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公开(公告)号：US09018411B2
公开(公告)日：2015-04-28
申请号：US12962544
申请日：2010-12-07
申请人： John P. Toscano , Art Sutton , Vincent J. Kalish , Frederick Arthur Brookfield , Stephen Martin Courtney , Lisa Marie Frost
发明人： John P. Toscano , Art Sutton , Vincent J. Kalish , Frederick Arthur Brookfield , Stephen Martin Courtney , Lisa Marie Frost
IPC分类号： C07C239/08 , A61K31/215 , C07C259/10 , C07C259/06 , C07C271/08 , C07C311/51 , C07C311/53 , C07C317/14 , C07D207/16 , C07D213/40 , C07D213/71 , C07D295/205 , C07D307/82 , C07D309/12 , C07D333/34
CPC分类号： C07D333/34 , C07C233/01 , C07C233/64 , C07C259/06 , C07C259/10 , C07C271/08 , C07C311/51 , C07C311/53 , C07C317/14 , C07C317/28 , C07C317/32 , C07C2601/08 , C07C2601/14 , C07D207/16 , C07D213/40 , C07D213/71 , C07D295/205 , C07D295/215 , C07D307/82 , C07D309/12
摘要： The invention provides certain bis-acylated hydroxylamine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.
摘要翻译： 本发明提供某些双酰化羟胺衍生物化合物，包含这些化合物的药物组合物和试剂盒，以及使用这些化合物或药物组合物的方法。 特别地，本发明提供了使用这些化合物或药物组合物治疗，预防或延缓疾病或病症发作和/或发展的方法。 在一些实施方案中，疾病或病症选自心血管疾病，缺血，再灌注损伤，癌性疾病，肺动脉高压和对硝酰基治疗有反应的病症。
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公开(公告)号：US20110118258A1
公开(公告)日：2011-05-19
申请号：US12599116
申请日：2008-05-15
申请人： Stephen Martin Courtney , Mark Whittaker , Owen Clifford Mather , Christopher John Yarnold , Oliver Robin Barker , Christian Aldo Georges Napoleon Montalbetti , Thomas Hesterkamp , Mihaly Daniel Gardiner
发明人： Stephen Martin Courtney , Mark Whittaker , Owen Clifford Mather , Christopher John Yarnold , Oliver Robin Barker , Christian Aldo Georges Napoleon Montalbetti , Thomas Hesterkamp , Mihaly Daniel Gardiner
IPC分类号： A61K31/517 , C07D239/84 , C07D413/12 , C07D409/08 , C07D405/10 , C07D401/10 , C07D403/10 , C07D403/12 , A61K31/5377 , A61P35/00 , A61P29/00 , A61P31/12
CPC分类号： C07D239/84 , C07D401/04 , C07D403/10 , C07D405/04 , C07D409/04
摘要： Compounds of general formula (I); or a stereoisomers, tautomers, pharmaceutically acceptable salts, or prodrugs thereof, wherein R1, R2, R3, R4, R5, R6, R8 and R9 are as defined herein, are useful for the treatment of diseases and conditions which are mediated by excessive or inappropriate Hsp90 activity such as cancers, viral infection and inflammatory diseases or conditions.
