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1. 发明申请

US20160060224A1 N-MYRISTOYL TRANSFERASE INHIBITORS 有权
标题翻译： N-肉豆蔻酰转移酶抑制剂
公开(公告)号：US20160060224A1
公开(公告)日：2016-03-03
申请号：US14840660
申请日：2015-08-31
申请人： Stephen Brand , Paul Wyatt , Stephen Thompson , Victoria Smith , Tracy Bayliss , Justin Harrison , Neil Norcross , Laura Cleghorn , Ian Gilbert , Ruth Brenk
发明人： Stephen Brand , Paul Wyatt , Stephen Thompson , Victoria Smith , Tracy Bayliss , Justin Harrison , Neil Norcross , Laura Cleghorn , Ian Gilbert , Ruth Brenk
IPC分类号： C07D231/42 , C07D401/12 , C07D403/12 , C07D401/14
CPC分类号： C07D231/42 , A61K31/415 , C07D213/75 , C07D239/69 , C07D263/50 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D487/04
摘要： The present invention relates to N-heterocyclic sulphonamide compounds, in particular pyrazole sulphonamide compounds, and their use as N-myristoyl transferase inhibitors.
摘要翻译：本发明涉及N-杂环磺酰胺化合物，特别是吡唑磺酰胺化合物及其作为N-肉豆蔻酰转移酶抑制剂的用途。

2. 发明授权

US09156811B2 N-myristoyl transferase inhibitors 有权
标题翻译： N-肉豆蔻酰转移酶抑制剂
公开(公告)号：US09156811B2
公开(公告)日：2015-10-13
申请号：US13061811
申请日：2009-08-29
申请人： Stephen Brand , Paul Wyatt , Stephen Thompson , Victoria Smith , Tracy Bayliss , Justin Harrison , Neil Norcross , Laura Cleghorn , Ian Gilbert , Ruth Brenk
发明人： Stephen Brand , Paul Wyatt , Stephen Thompson , Victoria Smith , Tracy Bayliss , Justin Harrison , Neil Norcross , Laura Cleghorn , Ian Gilbert , Ruth Brenk
IPC分类号： A61K31/415 , C07D231/42 , C07D401/04 , C07D213/75 , C07D239/69 , C07D263/50 , C07D403/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D487/04
CPC分类号： C07D231/42 , A61K31/415 , C07D213/75 , C07D239/69 , C07D263/50 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D487/04
摘要： The present invention relates to N-heterocyclic sulphonamide compounds, in particular pyrazole sulphonamide compounds, and their use as N-myristoyl transferase inhibitors.
摘要翻译：本发明涉及N-杂环磺酰胺化合物，特别是吡唑磺酰胺化合物及其作为N-肉豆蔻酰转移酶抑制剂的用途。

3. 发明申请

US20110312921A1 N-Myristoyl Transferase Inhibitors 有权
标题翻译： N-肉豆蔻酰转移酶抑制剂
公开(公告)号：US20110312921A1
公开(公告)日：2011-12-22
申请号：US13061811
申请日：2009-08-29
申请人： Stephen Brand , Paul Wyatt , Stephen Thompson , Victoria Smith , Tracy Bayliss , Justin Harrison , Neil Norcross , Laura Cleghorn , Ian Gilbert , Ruth Brenk
发明人： Stephen Brand , Paul Wyatt , Stephen Thompson , Victoria Smith , Tracy Bayliss , Justin Harrison , Neil Norcross , Laura Cleghorn , Ian Gilbert , Ruth Brenk
IPC分类号： A61K31/635 , A61K31/415 , A61K31/4709 , A61K31/5377 , A61K31/437 , A61K31/427 , A61K31/538 , A61P35/00 , A61P31/00 , A61P3/10 , A61P25/00 , A61P33/00 , A61P31/10 , A61P31/12 , A61K31/4155
CPC分类号： C07D231/42 , A61K31/415 , C07D213/75 , C07D239/69 , C07D263/50 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D487/04
摘要： The present invention relates to N-heterocyclic sulphonamide compounds, in particular pyrazole sulphonamide compounds, and their use as N-myristoyl transferase inhibitors.
摘要翻译：本发明涉及N-杂环磺酰胺化合物，特别是吡唑磺酰胺化合物及其作为N-肉豆蔻酰转移酶抑制剂的用途。

