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    Quinazoline derivatives
    1.
    发明授权
    Quinazoline derivatives 有权
    喹唑啉衍生物

    公开(公告)号：US09273013B2

    公开(公告)日：2016-03-01

    申请号：US13744878

    申请日：2013-01-18

    申请人： Janssen Pharmaceutica N.V.

    发明人： Eddy Jean Edgard Freyne ,  Timothy Pietro Suren Perera ,  Peter Jacobus Johannes Antonius Buijnsters ,  Marc Willems ,  Gaston Stanislas Marcella Diels ,  Werner Constant Johan Embrechts ,  Peter Ten Holte ,  Frederik Jan Rita Rombouts ,  Carsten Schultz-Fademrecht

    IPC分类号： C07D239/02 ,  C07D239/94 ,  C07D239/88 ,  C07D239/93 ,  C07C229/16 ,  C07C229/40

    CPC分类号： C07D498/06 ,  C07C229/16 ,  C07C229/40 ,  C07D239/88 ,  C07D239/93 ,  C07D239/94

    摘要： The present invention concerns the compounds of formula wherein Z represents NH; Y represents —C3-9alkyl-, —C2-9alkenyl-, —C3-7alkyl-CO—NH optionally substituted with amino, mono- or di(C1-4alkyl)amino or C1-4alkyloxycarbonylamino-, —C3-7alkenyl-CO—NH— optionally substituted with amino, mono- or di(C1-4alkyl)amino- or C1-4alkyloxycarbonylamino-, C1-5alkyl-NR13—C1-5alkyl-, —C1-5alkyl-NR14—CO—C1-5alkyl-, —C1-6alkyl-CO—NH—, —C1-5alkyl-CO NR15—C1-5alkyl-, —C1-3alkyl-NH—CO-Het20-, —C1-2alkyl-CO-Het21-CO—, —C1-2alkyl-NH—CO—CR16R17—NH—, —C1-2alkyl-CO—NH—CR18R19—CO—, —C1-2alkyl-CO—NR20—C1-3alkyl-CO—, or —NR22—CO—C1-3alkyl-NH—; X1 represents a direct bond, O or —O—C1-2alkyl-; X2 represents a direct bond, —CO—C1-2alkyl-, NR12, —NR12—C1-2alkyl, —O—N═CH— or —C1-2alkyl-; R1 and R2 are hydrogen or halo; R3 are hydrogen; R4 represents hydrogen or C1-4alkyloxy; R12 and R13 are hydrogen or C1-4alkyl; R14 and R15 are hydrogen; R16 and R17 each independently represent hydrogen or C1-4alkyl; R18 and R19 are hydrogen or C1-4alkyl optionally substituted with phenyl or hydroxy; R20 and R21 are hydrogen or C1-4alkyl optionally substituted with C1-4alkyloxy; Het20, Het21 and Het22 are a heterocycle selected from the group consisting pyrrolidinyl, 2-pyrrolidinonyl or piperidinyl optionally substituted with hydroxy.

    摘要翻译： 本发明涉及下式的化合物其中Z代表NH; Y代表任选被氨基，一或二（C 1-4烷基）氨基或C 1-4烷氧基羰基氨基 - ， - C 3-7烯基-CO-的氨基取代的-C 3-9烷基 - ， - C 2-9烯基 - ， - 氨基，一或二（C 1-4烷基）氨基 - 或C 1-4烷氧基羰基氨基 - ，C 1-5烷基-NR 13 -C 1-5烷基 - ， - C 1-5烷基-NR 14 -CO-C 1-5烷基 - C 1-6烷基-CO-NH - ， - C 1-5烷基-CO NR 15 -C 1-5烷基 - ， - C 1-3烷基-NH-CO-Het 20 - ， - C 1-2烷基-CO-Het 21 -CO-， - C 1-2烷基 -NH-CO-CR16R17-NH-，-C1-2烷基-CO-NH-CR18R19-CO-，-C1-2烷基-CO-NR20-C1-3烷基-CO-或-NR22-CO-C1-3烷基 - NH-; X1表示直接键，O或-O-C 1-2烷基 - ; X 2表示直接键，-CO-C 1-2烷基 - ，NR 12，-NR 12 -C 1-2烷基，-O-N = CH-或-C 1-2烷基 - ; R1和R2是氢或卤素; R3是氢; R4代表氢或C1-4烷氧基; R 12和R 13是氢或C 1-4烷基; R14和R15是氢; R 16和R 17各自独立地表示氢或C 1-4烷基; R 18和R 19是氢或任选被苯基或羟基取代的C 1-4烷基; R 20和R 21是氢或任选被C 1-4烷氧基取代的C 1-4烷基; Het20，Het21和Het22是选自吡咯烷基，2-吡咯烷基或任选被羟基取代的哌啶基的杂环。

