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1. 发明申请

US20050197328A1 Imidazopyridine derivatives as kinase inhibitors 失效
标题翻译：咪唑并吡啶衍生物作为激酶抑制剂
公开(公告)号：US20050197328A1
公开(公告)日：2005-09-08
申请号：US10508760
申请日：2003-03-21
申请人： Nicholas Bailey , Mark Bamford , Haifeng Cui , Stephen Garland , Krista Goodman , Mark Hilfiker , Dennis Lee , Terence Panchal , Robert Stavenger , David Wilson , Jason Witherington
发明人： Nicholas Bailey , Mark Bamford , Haifeng Cui , Stephen Garland , Krista Goodman , Mark Hilfiker , Dennis Lee , Terence Panchal , Robert Stavenger , David Wilson , Jason Witherington
IPC分类号： C07D473/36 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/52 , A61K31/5377 , A61P1/04 , A61P11/06 , A61P19/10 , A61P25/16 , A61P25/28 , A61P29/00 , A61P35/00 , A61P43/00 , C07D471/04 , A61K31/551 , A61K31/498 , A61K31/503 , C07D473/14 , C07D487/02
CPC分类号： C07D471/04
摘要： A compound of the formula and physiologically acceptable salts and or N-oxides thereof wherein, X1 is N or CR3; X2 is N or CR4; X3 is N or CR5; X4 is N or CR6. with the proviso that at least one but not more than two of X1, X2, X3 and X4 represents N. R1 is a 5-, or 6-membered heterocyclic group selected from group a, b, c or d wherein X5 is a group selected from N or CR7 and X6 is a group selected from O, S or NR8; X7 and X8 which may be the same or different is a group selected from N or CR9; X9 is a group selected from O, S or NR8 and X10 is N or CR10; X11, X12 and X13 may be the same or different and selected from a group N or CR11; processes for their preparation, pharmaceutical compositions containing them and their use in medicine.
摘要翻译：下式的化合物及其生理上可接受的盐和/或其N-氧化物，其中X 1是N或CR 3; X 2是N或CR 4; X 3是N或CR 5; X 4是N或CR 6。条件是X 1，X 2，X 3和X 4中的至少一个但不多于两个， SUB>表示N. R 1是选自a，b，c或d的5-或6-元杂环基，其中X 5是选自 N或CR 7和X 6是选自O，S或NR 8的基团; 可以相同或不同的是选自N或CR 9的基团;其中X 1和X 3可以相同或不同。 X 9是选自O，S或NR 8和X 10的基团是N或CR 10; X 11，X 12和X 13可以相同或不同，选自基团N或CR 13， 11 其制备方法，含有它们的药物组合物及其在医药中的用途。

2. 发明申请

US20050101570A1 Preparation of purines 失效
公开(公告)号：US20050101570A1
公开(公告)日：2005-05-12
申请号：US11011352
申请日：2004-12-14
申请人： John Mansfield Dales
发明人： John Mansfield Dales
IPC分类号： C07D473/40 , C07D473/00 , C07D473/32 , A61K31/675 , A61K31/522 , C07D473/14
CPC分类号： C07D473/00
摘要： A process for the preparation of a compound of formula (A) wherein: X is hydrogen or hydroxy, chloro, C1-6 alkoxy or pheny C1-6 alkoxy; and Ra and Rb are hydrogen, or acyl or phosphate derivatives thereof, which process comprises: (i) the preparation of a compound of formula (I) wherein R1 is C1-6 alkyl, or phenyl C1-6 alkyl in which the phenyl group is optionally substituted; R2 is hydrogen, hydroxy, chlorine, C1-6 alkoxy, phenyl C1-6 alkoxy or amino; and R3 is halogen, C1-6 alkylthio, C1-6 alkylsulphonyl, azido, an amino group or a protected amino group, which preparation comprises the reaction of a compound of formula (II) wherein R2 and R3 are as defined for formula (I) with a compound of formula (V) wherein L is a leaving group and R1 is as defined for formula (I), to give a compound of formula (VI), and thereafter converting the intermediate compound of formula (VI) to a compound of formula (I) via decarboxylation, and as necessary or desired, interconverting variables R1, R2 and R3 to further values of R1, R2 and R3; (ii) the conversion of the resulting compound of formula (I) to a compound of formula (A) by converting variable R3, when other than amino, to amino, reducing the ester groups CO2R1 to CH2OH and optionally forming acyl or phosphate derivates thereof, and as necessary or desired converting variable R2 in the compound of formula (I) to variable X in the compound of formula (A); characterized in that R2 is chloro in formula (I).

