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1. 发明申请

US20080070914A1 5-Membered Annelated Heterocyclic Pyrimidines As Kinase Inhibitors 有权
标题翻译：作为激酶抑制剂的5-Membined Annelated Heterocyclic Pyrimidines
公开(公告)号：US20080070914A1
公开(公告)日：2008-03-20
申请号：US11813656
申请日：2006-01-09
申请人： Eddy Freyne , Jean Lacrampe , Timothy Perera , Peter Ten Holte , Yannick Ligny , Delphine Lardeau , Tom Lavrijssen
发明人： Eddy Freyne , Jean Lacrampe , Timothy Perera , Peter Ten Holte , Yannick Ligny , Delphine Lardeau , Tom Lavrijssen
IPC分类号： A61K31/497 , A61K31/535 , A61P43/00 , C07D413/00 , C07D473/00
CPC分类号： C07D473/32 , C07D487/04
摘要： This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, Q1, Q2, X1, X2, Y and Z have defined meanings, having cell cycle kinase inhibiting enzymatic activity, their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明包括式（I）的新化合物，其中R 1，R 2，R 3，R 4， >，R 5，R 6，Q 1，Q 2，X 1，...，SUP Y，Z定义含有细胞周期激酶抑制酶活性，其制备方法，含有它们的组合物及其作为药物的用途。

2. 发明申请

US20080039477A1 Pyrazolopyrimidines as Cell Cycle Kinase Inhibitors 有权
标题翻译：吡唑并嘧啶作为细胞周期激酶抑制剂
公开(公告)号：US20080039477A1
公开(公告)日：2008-02-14
申请号：US11813654
申请日：2006-01-09
申请人： Eddy Freyne , Jean Fernand Armand Lacrampe , Timothy Pietro Suren Perera , Peter Ten Holte , Yannick Aime Eddy Ligny , Delphine Yvonne Raymonde Lardeau , Tom Lavrijssen
发明人： Eddy Freyne , Jean Fernand Armand Lacrampe , Timothy Pietro Suren Perera , Peter Ten Holte , Yannick Aime Eddy Ligny , Delphine Yvonne Raymonde Lardeau , Tom Lavrijssen
IPC分类号： A61K31/52 , A61P35/00 , C07D473/00
CPC分类号： C07D487/04
摘要： This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, X1 and X2 have defined meanings, having cell cycle kinase inhibiting enzymatic activity, their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明包括式（I）的新化合物，其中R 1，R 2，R 3，R 4， >，R 5，R 6，X 1和X 2具有定义的含义，具有抑制细胞周期激酶酶活性，它们的制备，含有它们的组合物及其作为药物的用途。

3. 发明授权

US07947694B2 Substituted pyrazolo[3,4-D]pyrimidines as cell cycle kinase inhibitors 有权
标题翻译：取代的吡唑并[3,4-D]嘧啶作为细胞周期激酶抑制剂
公开(公告)号：US07947694B2
公开(公告)日：2011-05-24
申请号：US11813654
申请日：2006-01-09
申请人： Eddy Jean Edgard Freyne , Jean Fernand Armand Lacrampe , Timothy Pietro Suren Perera , Peter Ten Holte , Yannick Aimé Eddy Ligny , Delphine Yvonne Raymonde Lardeau , Tom Lavrijssen
发明人： Eddy Jean Edgard Freyne , Jean Fernand Armand Lacrampe , Timothy Pietro Suren Perera , Peter Ten Holte , Yannick Aimé Eddy Ligny , Delphine Yvonne Raymonde Lardeau , Tom Lavrijssen
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, X1 and X2 have defined meanings, having cell cycle kinase inhibiting enzymatic activity, their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明包括式（I）的新化合物，其中R 1，R 2，R 3，R 4，R 5，R 6，X 1和X 2具有定义的含义，具有抑制细胞周期激酶的酶活性，其制备方法，含有它们的组合物及其作为医学。