    Quinazoline derivatives
    2.
    发明授权
    Quinazoline derivatives 有权
    喹唑啉衍生物

    公开(公告)号：US08394786B2

    公开(公告)日：2013-03-12

    申请号：US12624637

    申请日：2009-11-24

    申请人： Eddy Jean Edgard Freyne ,  Timothy Pietro Suren Perera ,  Peter Jacobus Johannes Antonius Buijnsters ,  Marc Willems ,  Gaston Stanislas Marcella Diels ,  Werner Constant Johan Embrechts ,  Peter ten Holte ,  Frederik Jan Rita Rombouts ,  Carsten Schultz-Fademrecht

    发明人： Eddy Jean Edgard Freyne ,  Timothy Pietro Suren Perera ,  Peter Jacobus Johannes Antonius Buijnsters ,  Marc Willems ,  Gaston Stanislas Marcella Diels ,  Werner Constant Johan Embrechts ,  Peter ten Holte ,  Frederik Jan Rita Rombouts ,  Carsten Schultz-Fademrecht

    IPC分类号： A61K31/33 ,  C07D487/00

    CPC分类号： C07D498/06 ,  C07C229/16 ,  C07C229/40 ,  C07D239/88 ,  C07D239/93 ,  C07D239/94

    摘要： The present invention concerns the compounds of formula wherein Z represents NH; Y represents —C3-9alkyl-, —C2-9alkenyl-, —C3-7alkyl-CO—NH optionally substituted with amino, mono- or di(C1-4alkyl)amino or C1-4alkyloxycarbonylamino-, —C3-7alkenyl-CO—NH— optionally substituted with amino, mono- or di(C1-4alkyl)amino- or C1-4alkyloxycarbonylamino-, C1-5alkyl-NR13—C1-5alkyl-, —C1-5alkyl-NR14—CO—C1-5alkyl-, —C1-6alkyl-CO—NH—, —C1-5alkyl-CONR15—C1-5alkyl-, —C1-3alkyl-NH—CO-Het20-, —C1-2alkyl-CO-Het21-CO—, —C1-2alkyl-NH—CO—CR16R17—NH—, —C1-2alkyl-CO—NH—CR18R19—CO—, —C1-2alkyl-CO—NR20—C1-3alkyl-CO—, or —NR22—CO—C1-3alkyl-NH—; X1 represents a direct bond, O or —O—C1-2alkyl-; X2 represents a direct bond, —CO—C1-2alkyl-, NR12, —NR12—C1-2alkyl-, —O—N═CH— or —C1-2alkyl-; R1 and R2 are hydrogen or halo; R3 are hydrogen; R4 represents hydrogen or C1-4alkyloxy; R12 and R13 are hydrogen or C1-4alkyl; R14 and R15 are hydrogen; R16 and R17 each independently represent hydrogen or C1-4alkyl; R18 and R19 are hydrogen or C1-4alkyl optionally substituted with phenyl or hydroxy; R20 and R21 are hydrogen or C1-4alkyl optionally substituted with C1-4alkyloxy; Het20, Het21 and Het22 are a heterocycle selected from the group consisting pyrrolidinyl, 2-pyrrolidinonyl or piperidinyl optionally substituted with hydroxy.

