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11. 发明申请

US20080207609A1 Pharmaceutical compounds 有权
标题翻译：药物化合物
公开(公告)号：US20080207609A1
公开(公告)日：2008-08-28
申请号：US11893625
申请日：2007-08-16
申请人： Stephen J. Shuttleworth , Adrian J. Folkes , Irina S. Chuckowree , Nan Chi Wan , Timothy C. Hancox , Stewart J. Baker , Sukhjit Sohal , Mohammed A. Latif
发明人： Stephen J. Shuttleworth , Adrian J. Folkes , Irina S. Chuckowree , Nan Chi Wan , Timothy C. Hancox , Stewart J. Baker , Sukhjit Sohal , Mohammed A. Latif
IPC分类号： A61K31/5377 , C07D413/14 , A61P37/00 , A61P9/00 , A61P35/00
CPC分类号： C07D495/04
摘要： Fused pyrimidines of formula (I): wherein R1-R3, A and n have any of the values described in the specification; and pharmaceutically acceptable salts thereof; have activity as inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behavior associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.
摘要翻译：式（I）的稠合嘧啶：其中R 1 -R 3，A和n具有说明书中描述的任何值; 及其药学上可接受的盐; 具有作为PI3K抑制剂的活性，因此可用于治疗与PI3激酶例如癌症，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌失调和神经系统疾病相关的异常细胞生长，功能或行为引起的疾病和障碍疾病还描述了合成化合物的方法。

12. 发明申请

US20120035208A1 PYRAZOLOPYRIDINE PI3K INHIBITOR COMPOUNDS AND METHODS OF USE 有权
标题翻译：吡唑并吡啶PI3K抑制剂化合物及其使用方法
公开(公告)号：US20120035208A1
公开(公告)日：2012-02-09
申请号：US13129091
申请日：2009-11-19
申请人： Jennafer Dotson , Timothy Heffron , Alan G. Olivero , Daniel P. Sutherlin , Steven Staben , Shumei Wang , Bing-Yan Zhu , Irina S. Chuckowree , Adrian J. Folkes , Nan Chi Wan
发明人： Jennafer Dotson , Timothy Heffron , Alan G. Olivero , Daniel P. Sutherlin , Steven Staben , Shumei Wang , Bing-Yan Zhu , Irina S. Chuckowree , Adrian J. Folkes , Nan Chi Wan
IPC分类号： A61K31/437 , C12N9/99 , A61P35/00 , A61P35/02 , A61P29/00 , A61P3/10 , A61P25/00 , A61P9/00 , A61P1/16 , A61P31/12 , A61P7/00 , C07D471/04 , A61P37/02
CPC分类号： C07D471/04
摘要： Compounds of Formula (I), and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer or inflammation mediated by lipid kinases. Methods of using compounds of Formula (I) for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译：式（I）化合物，并且包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和其药学上可接受的盐可用于抑制脂质激酶，包括p110α和PI3K的其他同种型，并用于治疗疾病如癌症或炎症介导通过脂质激酶。公开了使用式（I）化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理条件中的这种疾病的方法。

13. 发明授权

US08653098B2 Pyrazolopyridine PI3K inhibitor compounds and methods of use 有权
标题翻译：吡唑并吡啶PI3K抑制剂化合物及其使用方法
公开(公告)号：US08653098B2
公开(公告)日：2014-02-18
申请号：US13129091
申请日：2009-11-19
申请人： Jennafer Dotson , Timothy Heffron , Alan G. Olivero , Daniel P. Sutherlin , Steven Staben , Shumei Wang , Bing-Yan Zhu , Irina S. Chuckowree , Adrian J. Folkes , Nan Chi Wan
发明人： Jennafer Dotson , Timothy Heffron , Alan G. Olivero , Daniel P. Sutherlin , Steven Staben , Shumei Wang , Bing-Yan Zhu , Irina S. Chuckowree , Adrian J. Folkes , Nan Chi Wan
IPC分类号： A61K31/44 , C07D491/02 , C07D498/02
CPC分类号： C07D471/04
摘要： Compounds of Formula (I), and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer or inflammation mediated by lipid kinases. Methods of using compounds of Formula (I) for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译：式（I）化合物，并且包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和其药学上可接受的盐可用于抑制脂质激酶，包括p110α和PI3K的其他同种型，并用于治疗疾病如癌症或炎症介导通过脂质激酶。公开了使用式（I）化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理条件中的这种疾病的方法。

14. 发明授权

US08153639B2 Substituted thieno- and furano- fused pyrimidines as PI3K inhibitors 有权
标题翻译：取代的噻吩并呋喃并呋喃并嘧啶作为PI3K抑制剂
公开(公告)号：US08153639B2
公开(公告)日：2012-04-10
申请号：US12299600
申请日：2007-05-04
申请人： Irina S. Chuckowree , Adrian J. Folkes , Paul Goldsmith , Timothy C. Hancox , Stephen J. Shuttleworth
发明人： Irina S. Chuckowree , Adrian J. Folkes , Paul Goldsmith , Timothy C. Hancox , Stephen J. Shuttleworth
IPC分类号： C07D495/04 , A61K31/519 , A61P35/00
CPC分类号： C07D493/04 , C07D495/04
摘要： Fused pyrimidines of formula (I): wherein A, n, R1, R2, and R3 have any of the values defined herein and the pharmaceutically acceptable salts thereof have activity as inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behavior associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.
摘要翻译：式（I）的稠合嘧啶：其中A，n，R 1，R 2和R 3具有本文定义的任何值，并且其药学上可接受的盐具有作为PI3K抑制剂的活性，因此可用于治疗由与PI3激酶相关的异常细胞生长，功能或行为，如癌症，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌失调和神经障碍。还描述了合成化合物的方法。

