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1.发明授权Nitroxide modified non-steroidal anti-inflammatory compounds and uses thereof in the treatment and prevention of diseases or disorders 有权硝基氧化物修饰的非甾体抗炎化合物及其在治疗和预防疾病或病症中的用途公开(公告)号：US09012647B2
公开(公告)日：2015-04-21
申请号：US13440092
申请日：2012-04-05
申请人： David A. Wink , Wilmarie Flores-Santana , S. Bruce King , Murali Krishna Cherukuri , James B. Mitchell
发明人： David A. Wink , Wilmarie Flores-Santana , S. Bruce King , Murali Krishna Cherukuri , James B. Mitchell
IPC分类号： A61K31/445 , C07D211/00 , C07D401/12 , C07D211/94 , A61K47/48
CPC分类号： C07D401/12 , A61K47/48061 , A61K47/545 , C07D211/94
摘要： Disclosed are nitroxide modified NSAID compounds of the formula (I) or a pharmaceutically acceptable salt or enantiomer thereof: in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and n are defined herein and pharmaceutical compositions thereof. Further disclosed is a method of treating or preventing various disorders, such as inflammation, cancer, diabetes, a cardiovascular disorder, weight gain, polyps, and/or chronic pain, in a patient comprising administering an effective amount of a compound or pharmaceutically acceptable salt or enantiomer of formula (I). A method of imaging the compound or pharmaceutically acceptable salt or enantiomer of formula (I) in the body of the animal is also provided.
摘要翻译： 公开了式（I）的硝基氧改性的NSAID化合物或其药学上可接受的盐或对映异构体：其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9，R 10，R 11和n如本文所定义 及其药物组合物。 进一步公开的是在患者中治疗或预防各种疾病，例如炎症，癌症，糖尿病，心血管疾病，体重增加，息肉和/或慢性疼痛的方法，包括给予有效量的化合物或药学上可接受的盐 或式（I）的对映异构体。 还提供了在动物体内成像式（I）的化合物或药学上可接受的盐或对映异构体的方法。
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2.发明申请公开(公告)号：US20120263650A1
公开(公告)日：2012-10-18
申请号：US13440092
申请日：2012-04-05
申请人： David A. Wink , Wilmarie Flores-Santana , S. Bruce King , Murali Krishna Cherukuri , James B. Mitchell
发明人： David A. Wink , Wilmarie Flores-Santana , S. Bruce King , Murali Krishna Cherukuri , James B. Mitchell
IPC分类号： C07D401/12 , A61K49/00 , A61K31/454 , A61P35/00 , C07D211/94 , A61K31/621
CPC分类号： C07D401/12 , A61K47/48061 , A61K47/545 , C07D211/94
摘要： Disclosed are nitroxide modified NSAID compounds of the formula (I) or a pharmaceutically acceptable salt or enantiomer thereof: in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and n are defined herein and pharmaceutical compositions thereof. Further disclosed is a method of treating or preventing various disorders, such as inflammation, cancer, diabetes, a cardiovascular disorder, weight gain, polyps, and/or chronic pain, in a patient comprising administering an effective amount of a compound or pharmaceutically acceptable salt or enantiomer of formula (I). A method of imaging the compound or pharmaceutically acceptable salt or enantiomer of formula (I) in the body of the animal is also provided.
摘要翻译： 公开了式（I）的硝基氧改性的NSAID化合物或其药学上可接受的盐或对映异构体：其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9，R 10，R 11和n如本文所定义 及其药物组合物。 进一步公开的是在患者中治疗或预防各种疾病，例如炎症，癌症，糖尿病，心血管疾病，体重增加，息肉和/或慢性疼痛的方法，包括给予有效量的化合物或药学上可接受的盐 或式（I）的对映异构体。 还提供了在动物体内成像式（I）的化合物或药学上可接受的盐或对映异构体的方法。
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公开(公告)号：US08486957B2
公开(公告)日：2013-07-16
申请号：US12711306
申请日：2010-02-24
IPC分类号： A61K31/475 , A61K41/00 , A61K31/44 , A61K45/06 , C07D471/14
CPC分类号： C07D471/14 , A61K31/44 , A61K31/475 , A61K41/00 , A61K45/06 , A61K2300/00
摘要： A method of treating cancer in a subject in need thereof comprises administering said subject reserpine, yohimbine, an analog thereof, or a pharmaceutically acceptable salt or prodrug thereof, in an amount effective to treat the cancer. Compounds and compositions useful for carrying out the method are also described.
