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42 条记录 (耗时 0.03 秒)

    N-[4-(heteroarylmethyl)phenyl]-heteroarylamines
    1.
    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。

    6-�triazolyl�3-(trifluoromethyl)phenyl!methyl!-2-quinolines and -quinolinethiones
    4.
    发明授权
    6-�triazolyl�3-(trifluoromethyl)phenyl!methyl!-2-quinolines and -quinolinethiones 失效
    6- [三唑基[3-（三氟甲基）苯基]甲基] -2-喹啉和喹啉硫酮

    公开(公告)号：US5922734A

    公开(公告)日：1999-07-13

    申请号：US860239

    申请日：1997-06-16

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

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

    IPC分类号： C07D401/06 ,  A61K8/14 ,  A61K8/49 ,  A61K31/47 ,  A61P17/00 ,  A61P43/00 ,  C07D521/00

    CPC分类号： C07D249/08 ,  C07D231/12 ,  C07D233/56

    摘要： This invention is concerned with the compounds of formula ##STR1## the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof,wherein: R.sup.1 is hydrogen, amino or C.sub.1-4 alkyl; R.sup.2 is hydrogen, halo or C.sub.1-4 alkyl; R.sup.3 is hydrogen, halo or C.sub.1-4 alkyl; Y is 0 or S, and --X.sup.1 .dbd.X.sup.2 --is a bivalent radical having the formula --N.dbd.CH--(a-1) or --CH.dbd.N--(a-2);compositions containing the same, and processes of preparing these compounds. It further relates to their use as a medicine, in particular their use as a medicine to treat keratinization disorders.

    摘要翻译： PCT No.PCT / EP95 / 05173 Sec。 371日期：1997年6月16日 102（e）日期1996年6月16日PCT 1995年12月21日PCT PCT。 WO96 / 20200 PCT出版物 日期：1996年7月4日本发明涉及药学上可接受的酸加成盐及其立体化学异构形式的化合物，其中：R1是氢，氨基或C1-4烷基; R2是氢，卤素或C1-4烷基; R3是氢，卤素或C1-4烷基; Y为0或S，-X1 = X2-为具有式-N = CH-（a-1）或-CH = N-（a-2）的二价基团。 含有它们的组合物，以及制备这些化合物的方法。 它还涉及它们作为药物的用途，特别是它们作为治疗角质化障碍的药物的用途。

    N-[4-(heteroarylmethyl)phenyl]-heteroarylamines
    5.
    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
    6.
    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。

    Farnesyl transferase inhibiting 1,8-annelated quinolinone derivatives substituted with N- or C-linked imidazoles
    8.
    发明授权
    Farnesyl transferase inhibiting 1,8-annelated quinolinone derivatives substituted with N- or C-linked imidazoles 有权
    抑制由N-或C-连接的咪唑取代的1,8-环化喹啉酮衍生物的法呢基转移酶

    公开(公告)号：US06187786B1

    公开(公告)日：2001-02-13

    申请号：US09380856

    申请日：1999-12-20

    申请人： Marc Gaston Venet ,  Patrick René Angibaud ,  Yannick Aimé Eddy Ligny ,  Virginie Sophie Poncelet ,  Gerard Charles Sanz

    发明人： Marc Gaston Venet ,  Patrick René Angibaud ,  Yannick Aimé Eddy Ligny ,  Virginie Sophie Poncelet ,  Gerard Charles Sanz

    IPC分类号： A61K31473

    CPC分类号： C07D471/06 ,  C07D455/04

    摘要： This invention concerns compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein the dotted line represents an optional bond; X is oxygen or sulfur; —A— is a bivalent radical of formula; R1 and R2 each independently are hydrogen, hydroxy, halo, cyano, C1-6alkyl, trihalomethyl, trihalomethoxy, C2-6alkenyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkyloxyC1-6alkyloxy, C1-6alkyloxycarbonyl, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, Ar, Ar—C1-6alkyl, Ar-oxy, Ar—C1-6alkyloxy; or when on adjacent positions R1 and R2 taken together may form a bivalent radical; R3 and R4 each independently are hydrogen, halo, cyano, C1-6alkyl, C1-6alkyloxy, Ar-oxy, C1-6alkylthio, di(C1-6alkyl)amino, trihalomethyl, trihalomethoxy, or when on adjacent positions R3 and R4 taken together may form a bivalent radical; R5 is an imidazolyl substituted with hydrogen or C1-6alkyl; R6 hydrogen, hydroxy, halo, cyano, optionally substituted C1-6alkyl, C1-6alkyloxycarbonyl or Ar; or a radical of formula —O—R7, —S—R8, —N—R8R9; and Ar is optionally substituted phenyl; having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

