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    Respiratory syncytial virus replication inhibitors
    6.
    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.

    Piperdine-amino-benzimidazole derivatives as inhibitors of respiratory syncytial virus replication
    8.
    发明授权
    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.

    AMINO-BENZIMIDAZOLES DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION
    9.
    发明申请
    AMINO-BENZIMIDAZOLES DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION 审中-公开
    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。

    Triazolobenzazepine derivatives
    10.
    发明授权
    Triazolobenzazepine derivatives 失效
    三唑并苯并吖嗪衍生物

    公开(公告)号：US5932569A

    公开(公告)日：1999-08-03

    申请号：US433388

    申请日：1996-05-08

    申请人： Frans Eduard Janssens ,  Jean Fernand Armand Lacrampe ,  Isabelle Noelle Constance Pilatte

    发明人： Frans Eduard Janssens ,  Jean Fernand Armand Lacrampe ,  Isabelle Noelle Constance Pilatte

    IPC分类号： A61K31/55 ,  A61P37/08 ,  C07D487/04 ,  C07D519/00 ,  C07D223/18

    CPC分类号： C07D487/04

    摘要： Antiallergic triazolobenzazepines of formula ##STR1## wherein each of the dotted lines independently represents an optional bond; R.sup.1 represents hydrogen, halo, C.sub.1-4 alkyl, hydroxy or C.sub.1-4 alkyloxy; R.sup.2 represents hydrogen, halo, C.sub.1-4 alkyl, hydroxy or C.sub.1-4 alkyloxy; R.sup.3 represents hydrogen, C.sub.1-4 alkyl or halo; --B.dbd.D-- is a bivalent radical of formula --C(R.sup.4).dbd.N--(a-1); or --N.dbd.C(R.sup.5)-- (a-2); R.sup.4 and R.sup.5 represent hydrogen, C.sub.1-4 alkyl, ethenyl substituted with hydroxycarbonyl or C.sub.1-4 alkyloxycarbonyl, C.sub.1-4 alkyl substituted with hydroxycarbonyl or C.sub.1-4 alkyloxycarbonyl, hydroxyC.sub.1-4 alkyl, formyl or hydroxycarbonyl; R.sup.5 also represents phenyl or pyridinyl; L represents hydrogen; C.sub.1-6 alkyl; substituted C.sub.1-6 alkyl, C.sub.3-6 alkenyl; C.sub.3-6 alkenyl substituted with aryl or, L represents a radical of formula -Alk-Y-Het.sup.1 (b-1), -Alk-NH--CO--Het.sup.2 (b-2) or --Alk-Het.sup.3 (b-3). Compositions comprising said compounds, processes of preparing the same, and intermediates in the preparation thereof.

    摘要翻译： PCT No.PCT / EP93 / 03320 Sec。 371日期1995年5月8日 102（e）日期1995年5月8日PCT提交1993年11月25日PCT公布。 公开号WO94 / 13671 日期1994年6月23日具有下式的抗变应性三唑并苯并吖嗪：其中每个虚线独立地表示任选的键; R 1表示氢，卤素，C 1-4烷基，羟基或C 1-4烷氧基; R 2表示氢，卤素，C 1-4烷基，羟基或C 1-4烷氧基; R3表示氢，C1-4烷基或卤素; -B = D-是式-C（R4）= N-（a-1）的二价基团; 或-N = C（R5） - （a-2）; R 4和R 5表示氢，C 1-4烷基，被羟基羰基或C 1-4烷氧基羰基取代的乙烯基，被羟基羰基或C 1-4烷氧基羰基取代的C 1-4烷基，羟基C 1-4烷基，甲酰基或羟基羰基; R5也表示苯基或吡啶基; L表示氢; C 1-6烷基; 取代的C 1-6烷基，C 3-6烯基; 由芳基取代的C 3-6链烯基，或L表示式-Alk-Y-Het1（b-1），-Alk-NH-CO-Het2（b-2）或-Alk-Het3（b-3）的基团。 包含所述化合物的组合物，其制备方法以及其制备中的中间体。