摘要翻译： 通式（I）的化合物; 或其立体异构体，互变异构体，药学上可接受的盐或前药，其中R 1，R 2，R 3，R 4，R 5，R 6，R 8和R 9如本文所定义，可用于治疗疾病和病症， 不适当的Hsp90活动如癌症，病毒感染和炎性疾病或病症。
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公开(公告)号：US07138425B2
公开(公告)日：2006-11-21
申请号：US10506388
申请日：2003-03-06
IPC分类号： A61K31/4035 , A61K31/423 , A61K31/428 , C07D209/48 , C07D263/54 , C07D263/57 , C07D277/62
CPC分类号： C07D413/10 , C07D413/14
摘要： The present invention relates to phthalimide carboxylic acid derivatives of formula (I), methods for their preparation, pharmaceutical compositions containing them and their use in medicine, specifically in the treatment of cancer. (I), wherein X is O or S; R1 is a phthalimide carboxylic acid group of formula (II). R is hydrogen, C1–C6 alkyl, aryl or C1–C3 alkylaryl and R2, R3 and R4 represent various substituents
摘要翻译： 本发明涉及式（I）的邻苯二甲酰亚胺羧酸衍生物，其制备方法，含有它们的药物组合物及其在医药中的用途，特别涉及治疗癌症。 （I），其中X为O或S; R 1是式（II）的邻苯二甲酰亚胺羧酸基团。 R是氢，C 1 -C 6烷基，芳基或C 1 -C 3烷基芳基， SUP> 2，R 3和R 4表示各种取代基
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24.发明申请N-HYDROXYLSULFONAMIDE DERIVATIVES AS NEW PHYSIOLOGICALLY USEFUL NITROXYL DONORS 有权N-羟基磺酰胺衍生物作为新生物学上有用的硝基衍生物公开(公告)号：US20120258965A1
公开(公告)日：2012-10-11
申请号：US13531364
申请日：2012-06-22
申请人： John P. TOSCANO , Frederick Arthur Brookfield , Andrew D. Cohen , Stephen Martin Courtney , Lisa Marie Frost , Vincent Jacob Kalish
发明人： John P. TOSCANO , Frederick Arthur Brookfield , Andrew D. Cohen , Stephen Martin Courtney , Lisa Marie Frost , Vincent Jacob Kalish
IPC分类号： A61K31/381 , C07D333/38 , C07D409/06 , C07D409/04 , A61P9/10 , A61K31/4535 , A61K31/496 , A61P9/00 , A61P9/04 , C07D409/12 , A61K31/5377
CPC分类号： C07C317/48 , C07C311/48 , C07D295/155 , C07D295/16 , C07D295/192 , C07D295/26 , C07D333/26 , C07D333/36 , C07D333/38
摘要： The invention relates to N-hydroxylsulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxylsulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxylsulfonamide derivatives.
摘要翻译： 本发明涉及在生理条件下提供硝酰基（HNO）的N-羟基磺酰胺衍生物，并且可用于治疗和/或预防对硝酰病治疗有反应的疾病或病症的发作和/或发展，包括心力衰竭和缺血/再灌注 伤害。 新型N-羟基磺酰胺衍生物在生理条件下以控制速率释放NHO，并且通过改变N-羟基磺酰胺衍生物上官能团的性质和位置来调节HNO释放速率。
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25.发明申请N-Hydroxylsulfonamide Derivatives as New Physiologically Useful Nitroxyl Donors 审中-公开N-羟基磺酰胺衍生物作为新的生理用途的硝基氧供体公开(公告)号：US20110306614A1
公开(公告)日：2011-12-15
申请号：US13213480
申请日：2011-08-19
申请人： John P. Toscano , Frederick Arthur Brookfield , Andrew D. Cohen , Stephen Martin Courtney , Lisa Marie Frost , Vincent Jacob Kalish
发明人： John P. Toscano , Frederick Arthur Brookfield , Andrew D. Cohen , Stephen Martin Courtney , Lisa Marie Frost , Vincent Jacob Kalish
IPC分类号： A61K31/5377 , C07D295/135 , A61K31/185 , A61K31/5375 , A61K31/495 , A61K31/4453 , C07D307/82 , C07D333/62 , C07D215/36 , C07D235/28 , C07D277/80 , C07D263/58 , A61K31/343 , A61K31/381 , A61K31/47 , A61K31/4184 , A61K31/427 , A61K31/423 , C07D333/34 , C07D413/04 , C07D241/14 , A61K31/4965 , A61P9/00 , A61P9/04 , C07C311/48
CPC分类号： C07C311/48 , C07C317/14 , C07C323/67 , C07D213/74 , C07D231/18 , C07D261/10 , C07D263/58 , C07D285/125 , C07D295/096 , C07D307/82 , C07D309/12 , C07D317/14 , C07D333/34 , C07D333/62
摘要： The invention relates to N-hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxysulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxysulfonamide derivatives.