3. 发明申请

US20050080261A1 Purine inhibitors of cyclin dependent kinase 2 and IkappaB-alpha 失效
标题翻译：细胞周期蛋白依赖性激酶2和IkappaB-α的嘌呤抑制剂
公开(公告)号：US20050080261A1
公开(公告)日：2005-04-14
申请号：US10794828
申请日：2004-03-03
申请人： Robert Lum , Cheri Blum , Richard Mackman , Michael Wick , Steven Schow , Jeffery Zablocki , Prabha Ibrahim
发明人： Robert Lum , Cheri Blum , Richard Mackman , Michael Wick , Steven Schow , Jeffery Zablocki , Prabha Ibrahim
IPC分类号： B60R1/00 , C07D473/16 , C07D473/40 , G08G1/16 , C07D473/10 , C07D473/14
CPC分类号： B60R1/00 , C07D473/16 , C07D473/40 , G08G1/163
摘要： Compounds of the following formula are provided: In the Formula (I), R1 is —X—R1′; in which R1′ is optionally substituted lower alkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted heterocyclyl, and X is —NH—. R2 is lower alkyl optionally substituted with one, two or three groups chosen from hydroxy, lower alkoxy, and halogen. And R3 is —NR4R5; in which R4 is hydrogen and R5 is lower alkyl substituted with amino; or (ii) R4 and R5 are both lower alkyl optionally substituted with one, two or three groups chosen from hydroxy and amino. It is to be understood that R1′ is not cyclohexylmethyl, phenyl, substituted phenyl, benzyl, phenylethyl, or m-hydroxybenzyl. The compounds inhibit CDK-2 activity and are useful for treating disorders characterized by undesirable cell proliferation.
摘要翻译：提供下式的化合物：式（I）中，R 1为-X-R 1'; 其中R 1'为任选取代的低级烷基，任选取代的芳基，任选取代的杂芳基或任选取代的杂环基，X为-NH-。 R2是任选被一个，两个或三个选自羟基，低级烷氧基和卤素的基团取代的低级烷基。并且R 3是-NR 4 R 5; 其中R4是氢，R5是被氨基取代的低级烷基; 或（ii）R 4和R 5均为任选被一个，两个或三个选自羟基和氨基的基团取代的低级烷基。应当理解，R1'不是环己基甲基，苯基，取代的苯基，苄基，苯乙基或间羟基苄基。该化合物抑制CDK-2活性，并且可用于治疗以不期望的细胞增殖为特征的疾病。

4. 发明申请

US20050026938A1 Purine inhibitors of protein kinases, G proteins and polymerases 审中-公开
标题翻译：蛋白激酶，G蛋白和聚合酶的嘌呤抑制剂
公开(公告)号：US20050026938A1
公开(公告)日：2005-02-03
申请号：US10930547
申请日：2004-08-30
申请人： Nathanael Gray , Peter Schultz , Sung-Hou Kim , Laurent Meijer
发明人： Nathanael Gray , Peter Schultz , Sung-Hou Kim , Laurent Meijer
IPC分类号： A61K31/52 , A61P25/28 , A61P35/00 , C07D473/16 , C07D473/14
CPC分类号： A61K31/52 , C07D473/16
摘要： The present invention relates to purine analogs that inhibit, inter alia, protein kinases, G-proteins and polymerases. In addition, the present invention relates to methods of using such purine analogs to inhibit protein kinases, G-proteins, polymerases and other cellular processes and to treat cellular proliferative diseases.
摘要翻译：本发明涉及嘌呤类似物，其特别是抑制蛋白激酶，G蛋白和聚合酶。此外，本发明涉及使用这种嘌呤类似物来抑制蛋白激酶，G蛋白，聚合酶和其它细胞过程以及治疗细胞增殖性疾病的方法。

