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    Respiratory syncytial virus replication inhibitors
    1.
    发明授权
    Respiratory syncytial virus replication inhibitors 失效

    公开(公告)号：US07071192B1

    公开(公告)日：2006-07-04

    申请号：US10019376

    申请日：2000-06-20

    申请人： Frans Eduard Janssens ,  Jean Fernand Armand Lacrampe ,  Jérôme Emile Georges Guillemont ,  Marc Gaston Venet ,  Koenraad Jozef Lodewijk Marcel Andries

    发明人： Frans Eduard Janssens ,  Jean Fernand Armand Lacrampe ,  Jérôme Emile Georges Guillemont ,  Marc Gaston Venet ,  Koenraad Jozef Lodewijk Marcel Andries

    IPC分类号： A61P31/00 ,  A61K31/495 ,  A61K31/445 ,  C07D239/00 ,  C07D215/00

    CPC分类号： C07D401/14 ,  C07D409/14 ,  C07D471/04 ,  Y02P20/55

    摘要： The present invention concerns compounds of formula (I), prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof wherein -a1=a2-a3=a4-represents a radical of formula —CH═CH—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 formulae (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), wherein Alk is C1-6alkanediyl; Y1 is a bivalent radical of formula —NR2— or —CH(NR2R4)—; X1 is NR4, S, S(═O), S(═O)2, O, CH2, C(═O), CH(═CH2), CH(OH), CH(CH3), CH(OCH3), CH(SCH3), CH(NR5aR5b), CH2—NR4 or NR4—CH2; X2 is a direct bond, CH2, C(═O), NR4, C1-4alkyl-NR4, NR4—C1-4alkyl, t is 2 to 5; u is 1 to 5; v is 2 or 3; and whereby each hydrogen in Alk and in (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), may optionally be replaced by R3: provided that when R3 is hydroxy or C1-6alkyloxy, then R3 cannot replace a hydrogen atom in the a position relative to a nitrogen atom; G is a direct bond or optionally substituted C1-10alkanediyl; R1 is an optionally substituted bicyclic heterocycle; R2 is hydrogen, formyl, C1-6alkylcarbonyl, Hetcarbonyl, pyrrolidinyl, piperidinyl, homopiperidinyl, C3-7cycloalkyl or C1-10alkyl substituted with N(R6)2 and optionally with another substituent; R3 is hydrogen, hydroxy, C1-6alkyl, C1-6alkyloxy, aryl C1-6alkyl or aryl C1-6alkyloxy, R4 is hydrogen, C1-6alkyl or aryl C1-6alkyl; R5a, R5b, R5c and R5d are hydrogen or C1-6alkyl; or R5a and R5b, or R5c and R5d taken together from a bivalent radical of formula —(CH2)5- wherein S is 4 or 5; R6 is hydrogen, C1-4alkyl, formyl, hydroxy C1-6alkyl, C1-6alkylcarbonyl or C1-6alkyloxycarbonyl; aryl is optionally substituted phenyl; Het is pyridyl, pyrimidinyl, pyridazinyl, pyridazinyl; as respiratory syncytial virus replication inhibitors; their preparation, compositions containing them and their use as a medicine.

    Respiratory syncytial virus replication inhibitors
    7.
    发明授权
    Respiratory syncytial virus replication inhibitors 失效

    公开(公告)号：US07407969B2

    公开(公告)日：2008-08-05

    申请号：US11247392

    申请日：2005-10-11

    申请人： Frans Eduard Janssens ,  Jean Fernand Armand Lacrampe ,  Jerome Emile Geroges Guilemont ,  Marc G Venet ,  Koenraad Jozef Lodewijk Marcel Andries

    发明人： Frans Eduard Janssens ,  Jean Fernand Armand Lacrampe ,  Jerome Emile Geroges Guilemont ,  Marc G Venet ,  Koenraad Jozef Lodewijk Marcel Andries

    IPC分类号： A61P11/00 ,  A61P31/12 ,  A61K31/4709 ,  A61K31/4375 ,  A61K31/437 ,  A61K31/498 ,  A61K31/4409 ,  A61K31/436 ,  C07D471/04 ,  C07D417/14 ,  C07D413/14 ,  C07D409/14 ,  C07D401/06 ,  C07D491/056

    CPC分类号： C07D401/14 ,  C07D409/14 ,  C07D471/04 ,  Y02P20/55

    摘要： The present invention concerns compounds of formula (I), prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof wherein -a1=a2-a3=a4- represents a radical of formula —CH═CH—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 formulae (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), wherein Alk is C1-6alkanediyl; Y1 is a bivalent radical of formula —NR2— or —CH(NR2R4); X1 is NR4, S, S(═O), S(═O)2, O, CH2, C(═O), CH(═CH2), CH(OH), CH(CH3), CH(OCH3), CH(SCH3), CH(NR5aR5b), CH2—NR4 or NR4—CH2; X2 is a direct bond, CH2, C(═O), NR4, C1-4alkyl-NR4, NR4—C1-4alkyl, t is 2 to 5; u is 1 to 5; v is 2 or 3; and whereby each hydrogen in Alk and in (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), may optionally be replaced by R3; provided that when R3 is hydroxy or C1-6alkyloxy, then R3 cannot replace a hydrogen atom in the α position relative to a nitrogen atom; G is a direct bond or optionally substituted C1-10alkanediyl; R1 is an optionally substituted bicyclic heterocycle; R2 is hydrogen, formyl, C1-6alkylcarbonyl, Hetcarbonyl, pyrrolidinyl, piperidinyl, homopiperidinyl, C3-7cycloalkyl or C1-10alkyl substituted with N(R6)2 and optionally with another substituent; R3 is hydrogen, hydroxy, C1-6alkyl, C1-6alkyloxy, arylC1-6alkyl or arylC1-6alkyloxy, R4 is hydrogen, C1-6alkyl or arylC1-6alkyl; R5a, R5b, R5c and R5d are hydrogen or C1-6alkyl; or R5a and R5b, or R5c and R5d taken together from a bivalent radical of formula —(CH2)S— wherein S is 4 or 5; R6 is hydrogen, C1-4alkyl, formyl, hydroxyC1-6alkyl, C1-6alkylcarbonyl or C1-6alkyloxycarbonyl; aryl is optionally substituted phenyl; Het is pyridyl, pyrimidinyl, pyryzinyl, pyridazinyl; as respiratory syncytial virus replication inhibitors; their preparation, compositions containing them and their use as a medicine.

    Antibacterial quinoline derivatives
    8.
    发明授权
    Antibacterial quinoline derivatives 有权
    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。