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1. 发明申请

US20050004125A1 Heteroaryl amines as glycogen synthase kinase 3beta inhibitors (gsk3 inhibitors) 有权
标题翻译：杂芳基胺作为糖原合酶激酶3β抑制剂（gsk3抑制剂）
公开(公告)号：US20050004125A1
公开(公告)日：2005-01-06
申请号：US10493452
申请日：2002-10-29
申请人： Eddy Jean Edgard Freyne , Peter Jacobus Buijnsters , Marc Willems , Werner Embrechts , Christopher Love , Paul Janssen , Paulus Lewi , Jan Heeres , Marc de Jonge , Lucien Koymans , Hendrik Vinkers , Koen Van Aken , Gaston Diels
发明人： Eddy Jean Edgard Freyne , Peter Jacobus Buijnsters , Marc Willems , Werner Embrechts , Christopher Love , Paul Janssen , Paulus Lewi , Jan Heeres , Marc de Jonge , Lucien Koymans , Hendrik Vinkers , Koen Van Aken , Gaston Diels
IPC分类号： A61K31/435 , A61K31/4406 , A61K31/50 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/5377 , A61P3/10 , A61P17/00 , A61P21/04 , A61P25/00 , A61P25/04 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P29/00 , A61P31/18 , A61P35/00 , A61P35/02 , C07D213/53 , C07D213/74 , C07D239/42 , C07D239/48 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , A61K31/4965
CPC分类号： C07D213/74 , C07D239/42 , C07D239/48 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： This invention concerns a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A is a 6-membered heterocycle; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyloxyC1-6alkylcarbonyl; X is a direct bond or a linker atom or group; Z is a direct bond or a linker atom or group; R2 is hydrogen, C1-10alkyl, C2-10alkenyl, C2-10alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R3 is hydrogen; hydroxy; halo; optionally substituted C1-6alkyl or C2-6alkenyl or C2-6alkynyl; C1-6alkyloxy; C1-6alkylthio; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; R21; R21—C1-6alkyl; R21—O—; R21—S—; R21—C(═O)—; R21—S(═O)p—; R7—S(═O)p—; R7—S(═O)p—NH—; R21—S(═O)p—NH—; R7—C(═O)—; —NHC(═O)H; —C(═O)NHNH2; R7—C(═O)—NH—; R21—C(═O)—NH—; —C(═NH)R7—C(═NH)R21; R4 is an optionally substituted heterocycle provided that —X—R2 and/or R3 is other than hydrogen; their use, pharmaceutical compositions comprising them and processes for their preparation.
摘要翻译：本发明涉及式的化合物N-氧化物，药学上可接受的加成盐，季胺及其立体化学异构形式，其中环A是6-元杂环; R 1是氢; 芳基; 甲酰基 C 1-6烷基羰基; 任选取代的C 1-6烷基; C 1-6烷氧基羰基; 任选取代的C 1-6烷氧基C 1-6烷基羰基; X是直接键或连接原子或基团; Z是直接键或连接原子或基团; R 2是氢，C 1-10烷基，C 2-10烯基，C 2-10炔基，碳环或杂环，所述基团中的每一个可任选被取代; R 3是氢; 羟基; 光环; 任选取代的C 1-6烷基或C 2-6烯基或C 2-6炔基; C 1-6烷氧基; C 1-6烷硫基; C 1-6烷氧基羰基; C 1-6烷基羰基氧基; 羧基; 氰基; 硝基氨基; 单或二（C 1-6烷基）氨基; 多卤代C 1-6烷基; 多卤代C 1-6烷氧基; 多卤代C 1-6烷硫基; R 21; R 21 -C 1-6烷基; R 21 -O- R 21 -S-; R 21 -C（= O） - ; R 21 -S（= O）p - ; R 7 -S（= O）p-; R 7 -S（= O）p-NH-; R 21 -S（= O）p -NH-; R 7 -C（= O） - ; -NHC（= O）H; -C（= O）NHNH 2; R 7 -C（= O）-NH-; R 21 -C（= O）-NH-; -C（= NH）R 7 -C（= NH）R 21; R 4是任选取代的杂环，条件是-X-R 2和/或R 3不是氢; 其用途，包含它们的药物组合物及其制备方法。

2. 发明申请

US20060247237A1 Macrocyclic quinazoline derivatives as antiproliferative agents 有权
公开(公告)号：US20060247237A1
公开(公告)日：2006-11-02
申请号：US10558007
申请日：2004-05-25
申请人： Eddy Jean Freyne , Timothy Perera , Peter Jacobus Buijnsters , Marc Willems , Gaston Diels , Werner Embrechts
发明人： Eddy Jean Freyne , Timothy Perera , Peter Jacobus Buijnsters , Marc Willems , Gaston Diels , Werner Embrechts
IPC分类号： A61K31/5377 , A61K31/519 , C07D487/22
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.