    摘要翻译： 本发明涉及下式的化合物其中Z代表NH; Y代表任选被氨基，一或二（C 1-4烷基）氨基或C 1-4烷氧基羰基氨基 - ， - C 3-7烯基-CO-的氨基取代的-C 3-9烷基 - ， - C 2-9烯基 - ， - 氨基，一或二（C 1-4烷基）氨基 - 或C 1-4烷氧基羰基氨基 - ，C 1-5烷基-NR 13 -C 1-5烷基 - ， - C 1-5烷基-NR 14 -CO-C 1-5烷基 - C 1-6烷基-CO-NH - ， - C 1-5烷基-CONR 15 -C 1-5烷基 - ， - C 1-3烷基-NH-CO-Het 20 - ， - C 1-2烷基-CO-Het 21 -CO-， - C 1-2烷基 - NH-CO-CR16R17-NH-，-C1-2烷基-CO-NH-CR18R19-CO-，-C1-2烷基-CO-NR20-C1-3烷基-CO-或-NR22-CO-C1-3烷基-NH - ; X1表示直接键，O或-O-C 1-2烷基 - ; -X 2表示直接键，-CO-C 1-2烷基 - ，NR 12，-NR 12 -C 1-2烷基 - ， - O-N = CH-或-C 1-2烷基 - ; R1和R2是氢或卤素; R3是氢; R4代表氢或C1-4烷氧基; R 12和R 13是氢或C 1-4烷基; R14和R15是氢; R 16和R 17各自独立地表示氢或C 1-4烷基; R 18和R 19是氢或任选被苯基或羟基取代的C 1-4烷基; R 20和R 21是氢或任选被C 1-4烷氧基取代的C 1-4烷基; Het20，Het21和Het22是选自吡咯烷基，2-吡咯烷基或任选被羟基取代的哌啶基的杂环。

    Macrocyclic quinazoline derivatives as antiproliferative agents
    4.
    发明授权
    Macrocyclic quinazoline derivatives as antiproliferative agents 有权
    大环喹唑啉衍生物作为抗增殖剂

    公开(公告)号：US07648975B2

    公开(公告)日：2010-01-19

    申请号：US10558007

    申请日：2004-05-25

    申请人： Eddy Jean Edgard Freyne ,  Timothy Pietro Suren Perera ,  Peter Jacobus Johannes Antonius Buijnsters ,  Marc Willems ,  Gaston Stanislas Marcella Diels ,  Werner Constant Johan Embrechts

    发明人： Eddy Jean Edgard Freyne ,  Timothy Pietro Suren Perera ,  Peter Jacobus Johannes Antonius Buijnsters ,  Marc Willems ,  Gaston Stanislas Marcella Diels ,  Werner Constant Johan Embrechts

    IPC分类号： A01N43/00 ,  A61K31/33 ,  C07D487/00 ,  C07D491/00 ,  C07D513/00

    CPC分类号： C07D498/06 ,  C07C229/16 ,  C07C229/40 ,  C07D239/88 ,  C07D239/93 ,  C07D239/94

    摘要： The present invention concerns the compounds of formula (I) the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents O, CH2, NH or S; in particular Z represents NH; Y represents —C3-9alkyl-, —C3-9alkenyl-, —C3-9alkynyl-, —C3-7alkyl-CO—NH— optionally substituted with amino, mono- or di(C1-4alkyl)amino or C1-4 alkyloxycarbonylamino-, —C3-7alkenyl-CO—NH— optionally substituted with amino, mono- or di(C1-4alkyl)amino- or C1-4alkyloxycarbonylamino-, C1-5alkyl-oxy-C1-5alkyl-, —C1-5alkyl NR13—, —C1-5alkyl-, —C1-5alkyl-NR14—CO—C1-5alkyl-, —C1-5alkyl-CO NR15—C1-5alkyl-, —C1-6alkyl-CO—NH—, —C1-6alkyl-NH—CO—, —C1-3alkyl-NH—CS-Het20-, —C1-3alkyl-NH—CO-Het20, —C1-2alkyl-CO-Het21-CO—, -Het22-CH2—CO—NH—C1-3alkyl-, —CO—NH—C1-6alkyl-, —NH—CO—C1-6alkyl-, —CO—C1-7alkyl-, —C1-7alkyl-CO—, —C1-6alkyl-CO—C1-6alkyl-, —C1-2alkyl-NH—CO—CR16R17—NH—, —C1-2alkyl-CO—NH—CR18R19—CO—, —C1-2alkyl-CO—NR20—C1-3alkyl-CO—, C1-2alkyl-NR21—CH2—CO—NH—C1-3alkyl-, or NR22—CO—C1-3alkyl-NH—, X1 represents a direct bond, O or —O—C1-2alkyl-, CO, —CO—C1-2alkyl-, NR11, —NR11—C1-2alkyl-, —CH2—, —O—N═CH— or —C1-2alkyl-; X2 represents a direct bond, O, —O—C1-2alkyl-, CO, —CO—C1-2alkyl-, NR12, —NR12—C1-2alkyl-, —CH2—, —O—N═CH— or —C1-2alkyl-. The growth inhibitory effect anti-tumour activity of the present compounds has been demonstrated in vitro, in enzymatic on the receptor tyrosine kinase EGFR.

