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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.

    N-[4-(heteroarylmethyl)phenyl]-heteroarylamines
    3.
    发明授权
    N-[4-(heteroarylmethyl)phenyl]-heteroarylamines 有权
    N- [4-（杂芳基甲基）苯基] - 杂芳基胺

    公开(公告)号：US07378433B2

    公开(公告)日：2008-05-27

    申请号：US11639043

    申请日：2006-12-13

    申请人： Marc Gaston Venet ,  Dominique Jean-Pierre Mabire ,  Jean Fernand Armand Lacrampe ,  Gerard Charles Sanz

    发明人： Marc Gaston Venet ,  Dominique Jean-Pierre Mabire ,  Jean Fernand Armand Lacrampe ,  Gerard Charles Sanz

    IPC分类号： A61K31/425 ,  C07D257/04

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D513/04

    摘要： The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C1-6alkyl or aryl; R2 is hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl, optionally substituted pyrrolidinyl or aryl; R3 is hydrogen, optionally substituted C1-6alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.

    摘要翻译： 本发明涉及式I化合物的N-氧化物，其药学上可接受的加成盐和立体化学异构形式，其中R 1是氢，羟基，C 1-6 - 烷基或芳基; R 2是氢; 任选取代的C 1-12烷基; C 3-7环烷基; C 2-8链烯基，任选取代的吡咯烷基或芳基; R 3是氢，任选取代的C 1-6烷基或芳基; Het是选自咪唑基，三唑基，四唑基和吡啶基的任选取代的不饱和杂环; 是任选取代的不饱和单环或双环杂环; 并且芳基是任选取代的苯基。 本发明还涉及其制备方法和包含所述新化合物的组合物，以及它们作为药物的用途。

    IL-5 inhibiting 6-azauracil derivatives
    6.
    发明授权
    IL-5 inhibiting 6-azauracil derivatives 失效
    IL-5抑制6-氮尿嘧啶衍生物

    公开(公告)号：US06867207B2

    公开(公告)日：2005-03-15

    申请号：US09891888

    申请日：2001-06-26

    申请人： Jean Fernand Armand Lacrampe ,  Eddy Jean Edgard Freyne ,  Marc Gaston Venet ,  Gustaaf Maria Boeckx

    发明人： Jean Fernand Armand Lacrampe ,  Eddy Jean Edgard Freyne ,  Marc Gaston Venet ,  Gustaaf Maria Boeckx

    IPC分类号： A61P37/08 ,  C07D401/10 ,  C07D403/10 ,  C07D403/12 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14 ,  C07D253/065 ,  A61K31/53 ,  A61K17/00

    CPC分类号： C07D401/10 ,  C07D403/10 ,  C07D403/12 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14

    摘要： The present invention is concerned with the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, p and q are 0, 1, 2, 3 or 4 and q is also 5; X is O, S, NR3 or a direct bond; R1 is hydrogen, hydroxy, halo, optionally substituted amino, optionally substituted C1-6alkyl, C1-6alkyloxy, C3-7cycloalkyl or aryl; R2 is aryl, Het1, C3-7cycloalkyl, optionally substituted C1-6alkyl; and if X is O, S or NR3, then R2 may also be a carbonyl or thiocarbonyl linked substituent; R3 is hydrogen or C1-4alkyl; R4 and R5 independently are optionally substituted C1-6alkyl, halo, hydroxy, mercapto, C1-6alkyloxy, C1-6akylthio, C1-6alkylcarbonyloxy, aryl, cyano, nitro, Het3, R6 or NR7R8; R6 is substituted sulfonyl or sulfinyl; R7 and R8 are hydrogen, optionally substituted C1-4alkyl, aryl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl, Het3 and R6; R9 and R10 are each independently selected from hydrogen, optionally substituted C1-4alkyl, phenyl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl, Het3 and R6; R11 is hydroxy, mercapto, cyano, nitro, halo, trihalomethyl, C1-4alkyloxy, carboxyl, C1-4alkyloxycarbonyl, trihaloC1-4alkylsulfonyloxy, R6, NR7R8, C(═O)NR7R8, aryl, aryloxy, arylcarbonyl, C3-7cycloalkyl, C3-7cycloalkyloxy, phthalimide-2-yl, Het3 and C(═O)Het3; R12 and R13 are each independently selected from hydrogen, optionally substituted C1-4alkyl, phenyl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl and R6; aryl is optionally substituted phenyl; Het1, Het2 and Het3 are optionally substituted heterocycles; to processes for their preparation and compositions comprising them. It further relates to their use as a medicine.

