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    1,2-annelated quinoline derivatives
    1.
    发明授权
    1,2-annelated quinoline derivatives 有权

    公开(公告)号：US06914066B2

    公开(公告)日：2005-07-05

    申请号：US10179444

    申请日：2002-06-24

    申请人： Patrick René Angibaud ,  Marc Gaston Venet ,  Xavier Marc Bourdrez

    发明人： Patrick René Angibaud ,  Marc Gaston Venet ,  Xavier Marc Bourdrez

    IPC分类号： C07D215/06 ,  A61K31/4365 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/498 ,  A61K31/519 ,  A61P35/00 ,  C07D215/18 ,  C07D401/06 ,  C07D403/06 ,  C07D471/04 ,  C07D487/04 ,  A61K31/435 ,  A61K31/517

    CPC分类号： C07D401/06 ,  A61K31/4745 ,  A61K31/498 ,  A61K31/519 ,  C07D403/06 ,  C07D471/04 ,  C07D487/04

    摘要： This invention concerns compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein ═X1—X2—X3— is a trivalent radical,; >Y1—Y2— is a trivalent radical; r and s are each independently 0, 1, 2, 3, 4 or 5; t is 0, 1, 2 or 3; each R1 and R2 are independently hydroxy, halo, cyano, C1-6alkyl, trihalomethyl, trihalomethoxy, C2-6alkenyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkylthio, C1-6alkyloxyC1-6alkyloxy, C1-6alkyloxycarbonyl, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)amino, mono- or di(C1-6alkylaminoC1-6alkyloxy, aryl, arylC1-6alkyl, aryloxy or arylC1-6alkyloxy, hydroxycarbonyl, C1-6alkyloxycarbonyl; or two R1 or R2 on adjacent positions form together a bivalent radical; R3 is hydrogen, halo, C1-6alkyl, cyano, haloC1-6alkyl, hydroxyC1-6alkyl, cyanoC1-6alkyl, aminoC1-6alkyl, C1-6alkyloxyC1-6alkyl, C1-6alkylthio-C1-6alkyl, aminocarbonylC1-6alkyl, hydroxycarbonyl, hydroxycarbonylC1-6alkyl, C1-6alkyoxycarbonylC1-6alkyl, C1-6alkylcarbonylC1-6alkyl, C1-6alkyloxycarbonyl, aryl, arylC1-6alkyloxyC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, or a radical of formula —O—R10, —S—R10 or —NR11R12; R4 is an optionally substituted imidazolyl; aryl is an optionally substituted phenyl or naphthalenyl; having farnesyl transferase and geranylgeranyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

    1,2-annelated quinoline derivatives
    2.
    发明授权
    1,2-annelated quinoline derivatives 有权
    1,2-annelated喹啉衍生物

    公开(公告)号：US06458800B1

    公开(公告)日：2002-10-01

    申请号：US09868992

    申请日：2001-08-29

    申请人： Patrick René Angibaud ,  Marc Gaston Venet ,  Xavier Marc Bourdrez

    发明人： Patrick René Angibaud ,  Marc Gaston Venet ,  Xavier Marc Bourdrez

    IPC分类号： C07D47104

    CPC分类号： C07D401/06 ,  A61K31/4745 ,  A61K31/498 ,  A61K31/519 ,  C07D403/06 ,  C07D471/04 ,  C07D487/04

    摘要： This invention concerns compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein ═X1—X2—X3— is a trivalent radical,; >Y1—Y2— is a trivalent radical; r and s are each independently 0, 1, 2, 3, 4 or 5; t is 0, 1, 2 or 3; each R1 and R2 are independently hydroxy, halo, cyano, C1-6alkyl, trihalomethyl, trihalomethoxy, C2-6alkenyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkylthio, C1-6alkyloxyC1-6alkyloxy, C1-6alkyloxycarbonyl, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)amino, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, aryl, arylC1-6alkyl, aryloxy or arylC1-6alkyloxy, hydroxycarbonyl, C1-6alkyloxycarbonyl; or two R1 or R2 on adjacent positions form together a bivalent radical; R3 is hydrogen, halo, C1-6alkyl, cyano, haloC1-6alkyl, hydroxyC1-6alkyl, cyanoC1-6alkyl, aminoC1-6alkyl, C1-6alkyloxyC1-6alkyl, C1-6alkylthio-C1-6alkyl, aminocarbonylC1-6alkyl, hydroxycarbonyl, hydroxycarbonylC1-6alkyl, C1-6alkyloxycarbonylC1-6alkyl, C1-6alkylcarbonylC1-6alkyl, C1-6alkyloxycarbonyl, aryl, arylC1-6alkyloxyC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, or a radical of formula —O—R10, —S—R10 or —NR11R12; R4 is an optionally substituted imidazolyl; aryl is an optionally substituted phenyl or naphthalenyl; having farnesyl transferase and geranylgeranyl 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= X 1 -X 2 -X 3 - 是三价基团; Y1-Y2-是三价基; r和s各自独立地为0,1,2,3,4或5; t为0,1,2或3; 每个R 1和R 2独立地是羟基，卤素，氰基，C 1-6烷基，三卤甲基，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烷硫基，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， 单或二（C 1-6烷基）氨基，单或二（C 1-6烷基）氨基C 1-6烷氧基，芳基，芳基C 1-6烷基，芳氧基或芳基C 1-6烷氧基，羟基羰基，C 1-6烷氧基羰基; 或相邻位置上的两个R1或R2一起形成二价基团; R 3是氢，卤素，C 1-6烷基，氰基，卤代C 1-6烷基，羟基C 1-6烷基，氰基C 1-6烷基，氨基C 1-6烷基，C 1-6烷氧基C 1-6烷基，C 1-6烷硫基-C 1-6烷基，氨基羰基C 1-6烷基，羟基羰基，羟基羰基C1- C 1-6烷氧基羰基C 1-6烷基，C 1-6烷基羰基C 1-6烷基，C 1-6烷氧基羰基，芳基，芳基C 1-6烷氧基C 1-6烷基，一或二（C 1-6烷基）氨基C 1-6烷基，或式-O-R 10基团， S-R10或-NR11R12; R4是任选取代的咪唑基; 芳基是任选取代的苯基或萘基; 具有法呢基转移酶和香叶基香叶基转移酶抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

