专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

11. 发明授权

US08394786B2 Quinazoline derivatives 有权
标题翻译：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。

12. 发明申请

US20100204197A1 PYRROLOPYRIMIDINES 有权
标题翻译：吡咯烷酮
公开(公告)号：US20100204197A1
公开(公告)日：2010-08-12
申请号：US12670670
申请日：2008-07-25
申请人： Gaston Stanislas Marcella Diels , Peter Ten Holte , Eddy Jean Edgard Freyne , Thierry Andre Regis Grand-Perret , Kristof Van Emelen , Werner Constant Johan Embrechts , Pascal Ghislain André Bonnet
发明人： Gaston Stanislas Marcella Diels , Peter Ten Holte , Eddy Jean Edgard Freyne , Thierry Andre Regis Grand-Perret , Kristof Van Emelen , Werner Constant Johan Embrechts , Pascal Ghislain André Bonnet
IPC分类号： A61K31/397 , C07D498/18 , A61K31/33 , C07D487/18 , A61K31/496 , A61K31/5377 , A61P19/02 , A61P9/10 , A61P35/00
CPC分类号： C07D498/08 , C07D487/08
摘要： The present invention relates to compounds or pharmaceutically-acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to compounds that are polo-like kinase (PLKs) inhibitors useful for the treatment of disease states mediated by PLK, especially PLK4, in particular such compounds that are useful in the treatment of pathological processes which involve an aberrant cellular proliferation, such as tumour growth, rheumatoid arthritis, restenosis and atherosclerosis.
摘要翻译：本发明涉及其化合物或药学上可接受的盐，其制备方法，含有它们的药物组合物及其在治疗中的用途。本发明特别涉及可用于治疗由PLK，特别是PLK4介导的疾病状态的polo样激酶（PLK）抑制剂的化合物，特别是可用于治疗涉及异常细胞增殖的病理过程的这类化合物，如肿瘤生长，类风湿关节炎，再狭窄和动脉粥样硬化。

13. 发明授权

US07648975B2 Macrocyclic quinazoline derivatives as antiproliferative agents 有权
标题翻译：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。

14. 发明授权

US06403805B1 1,3-dihydro-1-(phenylalkyl)-2H-imidazol-2-one derivatves 有权
标题翻译： 1,3-二氢-1-（苯基烷基）-2H-咪唑-2-酮化合物
公开(公告)号：US06403805B1
公开(公告)日：2002-06-11
申请号：US09362007
申请日：1999-07-27
申请人： Eddy Jean Edgard Freyne , Gaston Stanislas Marcella Diels , José Ignacio Andrés-Gil , Francisco Javier Fernández-Gadea
发明人： Eddy Jean Edgard Freyne , Gaston Stanislas Marcella Diels , José Ignacio Andrés-Gil , Francisco Javier Fernández-Gadea
IPC分类号： C07D23332
CPC分类号： C07D401/06 , C07D233/36 , C07D233/38 , C07D233/70
摘要： The present invention describes compounds useful for treating warm-blooded animals suffering from disease states related to an abnormal enzymatic or catalytic activity of phosphodiesterase IV (PDE IV), and/or disease states related to a physiologically detrimental excess of cytokines, in particular allergic, atopic and inflammatory diseases, said compounds having the formula the N-oxide forms, the pharmaceutically acceptable acid or base addition salts and the stereochemically isomeric forms thereof.
摘要翻译：本发明描述了可用于治疗患有与磷酸二酯酶IV（PDE IV）的异常酶促或催化活性相关的疾病状态的温血动物的化合物和/或与生理上有害的细胞因子过量相关的疾病状态，特别是过敏性疾病，特应性和炎症性疾病，所述具有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。