摘要翻译： 本发明涉及在生理条件下给予硝酰基（HNO）的N-羟基磺酰胺衍生物，并且可用于治疗和/或预防对硝酰病治疗有反应的疾病或病症的发作和/或发展，包括心力衰竭和缺血/再灌注 伤害。 新的N-羟基磺酰胺衍生物在生理条件下以受控的速率释放NHO，并且通过改变N-羟基磺酰胺衍生物上官能团的性质和位置来调节HNO释放速率。
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26.发明申请公开(公告)号：US20110144067A1
公开(公告)日：2011-06-16
申请号：US12962572
申请日：2010-12-07
申请人： John P. Toscano , Art Sutton , Vincent J. Kalish , Frederick Arthur Brookfield , Stephen Martin Courtney , Lisa Marie Frost
发明人： John P. Toscano , Art Sutton , Vincent J. Kalish , Frederick Arthur Brookfield , Stephen Martin Courtney , Lisa Marie Frost
IPC分类号： A61K31/635 , C07C303/36 , C07D401/02 , C07D211/00 , C07D265/30 , C07D413/02 , A61K31/63 , A61P9/12 , A61P9/10
CPC分类号： C07C311/48 , C07C311/51 , C07C317/14 , C07C317/32 , C07C2601/14 , C07D207/06 , C07D207/16 , C07D209/48 , C07D211/46 , C07D211/58 , C07D211/62 , C07D213/40 , C07D213/46 , C07D213/59 , C07D213/71 , C07D213/74 , C07D233/38 , C07D241/04 , C07D241/08 , C07D295/192 , C07D295/195 , C07D295/205 , C07D307/82 , C07D309/12 , C07D317/30 , C07D333/34 , C07D401/04 , C07D413/04
摘要： The invention provides certain N-acyloxysulfonamide and N-hydroxy-N-acylsulfonamide derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.
摘要翻译： 本发明提供某些N-酰氧基亚磺酰胺和N-羟基-N-酰基磺酰胺衍生物化合物，包含这些化合物的药物组合物和试剂盒，以及使用这些化合物或药物组合物的方法。 特别地，本发明提供了使用这些化合物或药物组合物治疗，预防或延缓疾病或病症发作和/或发展的方法。 在一些实施方案中，疾病或病症选自心血管疾病，缺血，再灌注损伤，癌性疾病，肺动脉高压和对硝酰基治疗有反应的病症。
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27.发明申请N-HYDROXYLSULFONAMIDE DERIVATIVES AS NEW PHYSIOLOGICALLY USEFUL NITROXYL DONORS 有权N-羟基磺酰胺衍生物作为新生物学上有用的硝基衍生物公开(公告)号：US20090163487A1
公开(公告)日：2009-06-25
申请号：US12239705
申请日：2008-09-26
申请人： John P. Toscano , Frederick Arthur Brookfield , Andrew D. Cohen , Stephen Martin Courtney , Lisa Marie Frost , Vincent Jacob Kalish
发明人： John P. Toscano , Frederick Arthur Brookfield , Andrew D. Cohen , Stephen Martin Courtney , Lisa Marie Frost , Vincent Jacob Kalish
IPC分类号： A61K31/5377 , C07C311/16 , A61K31/24 , A61K31/195 , A61K31/18 , C07D265/30 , A61K31/5375 , C07D413/12 , A61P9/04
CPC分类号： C07C317/48 , C07C311/48 , C07D295/155 , C07D295/16 , C07D295/192 , C07D295/26 , C07D333/26 , C07D333/36 , C07D333/38
摘要： The invention relates to N-hydroxylsulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxylsulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxylsulfonamide derivatives.