3. 发明申请

US20060183747A1 Triazolopyrimidine derivatives as glycogen synthase kinase 3 inhibitors 有权
公开(公告)号：US20060183747A1
公开(公告)日：2006-08-17
申请号：US10565065
申请日：2004-07-12
申请人： Eddy Freyne , Christopher Love , Ludwig Cooymans , Nele Vandermaesen , Peter Jacobus Buijnsters , Marc Willems , Werner Embrechts
发明人： Eddy Freyne , Christopher Love , Ludwig Cooymans , Nele Vandermaesen , Peter Jacobus Buijnsters , Marc Willems , Werner Embrechts
IPC分类号： A61K31/519 , C07D487/02
CPC分类号： C07D487/04
摘要： 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.

4. 发明申请

US20070078132A1 Pyrido-and pyrimidopyrimidine derivatives as anti-profilerative agents 有权
公开(公告)号：US20070078132A1
公开(公告)日：2007-04-05
申请号：US10596512
申请日：2004-12-15
申请人： Eddy Freyne , Marc Willems , Pierre Storck , Virginie Poncelet , Kristof Van Emelen , Peter Jacobus Johnnes Buijnsters , Werner Embrechts , Timothy Perera
发明人： Eddy Freyne , Marc Willems , Pierre Storck , Virginie Poncelet , Kristof Van Emelen , Peter Jacobus Johnnes Buijnsters , Werner Embrechts , Timothy Perera
IPC分类号： A61K31/5377 , A61K31/535 , A61K31/525 , C07D491/22
CPC分类号： C07D498/16 , C07D471/04 , C07D487/04 , C07D487/16 , C07D487/22
摘要： The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein a1-a2=a3-a4 represents a divalent radical selected from N—CH═CH—CH, N—CH═N—CH or CH—CH═N—CH; Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR13—C1-5alkyl-, —C1-6alkyl-NH—CO— or —CO—NH—C1-6alkyl-; X1 represents —O— or —NR11—; X2 represents —C1-2alkyl-, —O—C1-2alkyl, —O— or —O—CH2—; R1 represents hydrogen or halo; R2 represents hydrogen, cyano, halo, hydroxycarbonyl-, C1-4alkyloxycarbonyl-, Het16-carbonyl- or Ar5; R3 represents hydrogen; R4 represents hydroxy, C1-4alkyloxy-, Ar4—C1-4alkyloxy or R4 represents C1-4alkyloxy substituted with one or where possible two or more substituents selected from C1-4alkyloxy- or Het2-; R11 represents hydrogen; R12 represents hydrogen, C1-4alkyl- or C1-4alkyl-oxy-carbonyl-; R13 represents Het14-C1-4alkyl, in particular morpholinyl-C1-4alkyl; Het2 represents a heterocycle selected from morpholinyl or piperidinyl optionally substituted with C1-4alkyl-, preferably methyl; Het14 represents morpholinyl; Het16 represents a heterocycle selected from morpholinyl or pyrrolidinyl; Ar4 represents phenyl; Ar5 represents phenyl optionally substituted with cyano.

5. 发明授权

US08916575B2 Quinazoline derivatives for the treatment of viral infections and further diseases 有权
标题翻译：喹唑啉衍生物用于治疗病毒感染和进一步疾病
公开(公告)号：US08916575B2
公开(公告)日：2014-12-23
申请号：US14118527
申请日：2012-05-18
申请人： David McGowan , Pierre Jean-Marie Bernard Raboisson , Tim Hugo Maria Jonckers , Stefaan Julien Last , Werner Embrechts , Serge Maria Aloysius Pieters
发明人： David McGowan , Pierre Jean-Marie Bernard Raboisson , Tim Hugo Maria Jonckers , Stefaan Julien Last , Werner Embrechts , Serge Maria Aloysius Pieters
IPC分类号： A01N43/54 , C07D239/72 , C07D401/00
CPC分类号： C07D491/056 , C07D239/95 , C07D295/192 , C07D401/06 , C07D403/04
摘要： This invention relates to quinazoline derivatives, processes for their preparation, pharmaceutical compositions, and their use in therapy of disorders in which the modulation of toll-like-receptors is involved.
摘要翻译：本发明涉及喹唑啉衍生物，其制备方法，药物组合物及其在治疗涉及toll样受体调节的病症中的用途。

