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1. 发明申请

US20120238541A1 PHARMACEUTICAL COMPOUNDS 失效
标题翻译：药物化合物
公开(公告)号：US20120238541A1
公开(公告)日：2012-09-20
申请号：US13496287
申请日：2010-09-17
申请人： Mark Peter Bell , Timothy Harrison , Sumita Bhattacharyya , James Samuel Shane Rountree , Frank Burkamp , Stephen Price , Calum MacLeod , Richard Leonard Elliott , Phillip Smith , Toby Jonathan Blench , Colin Roderick O'Dowd , Lixin Zhang , Graham Peter Trevitt , Hazel Joan Dyke
发明人： Mark Peter Bell , Timothy Harrison , Sumita Bhattacharyya , James Samuel Shane Rountree , Frank Burkamp , Stephen Price , Calum MacLeod , Richard Leonard Elliott , Phillip Smith , Toby Jonathan Blench , Colin Roderick O'Dowd , Lixin Zhang , Graham Peter Trevitt , Hazel Joan Dyke
IPC分类号： A61K31/4188 , A61K31/352 , C07D405/10 , A61K31/4155 , A61K31/496 , A61K31/4178 , C07D491/052 , A61K31/436 , A61K31/4162 , C07D491/147 , A61K31/437 , C07D413/10 , A61K31/5377 , A61K31/422 , A61K31/4192 , C07D498/04 , A61K31/5383 , A61K31/397 , C07C225/20 , A61P35/00 , C07D493/04 , A61K31/357 , C07D311/26
CPC分类号： C07D311/26 , C07D407/04 , C07D491/04
摘要： The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.
摘要翻译：本发明涉及作为丝氨酸 - 苏氨酸激酶AKT抑制剂的特定活性的一系列化合物。还提供了包含其的药物组合物以及用于治疗癌症的方法。

2. 发明授权

US08546376B2 Pharmaceutical compounds 失效
标题翻译：药物化合物
公开(公告)号：US08546376B2
公开(公告)日：2013-10-01
申请号：US13496287
申请日：2010-09-17
申请人： Mark Peter Bell , Timothy Harrison , Sumita Bhattacharyya , James Samuel Shane Rountree , Frank Burkamp , Stephen Price , Calum MacLeod , Richard Leonard Elliott , Phillip Smith , Toby Jonathan Blench , Colin Roderick O'Dowd , Lixin Zhang , Graham Peter Trevitt , Hazel Joan Dyke
发明人： Mark Peter Bell , Timothy Harrison , Sumita Bhattacharyya , James Samuel Shane Rountree , Frank Burkamp , Stephen Price , Calum MacLeod , Richard Leonard Elliott , Phillip Smith , Toby Jonathan Blench , Colin Roderick O'Dowd , Lixin Zhang , Graham Peter Trevitt , Hazel Joan Dyke
IPC分类号： A61K31/4188 , A61K31/352 , A61K31/357 , A61K31/397 , A61K31/4155 , A61K31/4162 , A61K31/4178 , A61K31/4192 , A61K31/422 , A61K31/436 , A61K31/437 , A61K31/496 , A61K31/5377 , A61K31/5383 , A61P35/00 , C07C225/20 , C07D311/26 , C07D405/10 , C07D413/10 , C07D491/052 , C07D491/147 , C07D493/04 , C07D498/04
CPC分类号： C07D311/26 , C07D407/04 , C07D491/04
摘要： The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.
摘要翻译：本发明涉及作为丝氨酸 - 苏氨酸激酶AKT抑制剂的特定活性的一系列化合物。还提供了包含其的药物组合物以及用于治疗癌症的方法。

