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1. 发明申请

US20050176713A1 Amide derivatives as glycogen synthase kinase 3-beta inhibitors 有权
公开(公告)号：US20050176713A1
公开(公告)日：2005-08-11
申请号：US10493454
申请日：2002-10-29
申请人： Eddy Jean Freyne , Peter Jacobus Johannes Buijnsters , Marc Willems , Werner Constant Embrechts , Jean Fernand Lacrampe , Paul Adriaan Janssen , Herwig Josephus Janssen , Paul Janssen , Graziella Janssen , Jasmine Janssen , Maroussia Godelieve Janssen , Theodora Joanna Arts , Paulus Lewi , Jan Heeres , Marc de Jonge , Lucien Maria Koymans , Frederik Frans Daeyaert , Rony Nuydens , Marc Mercken
发明人： Eddy Jean Freyne , Peter Jacobus Johannes Buijnsters , Marc Willems , Werner Constant Embrechts , Jean Fernand Lacrampe , Paul Adriaan Janssen , Herwig Josephus Janssen , Paul Janssen , Graziella Janssen , Jasmine Janssen , Maroussia Godelieve Janssen , Theodora Joanna Arts , Paulus Lewi , Jan Heeres , Marc de Jonge , Lucien Maria Koymans , Frederik Frans Daeyaert , Rony Nuydens , Marc Mercken
IPC分类号： A61K31/44 , A61K31/4409 , A61K31/505 , A61K31/506 , A61K31/5377 , A61P3/10 , A61P7/00 , A61P17/00 , A61P21/04 , A61P25/00 , A61P25/04 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P29/00 , A61P35/00 , A61P43/00 , C07D213/81 , C07D213/82 , C07D239/42 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/12 , C07D407/12 , C07D413/12 , C07D413/14 , C07D417/12 , A61K31/655 , A61K31/4965
CPC分类号： C07D213/81 , C07D213/82 , C07D239/42 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D413/14 , 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 represents 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 O or S; 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; R4a or R4b each independently represent hydrogen, R8, —Y1—NR9—Y2—NR10R11, —Y1—NR9—Y1—R8, —Y1—NR9R10; provided that —X—R2 and/or R3 is other than hydrogen; their use, pharmaceutical compositions comprising them and processes for their preparation.

2. 发明授权

US07241763B2 3-furanyl analogs of toxoflavine as kinase inhibitors 失效
标题翻译：毒素黄嘌呤的3-呋喃基类似物作为激酶抑制剂
公开(公告)号：US07241763B2
公开(公告)日：2007-07-10
申请号：US10520641
申请日：2003-07-08
申请人： Jean Fernand Armand LaCrampe , Richard William Connors , Chih Yung Ho , Alan Richardson , Eddy Jean Edgard Freyne , Peter Jacobus Johannes Buijnsters , Annette Cornelia Bakker
发明人： Jean Fernand Armand LaCrampe , Richard William Connors , Chih Yung Ho , Alan Richardson , Eddy Jean Edgard Freyne , Peter Jacobus Johannes Buijnsters , Annette Cornelia Bakker
IPC分类号： C07D407/04 , C07D487/04 , A61K31/53 , A61P35/00 , A61P19/02
CPC分类号： C07D487/04
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 m, n, R1, R2, R3, R4 and R5 are as defined herein, the use of such compounds as inhibitors of cyclin-dependent serine/threonine kinases (Cdks), as well as kinases and phosphatases involved in cell cycle regulation such as the tyrosine kinases Wee1, Mik1 and Myt1 or the tyrosine dephosphatases such as Cdc25 and Pyp3. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating cell proliferative disorders such as atherosclerosis, restenosis and cancer.
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m，n，R 1，R 2， R 3，R 4和R 5如本文所定义，使用这些化合物作为细胞周期蛋白依赖性丝氨酸/苏氨酸激酶的抑制剂（Cdks），以及参与细胞周期调节的激酶和磷酸酶，例如酪氨酸激酶Wee1，Mik1和Myt1或酪氨酸脱磷酶如Cdc25和Pyp3。本发明进一步涉及包含本发明化合物的药物组合物和治疗细胞增殖性疾病如动脉粥样硬化，再狭窄和癌症的方法。

