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    • 5. 发明申请
      US20060183747A1 Triazolopyrimidine derivatives as glycogen synthase kinase 3 inhibitors 有权
    • Triazolopyrimidine derivatives as glycogen synthase kinase 3 inhibitors
    • US20060183747A1
    • 2006-08-17
    • US10565065
    • 2004-07-12
    • Eddy Freyne , Christopher Love , Ludwig Cooymans , Nele Vandermaesen , Peter Jacobus Buijnsters , Marc Willems , Werner Embrechts
    • Eddy Freyne , Christopher Love , Ludwig Cooymans , Nele Vandermaesen , Peter Jacobus Buijnsters , Marc Willems , Werner Embrechts
    • A61K31/519 , C07D487/02
    • C07D487/04
    • This invention concerns compounds of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A represents phenyl, pyridyl, pyrimidinyl, pyridazinyl or pyrazinyl; R1 represents hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; C1-6alkyl substituted with formyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy; or optionally substituted C1-6alkyloxyC1-6alkylcarbonyl; X1 represents a direct bond; —(CH2)n3— or —(CH2)n4—X1a—X1b—; R2 represents optionally substituted C3-7cycloalkyl; phenyl; a 4, 5, 6- or 7-membered monocyclic heterocycle containing at least one hetetoatom selected from O, S or N; benzoxazolyl or a radical of formula X2 represents a direct bond; —NR1—; —NR1—(CH2)n3—; —O—; —O—(CH2)n3—; —C(═O)—; —C(═O)—(CH2)n3—; —C(═O)—NR5—(CH2)n3—; —C(═S)—; —S—; —S(═O)n1—; —(CH2)n3—; —(CH2)n4—X1a—X1b—; —X1a—X1b—(CH2)n4—; —S(═O)n1—NR5—(CH2)n3—NR5— or —S(═O)n1—NR5—(CH2)n3—; R3 represents an optionally substituted 5- or 6-membered monocyclic heterocycle containing at least one heteroatom selected from O, S or N, or a 9- or 10-membered bicyclic heterocycle containing at least one heteroatom selected from O, S or N; R4 represents hydrogen; halo; hydroxy; optionally substituted C1-4alkyl; optionally substituted C2-4alkenyl or C2-4alkynyl; polyhaloC1-3alkyl; optionally substituted C1-4alkyloxy; polyhaloC1-3alkyloxy; C1-4alkylthio; polyhaloC1-3alkylthio; C1-4alkyloxycarbonyl; C1-4alkylcarbonyloxy; C1-4alkylcarbonyl; polyhaloC1-4alkylcarbonyl; nitro; cyano; carboxyl; NR9R10; C(═O)NR9R10; —NR5—C(═O)—NR9R10; —NR5—C(═O)—R11; —S(═O)n1—R11; —NR5—S(═O)n1—R11; —S—CN; —NR5—CN; their use, pharmaceutical compositions comprising them and processes for their preparation.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 9. 发明申请
      US20120065395A1 2,4 (4,6) PYRIMIDINE DERIVATIVES 有权
    • 2,4 (4,6) PYRIMIDINE DERIVATIVES
    • US20120065395A1
    • 2012-03-15
    • US13277651
    • 2011-10-20
    • Eddy Jean Edgard Freyne , Marc Willems , Werner Constant Johan Embrechts , Kristof Van Emelen , Sven Franciscus Anna Van Brandt , Frederik Jan Rita Rombouts
    • Eddy Jean Edgard Freyne , Marc Willems , Werner Constant Johan Embrechts , Kristof Van Emelen , Sven Franciscus Anna Van Brandt , Frederik Jan Rita Rombouts
    • C07D239/48 , C07D405/12 , C07D403/12
    • C07D487/18 , C07D487/08 , C07D487/22 , C07D498/08 , C07D498/18