    摘要翻译： 本发明涉及配制N-氧化物的化合物，其药学上可接受的加成盐及其立体化学异构形式，p和q分别为0,1,2,3或4，q也为5; X是O，S，NR 3或直接键; R 1是氢，羟基，卤素，任选取代的氨基，任选取代的C 1-6烷基，C 1-6烷氧基，C 3-7环烷基或芳基; R 2是芳基，Het 1，C 3-7环烷基，任选取代的C 1-6烷基; 并且如果X是O，S或NR 3，则R 2也可以是羰基或硫代羰基连接的取代基; R 3是氢或C 1-4烷基; R 4和R 5独立地是任选取代的C 1-6烷基，卤素，羟基，巯基，C 1-6烷氧基，C 1-6烷硫基，C 1-6烷基羰基氧基，芳基，氰基，硝基，Het 3， 或NR 7 R 8; R 6是取代的磺酰基或亚磺酰基; R 7和R 8是氢，任选取代的C 1-4烷基，芳基，羰基或硫代羰基连接的取代基，C 3-7环烷基，Het 3和R 6; R 9和R 10各自独立地选自氢，任选取代的C 1-4烷基，苯基，羰基或硫代羰基连接的取代基，C 3-7环烷基，Het 3和R 6; R 11是羟基，巯基，氰基，硝基，卤素，三卤代甲基，C 1-4烷氧基，羧基，C 1-4烷氧基羰基，三卤代C 1-4烷基磺酰氧基，R 6，NR 7 R 8，C（= O） NR 7 R 8，芳基，芳氧基，芳基羰基，C 3-7环烷基，C 3-7环烷氧基，邻苯二甲酰亚胺-2-基，Het 3和C（= O）Het 3; R 12和R 13各自独立地选自氢，任选取代的C 1-4烷基，苯基，羰基或硫代羰基连接的取代基，C 3-7环烷基和R 6; 芳基是任选取代的苯基; Het <1>，Het <

    N-[4-(heteroarylmethyl)phenyl]-heteroarylamines
    7.
    发明授权
    N-[4-(heteroarylmethyl)phenyl]-heteroarylamines 有权
    N- [4-（杂芳基甲基）苯基] - 杂芳基胺

    公开(公告)号：US06486187B1

    公开(公告)日：2002-11-26

    申请号：US09624966

    申请日：2000-07-25

    申请人： Marc Gaston Venet ,  Dominique Jean-Pierre Mabire ,  Jean Fernand Armand Lacrampe ,  Gerard Charles Sanz

    发明人： Marc Gaston Venet ,  Dominique Jean-Pierre Mabire ,  Jean Fernand Armand Lacrampe ,  Gerard Charles Sanz

    IPC分类号： A61K31422

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D513/04

    摘要： The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C1-6alkyl or aryl; R2 is hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl, optionally substituted pyrrolidinyl or aryl; R3 is hydrogen, optionally substituted C1-6alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.

    摘要翻译： 本发明涉及配制N-氧化物的化合物，其药学上可接受的加成盐和立体化学异构形式，其中R 1是氢，羟基，C 1-6烷基或芳基; R2是氢; 任选取代的C 1-12烷基; C 3-7环烷基; C 2-8烯基，任选取代的吡咯烷基或芳基; R3是氢，任选取代的C 1-6烷基或芳基; Het是选自咪唑基，三唑基，四唑基和吡啶基的任选取代的不饱和杂环;是任选取代的不饱和单环或双环杂环; 并且芳基是任选取代的苯基。 本发明还涉及其制备方法和包含所述新化合物的组合物，以及它们作为药物的用途。

    N-[4-(heteroarylmethyl)phenyl]-heteroarylamines
    9.
    发明授权
    N-[4-(heteroarylmethyl)phenyl]-heteroarylamines 有权
    N- [4-（杂芳基甲基）苯基] - 杂芳基胺

    公开(公告)号：US06833375B2

    公开(公告)日：2004-12-21

    申请号：US10238686

    申请日：2002-09-10

    申请人： Marc Gaston Venet ,  Dominique Jean-Pierre Mabire ,  Jean Fernand Armand Lacrampe ,  Gerard Charles Sanz

    发明人： Marc Gaston Venet ,  Dominique Jean-Pierre Mabire ,  Jean Fernand Armand Lacrampe ,  Gerard Charles Sanz

    IPC分类号： C07D41710

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D513/04

    摘要： The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C1-6alkyl or aryl; R2 is hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl, optionally substituted pyrrolidinyl or aryl; R3 is hydrogen, optionally substituted C1-6alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.

    摘要翻译： 本发明涉及配制N-氧化物的化合物，其药学上可接受的加成盐和立体化学异构形式，其中R 1是氢，羟基，C 1-6烷基或芳基; R 2是氢; 任选取代的C 1-12烷基; C 3-7环烷基; C 2-8烯基，任选取代的吡咯烷基或芳基; R 3是氢，任选取代的C 1-6烷基或芳基; Het是选自咪唑基，三唑基，四唑基和吡啶基的任选取代的不饱和杂环;是任选取代的不饱和单环或双环杂环; 并且芳基是任选取代的苯基。 本发明还涉及其制备方法和包含所述新化合物的组合物，以及它们作为药物的用途。