3. 发明授权

US07655642B2 3-cyano-quinoline derivatives with antiproliferative activity 有权
标题翻译：具有抗增殖活性的3-氰基 - 喹啉衍生物
公开(公告)号：US07655642B2
公开(公告)日：2010-02-02
申请号：US10596509
申请日：2004-12-15
申请人： Eddy Jean Edgard Freyne , Peter Jacobus Johannes Buijnsters , Kristof Van Emelen , Werner Constant Johan Embrechts , Timothy Pietro Suren Perera
发明人： Eddy Jean Edgard Freyne , Peter Jacobus Johannes Buijnsters , Kristof Van Emelen , Werner Constant Johan Embrechts , Timothy Pietro Suren Perera
IPC分类号： A01N43/00 , A61K31/33 , C07D487/00
CPC分类号： C07D215/54 , A61K31/4748 , C07D498/06
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 Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR12—C1-5alkyl-, —C1-6alkyl-NH—CO— or —CO—NH—C1-6alkyl-; X1 represents —O—; X2 represents a direct bond, —NR11—C1-2alkyl-, —NR11—CH2—, —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, hydroxy, C1-4alkyloxy-, Ar4—C1-4alkyloxy or R3 represents C1-4alkyloxy substituted with one or where possible two or more substituents selected from C1-4alkyloxy- or Het2-; R10 represents hydrogen; R11 represents hydrogen, C1-4alkyl- or C1-4alkyl-oxy-carbonyl-; R12 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.
摘要翻译：本发明涉及下式的化合物：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NH; Y表示-C3-9烷基，-C1-5烷基-NR12-C1-5烷基，-C 1-6烷基-NH-CO-或-CO-NH-C 1-6烷基; X1表示-O-; X 2表示直接键，-NR 11 -C 1-2烷基 - ， - NR 11 -CH 2 - ， - C 1-2烷基 - ， - O-C 1-2烷基，-O-或-O-CH 2 - 。 R1表示氢或卤素; R 2表示氢，氰基，卤素，羟基羰基 - ，C 1-4烷氧基羰基 - ，Het 16 - 羰基 - 或Ar 5; R 3表示氢，羟基，C 1-4烷氧基 - ，Ar 4 -C 1-4烷氧基或R 3表示被一个或多个可能的两个或多个选自C 1-4烷氧基 - 或Het 2 - 的取代基取代的C 1-4烷氧基; R10表示氢; R11表示氢，C1-4烷基或C1-4烷基 - 氧 - 羰基 - ; R12表示Het14-C1-4烷基，特别是吗啉基-C 1-4烷基; Het2表示选自任选被C 1-4烷基，优选甲基取代的吗啉基或哌啶基的杂环; Het14代表吗啉基; Het16表示选自吗啉基或吡咯烷基的杂环; Ar4表示苯基; Ar 5表示任选被氰基取代的苯基。

4. 发明申请

US20110009404A1 4-ARYL-2-ANILINO-PYRIMIDINES 有权
公开(公告)号：US20110009404A1
公开(公告)日：2011-01-13
申请号：US12921499
申请日：2009-03-09
申请人： Peter Jacobus Johannes Buijnsters , Marc Gustaaf Celine Verdonck , Kristof Van Emelen , Pascal Ghislain André Bonnet
发明人： Peter Jacobus Johannes Buijnsters , Marc Gustaaf Celine Verdonck , Kristof Van Emelen , Pascal Ghislain André Bonnet
IPC分类号： A61K31/5377 , C07D487/14 , C07D487/04 , A61K31/519 , A61K31/496 , A61P35/00
CPC分类号： C07D471/08 , C07D471/18 , C07D471/22 , C07D498/08 , C07D498/18
摘要： The present invention relates to compounds of Formula (Ia) or (Ib), the N-oxide forms, pharmaceutically acceptable addition salts, quaternary amines, stereoisomers, tautomers, racemics, metabolites, prodrugs, hydrates, or solvates thereof, wherein Y1, m, n, R1; X1; X2; R2; X3; X4; R3; and R4 have the meaning defined in the claims.The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to compounds that are kinase inhibitors useful for the treatment of disease states mediated by kinase, especially PLK4, in particular such compounds that are useful in the treatment of pathological processes which involve an aberrant cellular proliferation, such as tumor growth, rheumatoid arthritis, restenosis and atherosclerosis.
摘要翻译：本发明涉及式（Ia）或（Ib）的化合物，N-氧化物形式，药学上可接受的加成盐，季胺，立体异构体，互变异构体，外消旋学，代谢物，前药，水合物或溶剂化物，其中Y1，，n，R1; X1; X2; R2; X3; X4; R3; 和R4具有权利要求中限定的含义。本发明还涉及制备所述化合物的方法，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激酶，特别是PLK4介导的疾病状态的激酶抑制剂的化合物，特别是可用于治疗涉及异常细胞增殖的病理过程的化合物，例如肿瘤生长，类风湿关节炎，再狭窄和动脉粥样硬化。

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