannes Josephus Maria Willems , Bart Petrus Anna Maria Jozef Medaer , Elisabeth Therese Jeanne Pasquier , Paul Adriaan Jan Janssen , Jan Heeres , Ruben Gerardus George Leenders , Jérôme Emile Georges Guillemont
发明人： Didier Philippe Robert Schils , Joannes Josephus Maria Willems , Bart Petrus Anna Maria Jozef Medaer , Elisabeth Therese Jeanne Pasquier , Paul Adriaan Jan Janssen , Jan Heeres , Ruben Gerardus George Leenders , Jérôme Emile Georges Guillemont
IPC分类号： C07D239/48 , C07C255/42 , C07C253/30 , C07C253/20 , A61K31/505 , A61P31/18
CPC分类号： C07D239/48 , C07C253/20 , C07C253/30 , C07C255/42
摘要： Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]amino]benzonitrile of formula (I), a N-oxide, a pharmaceutically acceptable acid addition salt, a quaternary amine or a stereochemically isomeric form thereof are provided, said processes comprise: a) reacting 4-(2-cyanoethenyl)-2,6-dimethylbenzenamine with an intermediate of formula (III) in the presence of a suitable solvent; b) reacting an intermediate of formula (IV) with acrylonitrile in the presence of a suitable palladium catalyst, a suitable base and a suitable solvent; c) dehydrating the corresponding amide of the compound of formula (I).
摘要翻译：用于制备式（I）的4 - [[4 - [[4-（2-氰基乙烯基）-2,6-二甲基苯基] - 氨基] -2-嘧啶基]氨基]苄腈的方法，N-氧化物，提供药学上可接受的酸加成盐，季胺或其立体化学异构形式，所述方法包括：a）使4-（2-氰基乙烯基）-2,6-二甲基苯胺与式（III）的中间体在合适的溶剂; b）在合适的钯催化剂，合适的碱和合适的溶剂的存在下使式（Ⅳ）的中间体与丙烯腈反应; c）使相应的式（I）化合物的酰胺脱水。

19. 发明授权

US07338949B2 Mycobacterial inhibitors 有权
标题翻译：分枝杆菌抑制剂
公开(公告)号：US07338949B2
公开(公告)日：2008-03-04
申请号：US10596386
申请日：2005-01-21
申请人： Jérôme Emile Georges Guillemont , Elisabeth Therese Jeanne Pasquier
发明人： Jérôme Emile Georges Guillemont , Elisabeth Therese Jeanne Pasquier
IPC分类号： C07D413/06 , C07D413/14 , A61K31/5355 , A61P31/10
CPC分类号： C07D413/06 , C07D413/14
摘要： The present invention relates to novel substituted quinoline derivatives according to the general formula (Ia) or the general formula (Ib) salts, quaternary amines, stereochemically isomeric forms, tautomeric forms and N-oxide forms 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; R8 is oxo; or R7 and R8 taken together form the radical —CH═CH—N═; Z is CH2 or C(═O). The claimed compounds are useful for the treatment of mycobacterial diseases, particularly those diseases caused by pathogenic mycobacteria such as M. tuberculosis, M. bovis, M. avium, M. smegmatis and M. marinum. Also claimed is a pharmaceutical composition containing a compound of the present invention, 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，其盐，季胺，立体化学异构形式，互变异构形式和N-氧化物形式，其中R 1，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 8是氧代; 或R 7和R 8一起形成基团-CH-CH-N-; Z是CH 2或C（-O）。所要求保护的化合物可用于治疗分枝杆菌疾病，特别是由致病性分枝杆菌引起的疾病如结核分枝杆菌，牛分枝杆菌，鸟分枝杆菌，耻垢分枝杆菌和马氏海马。还要求保护的是含有本发明化合物，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的药物组合物及其制备方法。

20. 发明授权

US07173034B2 Respiratory syncytial virus replication inhibitors 失效
标题翻译：呼吸道合胞病毒复制抑制剂
公开(公告)号：US07173034B2
公开(公告)日：2007-02-06
申请号：US11144126
申请日：2005-06-03
申请人： Frans Eduard Janssens , Kathleen Petrus Marie-José Meersman , François Maria Sommen , Jérôme Emile Georges Guillemont , Jean Fernand Armand Lacrampe , Koenraad Jozef Lodewijk Marcel Andries
发明人： Frans Eduard Janssens , Kathleen Petrus Marie-José Meersman , François Maria Sommen , Jérôme Emile Georges Guillemont , Jean Fernand Armand Lacrampe , Koenraad Jozef Lodewijk Marcel Andries
IPC分类号： C07D401/12 , C07D401/06 , C07D401/14 , A61K31/4184
CPC分类号： A61K31/4184 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4745 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/551 , C07D235/24 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： This invention concerns the use of compounds of formula (I) wherein -a1=a2-a3=a4- is a radical of for CH═CH—, —N═CH—CH═CH—, —CH═N—CH═CH—, —CH═CH—N═CH—, —CH═CH—CH═N— wherein each hydrogen atom may optionally be substituted; Q is a radical of formulas (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7), (b-8), G is a direct bond or C1-10alkanediyl; R1 is an optionally substituted monocyclic heterocycle; for the manufacture of a medicament for the treatment of viral infections, in particular RSV infections. Certain compounds of formula (I) are new.
摘要翻译：本发明涉及式（I）化合物的用途，其中-a-1-a- 是式-CH = CH-CH = CH，-N-CH-CH-CH-，-CH-N-CH-CH-，-CH-CH-N-CH-，-CH -CH-CH-N-，其中每个氢原子可以任选被取代; Q是式（b-1），（b-2），（b-3），（b-4），（b-5），（b-6），（b-7） -8），G为直链或C 1-10烷二基; R 1是任选取代的单环杂环; 用于制备用于治疗病毒感染，特别是RSV感染的药物。某些式（I）化合物是新的。

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