3. 发明申请

US20160016948A1 AMINOPYRIMIDINE COMPOUNDS AS INHIBITORS OF T790M CONTAINING EGFR MUTANTS 有权
标题翻译：作为含有EGFR突变体的T790M的抑制剂的氨基嘧啶化合物
公开(公告)号：US20160016948A1
公开(公告)日：2016-01-21
申请号：US14745159
申请日：2015-06-19
申请人： Marian C. Bryan , Bryan Chan , Emily Hanan , Timothy Heffron , Hans Purkey , Richard Leonard Elliott , Robert Heald , Jamie Knight , Michael Lainchbury , Eileen M. Seward
发明人： Marian C. Bryan , Bryan Chan , Emily Hanan , Timothy Heffron , Hans Purkey , Richard Leonard Elliott , Robert Heald , Jamie Knight , Michael Lainchbury , Eileen M. Seward
IPC分类号： C07D471/04 , A61K45/06 , C07D498/10 , A61K31/5355 , A61K31/541 , C07D498/08 , A61K31/538 , C07D491/107 , A61K31/506 , A61K31/5377
CPC分类号： C07D471/04 , A61K31/506 , A61K31/5355 , A61K31/5377 , A61K31/538 , A61K31/541 , A61K45/06 , C07D491/107 , C07D498/08 , C07D498/10 , C07D519/00
摘要： This invention relates to novel compounds which are inhibitors of T790M containing EGFR mutants, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the prevention or treatment of cancer.
摘要翻译：本发明涉及作为含有EGFR突变体的T790M抑制剂的新化合物，含有它们的药物组合物，其制备方法及其在治疗中用于预防或治疗癌症的新化合物。

4. 发明授权

US07169924B2 Pyrimidinone derivatives and their use in the treatment of atherosclerosis 失效
公开(公告)号：US07169924B2
公开(公告)日：2007-01-30
申请号：US10398977
申请日：2001-10-05
申请人： Richard Leonard Elliott , Deirdre Mary Bernadette Hickey , Robert John Ife , Colin Andrew Leach , Ivan Leo Pinto , Stephen Allan Smith
发明人： Richard Leonard Elliott , Deirdre Mary Bernadette Hickey , Robert John Ife , Colin Andrew Leach , Ivan Leo Pinto , Stephen Allan Smith
IPC分类号： C07D239/70 , A61K31/517 , A61P9/01
CPC分类号： C07D239/36 , C07D239/70 , C07D239/91 , C07D401/12 , C07D403/12 , C07D409/14 , C07D471/04 , C07D487/04 , C07D495/04
摘要： Compound of formula (I): are disclosed in which: R1 is an aryl group, optionally substituted by 1, 2, 3 or 4 substituents which may be the same or different selected from C(1-6)alkyl, C(1-6)alkoxy, C(1-6)alkylthio, hydroxy, halogen, CN, and mono to perfluoro-C(1-4)alkyl; R2 is halogen, C(1-3)alkyl, C(1-3)alkoxy, hydroxyC(1-3)alkyl, C(1-3)alkylthio, C(1-3)alkylsulphinyl, aminoC(1-3)alkyl, mono- or di-C(1-3)alkylaminoC(1-3)alkyl, C(1-3)alkylcarbonylaminoC(1-3)alkyl, C(1-3)alkoxyC(1-3)alkylcarbonylaminoC(1-3)alkyl, C(1-3)alkylsulphonylaminoC(1-3)alkyl, C(1-3)alkylcarboxy, C(1-3)alkylcarboxyC(1-3)alkyl, and R3 is hydrogen, halogen, C(1-3)alkyl, or hydroxyC(1-3)alkcyl; or R2 and R3 together with the pyrimidone ring carbon atoms to which they are attached form a fused 5-or 6-membered carbocyclic ring; or R2 and R3 together with the pyrimidone ring carbon atoms to which they are attached form a fused benzo or heteroaryl ring ring optionally substituted by 1, 2, 3 or 4 substituents which may be the same or different selected from halogen, C(1-4)alkyl, cyano, C(1-6)alkoxy, C(1-6)alkylthio or mono to perfluoro-C(1-4)alkyl; R4 is hydrogen, C(1-6)alkyl which may be unsubstituted or substituted by 1, 2 or 3 substituents selected from hydroxy, halogen, OR7, COR7, carboxy, COOR7, CONR9R10, NR9R10, NR7COR8, mono- or di-(hydroxyC(1-6)alkyl) amino and N-hydroxyC(1-6)alkyl-N—C(1-6)allkylamino; or R4 is Het-C(0-4)alkyl in which Het is a 5- to 7- membered heterocyclyl ring comprising N and optionally O or S, and in which N may be substituted by COR7, COOR7, CONR9R10, or C(1-6)alkyl optionally substituted by 1, 2 or 3 substituents selected from hydroxy, halogen, OR7, COR7, carboxy, COOR7, CONR9R10 or NR9R10, for instance, piperidinyl-4-yl, pyrrolidin-3-yl; R5 is an aryl or a heteroaryl ring optionally substituted by 1, 2, 3 or 4 substituents which may be the same or different selectd from C(1-6)alkyl, C(1-6)alkoxy, C(1-6)alkylthio, arylC(1-6)alkoxy, hydroxy, halogen, CN, COR7, carboxy, COOR7, NR7COR8, CONR9R10, SO2NR9R10, NR7SO2R8, NR9R10, mono to perfluoro-C(1-4)alkyl and mono to perfluoro-C(1-4)alkoxy; R6 is an aryl or a heteroaryl ring which is further optionally substituted by 1, 2, 3 or 4 substituents which may be the same or different selected from C(1-18)alkyl, C(1-18)alkoxy, C(1-6)alkylthio, C(1-6)alkylsulfonyl, arylC(1-6)alkoxy, hydroxy, halogen, CN, COR7, carboxy, COOR7, CONR9R10, NR7COR8, SO2NR9R10, NR7SO2R8, NR9R10, mono to perfluoro-C(1-4)alkyl and mono to perfluoro-C(1-4)alkoxy, or C(5-10)alkyl; These compound are useful for treating diseases associated with abnormal activity of the phospholipase A2 enzyme, for example athereosclosis.

