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    Quinazoline derivatives
    3.
    发明申请
    Quinazoline derivatives 有权
    喹唑啉衍生物

    公开(公告)号：US20100105668A1

    公开(公告)日：2010-04-29

    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： A61K31/541 ,  C07D239/70 ,  A61K31/517 ,  C07D413/02 ,  A61K31/5377 ,  C07D417/02 ,  C07C211/00 ,  C07D239/72

    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
    4.
    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
    5.
    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。

    1,3-dihydro-1-(phenylalkenyl)-2H-imidazol-2-one derivatives having PDE IV and cytokine inhibiting activity
    7.
    发明授权
    1,3-dihydro-1-(phenylalkenyl)-2H-imidazol-2-one derivatives having PDE IV and cytokine inhibiting activity 失效
    具有PDE IV和细胞因子抑制活性的1,3-二氢-1-（苯基烯基）-2H-咪唑-2-酮衍生物

    公开(公告)号：US5952510A

    公开(公告)日：1999-09-14

    申请号：US945849

    申请日：1997-09-30

    申请人： Eddy Jean Edgard Freyne ,  Gaston Stanislas Marcella Diels ,  Jose Ignacio Andres-Gil ,  Francisco Javier Fernandez-Gadea

    发明人： Eddy Jean Edgard Freyne ,  Gaston Stanislas Marcella Diels ,  Jose Ignacio Andres-Gil ,  Francisco Javier Fernandez-Gadea

    IPC分类号： A61K31/415 ,  A61K31/4166 ,  A61P11/00 ,  A61P17/00 ,  A61P29/00 ,  A61P37/08 ,  C07D233/32 ,  C07D233/38 ,  C07D233/70

    CPC分类号： C07D233/32 ,  C07D233/70

    摘要： The present invention concerns the compounds of formula ##STR1## the N-oxide forms, the pharmaceutically acceptable acid or base addition salts and the stereochemically isomeric forms thereof, wherein R.sup.1 and R.sup.2 each independently are hydrogen; C.sub.1-6 alkyl; difluoromethyl; trifluoromethyl; C.sub.3-6 cycloalkyl; a saturated 5-, 6 or 7-membered heterocycle containing one or two heteroatoms selected from oxygen, sulfur or nitrogen; indanyl; bicyclo�2.2.1!-2-heptenyl; bicyclo�2.2.1!heptanyl; C.sub.1-6 alkylsulfonyl; arylsulfonyl; or substituted C.sub.1-10 alkyl; R.sup.3 is hydrogen, halo or C.sub.1-6 alkyloxy; R.sup.4 is hydrogen; cyano; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkyloxycarbonyl or aryl; R.sup.5 is hydrogen; cyano; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkyloxycarbonyl or aryl; Y is a direct bond or C.sub.1-3 alkanediyl; --A--B-- is a bivalent radical of formula --CR.sup.6 .dbd.CR.sup.7 -- or --CHR.sup.6 --CHR.sup.7 --; L is hydrogen; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; C.sub.1-6 alkyloxycarbonyl; C.sub.1-6 alkylsulfonyl or arylsulfonyl; aryl is optionally substituted phenyl; Het is morpholinyl or optionally substituted piperidinyl, -piperazinyl, -pyridinyl;, -furanyl or -thienyl; having PDE IV and cytokine inhibiting activity. Further, pharmaceutical compositions, preparations and use as a medicine are described.

    摘要翻译： PCT No.PCT / EP96 / 01395 Sec。 371日期：1997年9月30日 102（e）1997年9月30日PCT PCT 1996年3月28日PCT公布。 WO96 / 31486 PCT公开号 日期：1996年10月10日本发明涉及N-氧化物形式的化合物，其药学上可接受的酸或碱加成盐及其立体化学异构形式，其中R 1和R 2各自独立地为氢; C 1-6烷基; 二氟甲基 三氟甲基 C 3-6环烷基; 含有一个或两个选自氧，硫或氮的杂原子的饱和的5-，6-或7-元杂环; 茚满基 双环[2.2.1] -2-庚烯基; 双环[2.2.1]庚基; C 1-6烷基磺酰基; 芳基磺酰基; 或取代的C 1-10烷基; R3是氢，卤素或C1-6烷氧基; R4是氢; 氰基; 任选取代的C 1-6烷基; C 1-6烷氧基羰基或芳基; R5是氢; 氰基; 任选取代的C 1-6烷基; C 1-6烷氧基羰基或芳基; Y是直接键或C1-3烷二基; -A-B-是式-CR6 = CR7-或-CHR6-CHR7-的二价基团; L是氢; 任选取代的C 1-6烷基; C 1-6烷基羰基; C 1-6烷氧基羰基; C 1-6烷基磺酰基或芳基磺酰基; 芳基是任选取代的苯基; 哌嗪基，呋喃基或噻吩基;吗啉基或任选取代的哌啶基，哌嗪基， 具有PDE IV和细胞因子抑制活性。 此外，描述了作为药物的药物组合物，制剂和用途。