15. 发明申请

US20090209559A1 PHARMACEUTICAL COMPOUNDS 有权
标题翻译：药物化合物
公开(公告)号：US20090209559A1
公开(公告)日：2009-08-20
申请号：US12299600
申请日：2007-05-04
申请人： Irina S. Chuckowree , Adrian J. Folkes , Paul Goldsmith , Timothy C. Hancox , Stephen J. Shuttleworth
发明人： Irina S. Chuckowree , Adrian J. Folkes , Paul Goldsmith , Timothy C. Hancox , Stephen J. Shuttleworth
IPC分类号： A61K31/519 , C07D495/02 , A61P35/00 , A61P37/00 , A61P9/00 , A61P31/12 , A61P29/00 , A61P5/00 , A61P25/00
CPC分类号： C07D493/04 , C07D495/04
摘要： Fused pyrimidines of formula (I): wherein A, n, R1, R2, and R3 have any of the values defined herein and the pharmaceutically acceptable salts thereof have activity as inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behavior associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.
摘要翻译：式（I）的稠合嘧啶：其中A，n，R 1，R 2和R 3具有本文定义的任何值，并且其药学上可接受的盐具有作为PI3K抑制剂的活性，因此可用于治疗由与PI3激酶相关的异常细胞生长，功能或行为，如癌症，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌失调和神经障碍。还描述了合成化合物的方法。

16. 发明授权

US06197811B1 Cytokine production inhibitors 失效
标题翻译：细胞因子生成抑制剂
公开(公告)号：US06197811B1
公开(公告)日：2001-03-06
申请号：US09292961
申请日：1999-04-16
申请人： Martin A. Hayes , David J. Hardick , Jenny S. Tang , Hamish Ryder , Adrian J. Folkes , Toshio Tatsuoka , Masashi Matsui
发明人： Martin A. Hayes , David J. Hardick , Jenny S. Tang , Hamish Ryder , Adrian J. Folkes , Toshio Tatsuoka , Masashi Matsui
IPC分类号： A61K3135
CPC分类号： C07D309/32
摘要： A compound selected from the group consisting of a 5,6-dihydro-&agr;-pyrone of formula (I): wherein bond a is oriented either or ; X is O or NH; R1 is selected from the group consisting of: a group R3(O)C— wherein R3 is selected from the group consisting of: (i) a group of formula R4—CH═CH— wherein R4 is C1-C20 alkyl, C2-C20 alkenyl, an aryl group, or a 5- or 6-membered unsaturated heterocyclic ring containing one or two O, N or S atoms, (ii) C2-C20 alkyl; and (iii) an aryl group or a substituent which is a fused ring system of formula (1) or (2): wherein each of R′ and R″, which are the same or different and may occupy any position on ring a or ring b of said fused ring system, is H or C1-C6 alkyl; a group ArCH2— wherein Ar is an aryl group; and a group R5O—CH2— wherein R5 is C1-C6 alkyl optionally interrupted by one or two O atoms; and R2 is CH3 or, when R1 is a group of formula (A) as defined below, R2 is R6OOC— or R6NOC— wherein R6 is C1-C6 alkyl; and the pharmaceutically and veterinarily acceptable salts and esters thereof; with the exception of compounds wherein bond a is oriented , X is O and R1 is a group of formula (A): wherein R11 and R21 are H when R2 in formula (I) is CO2H or CH3, or one of R11 and R21 is H and the other is OH when R2 in formula (I) is CO2H.
摘要翻译：选自式（I）的5,6-二氢-α-吡喃酮的化合物：其中键合a定向为或; X是O或NH; R1选自：组R3 （O）C-，其中R 3选自：（i）式R 4 -CH = CH-的基团，其中R 4是C 1 -C 20烷基，C 2 -C 20烯基，芳基或5-或含有一个或两个O，N或S原子的6元不饱和杂环，（ii）C 2 -C 20烷基;和（iii）作为式（1）或（2）的稠环体系的芳基或取代基，：其中R'和R“各自相同或不同并且可以占据所述稠环系统的环a或环b上的任何位置是H或C 1 -C 6烷基;基团ArCH 2 - 其中Ar是芳基; 和R5O-CH2-基团，其中R5是任选被一个或两个O原子中断的C 1 -C 6烷基; 并且R 2是CH 3，或者当R 1是如下定义的式（A）的基团时，R 2是R 60 OC-或R 6 NOC - ，其中R 6是C 1 -C 6烷基;和其药学和兽医学上可接受的盐和酯; 除了其中键a取向的化合物的化合物除外，X是O，R1是式（A）的基团：当式（I）中的R 2为CO 2 H或CH 3时，R 11和R 21为H，或者R 11和R 21中的一个为H，另一个为OH，式（I）中的R 2为CO 2 H.

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