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1. 发明申请

US20130116243A1 INHIBITORS OF AKT ACTIVITY 有权
标题翻译： AKT活动的抑制剂
公开(公告)号：US20130116243A1
公开(公告)日：2013-05-09
申请号：US13517219
申请日：2010-12-23
申请人： Lixin Zhang , Graham Peter Trevitt , Hugues Miel , Frank Burkamp , Timothy Harrison , Andrew John Wilkinson , Charles-Henry Fabritius
发明人： Lixin Zhang , Graham Peter Trevitt , Hugues Miel , Frank Burkamp , Timothy Harrison , Andrew John Wilkinson , Charles-Henry Fabritius
IPC分类号： A61K31/47 , C07D215/38 , C07D471/04 , A61K31/4745 , A61K31/5377 , A61P35/00 , A61K31/5383 , C07D498/14 , C07D515/04 , A61K31/542 , A61K31/551 , C07D215/20 , C07D498/04
CPC分类号： C07D498/04 , C07D471/04 , C07D498/14
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

US09221838B2 Inhibitors of AKT activity 有权
标题翻译： AKT活性抑制剂
公开(公告)号：US09221838B2
公开(公告)日：2015-12-29
申请号：US13517219
申请日：2010-12-23
申请人： Lixin Zhang , Graham Peter Trevitt , Hugues Miel , Frank Burkamp , Timothy Harrison , Andrew John Wilkinson , Charles-Henry Fabritius
发明人： Lixin Zhang , Graham Peter Trevitt , Hugues Miel , Frank Burkamp , Timothy Harrison , Andrew John Wilkinson , Charles-Henry Fabritius
IPC分类号： C07D498/04 , C07D498/14 , C07D405/04 , C07D471/04
CPC分类号： C07D498/04 , C07D471/04 , C07D498/14
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

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。

4. 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。

5. 发明申请

US20080300261A1 Arylacetic Acids and Related Compounds for Treatment of Alzheimer's Disease 审中-公开
标题翻译：用于治疗阿尔茨海默氏病的芳乙酸和相关化合物
公开(公告)号：US20080300261A1
公开(公告)日：2008-12-04
申请号：US11658242
申请日：2005-07-19
申请人： Peter Blurton , Frank Burkamp , Ian Churcher , Timothy Harrison , Joseph Neduvelil
发明人： Peter Blurton , Frank Burkamp , Ian Churcher , Timothy Harrison , Joseph Neduvelil
IPC分类号： A61K31/495 , A61K31/192 , A61K31/44 , C07C69/614 , C07D241/04 , C07D213/55
CPC分类号： A61K31/215
摘要： Compounds of formula I are useful in treatment of diseases associated with the deposition of β-amyloid in the brain.
摘要翻译：式I化合物可用于治疗与脑中β-淀粉样蛋白沉积相关的疾病。

6. 发明申请

US20110294766A1 16 Alpha, 17 Alpha-Acetal Glucocorticosteroidal Derivatives and their Use 审中-公开
标题翻译： 16 Alpha，17 Alpha-Acetal糖皮质激素衍生物及其用途
公开(公告)号：US20110294766A1
公开(公告)日：2011-12-01
申请号：US12919160
申请日：2009-02-27
申请人： Frank Burkamp , Tesfaledet Mussie , Paul Andersson , Inga-Britt Andersson , Sumita Bhatacharyya , Håkan Bladh , Svetlana Ivanova , Matti Lepistö
发明人： Frank Burkamp , Tesfaledet Mussie , Paul Andersson , Inga-Britt Andersson , Sumita Bhatacharyya , Håkan Bladh , Svetlana Ivanova , Matti Lepistö
IPC分类号： A61K31/58 , A61P37/08 , A61P11/06 , C07J71/00 , A61P11/00
CPC分类号： C07J71/00
摘要： The present invention provides compounds of formula (I) wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
摘要翻译：本发明提供式（I）化合物，其中R 1，R 2，R 3，R 4，R 5和R 6如说明书中所定义，其制备方法，含有它们的药物组合物及其在治疗中的用途。