    摘要翻译： 本发明涉及式（I）化合物的N-氧化物形式，其药学上可接受的加成盐和立体化学异构形式，其中Z代表O，CH2，NH或S; 特别是Z表示NH; 一个或多个（C 1-4烷基）氨基或C 1-4烷氧基羰基氨基 - 取代的C 1-3烷基 - ， - C 3-9烯基 - ， - C 3-9炔基 - ， - 一个或多个（C 1-4烷基）氨基 - 或C 1-4烷氧基羰基氨基 - ，C 1-5烷基 - 氧基-C 1-5烷基 - ， - C 1-5烷基NR 13 - ， - -C1-5烷基 - ， - C 1-5烷基-NR 14 -CO-C 1-5烷基 - ， - C 1-5烷基-CO NR 15 -C 1-5烷基 - ， - C 1-6烷基-CO-NH-，-C 1-6烷基-NH- CO-，-C 1-3烷基-NH-CS-Het20-，-C1-3烷基-NH-CO-Het20，-C1-2烷基-CO-Het21-CO-，-Het22-CH2-CO-NH-C1-3烷基 - ，-CO-NH-C 1-6烷基 - ， - NH-CO-C 1-6烷基 - ， - CO-C 1-7烷基 - ， - C 1-7烷基-CO-，-C 1-6烷基-CO-C 1-6烷基 - -C1-2烷基-NH-CO-CR16R17-NH-，-C1-2烷基-CO-NH-CR18R19-CO-，-C1-2烷基-CO-NR20-C1-3烷基-CO-，C1-2烷基-NR21- CH2-CO-NH-C1-3烷基 - 或NR22-CO-C1-3烷基-NH-，X1表示直接键，O或-O-C 1-2烷基 - ，CO，-CO-C 1-2烷基 - ，NR 11 ，-NR 11 -C 1-2烷基 - ， - CH 2 - ，--ON-CH-或-C 1-2烷基 - ; X2表示直接键合，O，-O-C 1-2烷基 - ，CO，-CO-C 1-2烷基 - ，NR 12，-NR 12 -C 1-2烷基 - ， - CH 2 - ，--ON-CH-或-C 1-2烷基 - 。 本发明化合物的生长抑制作用的抗肿瘤活性已在体外证明在酶对受体酪氨酸激酶EGFR的作用。

    C-5 substituted quinazolinone derivatives as selective estrogen receptor beta modulators
    7.
    发明授权
    C-5 substituted quinazolinone derivatives as selective estrogen receptor beta modulators 有权
    C-5取代喹唑啉酮衍生物作为选择性雌激素受体β调节剂

    公开(公告)号：US07456188B1

    公开(公告)日：2008-11-25

    申请号：US11411456

    申请日：2006-04-26

    申请人： James R. Corte ,  John K. Dickson ,  Timur Gungor

    发明人： James R. Corte ,  John K. Dickson ,  Timur Gungor

    IPC分类号： A61K31/517 ,  C07D239/88

    CPC分类号： C07D239/91 ,  C07D239/93

    摘要： The present application describes compounds according to Formula I, wherein Q, R1, R2 and X are described herein, that are useful as Estrogen Receptor Beta (ERβ) modulators. Additionally, the present application describes pharmaceutical compositions containing the compounds according to Formula I and optionally additional therapeutic agents. Finally, the present application describes methods utilizing the compounds according to Formula I for modulating the function of ERβ in the treatment of diseases and disorders associated with ERβ such as, for example, bone disorders; cardiovascular diseases; hypercholesterolemia; hypertriglyceridemia; vasomotor disorders; urogenital disorders; prostatic hypertrophy; endometrial hyperplasia; cancer and central nervous system disorders, such as, neurodegenerative disorders.

    摘要翻译： 本申请描述了根据式I的化合物，其中Q，R 1，R 2和X在本文中描述，其可用作雌激素受体β（ERβ）调节剂。 此外，本申请描述了含有根据式I的化合物和任选的另外的治疗剂的药物组合物。 最后，本申请描述了利用式I化合物调节ERbeta在治疗与ERBeta相关的疾病和病症（例如骨病）中的功能的方法; 心血管疾病; 高胆固醇血症 高甘油三酯血症 血管舒缩障碍 泌尿生殖系统疾病 前列腺肥大; 子宫内膜增生; 癌症和中枢神经系统疾病，如神经变性疾病。