    摘要翻译： 本发明涉及配制药学上可接受的酸加成盐和其立体化学异构形式的化合物，其中虚线表示任选的键; X是氧或硫; -A-是式的二价基团; R 1和R 2各自独立地为氢，羟基，卤素，氰基，C 1-6烷基，三卤代甲基，三卤甲氧基，C 2-6烯基，C 1-6烷氧基，羟基C 1-6烷氧基，C 1-6烷氧基C 1-6烷氧基，C 1-6烷氧基羰基，氨基C 1-6烷氧基， 或二（C 1-6烷基）氨基C 1-6烷氧基，Ar，Ar-C 1-6烷基，Ar-氧基，Ar-C 1-6烷氧基; 或者当在相邻位置R1和R2一起可以形成二价基团时; R 3和R 4各自独立地为氢，卤素，氰基，C 1-6烷基，C 1-6烷氧基，Ar-氧基，C 1-6烷硫基，二（C 1-6烷基）氨基，三卤甲基，三卤甲氧基， 可形成二价基团; R5是被氢或C1-6烷基取代的咪唑基; R6，氢，羟基，卤素，氰基，任选取代的C 1-6烷基，C 1-6烷氧基羰基或Ar; 或式-O-R7，-S-R8，-N-R8R9的基团; 和Ar是任选取代的苯基; 具有法呢基转移酶抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

    Farnesyl transferase inhibiting 2-quinolone derivatives
    9.
    发明授权
    Farnesyl transferase inhibiting 2-quinolone derivatives 失效

    公开(公告)号：US5968952A

    公开(公告)日：1999-10-19

    申请号：US66441

    申请日：1998-04-29

    申请人： Marc Gaston Venet ,  Patrick Rene Angibaud ,  Gerard Charles Sanz ,  David William End

    发明人： Marc Gaston Venet ,  Patrick Rene Angibaud ,  Gerard Charles Sanz ,  David William End

    IPC分类号： A61K31/00 ,  A61K31/47 ,  A61K31/4709 ,  A61P35/00 ,  A61P43/00 ,  C07D401/06 ,  C07D521/00 ,  C07D215/16 ,  C07D215/04 ,  C07D215/12

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06

    摘要： The present invention is concerned with compounds of formula (I), ##STR1## the stereoisomeric forms thereof and the pharmaceutically acceptable acid or base addition salts thereof, wherein the dotted line represents an optional bond; X is oxygen or sulfur; R.sup.1 is hydrogen, C.sub.1-12 alkyl, Ar.sup.1, Ar.sup.2 C.sub.1-6 alkyl, quinolinylC.sub.1-6 alkyl, pyridylC.sub.1-6 alkyl, hydroxyC.sub.1-6 alkyl, C.sub.1-6 alkyloxyC.sub.1-6 alkyl, mono- or di(C.sub.1-6 alkyl)-aminoC.sub.1-6 alkyl, aminoC.sub.1-6 alkyl, or a radical of formula --Alk.sup.1 --C(.dbd.O)--R.sup.9, --Alk.sup.1 --S(O)--R.sup.9 or --Alk.sup.1 --S(O).sub.2 --R.sup.9 ; R.sup.2 and R.sup.3 each independently are hydrogen, hydroxy, halo, cyano, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, hydroxyC.sub.1-6 alkyloxy, C.sub.1-6 alkyloxy-C.sub.1-6 alkyloxy, aminoC.sub.1-6 alkyloxy, mono- or di(C.sub.1-6 alkyl)aminoC.sub.1-6 alkyloxy, Ar.sup.1, Ar.sup.2 C.sub.1-6 alkyl, Ar.sup.2 oxy, Ar.sup.2 C.sub.1-6 alkyloxy, hydroxycarbonyl, C.sub.1-6 alkyloxycarbonyl, trihalomethyl, trihalomethoxy, C.sub.2-6 alkenyl; or when on adjacent positions R.sup.2 and R.sup.3 taken together may form a bivalent radical; R.sup.4 and R.sup.5 each independently are hydrogen, Ar.sup.1, C.sub.1-6 alkyl, C.sub.1-6 alkyloxyC.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylthio, amino, hydroxycarbonyl, C.sub.1-6 alkyloxycarbonyl, C.sub.1-6 alkylS(O)C.sub.1-6 alkyl or C.sub.1-6 alkylS(O).sub.2 --C.sub.1-6 alkyl; R.sup.6 and R.sup.7 each independently are hydrogen, halo, cyano, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy or Ar.sup.2 oxy; R.sup.8 is hydrogen, C.sub.1-6 alkyl, cyano, hydroxycarbonyl, C.sub.1-6 alkyloxycarbonyl, C.sub.1-6 alkylcarbonylC.sub.1-6 alkyl, cyanoC.sub.1-6 alkyl, C.sub.1-6 alkyloxy-carbonylC.sub.1-6 alkyl, hydroxycarbonylC.sub.1-6 alkyl, hydroxyC.sub.1-6 alkyl, aminoC.sub.1-6 alkyl, mono- or di(C.sub.1-6 alkyl)aminoC.sub.1-6 alkyl, haloC.sub.1-6 alkyl, C.sub.1-6 alkyloxy-C.sub.1-6 alkyl, aminocarbonylC.sub.1-6 alkyl, Ar.sup.1, Ar.sup.2 C.sub.1-6 alkyloxyC.sub.1-6 alkyl, C.sub.1-6 alkylthioC.sub.1-6 alkyl; R.sup.10 is hydrogen, C.sub.1-6 alkyl or halo; R.sup.11 is hydrogen or C.sub.1-6 alkyl; having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