    • The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z1 and Z2 represent NH; Y represents —C3-9alkyl-, —C3-9 alkenyl-, —C1-5alkyl-NR6—C1-5alkyl-, —C1-5alkyl-NR7—CO—C1-5alkyl-, —C1-6alkyl-CO—NH—, —C1-6alkyl-NH—CO—, —C1-2alkyl-CO-Het10-CO—, —C1-3alkyl-NH—CO-Het3-, -Het4-C1-3alkyl-CO—NH—C1-3alkyl-, —C1-2alkyl-NH—CO-L1-NH—, —NH—CO-L2-NH—, —C1-2alkyl-CO—NH-L3-CO—, —C1-2alkyl-NH—CO-L1-NH—CO—C1-3 alkyl-, —C1-2alkyl-CO—NH-L3-CO—NH—C1-3alkyl-, —C1-2alkyl-NR11—CH2—CO—NH—C1-3alkyl-, Het5-CO—C1-2alkyl-, —C1-5alkyl-CO—NH—C1-3alkyl-CO—NH—, —C1-5alkyl-NR13—CO—C1-3alkyl-NH—, —C1-3alkyl-NH—CO-Het27-CO—, or —C1-3alkyl-CO-Het28-CO—NH—; X1 represents a direct bond, O, —O—C1-2alkyl-, —CO—C1-2alkyl-, —NR16—C1-2alkyl-, —CO—NR17—, Het23-C1-2alkyl- or C1-2alkyl; X2 represents a direct bond, O, —O—C1-2alkyl-, —CO—C1-2alkyl-, —NR18—C1-2alkyl-, —CO—NR19—, Het24-C1-2alkyl- or C1-2alkyl; R1 and R5 each independently represent hydrogen, halo, C1-6alkyloxy- or C1-6alkyloxy- substituted with Het1 or C1-4alkyloxy-; R2 and R4 each independently represent hydrogen or halo; R3 represents hydrogen or cyano; R6, R7, R13, R17 and R19 represent hydrogen; R11 represents hydrogen or C1-4alkyl; R16 and R18 represent hydrogen, C1-4alkyl or Het17-C1-4alkyl-; L1, L2 and L3 each independently represents C1-8alkyl optionally substituted with one or where possible two or more substituents selected from phenyl, methylsulfide, cyano, polyhaloC1-4alkyl-phenyl-, C1-4alkyloxy, pyridinyl, mono- or di(C1-4alkyl)-amino- or C3-6cycloalkyl; Het1, Het2, Het17 each independently represent morpholinyl, oxazolyl, isoxazolyl, or piperazinyl; Het3, Het4, Het5 each independently represent morpholinyl, piperazinyl, piperidinyl or pyrrolidinyl; Het10 represents piperazinyl, piperidinyl, pyrrolidinyl or azetidinyl; Het22 represents morpholinyl, oxazolyl, isoxazolyl or piperazinyl wherein said Het22 is optionally substituted with C1-4alkyl; Het23 and Het24 each independently represent a heterocycle selected from pyrrolidinyl, piperazinyl or piperidinyl wherein said Het23 or Het24 are optionally substituted with Het22-carbonyl; Het27 and Het28 each independently represent a heterocycle selected from morpholinyl, piperazinyl, piperidinyl or pyrrolidinyl.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 10. 发明授权
      US07648975B2 Macrocyclic quinazoline derivatives as antiproliferative agents 有权
    • Macrocyclic quinazoline derivatives as antiproliferative agents
    • 大环喹唑啉衍生物作为抗增殖剂
    • US07648975B2
    • 2010-01-19
    • US10558007
    • 2004-05-25
    • Eddy Jean Edgard Freyne , Timothy Pietro Suren Perera , Peter Jacobus Johannes Antonius Buijnsters , Marc Willems , Gaston Stanislas Marcella Diels , Werner Constant Johan Embrechts
    • Eddy Jean Edgard Freyne , Timothy Pietro Suren Perera , Peter Jacobus Johannes Antonius Buijnsters , Marc Willems , Gaston Stanislas Marcella Diels , Werner Constant Johan Embrechts
    • A01N43/00 , A61K31/33 , C07D487/00 , C07D491/00 , C07D513/00
    • C07D498/06 , C07C229/16 , C07C229/40 , C07D239/88 , C07D239/93 , C07D239/94
    • 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.
    • 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
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