5. 发明申请

US20050009846A1 2,6,9-Substituted purine derivatives and their use in the treatment of proliferative disorders 失效
标题翻译： 2,6,9-取代的嘌呤衍生物及其在治疗增殖性疾病中的应用
公开(公告)号：US20050009846A1
公开(公告)日：2005-01-13
申请号：US10742237
申请日：2003-12-18
申请人： Peter Fischer , Mike Jarman , Ted McDonald , Bernard Nutley , Florence Raynaud , Stuart Wilson , Paul Workman
发明人： Peter Fischer , Mike Jarman , Ted McDonald , Bernard Nutley , Florence Raynaud , Stuart Wilson , Paul Workman
IPC分类号： A61K31/52 , A61P17/06 , A61P25/28 , A61P31/12 , A61P35/00 , A61P35/02 , A61P43/00 , C07D473/16 , C07D473/14
CPC分类号： C07D473/16
摘要： The present invention relates to compounds of formula I or a pharmaceutically acceptable salt thereof wherein R2 is 2-hydroxymethylpyrrolidin-1-yl, or NHCH(R4)CH(R3)OH, wherein R3 is hydrogen or methyl and R4 is methyl, ethyl or isopropyl; R6 is 3-nitrophenylamino, 3,4-dimethoxybenzylamino, 3-iodobenzyl-amino, pyrid-2-yl-methylamino, pyrid-4-yl-methylamino or indan-5-amino; R9 is isopropyl or cyclopentanyl. In a further aspect, the invention relates to pharmaceutical compositions comprising said compounds, and the use thereof in treating antiproliferative disorders and or viral disorders.
摘要翻译：本发明涉及式I化合物或其药学上可接受的盐，其中R2是2-羟甲基吡咯烷-1-基或NHCH（R4）CH（R3）OH，其中R3是氢或甲基，R4是甲基，乙基或异丙基 R6是3-硝基苯基氨基，3,4-二甲氧基苄基氨基，3-碘苄基 - 氨基，吡啶-2-基 - 甲基氨基，吡啶-4-基 - 甲基氨基或茚满-5-氨基; R9是异丙基或环戊基。在另一方面，本发明涉及包含所述化合物的药物组合物及其在治疗抗增生性疾病和/或病毒性疾病中的用途。

6. 发明申请

US20040204428A1 Derivatives of triazolyl-imidazopyridine and of the triazolylpurines useful as ligandsof the adenosine a2a receptor and their use as medicaments 失效
标题翻译：三唑基 - 咪唑并吡啶的衍生物和可用作腺苷a2a受体的配体的三唑基嘌呤及其作为药物的用途
公开(公告)号：US20040204428A1
公开(公告)日：2004-10-14
申请号：US10484491
申请日：2004-01-22
发明人： Tarzia Giorgio , Giovanni Piersanti , Luca Giorgi
IPC分类号： C07D473/14 , C07D471/02 , A61K031/52
CPC分类号： C07D471/04 , A61K31/198 , A61K31/435 , A61K31/52 , C07D473/34 , A61K2300/00
摘要： 1 Compounds of formula (I) wherein the groups are as defined in the description, said compounds being antagonists of the adenosine A2a receptor and useful as medicaments, in particular for the treatment of Parkinson's disease are disclosed.
摘要翻译：公开了式（I）化合物，其中基团如说明书中所定义，所述化合物是腺苷A2a受体的拮抗剂，可用作药物，特别是用于治疗帕金森病。

7. 发明申请

US20070142402A1 Kinase Inhibitors And Their Uses 有权
标题翻译：激酶抑制剂及其用途
公开(公告)号：US20070142402A1
公开(公告)日：2007-06-21
申请号：US11611568
申请日：2006-12-15
申请人： Pingyu Ding , Ankush Argade , Dane Goff , Rajinder Singh , Esteban Masuda , Vanessa Taylor , Sacha Holland
发明人： Pingyu Ding , Ankush Argade , Dane Goff , Rajinder Singh , Esteban Masuda , Vanessa Taylor , Sacha Holland
IPC分类号： A61K31/519 , A61K31/52 , A61K31/517 , C07D498/02 , C07D487/02 , C07D473/14
CPC分类号： C07D519/00 , A61K31/517 , C07D239/94 , C07D239/95 , C07D471/04 , C07D473/16 , C07D487/04 , C07D495/04 , C07D495/12
摘要： The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and/or prevent diseases associated with inappropriate kinase activity.
摘要翻译：本公开提供了抑制蛋白激酶（例如JAK，Ax1或Syk激酶）的化合物，包含该化合物的组合物和使用该化合物抑制蛋白激酶并治疗和/或预防与不适当激酶活性相关疾病的方法。