    Intermediate compounds in the preparation of farnnesyl transferase inhibiting 1,8-annelated quinolinone derivatives substituted with N-or C linked imidazoles
    10.
    发明授权
    Intermediate compounds in the preparation of farnnesyl transferase inhibiting 1,8-annelated quinolinone derivatives substituted with N-or C linked imidazoles 有权
    中间体化合物制备法尼烯基转移酶抑制被N-或C连接的咪唑取代的1,8-环化喹啉酮衍生物

    公开(公告)号：US06444812B1

    公开(公告)日：2002-09-03

    申请号：US09725391

    申请日：2000-11-29

    申请人： Marc Gaston Venet ,  Patrick René Angibaud ,  Yannick Aimé Eddy Ligny ,  Virginie Sophie Poncelet ,  Gerard Charles Sanz

    发明人： Marc Gaston Venet ,  Patrick René Angibaud ,  Yannick Aimé Eddy Ligny ,  Virginie Sophie Poncelet ,  Gerard Charles Sanz

    IPC分类号： C07D26538

    CPC分类号： C07D471/06 ,  C07D455/04

    摘要： This invention concerns intermediates in the preparation of compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein the dotted line represents an optional bond; X is oxygen or sulfur; —A— is a bivalent radical of formula; R1 and R2 each independently are hydrogen, hydroxy, halo, cyano, C1-6alkyl, trihalomethyl, trihalomethoxy, C2-6alkenyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkyloxyC1-6alkyloxy, C1-6alkyloxycarbonyl, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, Ar, Ar—C1-6alkyl, Ar-oxy, Ar—C1-6alkyloxy; or when on adjacent positions R1 and R2 taken together may form a bivalent radical; R3 and R4 each independently are hydrogen, halo, cyano, C1-6alkyl, C1-6alkyloxy, Ar-oxy, C1-6alkylthio, di(C1-6alkyl)amino, trihalomethyl, trihalomethoxy, or when on adjacent positions R3 and R4 taken together may form a bivalent radical; R5 is an imidazolyl substituted with hydrogen or C1-6alkyl; R6 hydrogen, hydroxy, halo, cyano, optionally substituted C1-6alkyl, C1-6alkyloxycarbonyl or Ar; or a radical of formula —O—R7, —S—R8, —N—R8R9; and Ar is optionally substituted phenyl; and of the preparation, thereof.

    摘要翻译： 本发明涉及制备药学上可接受的酸加成盐及其立体化学异构形式的化合物的中间体，其中虚线表示任选的键; X是氧或硫; -A-是式的二价基团; R 1和R 2各自独立地为氢，羟基，卤素，氰基，C 1-6烷基，三卤代甲基，三卤甲氧基，C 2-6烯基，C 1-6烷氧基，羟基C 1-6烷氧基，C 1-6烷氧基C 1-6烷氧基，C 1-6烷氧基羰基，氨基C 1-6烷氧基， 或二（C 1-6烷基）氨基C 1-6烷氧基，Ar，Ar-C 1-6烷基，Ar-氧基，Ar-C 1-6烷氧基; 或者当在相邻位置R1和R2一起可以形成二价基团时; R 3和R 4各自独立地为氢，卤素，氰基，C 1-6烷基，C 1-6烷氧基，Ar-氧基，C 1-6烷硫基，二（C 1-6烷基）氨基，三卤甲基，三卤甲氧基， 可形成二价基团; R5是被氢或C1-6烷基取代的咪唑基; R6，氢，羟基，卤素，氰基，任选取代的C 1-6烷基，C 1-6烷氧基羰基或Ar; 或式-O-R7，-S-R8，-N-R8R9的基团; 和Ar是任选取代的苯基; 及其制备方法。