摘要翻译： 本发明涉及在生理条件下提供硝酰基（HNO）的N-羟基磺酰胺衍生物，并且可用于治疗和/或预防对硝酰病治疗有反应的疾病或病症的发作和/或发展，包括心力衰竭和缺血/再灌注 伤害。 新型N-羟基磺酰胺衍生物在生理条件下以控制速率释放NHO，并且通过改变N-羟基磺酰胺衍生物上官能团的性质和位置来调节HNO释放速率。
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28.发明申请公开(公告)号：US20080194574A1
公开(公告)日：2008-08-14
申请号：US10596508
申请日：2004-12-16
申请人： Jan Eike Eikhoff , Mark Richard Ashton , Stephen Martin Courtney , Christopher John Yarnold , Maurizio Varrone , Pui Leng Loke , Thomas Herget , Wilfried Schwab , Doris Hafenbradl
发明人： Jan Eike Eikhoff , Mark Richard Ashton , Stephen Martin Courtney , Christopher John Yarnold , Maurizio Varrone , Pui Leng Loke , Thomas Herget , Wilfried Schwab , Doris Hafenbradl
IPC分类号： A61K31/4985 , C07D487/04 , C07D241/10 , A61K31/4965 , A61P31/00 , A61P37/00 , A61P25/16 , A61P25/28
CPC分类号： C07D401/04 , C07D241/20 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D409/14
摘要： The present invention relates to pyrazine derivatives according to the general formula (I) and pharmaceutically acceptable salts thereof and their use as pharmaceutical compounds as well as the use of these compounds for the preparation of a pharmaceutical composition for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, prion diseases, immunological diseases, autoimmune diseases, bipolar and clinical disorders, cardiovascular diseases, cell proliferative diseases, diabetes, inflammation, transplant rejections, erectile dysfunction, neurodegenerative diseases, stroke and especially for the treatment of herpesviral induced infections, including opportunistic infections as well as infections and diseases caused by human cytomegalovirus (HCMV).
摘要翻译： 本发明涉及根据通式（I）的吡嗪衍生物及其药学上可接受的盐及其作为药物化合物的用途，以及这些化合物在制备用于预防和/或治疗感染性疾病的药物组合物中的用途 疾病，包括机会性疾病，朊病毒疾病，免疫疾病，自身免疫性疾病，双相和临床病症，心血管疾病，细胞增殖性疾病，糖尿病，炎症，移植排斥，勃起功能障碍，神经变性疾病，中风，特别是治疗疱疹病毒诱导的感染 ，包括机会性感染以及由巨细胞病毒（HCMV）引起的感染和疾病。
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公开(公告)号：US07326727B2
公开(公告)日：2008-02-05
申请号：US10523118
申请日：2003-08-05
IPC分类号： A61K31/427
CPC分类号： C07D417/04 , C07D417/14
摘要： The invention provides a compound of formula (I) or a pharmaceutically acceptable salt or prodrug thereof: (I) wherein the groups Q, R2, R3, R4 and R5 represent various substituent groups, and their use as inhibitors of heparanase.
摘要翻译： 本发明提供式（I）化合物或其药学上可接受的盐或前药：（I）其中基团Q，R 2，R 3，R SUP > 4和R 5代表各种取代基，以及它们作为乙酰肝素酶的抑制剂的用途。
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公开(公告)号：US08592430B2
公开(公告)日：2013-11-26
申请号：US12599116
申请日：2008-05-15
申请人： Stephen Martin Courtney , Mark Whittaker , Owen Clifford Mather , Christopher John Yarnold , Oliver Robin Barker , Christian Aldo Georges Napoleon Montalbetti , Thomas Hesterkamp , Mihaly Daniel Gardiner
发明人： Stephen Martin Courtney , Mark Whittaker , Owen Clifford Mather , Christopher John Yarnold , Oliver Robin Barker , Christian Aldo Georges Napoleon Montalbetti , Thomas Hesterkamp , Mihaly Daniel Gardiner
IPC分类号： A61K31/517 , A61K31/519 , C07D239/84
CPC分类号： C07D239/84 , C07D401/04 , C07D403/10 , C07D405/04 , C07D409/04
摘要： Compounds of general formula (I); or a stereoisomers, tautomers, pharmaceutically acceptable salts, or prodrugs thereof, wherein R1, R2, R3, R4, R5, R6, R8 and R9 are as defined herein, are useful for the treatment of diseases and conditions which are mediated by excessive or inappropriate Hsp90 activity such as cancers, viral infection and inflammatory diseases or conditions.
摘要翻译： 通式（I）的化合物; 或其立体异构体，互变异构体，药学上可接受的盐或前药，其中R 1，R 2，R 3，R 4，R 5，R 6，R 8和R 9如本文所定义，可用于治疗疾病和病症， 不适当的Hsp90活动如癌症，病毒感染和炎性疾病或病症。
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