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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

US20080039472A1 Inhibitors of the Interaction Between Mdm2 and P53 有权
标题翻译： Mdm2和P53之间相互作用的抑制剂
公开(公告)号：US20080039472A1
公开(公告)日：2008-02-14
申请号：US11575552
申请日：2005-09-16
申请人： Jean Lacrampe , Christophe Meyer , Yannick Ligny , Imre Csoka , Luc Van Hijfte , Janine Arts , Bruno Schoentjes , Camille Wermuth , Bruno Giethlen , Jean-Marie Contreras , Muriel Joubert
发明人： Jean Lacrampe , Christophe Meyer , Yannick Ligny , Imre Csoka , Luc Van Hijfte , Janine Arts , Bruno Schoentjes , Camille Wermuth , Bruno Giethlen , Jean-Marie Contreras , Muriel Joubert
IPC分类号： A61K31/47 , A61K31/44 , A61K31/443 , A61K31/497 , A61P35/00 , C07D215/38 , C07D401/12 , C07D403/12 , C07D487/04 , C07D413/04 , C07D401/14 , C07D221/04 , A61P43/00 , A61K31/519 , A61K31/496 , A61K31/4439
CPC分类号： C07D403/12 , C07D401/12 , C07D401/14 , C07D413/14 , C07D471/04 , C07D487/04
摘要： The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, s, t, R1, R2, R3, R4, R5, R6, R7, X, Y, Q and Z have defined meanings.
摘要翻译：本发明提供式（I）化合物，其作为p53-MDM2相互作用抑制剂的用途以及包含所述式（I）化合物的药物组合物，其中n，m，p，s，t， 1，R 2，R 3，R 4，R 5，R 5， 6，R 7，X，Y，Q和Z具有定义的含义。

3. 发明授权

US06498158B1 Il-5 inhibiting 6-azauracil derivatives 失效
标题翻译： Il-5抑制6-氮尿嘧啶衍生物
公开(公告)号：US06498158B1
公开(公告)日：2002-12-24
申请号：US09856626
申请日：2001-05-22
申请人： Jean Fernand Armand Lacrampe , Yannick Ligny , Eddy Jean Edgard Freyne , Frederik Dirk Deroose
发明人： Jean Fernand Armand Lacrampe , Yannick Ligny , Eddy Jean Edgard Freyne , Frederik Dirk Deroose
IPC分类号： C07D253075
CPC分类号： C07D253/075 , C07D405/10 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14
摘要： The present invention is concerned with the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p is 0 to 3; q is 0 to 4; —A—B— represents —(CH2)r—, —(CH2)t—O—, —(CH2)t—S(═O)u— or —(CH2)t—NR3—; r is 2 to 4; t is 1 to 3; u is 0 to 2; X1 is O, S, NR3 or a direct bond; R1 and R4 are C1-6alkyl, halo, polyhaloC1-6alkyl, hydroxy, mercapto, C1-6alkyloxy, C1-6alkylthio, C1-6alkylcarbonyloxy, aryl, cyano, nitro, Het3, R6, NR7R8 or substituted C1-4alkyl; R2 is aryl, Het1, C3-7cycloalkyl, cyano, optionally substituted C1-6alkyl, —C(═Q)—X2—R15; R3 is hydrogen or C1-4alkyl; R15 is hydrogen, optionally substituted C1-6alkyl, C3-7cycloalkyl, aryl; where X2 is a direct bond, R15 may also be halo or Het1; where X2 is NR5, R15 may also be hydroxy; where X2 is C(═O)—NH—NH or NH—NH—C(═O), R15 may be replaced by R11; Q is O, S or NR3; X2 is O, S, NR5, C(═O)—NH—NH, NH—NH—C(═O) or a direct bond; R5 is hydrogen, C1-6alkyl, C1-6alkyloxy or arylC1-6alkyl; R6 is a sulfonyl or sulfinyl derivative; R7 and R8 are independently hydrogen, optionally substituted C1-4alkyl, aryl, a carbonyl containing moiety, C3-7cycloalkyl, —Y-C1-4alkanediyl-C(═O)—O—R14, Het3 and R6; R11 is hydroxy, mercapto, cyano, nitro, halo, trihalomethyl, C1-4alkyloxy, formyl, trihaloC1-4alkylsulfonyloxy, R6, NR7R8, C(═O)NR7R8, C1-4alkanediyl-C(═O)—O—R14, —C(═O)—O—R14, —Y-C1-4alkanediyl-C(═0)—O—R14, aryl, aryloxy, arylcarbonyl, C3-7cycloalkyl, C3-7cycloalkyloxy, phthalimide-2-yl, Het3, Het4 and C(═O)Het3; aryl is optionally substituted phenyl; Het1, Het2, Het3 and Het4 are optionally substituted heterocycles; to processes for their preparation and compositions comprising them. It further relates to their use as a medicine.
摘要翻译：本发明涉及配制N-氧化物的化合物，其药学上可接受的加成盐和立体化学异构形式，其中p为0-3; q为0〜4; -A-B-表示 - （CH 2）r - ， - （CH 2）t -O-， - （CH 2）t -S（= O）u - 或 - （CH 2）t -NR 3 - ; r为2〜4; t为1〜3; 你是0到2; X1是O，S，NR3或直接键; R 1和R 4是C 1-6烷基，卤素，多卤代C 1-6烷基，羟基，巯基，C 1-6烷氧基，C 1-6烷硫基，C 1-6烷基羰氧基，芳基，氰基，硝基，Het 3，R 6，NR 7 R 8或取代的C 1-4烷基; R 2是芳基，Het 1，C 3-7环烷基，氰基，任选取代的C 1-6烷基，-C（= Q）-X 2 -R 15; R3是氢或C1-4烷基; R 15是氢，任选取代的C 1-6烷基，C 3-7环烷基，芳基; 其中X2是直接键，R15也可以是卤素或Het1; 其中X2是NR5，R15也可以是羟基; 其中X 2是C（= O）-NH-NH或NH-NH-C（= O），R 15可以被R 11取代; Q是O，S或NR 3; X2是O，S，NR5，C（= O）-NH-NH，NH-NH-C（= O）或直接键; R5是氢，C1-6烷基，C1-6烷氧基或芳基C1-6烷基; R6是磺酰基或亚磺酰基衍生物; R 7和R 8独立地为氢，任选取代的C 1-4烷基，芳基，含羰基部分，C 3-7环烷基，-Y-C 1-4烷二基-C（= O）-O-R 14，Het 3

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