    6-azauracil derivatives as IL-5 inhibitors
    9.
    发明授权
    6-azauracil derivatives as IL-5 inhibitors 失效
    6-氮尿嘧啶衍生物作为IL-5抑制剂

    公开(公告)号：US06743792B2

    公开(公告)日：2004-06-01

    申请号：US09855068

    申请日：2001-05-14

    申请人： Eddy Jean Edgard Freyne ,  Gustaaf Maria Boeckx ,  Jean Pierre Frans Van Wauwe ,  Gaston Stanislas Marcella Diels

    发明人： Eddy Jean Edgard Freyne ,  Gustaaf Maria Boeckx ,  Jean Pierre Frans Van Wauwe ,  Gaston Stanislas Marcella Diels

    IPC分类号： C07D253075

    CPC分类号： A61K51/0491 ,  A61K31/53 ,  A61K51/04 ,  A61K51/0461 ,  C07D253/075 ,  C07D403/10 ,  C07D417/10

    摘要： The present invention is concerned with the use of compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p represents 0, 1, 2 or 3; q represents 0, 1, 2, 3 or 4; R1 represents hydrogen, C1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, mercapto, C1-6alkylthio, C3-7cycloalkyl, aryl or C1-6alkyl substituted with mono- or di(C1-6alkyl)-amino, C1-6alkyloxy, aryl or Het; R2 represents cyano or a radical of formula —C(═X)—Y—R5; wherein X represents O or S; Y represents O, S, NR6 or a direct bond; R5 represents hydrogen; C3-7cycloalkyl; aryl or optionally substituted C1-6alkyl; and where Y is a direct bond, R5 may also be halo or Het; R3 and R4 each independently represents halo, haloC1-6alkyl, C1-6alkyl, hydroxy, C1-6alkyloxy, C1-6alkylcarbonyloxy, mercapto, C1-6alkylthio, C1-6alkylsulfonyl, C1-6alkylsulfinyl, haloC1-6alkylsulfonyl, aryl, cyano, nitro, amino, mono- and di(C1-6alkyl)amino or (C1-6alkylcarbonyl)amino; aryl represents phenyl or substituted phenyl; and Het represents an optionally substituted heterocycle; in the manufacture of a medicament useful for treating eosinophil-dependent inflammatory diseases. The invention also relates to novel compounds, their preparation and compositions comprising them.

    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，其中p代表0,1,2或3; q表示0,1,2,3或4; R 1表示氢，C 1-6烷基，一或二（C 1-6烷基）氨基C 1-6烷氧基，巯基，C 1-6烷硫基，C 3-7环烷基，芳基或被单或二（C 1-6烷基） 氨基，C 1-6烷氧基，芳基或Het; R 2表示氰基或式-C（= X）-Y-R 5的基团; 其中X表示O或S; Y表示O，S，NR 6或直接键; R 5表示氢; C 3-7环烷基; 芳基或任选取代的C 1-6烷基; 并且其中Y是直接键，R 5也可以是卤素或Het; R 3和R 4各自独立地表示卤素，卤代C 1-6烷基，C 1-6烷基，羟基，C 1-6烷氧基，C 1-6烷基羰氧基，巯基，C 1-6烷硫基，C 1-6烷基磺酰基，C 1-6烷基亚磺酰基，卤代C 1-6烷基磺酰基， 芳基，氰基，硝基，氨基，单和二（C 1-6烷基）氨基或（C 1-6烷基羰基）氨基; 芳基表示苯基或取代的苯基; 并且Het表示任选取代的杂环; 在制备可用于治疗嗜酸性粒细胞依赖性炎性疾病的药物中。 本发明还涉及新化合物，其制备方法和包含它们的组合物。