4. 发明授权

US07947695B2 5-membered annelated heterocyclic pyrimidines as kinase inhibitors 有权
标题翻译： 5-元环状杂环嘧啶作为激酶抑制剂
公开(公告)号：US07947695B2
公开(公告)日：2011-05-24
申请号：US11813656
申请日：2006-01-09
申请人： Eddy Jean Edgard Freyne , Jean Fernand Armand Lacrampe , Timothy Pietro Suren Perera , Peter Ten Holte , Yannick Aimé Eddy Ligny , Delphine Yvonne Raymonde Lardeau , Tom Lavrijssen
发明人： Eddy Jean Edgard Freyne , Jean Fernand Armand Lacrampe , Timothy Pietro Suren Perera , Peter Ten Holte , Yannick Aimé Eddy Ligny , Delphine Yvonne Raymonde Lardeau , Tom Lavrijssen
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D473/32 , C07D487/04
摘要： This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, Q1, Q2, X1, X2, Y and Z have defined meanings, having cell cycle kinase inhibiting enzymatic activity, their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明包括式（I）的新化合物，其中R1，R2，R3，R4，R5，R6，Q1，Q2，X1，X2，Y和Z具有定义的含义，具有抑制细胞周期激酶的酶活性，含有它们的组合物及其作为药物的用途。

5. 发明授权

US08592441B2 Substituted indolyl alkyl amino derivatives as novel inhibitors of histone deacetylase 有权
公开(公告)号：US08592441B2
公开(公告)日：2013-11-26
申请号：US13447636
申请日：2012-04-16
申请人： Marc Gustaaf Celine Verdonck , Patrick René Angibaud , Bruno Roux , Isabelle Noëlle Constance Pilatte , Peter Ten Holte , Janine Arts , Kristof Van Emelen
发明人： Marc Gustaaf Celine Verdonck , Patrick René Angibaud , Bruno Roux , Isabelle Noëlle Constance Pilatte , Peter Ten Holte , Janine Arts , Kristof Van Emelen
IPC分类号： C07D401/14 , C07D409/14 , A61K31/506
CPC分类号： A61K31/506 , A61K31/454 , A61K31/4545 , C07D401/14 , C07D405/14 , C07D409/14 , C07D491/04 , C07D491/056
摘要： This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, X and Y have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.

6. 发明申请

US20120220615A1 SUBSTITUTED INDOLYL ALKYL AMINO DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE 有权
标题翻译：取代的吲哚基氨基酸衍生物作为HISTONE脱乙酰基酶的新型抑制剂
公开(公告)号：US20120220615A1
公开(公告)日：2012-08-30
申请号：US13447636
申请日：2012-04-16
申请人： Marc Gustaaf Celine Verdonck , Patrick René Angibaud , Bruno Roux , Isabelle Noëlle Constance Pilatte , Peter Ten Holte , Janine Arts , Kristof Van Emelen
发明人： Marc Gustaaf Celine Verdonck , Patrick René Angibaud , Bruno Roux , Isabelle Noëlle Constance Pilatte , Peter Ten Holte , Janine Arts , Kristof Van Emelen
IPC分类号： C07D401/14 , A61P35/04 , C07D491/04 , A61K31/506
CPC分类号： A61K31/506 , A61K31/454 , A61K31/4545 , C07D401/14 , C07D405/14 , C07D409/14 , C07D491/04 , C07D491/056
摘要： This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, X and Y have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明包括式（I）的新化合物，其中R1，R2，R3，X和Y具有定义的含义，具有组蛋白脱乙酰酶抑制酶活性; 其制剂，含有它们的组合物及其作为药物的用途。

7. 发明申请

US20110136841A1 SUBSTITUTED INDOLYL ALKYL AMINO DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE 有权
标题翻译：取代的吲哚基氨基酸衍生物作为HISTONE脱乙酰基酶的新型抑制剂
公开(公告)号：US20110136841A1
公开(公告)日：2011-06-09
申请号：US13027793
申请日：2011-02-15
申请人： Marc Gustaaf Celine Verdonck , Patrick René Angibaud , Bruno Roux , Isabelle Noëlle Constance Pilatee , Peter Ten Holte , Janine Arts , Kristof Van Emelen
发明人： Marc Gustaaf Celine Verdonck , Patrick René Angibaud , Bruno Roux , Isabelle Noëlle Constance Pilatee , Peter Ten Holte , Janine Arts , Kristof Van Emelen
IPC分类号： A61K31/506 , A61P35/00 , A61P35/02
CPC分类号： A61K31/506 , A61K31/454 , A61K31/4545 , C07D401/14 , C07D405/14 , C07D409/14 , C07D491/04 , C07D491/056
摘要： This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, X and Y have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明包括式（I）的新化合物，其中R1，R2，R3，X和Y具有定义的含义，具有组蛋白脱乙酰酶抑制酶活性; 其制剂，含有它们的组合物及其作为药物的用途。