    Farnesyl protein transferase inhibiting (imidazol-5-yl) methyl-2-quinolinone derivatives
    4.
    发明授权
    Farnesyl protein transferase inhibiting (imidazol-5-yl) methyl-2-quinolinone derivatives 有权
    法呢基蛋白转移酶抑制（咪唑-5-基）甲基-2-喹啉酮衍生物

    公开(公告)号：US06420387B1

    公开(公告)日：2002-07-16

    申请号：US09689211

    申请日：2000-10-12

    申请人： Marc Gaston Venet ,  Patrick René Angibaud ,  Philippe Muller ,  Gérard Charles Sanz

    发明人： Marc Gaston Venet ,  Patrick René Angibaud ,  Philippe Muller ,  Gérard Charles Sanz

    IPC分类号： A61K31445

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D401/14 ,  C07D405/14 ,  C07D407/14 ,  C07D413/14 ,  Y02P20/55

    摘要： This invention comprises the novel compounds of formula (I) wherein the dotted line represents an optional bond; X is oxygen or sulfur; R1 is hydrogen, C1-12alkyl, Ar1, Ar2C1-6alkyl, quinolinylC1-6alkyl, pyridylC1-6alkyl, hydroxyC1-6alkyl, C1-6alkyloxyC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, aminoC1-6alkyl, or a radical of formula —Alk1—C(═O)—R9, —Alk1—S(O)—R9 or —Alk1—S(O)2—R9; R2, R3 and R16 each independently are hydrogen, hydroxy, halo, cyano, C1-6alkyl, C1-6alkyloxy, hydroxyC1-6akyloxy, C1-6alkyloxyC1-6alkyloxy, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, Ar1, Ar2C1-6alkyl, Ar2oxy, Ar2C1-6alkyloxy, hydroxycarbonyl, C1-6alkyloxycarbonyl, trihalomethyl, trihalomethoxy, C2-6alkenyl; R4 and R5 each independently are hydrogen, halo, Ar1, C1-6alkyl, hydroxyC1-6alkyl, C1-6alkyloxyC1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, hydroxycarbonyl, C1-6alkyloxycarbonyl, C1-6alkylS(O)C1-6alkyl or C1-6alkylS(O)2C1-6alkyl; R6 and R7 each independently are hydrogen, halo, cyano, C1-6alkyl, 4,4-dimethyl-oxazolyl, C1-6alkyloxy or Ar2oxy; R8 is hydrogen, C1-6alkyl, cyano, hydroxycarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonylC1-6alkyl; cyanoC1-6alkyl, C1-6alkyloxycarbonylC1-6alkyl, carboxyC1-6alkyl, hydroxyC1-6alkyl, aminoC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, imidazolyl, haloC1-6alkyl, C1-6alkyloxyC1-6alkyl, aminocarbonylC1-6alkyl, or a radical of formula —O—R10, —SR10, —N—R11R12; R17 is hydrogen, halo, cyano, C1-6alkyl, C1-6alkyloxycarbonyl, Ar1; R18 is hydrogen, C1-6alkyl, C1-6alkyloxy or halo; R19 is hydrogen or C1-6alkyl; having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

    摘要翻译： 本发明包括式（I）的新化合物，其中虚线表示任选的键; X是氧或硫; R1是氢，C1-12烷基，Ar1，Ar2C1-6烷基，喹啉基C 1-6烷基，吡啶基C 1-6烷基，羟基C 1-6烷基，C 1-6烷氧基C 1-6烷基，一或二（C 1-6烷基）氨基C 1-6烷基，氨基C 1-6烷基或 式-Alk1-C（= O）-R9，-Alk1-S（O）-R9或-Alk1-S（O）2-R9的基团; R 2，R 3和R 16各自独立地是氢，羟基，卤素，氰基，C 1-6烷基，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，氨基C 1-6烷氧基，一或二（C 1-6烷基）氨基C 1-6烷氧基 Ar 1，Ar 2 C 1-6烷基，Ar 2氧基，Ar 2 C 1-6烷氧基，羟基羰基，C 1-6烷氧基羰基，三卤代甲基，三卤代甲氧基，C 2-6烯基; R 4和R 5各自独立地是氢，卤素，Ar 1，C 1-6烷基，羟基C 1-6烷基，C 1-6烷氧基C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，氨基，羟基羰基，C 1-6烷氧基羰基，C 1-6烷基S（O） C 1-6烷基或C 1-6烷基S（O）2 C 1-6烷基; R 6和R 7各自独立地为氢，卤素，氰基，C 1-6烷基，4,4-二甲基 - 恶唑基，C 1-6烷氧基或Ar 2氧基; R 8是氢，C 1-6烷基，氰基，羟基羰基，C 1-6烷氧基羰基，C 1-6烷基羰基C 1-6

    Farnesyl transferase inhibiting 1,8-annelated quinolinone derivatives substituted with N- or C-linked imidazoles
    9.
    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。