摘要翻译： 在有需要的受试者中治疗癌症的方法包括以有效治疗癌症的量施用所述受试者利血平，育亨宾，其类似物或其药学上可接受的盐或前药。 还描述了用于实施该方法的化合物和组合物。
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公开(公告)号：US20100239692A1
公开(公告)日：2010-09-23
申请号：US12678539
申请日：2008-09-19
IPC分类号： A61K33/00 , A61K31/185 , A61P7/04
CPC分类号： A61K31/58 , Y02A50/411
摘要： Provided herein are methods of treating hemolysis by administering an active compound in an amount sufficient to treat said hemolysis. It has been found that nitroxyl donors or similar compounds preferentially react with cell-free OxyHb, as compared to OxyHb encapsulated in a red blood cell, and reacts with MetHb to form iron-nitrosyl Hb or nitrite bound MetHb. It has also been found that such compounds reduce cell-free Hb and hemolysis. Active compounds are also contemplated for use in combination therapies, for example, in combination with the administration of red blood cells and/or an agent that promotes hematopoiesis, or in combination with the administration of a nitric oxide donor.
摘要翻译： 本文提供了通过施用足以治疗所述溶血的量的活性化合物来治疗溶血的方法。 已经发现，与包封在红细胞中的OxyHb相比，硝酰基供体或类似化合物优先与无细胞的OxyHb反应，并与MetHb反应形成亚硝酰基Hb或亚硝酸盐结合的MetHb。 还已经发现，这些化合物减少无细胞的Hb和溶血。 还考虑活性化合物用于组合疗法，例如与施用红细胞和/或促进造血作用的药剂组合，或与施用一氧化氮供体组合使用。
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公开(公告)号：US08269034B2
公开(公告)日：2012-09-18
申请号：US13177036
申请日：2011-07-06
申请人： S. Bruce King
发明人： S. Bruce King
IPC分类号： C07C69/76 , C07C207/00 , A61K31/235 , A61K31/04
CPC分类号： C07C207/04 , C07C2601/14
摘要： Active compounds of Formula I are described: wherein: R1 and R2 are each independently C1-C4 alkyl; or R1 and R2 together form a C2-C7 alkylene chain; and Z is a non-steroidal anti-inflammatory drug (NSAID); along with pharmaceutically acceptable salts and prodrug thereof, and methods of using the same.
摘要翻译： 描述了式I的活性化合物：其中：R 1和R 2各自独立地为C 1 -C 4烷基; 或R 1和R 2一起形成C 2 -C 7亚烷基链; Z是非甾体抗炎药（NSAID）; 以及其药学上可接受的盐和前药，及其使用方法。
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公开(公告)号：US20090137668A1
公开(公告)日：2009-05-28
申请号：US12293374
申请日：2007-04-13
申请人： S. Bruce King
发明人： S. Bruce King
CPC分类号： C07C207/04 , C07C2601/14
摘要： Active compounds of Formula (I) are described: wherein: R1 and R2 are each independently C1-C4 alkyl; or R1 and R2 together form a C2-C7 alkylene chain; and Z is a non-steroidal anti-inflammatory drug (NSAID); along with pharmaceutically acceptable salts and prodrug thereof, and methods of using the same.