8. 发明申请

US20100152174A1 MACROCYCLIC QUINAZOLE DERIVATIVES AND THEIR USE AS MTKI 审中-公开
标题翻译：大分子喹唑啉衍生物及其作为MTKI的用途
公开(公告)号：US20100152174A1
公开(公告)日：2010-06-17
申请号：US11720693
申请日：2005-12-08
申请人： Eddy Jean Edgard Freyne , Marc Willems , Peter Ten Holte , Alexandra Papanikos , Werner Constant John Embrechts , Pierre Henri Storck , Virginie Sophie Poncelet , Werner Constant Johan Embrechts , Pierre Henri Storck , Virginie Sophie Poncelet
发明人： Eddy Jean Edgard Freyne , Marc Willems , Peter Ten Holte , Alexandra Papanikos , Werner Constant John Embrechts , Pierre Henri Storck , Virginie Sophie Poncelet , Werner Constant Johan Embrechts , Pierre Henri Storck , Virginie Sophie Poncelet
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/517 , C07D498/04 , A61P35/00
CPC分类号： C07D498/06 , C07D498/08
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 NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR13—C1-5alkyl-, —C1-5alkyl-NR14—CO—C1-5alkyl-, —C1-2alkyl-NR21—H2—CO—NH—C1-3alkyl- or —C1-2alkyl-NR23—CO—CR16R17—NH—; X1 represents O or —O—C1-2alkyl-; X2 represents a direct bond, C1-2alkyl, —CO—C1-2alkyl or NR12—C1-2alkyl; R1 represents hydrogen or halo; R2 represents halo, acetylene or Het1; R3 represents hydrogen or cyano; R4 represents Ar4—C1-4alkyloxy-, C1-4alkyloxy- or C1-4alkyloxy substituted with one or where possible two or more substituents selected from Het2, NR7R8, hydroxy and C1-4alkyloxy-C1-4alkyloxy-; R7 represents hydrogen or C1-4alkyl; R8 represents C1-4alkyl substituted with NR25R26 or C1-4alkylsulfonyl; R12 represents hydrogen or C1-4alkyl-; R13 represents Ar6-sulfonyl or C1-6alkyloxycarbonyl optionally substituted with phenyl; R16 and R17 represents hydrogen, C1-4alkyl or R16 and R17 taken together with the carbon atom to which they are attached from a C3-6cycloalkyl; R23 represents C1-4alkyl and R23 represents hydrogen when R16 and R17 taken together with the carbon atom to which they are attached from a C3-6cycloalkyl; R25, R26, R27 and R28 each independently represent hydrogen or C1-4alkylcarbonyl; Het1 represents 2-bora-1,3-dioxolanyl; Het represents piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl or 1,1-dioxothiomorpholinyl wherein said Het2 is optionally substituted with C1-4alkyloxycarbonyl or NR27R28—C1-4alkyl; Ar4 and Ar5 represents phenyl; Ar6 represents phenyl optionally substituted with nitro.
摘要翻译：本发明涉及式（I）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表示NH; Y表示-C3-9烷基，-C1-5烷基-NR13-C1-5烷基，-C1-5烷基-NR14-CO-C1-5烷基，-C1-2烷基-NR21-H2-CO-NH-C1-3烷基 - 或-C1-2烷基-NR23-CO-CR16R17-NH-; X 1表示O或-O-C 1-2烷基 - ; X2表示直接键，C1-2烷基，-CO-C1-2烷基或NR12-C1-2烷基; R1表示氢或卤素; R2代表卤代，乙炔或Het1; R3表示氢或氰基; R 4表示被一个或多个可能的两个或多个选自Het 2，NR 7 R 8，羟基和C 1-4烷氧基-C 1-4烷氧基 - 的取代基取代的Ar 4 -C 1-4烷氧基 - ，C 1-4烷氧基 - 或C 1-4烷氧基。 R7代表氢或C1-4烷基; R8表示被NR25R26或C1-4烷基磺酰基取代的C1-4烷基; R 12表示氢或C 1-4烷基 - ; R 13表示Ar 6 - 磺酰基或任选被苯基取代的C 1-6烷氧基羰基; R 16和R 17表示氢，C 1-4烷基或R 16和R 17与它们与C 3-6环烷基连接的碳原子一起; 当R 16和R 17与C 3-6环烷基连接的碳原子一起时，R 23表示C 1-4烷基，R 23表示氢; R 25，R 26，R 27和R 28各自独立地表示氢或C 1-4烷基羰基; Het1代表2-硼-1,3-二氧戊环基; Het表示哌啶基，哌嗪基，吗啉基，硫代吗啉基或1,1-二氧代硫代吗啉基，其中所述Het2任选被C 1-4烷氧基羰基或NR 27 R 28 -C 1-4烷基取代; Ar 4和Ar 5表示苯基; Ar 6表示任选被硝基取代的苯基。