4. 发明申请

US20110130363A1 BENZOPYRAN AND BENZOXEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE 有权
标题翻译：苯并吡喃和苯唑西林PI3K抑制剂化合物及其使用方法
公开(公告)号：US20110130363A1
公开(公告)日：2011-06-02
申请号：US13018068
申请日：2011-01-31
申请人： Steven Do , Richard Goldsmith , Tim Heffron , Aleksandr Kolesnikov , Steven Staben , Alan G. Olivero , Michael Siu , Daniel P. Sutherlin , Bing-Yan Zhu , Paul Goldsmith , Tracy Bayliss , Adrian Folkes , Neil Pegg
发明人： Steven Do , Richard Goldsmith , Tim Heffron , Aleksandr Kolesnikov , Steven Staben , Alan G. Olivero , Michael Siu , Daniel P. Sutherlin , Bing-Yan Zhu , Paul Goldsmith , Tracy Bayliss , Adrian Folkes , Neil Pegg
IPC分类号： A61K31/69 , C07D313/06 , C07D333/00 , C07D491/14 , C07F5/02 , C07D249/10 , C07D405/14 , A61K31/335 , A61K31/381 , A61K31/4196 , A61K31/443 , A61K31/497 , C12N9/99 , A61P35/00 , A61P35/02
CPC分类号： C07F5/02 , A61K31/381 , A61K31/4155 , A61K31/4196 , A61K31/4245 , A61K31/427 , A61K31/429 , A61K31/4365 , A61K31/4436 , A61K31/496 , A61K31/53 , C07D495/04 , C07D495/14 , C07D513/14
摘要： Benzopyran and benzoxepin compounds of Formulas I and II, 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 mediated by lipid kinases. Methods of using compounds of Formulas I and II 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和II的苯并吡喃和苯并辛菌素化合物，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由脂质激酶介导。公开了使用式I和II的化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

5. 发明申请

US20090247567A1 BENZOPYRAN AND BENZOXEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE 有权
标题翻译：苯并吡喃和苯唑西林PI3K抑制剂化合物及其使用方法
公开(公告)号：US20090247567A1
公开(公告)日：2009-10-01
申请号：US12414403
申请日：2009-03-30
申请人： Steven Do , Richard Goldsmith , Tim Heffron , Aleksandr Kolesnikov , Steven Staben , Alan G. Olivero , Michael Siu , Daniel P. Sutherlin , Bing-Yan Zhu , Paul Goldsmith , Tracy Bayliss , Adrian Folkes , Neil Pegg
发明人： Steven Do , Richard Goldsmith , Tim Heffron , Aleksandr Kolesnikov , Steven Staben , Alan G. Olivero , Michael Siu , Daniel P. Sutherlin , Bing-Yan Zhu , Paul Goldsmith , Tracy Bayliss , Adrian Folkes , Neil Pegg
IPC分类号： A61K31/4353 , A61K31/429 , A61K31/38 , C07D491/044 , C07D513/04 , C07D495/04
CPC分类号： C07F5/02 , A61K31/381 , A61K31/4155 , A61K31/4196 , A61K31/4245 , A61K31/427 , A61K31/429 , A61K31/4365 , A61K31/4436 , A61K31/496 , A61K31/53 , C07D495/04 , C07D495/14 , C07D513/14
摘要： Benzopyran and benzoxepin compounds of Formulas I and II, 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 mediated by lipid kinases. Methods of using compounds of Formulas I and II 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和II的苯并吡喃和苯并辛菌素化合物，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由脂质激酶介导。公开了使用式I和II的化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