5. 发明授权

US5665717A Carbacephalosporin compound, their preparation and use 失效
标题翻译：碳青霉素化合物，其制备和用途
公开(公告)号：US5665717A
公开(公告)日：1997-09-09
申请号：US522411
申请日：1996-01-18
申请人： Richard Leonard Elliott , Neville Hubert Nicholson , Andrew Kenneth Takle
发明人： Richard Leonard Elliott , Neville Hubert Nicholson , Andrew Kenneth Takle
IPC分类号： A61K31/435 , A61P31/04 , C07D463/00 , A61K31/395 , C07D221/06
CPC分类号： C07D463/06 , C07D463/18 , Y02P20/55
摘要： Carbacephalosporin compounds of formula (I), ##STR1## salts thereof, processes for their synthesis and uses thereof, wherein: R.sup.1 is hydrogen, methoxy or formamido; R.sup.2 is an acyl group; CO.sub.2 R.sup.3 is a carboxy group or a carboxylate anion, or R.sup.3 is a carboxy protecting group or a pharmaceutically acceptable salt-forming group or in vivo hydrolysable ester group; R.sup.4, R.sup.5, R.sup.6 and R.sup.7 represent hydrogen or a substituent; R.sup.4 and R.sup.7 may be replaced by a chemical bond between the two carbon atoms shown; R.sup.5 and R.sup.6 may be linked together into a cyclic system. The compounds (I) have antibacterial properties.
摘要翻译： PCT No.PCT / EP94 / 00811 Sec。 371日期：1996年1月18日 102（e）日期1996年1月18日PCT 1994年3月10日PCT公布。公开号WO94 / 21633 1994年9月29日，具有式（I）的乙酰菌素化合物，其化合物及其用途，其中：R1是氢，甲氧基或甲酰氨基; R2是酰基; CO 2 R 3是羧基或羧酸根阴离子，或R3是羧基保护基或药学上可接受的成盐基团或体内可水解的酯基; R4，R5，R6和R7表示氢或取代基; R4和R7可以被所示的两个碳原子之间的化学键取代; R5和R6可以连接在一起成为循环系统。化合物（I）具有抗菌性。