15. 发明授权

US5994376A 1,3-dihydro-1-(phenylalkyl)-2H-imidazol-2-one compounds and their use for treating allergic, atopic or inflammatory diseases 失效
标题翻译： 1,3-二氢-1-（苯基烷基）-2H-咪唑-2-酮化合物及其用于治疗过敏性，特应性或炎性疾病的用途
公开(公告)号：US5994376A
公开(公告)日：1999-11-30
申请号：US930296
申请日：1997-09-29
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： C07D233/32 , A61K31/415 , A61K31/4166 , A61K31/44 , A61K31/4427 , A61K31/443 , A61P11/00 , A61P17/00 , A61P29/00 , A61P37/08 , C07D233/36 , C07D233/38 , C07D233/70 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/12
CPC分类号： C07D401/06 , C07D233/36 , C07D233/38 , C07D233/70
摘要： The present invention describes 1,3-dihydro-1-(phenylalkyl)-2H-imidazol-2-one compounds and their use for treating warm-blooded animals suffering from disease states related to an abnormal enzymatic or catalytic activity of phosphodiesterase IV (PDE IV), and/or disease states related to a physiologically detrimental excess of cytokines, in particular allergic, atopic and inflammatory diseases.
摘要翻译： PCT No.PCT / EP96 / 01394 Sec。 371日期：1997年9月29日 102（e）1997年9月29日PCT PCT 1996年3月28日PCT公布。出版物WO96 / 31485 日期：1996年10月10日本发明描述了1,3-二氢-1-（苯基烷基）-2H-咪唑-2-酮化合物及其用于治疗与异常酶促或催化活性有关的疾病状态的温血动物磷酸二酯酶IV（PDE IV）和/或与细胞因子的生理有害过量相关的疾病状态，特别是过敏性，特应性和炎性疾病。

16. 发明授权

US5869515A 1,3-dihydro-2H-imidazol-2-one compounds 失效
标题翻译： 1,3-二氢-2H-咪唑-2-酮化合物
公开(公告)号：US5869515A
公开(公告)日：1999-02-09
申请号：US930478
申请日：1997-09-29
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 , C07D405/04 , C07D405/06
CPC分类号： C07D405/04 , 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; R3 is hydrogen, halo or C.sub.1-6 alkyloxy ##STR2## is a bivalent radical of formula ##STR3## Alk is C1-4alkanediyl; --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; optionally substituted C.sub.3-6 alkenyl; optionally substituted piperidinyl; C.sub.1-6 alkylsulfonyl or arylsulfonyl; aryl is optionally substituted phenyl; Het.sup.1 is morpholinyl or optionally substituted pyridinyl, -furanyl, -thienyl, -hydroxypyridinyl, -imidazolyl, -thiazolyl, -oxazolyl, -isoquinolinyl, -quinolinonyl, -piperidinyl, -piperazinyl; and Het.sup.2 is morpholinyl or optionally substituted piperidinyl, -piperazinyl, -pyridinyl, -furanyl or -thienyl; having PDE IV and cytokine inhibiting activity. The invention also relates to processes for preparing the compounds of formula (I) and pharmaceutical compositions thereof.
摘要翻译： PCT No.PCT / EP96 / 01393 Sec。 371日期：1997年9月29日 102（e）1997年9月29日PCT PCT 1996年3月28日PCT公布。公开号WO96 / 31487 日期：1996年10月10日本发明涉及式（I）的化合物：（I）N-氧化物形式，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R1和R2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; R 3是氢，卤素或C 1-6烷氧基，是下式的二价基团：其中A k是C 1-4烷二基; -A-B-是下式的二价基团：-CR 6 = CR 7 - 或-CHR 6 -CHR 7 - ; 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; 任选取代的C 3-6烯基; 任选取代的哌啶基; C 1-6烷基磺酰基或芳基磺酰基; 芳基是任选取代的苯基; - Het1是吗啉基或任意取代的吡啶基， - 呋喃基， - 噻吩基， - 羟基吡啶基， - 咪唑基， - 噻唑基， - 恶唑基， - 异喹啉基， - 喹啉酮基， - 哌啶基，和Het2是吗啉基或任选取代的哌啶基，哌嗪基， - 吡啶基， - 呋喃基或 - 噻吩基; 具有PDE IV和细胞因子抑制活性。本发明还涉及制备式（I）化合物及其药物组合物的方法。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式