7. 发明申请

US20070135423A1 E-fluoro-4-(pyridin-2-yl)-piperidine-1-carboxamide derivatives and related compounds which modulate the function of the vanilloid-1 receptor (vr1) for the treatment of pain 审中-公开
标题翻译： E-fluor-4-（吡啶-2-基） - 哌啶-1-甲酰胺衍生物和调节香草素-1受体（vr1）功能的相关化合物用于治疗疼痛
公开(公告)号：US20070135423A1
公开(公告)日：2007-06-14
申请号：US10577585
申请日：2004-10-27
申请人： Tracy Bayliss , Rebecca Brown , Frank Burkamp , Brian Jones , Joseph Neduvelil
发明人： Tracy Bayliss , Rebecca Brown , Frank Burkamp , Brian Jones , Joseph Neduvelil
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/4545 , A61K31/454 , C07D417/02 , C07D413/02 , C07D401/02
CPC分类号： C07D451/04 , C07D401/04
摘要： Compounds of formula (I): wherein: A1 is phenyl, a six-membered aromatic heterocycle containing one, two or three nitrogen atoms, or a five-membered aromatic heterocycle containing up to four heteroatoms chosen from O, N and S, at most one heteroatom being O or S; A2 is phenyl, a six-membered aromatic heterocycle containing one, two or three nitrogen atoms, or a five-membered aromatic heterocycle containing up to four heteroatoms chosen from O, N and S, at most one heteroatom being O or S; L is a bond or C1-6alkylene; R1 and R2 independently chosen from hydrogen and C1-6alkyl or R1 and R2 may, together, form a methylene or ethylene bridge; W is halogen, C1-6alkyl, haloC1-6alkyl, C1-6alkoxy or haloC1-6alkoxy; X is O, S or NR3 or X, together with the atom to which it is attached, and Y, form an unsaturated five-membered ring together with A2; Y is a bond, C1-4alkylene, NH or NH(CH2)1-3; or a pharmaceutically acceptable salt thereof; other substituents are defined in claim 1; which are useful as therapeutic compounds, particularly in the treatment of pain and other conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VR1).
摘要翻译：式（I）化合物：其中：A 1是苯基，含有一个，两个或三个氮原子的六元芳族杂环，或含有至多四个选自以下的杂原子的五元芳族杂环： O，N和S，最多一个杂原子是O或S; A 2是苯基，含有一个，两个或三个氮原子的六元芳族杂环，或含有至多四个选自O，N和S的杂原子的五元芳族杂环，最多一个杂原子是O或S; L是键或C 1-6 - 亚烷基; R 1和R 2独立地选自氢和C 1-6烷基或R 1和R 2 > 2可以一起形成亚甲基或乙烯桥; W是卤素，C 1-6烷基，卤代C 1-6烷基，C 1-6 - 烷氧基或卤代C 1-6 烷氧基; X是O，S或NR 3或X，连同其所连接的原子，Y与A 2形成不饱和五元环; Y是一个键，C 1-4亚烷基，NH或NH（CH 2 CH 2）1-3。或其药学上可接受的盐; 其它取代基如权利要求1中所定义; 其可用作治疗化合物，特别是用于治疗通过调节香草素-1受体（VR1）的功能而改善的疼痛和其它病症。

8. 发明申请

US20060235021A1 Phenylpyridazine derivatives as ligands for gaba receptors 审中-公开
标题翻译：苯基哒嗪衍生物作为gaba受体的配体
公开(公告)号：US20060235021A1
公开(公告)日：2006-10-19
申请号：US10524173
申请日：2003-08-04
申请人： Wesley Blackaby , Peter Blurton , Frank Burkamp , Stephen Fletcher , Andrew Jennings , Richard Lewis , Angus Macleod , Leslie Street , Steve Thomas , Monique Van Niel , Kevin Wilson
发明人： Wesley Blackaby , Peter Blurton , Frank Burkamp , Stephen Fletcher , Andrew Jennings , Richard Lewis , Angus Macleod , Leslie Street , Steve Thomas , Monique Van Niel , Kevin Wilson
IPC分类号： A61K31/501 , C07D403/02 , A61K31/50
CPC分类号： C07D231/12 , C07D233/56 , C07D237/08 , C07D237/14 , C07D237/20 , C07D237/24 , C07D249/08 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D409/04 , C07D417/14
摘要： A class of 4-phenylpyridazine derivatives of Formula (I), being selective ligands for GABAA receptors, in particular having high affinity for the α2 and/or α3 and or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
摘要翻译：一类式（I）的4-苯基哒嗪衍生物，作为GABA A A受体的选择性配体，特别是对α2和/或α3和α5亚基具有高亲和力，因此具有益处在治疗和/或预防中枢神经系统的不利条件，包括焦虑，抽搐和认知障碍。

9. 发明授权

US08203004B2 Tetrahydroindole derivatives for treatment of alzheimer's disease 失效
标题翻译：用于治疗阿尔茨海默病的四氢吲哚衍生物
公开(公告)号：US08203004B2
公开(公告)日：2012-06-19
申请号：US12084814
申请日：2006-11-03
申请人： Frank Burkamp , Graham David Checksfield , Stephen Robert Fletcher , Stephen John Lewis , Edward Giles Mciver , Paul Joseph Oakley , Martin Richard Teall
发明人： Frank Burkamp , Graham David Checksfield , Stephen Robert Fletcher , Stephen John Lewis , Edward Giles Mciver , Paul Joseph Oakley , Martin Richard Teall
IPC分类号： C07D209/02 , C07D209/52
CPC分类号： C07D209/30 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/42 , C07D209/86 , C07D231/56 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04
摘要： Tetrahydroindole derivatives of formula (I): are disclosed. These compounds modulate the activity of gamma-secretase and hence find use in treatment or prevention of Alzheimer's disease.
摘要翻译：公开了式（I）的四氢吲哚衍生物：这些化合物调节γ-分泌酶的活性，因此可用于治疗或预防阿尔茨海默氏病。

10. 发明申请

US20100256105A1 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：US20100256105A1
公开(公告)日：2010-10-07
申请号：US12749919
申请日：2010-03-30
申请人： Frank Burkamp , Peter Hansen
发明人： Frank Burkamp , Peter Hansen
IPC分类号： A61K31/58 , C07J71/00 , A61P11/06 , A61P11/02
CPC分类号： A61K31/58 , C07J71/0047
摘要： The present invention provides compounds of formula (I) wherein n, p, R1, R2, X1, X2, X3, X4, X5, R3a, R3b, R4, R5 and R6 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
摘要翻译：本发明提供式（I）化合物，其中n，p，R1，R2，X1，X2，X3，X4，X5，R3a，R3b，R4，R5和R6如说明书中所定义，，含有它们的药物组合物及其在治疗中的用途。

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