6. 发明授权

US09422250B2 Pyrimidine derivatives for the treatment of viral infections 有权
标题翻译：嘧啶衍生物用于治疗病毒感染
公开(公告)号：US09422250B2
公开(公告)日：2016-08-23
申请号：US14110054
申请日：2012-04-10
申请人： David Mc Gowan , Pierre Jean-Marie Bernard Raboisson , Werner Embrechts , Tim Hugo Maria Jonckers , Stefaan Julien Last , Serge Maria Aloysius Pieters , Jaromir Vlach
发明人： David Mc Gowan , Pierre Jean-Marie Bernard Raboisson , Werner Embrechts , Tim Hugo Maria Jonckers , Stefaan Julien Last , Serge Maria Aloysius Pieters , Jaromir Vlach
IPC分类号： A61K31/535 , A61K31/50 , A61K31/495 , A61K31/505 , C07D239/04 , C07D401/12 , C07D413/12 , C07D471/04 , C07D403/12 , C07D405/12 , C07D239/48 , C07D487/04 , C07D495/04
CPC分类号： A61K31/505 , A61K31/506 , A61K31/5377 , C07D239/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D471/04 , C07D487/04 , C07D495/04
摘要： This invention relates to pyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections such as HCV or HBV.
摘要翻译：本发明涉及嘧啶衍生物，其制备方法，药物组合物及其在治疗病毒感染如HCV或HBV中的用途。

7. 发明申请

US20140045849A1 PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF VIRAL INFECTIONS 有权
标题翻译：用于治疗病毒感染的吡嗪衍生物
公开(公告)号：US20140045849A1
公开(公告)日：2014-02-13
申请号：US14110054
申请日：2012-04-10
申请人： David McGowan , Pierr Jeane-Marie Bernar Raboisson , Werner Embrechts , Tim Hugo Maria Jonckers , Stefaan Julien Last , Serge Maria Aloysius Pieters , Jaromir Vlach
发明人： David McGowan , Pierr Jeane-Marie Bernar Raboisson , Werner Embrechts , Tim Hugo Maria Jonckers , Stefaan Julien Last , Serge Maria Aloysius Pieters , Jaromir Vlach
IPC分类号： C07D239/48 , C07D413/12 , C07D487/04 , C07D403/12 , C07D405/12 , C07D495/04 , C07D401/12 , C07D471/04
CPC分类号： A61K31/505 , A61K31/506 , A61K31/5377 , C07D239/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D471/04 , C07D487/04 , C07D495/04
摘要： This invention relates to pyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections such as HCV or HBV.
摘要翻译：本发明涉及嘧啶衍生物，其制备方法，药物组合物及其在治疗病毒感染如HCV或HBV中的用途。

8. 发明申请

US20140073642A1 QUINAZOLINE DERIVATIVES FOR THE TREATMENT OF VIRAL INFECTIONS AND FURTHER DISEASES 有权
标题翻译：用于治疗病毒感染和进一步疾病的喹唑啉衍生物
公开(公告)号：US20140073642A1
公开(公告)日：2014-03-13
申请号：US14118527
申请日：2012-05-18
申请人： David McGowan , Pierre Jean-Marie Bernard Raboisson , Tim Hugo Maria Jonckers , Stefaan Julien Last , Werner Embrechts , Serge Maria Aloysius Pieters
发明人： David McGowan , Pierre Jean-Marie Bernard Raboisson , Tim Hugo Maria Jonckers , Stefaan Julien Last , Werner Embrechts , Serge Maria Aloysius Pieters
IPC分类号： C07D491/056 , C07D295/192 , C07D403/04 , C07D239/95 , C07D401/06
CPC分类号： C07D491/056 , C07D239/95 , C07D295/192 , C07D401/06 , C07D403/04
摘要： This invention relates to quinazoline derivatives, processes for their preparation, pharmaceutical compositions, and their use in therapy of disorders in which the modulation of toll-like-receptors is involved.
摘要翻译：本发明涉及喹唑啉衍生物，其制备方法，药物组合物及其在治疗涉及toll样受体调节的病症中的用途。

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