9. 发明授权

US08268833B2 Inhibitors of histone deacetylase 有权
标题翻译：组蛋白脱乙酰酶抑制剂
公开(公告)号：US08268833B2
公开(公告)日：2012-09-18
申请号：US12372801
申请日：2009-02-18
申请人： Patrick René Angibaud , Isabelle Noëlle Constance Pilatte , Sven Franciscus Anna Van Brandt , Bruno Roux , Peter Ten Holte , Marc Gustaaf Celine Verdonck , Lieven Meerpoel , Alexey Borisovich Dyatkin
发明人： Patrick René Angibaud , Isabelle Noëlle Constance Pilatte , Sven Franciscus Anna Van Brandt , Bruno Roux , Peter Ten Holte , Marc Gustaaf Celine Verdonck , Lieven Meerpoel , Alexey Borisovich Dyatkin
IPC分类号： C07D417/00 , C07D413/00 , C07D295/00 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00 , A61K31/445
CPC分类号： C07D413/12 , A61K31/40 , A61K31/402 , A61K31/435 , A61K31/4427 , A61K31/454 , A61K31/4545 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D207/09 , C07D207/14 , C07D211/14 , C07D211/58 , C07D213/78 , C07D217/02 , C07D217/04 , C07D217/16 , C07D239/42 , C07D295/155 , C07D295/26 , C07D307/68 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/06 , C07D409/12 , C07D409/14 , C07D413/04 , C07D471/04 , C07D471/10 , C07D513/04 , C12Q1/34 , C12Q1/48
摘要： This invention comprises the novel compounds of formula (I) wherein n, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明包括其中n，t，R 1，R 2，R 3，R 4，L，Q，X，Y，Z并具有定义的具有组蛋白脱乙酰酶抑制酶活性的式（I）化合物。其制剂，含有它们的组合物及其作为药物的用途。

10. 发明授权

US08158783B2 MTP inhibiting tetrahydro-naphthalene-1-carboxylic acid derivatives 有权
标题翻译： MTP抑制四氢 - 萘-1-羧酸衍生物
公开(公告)号：US08158783B2
公开(公告)日：2012-04-17
申请号：US12446581
申请日：2007-10-22
申请人： Lieven Meerpoel , Leo Jacobus Jozef Backx , Peter Ten Holte , Guuske Frederike Busscher
发明人： Lieven Meerpoel , Leo Jacobus Jozef Backx , Peter Ten Holte , Guuske Frederike Busscher
IPC分类号： A61K31/55 , A61K31/4439 , A61K31/165 , A61K31/5377 , C07D223/12 , C07D401/12 , C07D413/12 , C07C233/00
CPC分类号： C07C235/60 , C07C233/78 , C07C2602/10 , C07D207/14 , C07D213/82 , C07D223/12 , C07D265/30 , C07D401/12 , C07D413/12
摘要： The present invention is concerned with novel tetrahydro-naphthalene-1-carboxylic acid derivatives having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of atherosclerosis, pancreatitis, obesity, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes. Formula (I).
摘要翻译：本发明涉及具有apoB分泌/ MTP抑制活性和伴随降脂活性的新型四氢萘-1-羧酸衍生物。本发明还涉及制备这些化合物的方法，包含所述化合物的药物组合物以及所述化合物作为治疗动脉粥样硬化，胰腺炎，肥胖症，高甘油三酯血症，高胆固醇血症，高脂血症，糖尿病和II型糖尿病的药物的用途。式（I）。

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