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    Farnesyltransferase inhibiting quinazolinones
    16.
    发明授权
    Farnesyltransferase inhibiting quinazolinones 有权
    法呢基转移酶抑制喹唑啉酮

    公开(公告)号：US06358961B1

    公开(公告)日：2002-03-19

    申请号：US09687153

    申请日：2000-10-13

    申请人： Patrick René Angibaud ,  Marc Gaston Venet ,  Eddy Jean Edgard Freyne

    发明人： Patrick René Angibaud ,  Marc Gaston Venet ,  Eddy Jean Edgard Freyne

    IPC分类号： A61K31505

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D239/82 ,  C07D249/08 ,  C07D403/06 ,  C07D405/04

    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; 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, Ar1, Ar1C1-6alkyl, Ar1oxy, Ar1C1-6alkyloxy; 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, Ar1oxy, C1-6alkylthio, di(C1-6alkyl)amino, trihalomethyl, trihalomethoxy; R5 is hydrogen, halo, cyano, optionally substituted C1-6alkyl, C1-6alkyloxycarbonyl or Ar1; or a radical of formula —OR10, —SR10, —NR11R12; R6 is an optionally substituted imidazolyl moiety; R7 is hydrogen or C1-6alkyl provided that the dotted line does not represent a bond; R8 is hydrogen, C1-6alkyl or Ar2CH2 Het1CH2; R9 is hydrogen, C1-6alkyl, C1-6alkyloxy or halo, or R8 and R9 taken together may form a bivalent radical; Ar1 and Ar2 are optionally substituted phenyl and Het1 is optionally substituted pyridinyl; 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; 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 1，Ar 1 C 1-6烷基，Ar 1氧基，Ar 1 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 1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; R5是氢，卤素，氰基，任意取代的C 1-6烷基，C 1-6烷氧基羰基或Ar 1; 或式-OR 10，-SR 10，-NR 11 R 12的基团; R6是任选取代的咪唑基部分; R 7是氢或C 1-6烷基，条件是虚线不代表键; R8是氢，C1-6烷基或Ar2CH2Het1CH2; R9是氢，C1-6烷基，C1-6烷氧基或卤素，或R8和R9一起可以形成二价基; Ar1和Ar2是任选取代的苯基，Het1是任选取代的吡啶基; 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。

    1,2-annelated quinoline derivatives
    17.
    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
    18.
    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。