6. 发明授权

US08399690B2 4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulene compounds 有权
标题翻译： 4,5-二氢-6-氧杂-3-硫杂-1-氮杂 - 苯并[e]薁化合物
公开(公告)号：US08399690B2
公开(公告)日：2013-03-19
申请号：US13018068
申请日：2011-01-31
申请人： Steven Do , Richard Goldsmith , Tim Heffron , Aleksandr Kolesnikov , Steven Staben , Alan G. Olivero , Michael Siu , Daniel P. Sutherlin , Bing-Yan Zhu , Paul Goldsmith , Tracy Bayliss , Adrian Folkes , Neil Pegg
发明人： Steven Do , Richard Goldsmith , Tim Heffron , Aleksandr Kolesnikov , Steven Staben , Alan G. Olivero , Michael Siu , Daniel P. Sutherlin , Bing-Yan Zhu , Paul Goldsmith , Tracy Bayliss , Adrian Folkes , Neil Pegg
IPC分类号： C07D313/00 , C07D333/00
CPC分类号： C07F5/02 , A61K31/381 , A61K31/4155 , A61K31/4196 , A61K31/4245 , A61K31/427 , A61K31/429 , A61K31/4365 , A61K31/4436 , A61K31/496 , A61K31/53 , C07D495/04 , C07D495/14 , C07D513/14
摘要： Benzopyran and benzoxepin compounds of Formulas I and II, 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 mediated by lipid kinases. Methods of using compounds of Formulas I and II 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和II的苯并吡喃和苯并辛菌素化合物，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由脂质激酶介导。公开了使用式I和II的化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

7. 发明授权

US07846929B2 Phosphoinositide 3-kinase inhibitor compounds and methods of use 有权
标题翻译：磷酸肌醇3-激酶抑制剂化合物及其使用方法
公开(公告)号：US07846929B2
公开(公告)日：2010-12-07
申请号：US11789427
申请日：2007-04-24
申请人： Adrian Folkes , Stephen Shuttleworth , Sally Oxenford , Tim Hancox , Tracy Bayliss , Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Kimberly Malesky , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Vickie Tsui , Shumei Wang , Christian Wiesmann , Bing-Yan Zhu , Jennafer Dotson
发明人： Adrian Folkes , Stephen Shuttleworth , Sally Oxenford , Tim Hancox , Tracy Bayliss , Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Kimberly Malesky , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Vickie Tsui , Shumei Wang , Christian Wiesmann , Bing-Yan Zhu , Jennafer Dotson
IPC分类号： A61K31/5377 , C07D413/14
CPC分类号： C07D491/04 , C07D495/04
摘要： Compounds of Formulas Ia and Ib, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia and Ib 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Ia和Ib的化合物，并且包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的盐可用于抑制脂质激酶（包括PI3K）和用于治疗由脂质激酶介导的癌症等疾病。公开了将式Ia和Ib化合物用于体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

8. 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。

9. 发明授权

US08383620B2 Phosphoinositide 3-kinase inhibitor compounds and methods of use 有权
公开(公告)号：US08383620B2
公开(公告)日：2013-02-26
申请号：US12978106
申请日：2010-12-23
申请人： Tracy Bayliss , Irina Chuckowree , Adrian Folkes , Sally Oxenford , Nan Chi Wan , Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Simon Mathieu , Alan Olivero , Steven Staben , Daniel P. Sutherlin , Bing-Yan Zhu
发明人： Tracy Bayliss , Irina Chuckowree , Adrian Folkes , Sally Oxenford , Nan Chi Wan , Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Simon Mathieu , Alan Olivero , Steven Staben , Daniel P. Sutherlin , Bing-Yan Zhu
IPC分类号： A61K31/535
CPC分类号： A61K31/5377 , A61K31/519 , C07D413/14 , C07D491/04 , C07D495/04
摘要： Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

10. 发明申请

US20090233947A1 2,3-Substituted fused bicyclic pyrimidin-4(3H)-ones which modulating the function of the vanilloid -1 receptor (VR1) 审中-公开
标题翻译：调节香草素-1受体（VR1）功能的2,3-取代的稠合双环嘧啶-4（3H） - 酮
公开(公告)号：US20090233947A1
公开(公告)日：2009-09-17
申请号：US11920065
申请日：2006-05-10
申请人： Tracy Bayliss , Rebecca Elizabeth Brown , Gregory John HollingWorth , A. Brian Jones
发明人： Tracy Bayliss , Rebecca Elizabeth Brown , Gregory John HollingWorth , A. Brian Jones
IPC分类号： A61K31/522 , C07D473/30 , A61P25/00
CPC分类号： C07D473/04
摘要： Compounds of formula (I) 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, also known as TRPV1).
摘要翻译：可用作治疗化合物的式（I）化合物，特别是用于治疗通过调节香草素-1受体（VR1，也称为TRPV1）的功能而改善的疼痛和其它病症。

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