8. 发明申请

US20060074095A1 Novel purine derivatives, preparation method and use as medicines 审中-公开
标题翻译：新型嘌呤衍生物，作为药物的制备方法和用途
公开(公告)号：US20060074095A1
公开(公告)日：2006-04-06
申请号：US11285870
申请日：2005-11-23
申请人： Florence Bordon-Pallier , Jean-Luc Haesslein
发明人： Florence Bordon-Pallier , Jean-Luc Haesslein
IPC分类号： A61K31/52 , C07D473/14
CPC分类号： C07D473/16 , C07D473/40
摘要： The use of purine derivatives of formula (I): as cdk kinase inhibitors for the prevention and treatment of fungal infections. Also disclosed are novel methods and intermediates for the production of compounds of formula I, as well as pharmaceutical compositions containing said compounds.
摘要翻译：使用式（I）的嘌呤衍生物：作为用于预防和治疗真菌感染的cdk激酶抑制剂。还公开了用于制备式I化合物的新方法和中间体，以及含有所述化合物的药物组合物。

9. 发明申请

US20050256069A1 IRNA agents with biocleavable tethers 有权
标题翻译：具有生物可清除系绳的IRNA试剂
公开(公告)号：US20050256069A1
公开(公告)日：2005-11-17
申请号：US10985426
申请日：2004-11-09
申请人： Muthiah Manoharan , Kallanthottathil Rajeev
发明人： Muthiah Manoharan , Kallanthottathil Rajeev
IPC分类号： A61K31/70 , A61K48/00 , C07D473/14 , C07H21/02 , C12Q1/68
CPC分类号： C12N15/113 , C12N15/111 , C12N2310/14 , C12N2310/323 , C12N2310/3511 , C12N2320/51
摘要： The invention relates to iRNA agents, which preferably include a monomer in which the ribose moiety has been replaced by a moiety other than ribose that further includes a tether having one or more linking groups, in which at least one of the linking groups is a cleavable linking group. The tether in turn can be connected to a selected moiety, e.g., a ligand, e.g., a targeting or delivery moiety, or a moiety which alters a physical property. The cleavable linking group is one which is sufficiently stable outside the cell such that it allows targeting of a therapeutically beneficial amount of an iRNA agent (e.g., a single stranded or double stranded iRNA agent), coupled by way of the cleavable linking group to a targeting agent—to targets cells, but which upon entry into a target cell is cleaved to release the iRNA agent from the targeting agent. The inclusion of such a monomer can allow for modulation of a property of the iRNA agent into which it is incorporated, e.g., by using the non-ribose moiety as a point to which a ligand or other entity, e.g., a lipophilic moiety. e.g., cholesterol, is is directly, or indirectly, tethered. The invention also relates to methods of making and using such modified iRNA agents.
摘要翻译：本发明涉及iRNA试剂，其优选包括其中核糖部分已被核糖替代的单体，其进一步包括具有一个或多个连接基团的系链，其中至少一个连接基团是可切割的连接组。系链又可以连接到所选择的部分，例如配体，例如靶向或递送部分，或改变物理性质的部分。可切割连接基团是在细胞外部足够稳定的连接基团，使得其允许靶向治疗有益量的iRNA试剂（例如，单链或双链iRNA试剂），其通过可切割连接基团连接至靶向细胞靶向细胞，但是在进入靶细胞时被切割以从靶向剂释放iRNA试剂。包含这样的单体可以允许调节掺入其中的iRNA试剂的性质，例如通过使用非核糖部分作为配体或其它实体例如亲油部分的点。例如胆固醇，是直接的或间接地束缚的。本发明还涉及制备和使用这种修饰的iRNA试剂的方法。

10. 发明申请

US20050080098A1 Crystal and solvate of 2-amino-6-benzyloxypurine and production methods thereof 有权
标题翻译： 2-氨基-6-苄氧基嘌呤的结晶和溶剂合物及其制备方法
公开(公告)号：US20050080098A1
公开(公告)日：2005-04-14
申请号：US10500451
申请日：2003-04-03
申请人： Taketo Hayashi , Takehiko Kawakami , Yoshihiko Iwanaga , Yosuke Watanabe
发明人： Taketo Hayashi , Takehiko Kawakami , Yoshihiko Iwanaga , Yosuke Watanabe
IPC分类号： C07D473/18 , A61K31/522 , C07D473/14
CPC分类号： C07D473/18
摘要： The present invention can provide a solvate, a cubic crystal and a columnar crystal of 2-amino-6-benzyloxypurine by crystallization from (1) a solvent containing at least one kind of solvent selected from the group consisting of alcohol and water, (2) alcohol or (3) a water-containing solvent.
摘要翻译：本发明可以通过从（1）含有选自醇和水中的至少一种溶剂的溶剂（2）得到2-氨基-6-苄氧基嘌呤的溶剂合物，立方晶体和柱状晶体，（2））醇或（3）含水溶剂。

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