6. 发明申请

US20100311740A1 IMIDAZOPYRIDINE DERIVATIVES AS ACID PUMP ANTAGONISTS 审中-公开
标题翻译：咪唑吡啶衍生物作为酸性尿素拮抗剂
公开(公告)号：US20100311740A1
公开(公告)日：2010-12-09
申请号：US11993084
申请日：2006-06-28
申请人： Mark James Bamford , Richard Leonard Elliott , Gerard Martin Paul Giblin , Antoinette Naylor , Terence Aaron Chal , Andrew Kenneth Takle , Jason Witherington
发明人： Mark James Bamford , Richard Leonard Elliott , Gerard Martin Paul Giblin , Antoinette Naylor , Terence Aaron Chal , Andrew Kenneth Takle , Jason Witherington
IPC分类号： A61K31/5377 , C07D471/04 , A61K31/437 , A61P1/04 , A61K31/496
CPC分类号： C07D471/04
摘要： This invention relates to newly identified imidazopyridine compounds of formula (I), to the use of such compounds in treating GERD and the like.
摘要翻译：本发明涉及新发现的式（I）咪唑并吡啶化合物，涉及这些化合物在治疗GERD等中的应用。

7. 发明授权

US06762034B1 Resorufin derivatives as substrates for CYP3A4 失效
标题翻译： Resorufin衍生物作为CYP3A4的底物
公开(公告)号：US06762034B1
公开(公告)日：2004-07-13
申请号：US09890009
申请日：2002-01-02
申请人： Jacqueline Carol Bloomer , Richard Leonard Elliott , Colin Andrew Leach
发明人： Jacqueline Carol Bloomer , Richard Leonard Elliott , Colin Andrew Leach
IPC分类号： C12Q126
CPC分类号： C12Q1/26 , C07D265/38 , G01N2333/795 , G01N2333/80 , G01N2333/90245
摘要： Resorufin derivative as a substance for cytochrome P450 enzyme.
摘要翻译： Resorufin衍生物作为细胞色素P450酶的物质。

8. 发明授权

US06756209B1 7-Alkoxycoumarins as CYP2C9 substrates and activity assay 失效
标题翻译： 7-烷氧基香豆素作为CYP2C9底物和活性测定
公开(公告)号：US06756209B1
公开(公告)日：2004-06-29
申请号：US09806877
申请日：2001-06-11
申请人： Ramesh B. Bambal , Richard Leonard Elliott
发明人： Ramesh B. Bambal , Richard Leonard Elliott
IPC分类号： C12Q134
CPC分类号： C07D311/16 , C12Q1/26
摘要： Coumarin derivatives as substrates for cytochrome P450 enzyme.
摘要翻译：香豆素衍生物作为细胞色素P450酶的底物。

9. 发明申请

US20080255358A1 Derivatives of Imidazo [1,2-A] Pyridine Useful as Medicaments For Treating Gastrointestinal Diseases 审中-公开
标题翻译：咪唑并[1,2-A]吡啶的衍生物可用作治疗胃肠道疾病的药物
公开(公告)号：US20080255358A1
公开(公告)日：2008-10-16
申请号：US11909114
申请日：2006-03-22
申请人： Mark James Bamford , Emmanuel Hubert Demont , Richard Leonard Elliott , Gerard Martin Paul Giblin , Antoinette Naylor , Terence Aaron Panchal , Jason Witherington
发明人： Mark James Bamford , Emmanuel Hubert Demont , Richard Leonard Elliott , Gerard Martin Paul Giblin , Antoinette Naylor , Terence Aaron Panchal , Jason Witherington
IPC分类号： C07D401/14 , C07D471/04 , A61P1/00
CPC分类号： C07D471/04
摘要： Disclosed are imidazopyridine compounds having the formula:
摘要翻译：公开了具有下式的咪唑并吡啶化合物：

10. 发明授权

US07410984B2 Compounds 失效
标题翻译：化合物
公开(公告)号：US07410984B2
公开(公告)日：2008-08-12
申请号：US10524028
申请日：2003-08-08
申请人： Jason Witherington , Richard Leonard Elliott
发明人： Jason Witherington , Richard Leonard Elliott
IPC分类号： C07D211/72 , A61K31/44
CPC分类号： C07D213/64 , C07D211/76 , C07D401/12
摘要： The present invention relates to novel pyridone derivatives capable of inhibiting α4 integrin mediated cell adhesion, processes for their preparation, compositions comprising them and their use in the treatment of diseases capable of being modulated by the inhibition of cell adhesion.
摘要翻译：本发明涉及能够抑制α4H整联蛋白介导的细胞粘附的新型吡啶酮衍生物，其制备方法，包含它们的组合物及其在治疗能够通过抑制细胞调节的疾病中的用途附着力。

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