摘要翻译： 描述了式（I）的活性化合物：其中：R 1和R 2各自独立地为C 1 -C 4烷基; 或R 1和R 2一起形成C 2 -C 7亚烷基链; Z是非甾体抗炎药（NSAID）; 以及其药学上可接受的盐和前药，及其使用方法。
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公开(公告)号：US07294748B2
公开(公告)日：2007-11-13
申请号：US11247045
申请日：2005-10-11
IPC分类号： C07C13/00
CPC分类号： G01N33/68 , G01N21/6428 , G01N33/574 , G01N33/6815 , Y10T436/156666 , Y10T436/182 , Y10T436/24
摘要： The present invention provides compounds of Formula I: wherein: R1 is a label (e.g., a detectable groups; an anti-tumor agent)s; L is present or absent and when present is a linking group; and x represents an integer from 1 to 10; or a pharmaceutically acceptable salt thereof. The compounds are useful for, among other things, identifying cysteine sulfenic acids in proteins and monitoring oxidative damage in proteins and cells.
摘要翻译： 本发明提供了式I的化合物：其中：R 1是标记（例如可检测的基团;抗肿瘤剂）; L存在或不存在，并且当存在时是连接基团; x表示1〜10的整数， 或其药学上可接受的盐。 该化合物尤其可用于鉴定蛋白质中的半胱氨酸亚磺酸并监测蛋白质和细胞中的氧化损伤。
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公开(公告)号：US20130040919A1
公开(公告)日：2013-02-14
申请号：US13589422
申请日：2012-08-20
申请人： S. Bruce King
发明人： S. Bruce King
IPC分类号： A61K31/235 , A61K31/621 , A61P29/00 , A61K31/24 , A61P9/00 , A61P9/04 , C07C207/04 , A61K31/22
CPC分类号： C07C207/04 , C07C2601/14
摘要： Active compounds of Formula I are described: wherein: R1 and R2 are each independently C1-C4 alkyl; or R1 and R2 together form a C2-C7 alkylene chain; and Z is a non-steroidal anti-inflammatory drug (NSAID); along with pharmaceutically acceptable salts and prodrug thereof, and methods of using the same.
摘要翻译： 描述了式I的活性化合物：其中：R 1和R 2各自独立地为C 1 -C 4烷基; 或R 1和R 2一起形成C 2 -C 7亚烷基链; Z是非甾体抗炎药（NSAID）; 以及其药学上可接受的盐和前药，及其使用方法。
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公开(公告)号：US20110263674A1
公开(公告)日：2011-10-27
申请号：US13177036
申请日：2011-07-06
申请人： S. Bruce King
发明人： S. Bruce King
IPC分类号： A61K31/235 , A61K31/216 , A61K31/245 , C07D207/33 , A61P9/00 , C07C317/32 , C07C225/22 , C07C69/78 , C07C69/612 , A61P9/04 , A61K31/40 , C07C69/734
CPC分类号： C07C207/04 , C07C2601/14
摘要： Active compounds of Formula I are described: wherein: R1 and R2 are each independently C1-C4 alkyl; or R1 and R2 together form a C2-C7 alkylene chain; and Z is a non-steroidal anti-inflammatory drug (NSAID); along with pharmaceutically acceptable salts and prodrug thereof, and methods of using the same.
摘要翻译： 描述了式I的活性化合物：其中：R 1和R 2各自独立地为C 1 -C 4烷基; 或R 1和R 2一起形成C 2 -C 7亚烷基链; Z是非甾体抗炎药（NSAID）; 以及其药学上可接受的盐和前药，及其使用方法。
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公开(公告)号：US20100173970A1
公开(公告)日：2010-07-08
申请号：US12710778
申请日：2010-02-23
申请人： S. Bruce King
发明人： S. Bruce King
IPC分类号： A61K31/40 , A61K31/216 , A61K31/24 , C07D207/335 , C07C69/76 , A61P9/00 , A61P9/04
CPC分类号： C07C207/04 , C07C2601/14
摘要： Active compounds of Formula I are described: wherein: R1 and R2 are each independently C1-C4 alkyl; or R1 and R2 together form a C2-C7 alkylene chain; and Z is a non-steroidal anti-inflammatory drug (NSAID); along with pharmaceutically acceptable salts and prodrug thereof, and methods of using the same.
摘要翻译： 描述了式I的活性化合物：其中：R 1和R 2各自独立地为C 1 -C 4烷基; 或R 1和R 2一起形成C 2 -C 7亚烷基链; Z是非甾体抗炎药（NSAID）; 以及其药学上可接受的盐和前药，及其使用方法。
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