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公开(公告)号：US20100221182A1
公开(公告)日：2010-09-02
申请号：US12448575
申请日：2007-12-21
申请人： Ajay Purohit , Thomas D, Harris , Heike S. Radeke , Simon P. Robinson , Ming Yu , David S. Casebier , Michael T. Azure
发明人： Ajay Purohit , Thomas D, Harris , Heike S. Radeke , Simon P. Robinson , Ming Yu , David S. Casebier , Michael T. Azure
IPC分类号： A61K51/04 , C07D233/88 , C07C279/08 , C07C215/30 , C07D295/14
CPC分类号： A61K51/04 , A61K51/0453 , A61K51/0459 , C07B59/001 , C07B2200/05 , C07C215/60 , C07C217/70 , C07C279/06 , C07C279/08
摘要： Novel compounds that find use as imaging agents within nuclear medicine applications (PET imaging) for imaging of cardiac innervation are disclosed. These PET based radiotracers may exhibit increased stability, decreased NE release (thereby reducing side effects), improved quantitative data, and/or high affinity for VMAT over prior radiotracers. Methods of using the compounds to image cardiac innervation are also provided. In some instances the compounds are developed by derivatizing certain compounds with 18F in a variety of positions: aryl, alkyl, a keto, benzylic, beta-alkylethers, gamma-propylalkylethers and beta-proplylalkylethers. Alternatively or additionally, a methyl group a is added to the amine, and/or the catechol functionality is either eliminated or masked as a way of making these compounds more stable.
摘要翻译： 公开了用于心脏神经支配成像的核医学应用（PET成像）中用作成像剂的新型化合物。 这些基于PET的放射性示踪剂可能表现出增加的稳定性，减少NE释放（从而减少副作用），改进的定量数据，和/或对先前的放射性示踪剂对VMAT的高亲和力。 还提供了使用化合物成像心脏神经支配的方法。 在某些情况下，化合物通过在各种位置上衍生化某些化合物而形成：芳基，烷基，酮基，苄基，β-烷基醚，γ-丙基烷基醚和β-丙基烷基醚。 或者或另外，将甲基a加入到胺中，和/或儿茶酚官能团被消除或掩蔽，作为使这些化合物更稳定的方式。
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公开(公告)号：US09408927B2
公开(公告)日：2016-08-09
申请号：US12919600
申请日：2009-02-27
CPC分类号： A61K51/0459
摘要： The present invention is directed, in part, to compounds and methods for imaging the central nervous system or cancer, comprising administering to a subject a contrast agent which comprises a compound that binds MC-I, and an imaging moiety, and scanning the subject using diagnostic imaging.
摘要翻译： 本发明部分地涉及用于对中枢神经系统或癌症进行成像的化合物和方法，包括向受试者施用包含结合MC-1的化合物和成像部分的造影剂，并使用 诊断成像。
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3.发明授权Compositions, methods, and systems for the synthesis and use of imaging agents 有权用于合成和使用成像剂的组合物，方法和系统公开(公告)号：US09550000B2
公开(公告)日：2017-01-24
申请号：US14343627
申请日：2012-09-07
申请人： Simon P. Robinson , Ming Yu
发明人： Simon P. Robinson , Ming Yu
IPC分类号： A61K51/00 , A61M36/14 , A61K51/04 , C07C279/04 , C07D233/46 , C07D209/14 , C07C257/14 , C07C279/06 , C07C279/08 , C07C279/12 , C07C279/14 , C07C281/18 , C07C217/70
CPC分类号： A61K51/0459 , A61K51/04 , A61K51/041 , A61K51/0453 , A61K51/0497 , C07B2200/05 , C07C217/70 , C07C257/14 , C07C279/04 , C07C279/06 , C07C279/08 , C07C279/12 , C07C279/14 , C07C281/18 , C07D209/14 , C07D233/46
摘要： The present invention relates to systems, compositions, and methods for the synthesis and use of imaging agents, or precursors thereof. An imaging agent precursor may be converted to an imaging agent using the methods described herein. In some cases, the imaging agent is enriched in 18F. In some cases, an imaging agent may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs. In some embodiments, methods and compositions for assessing perfusion and innervation mismatch in a portion of a subject are provided.
摘要翻译： 本发明涉及用于合成和使用成像剂或其前体的体系，组合物和方法。 成像剂前体可以使用本文所述的方法转化成成像剂。 在某些情况下，成像剂富集于18F。 在一些情况下，成像剂可用于对受试者感兴趣的区域进行成像，包括但不限于心脏，心血管系统，心脏血管，脑和其他器官。 在一些实施例中，提供了用于评估受试者的一部分中的灌注和神经支配失配的方法和组合物。
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公开(公告)号：US08491868B2
公开(公告)日：2013-07-23
申请号：US12448575
申请日：2007-12-21
申请人： Ajay Purohit , Thomas D. Harris , Heike S. Radeke , Simon P. Robinson , Ming Yu , David S. Casebier , Michael T. Azure
发明人： Ajay Purohit , Thomas D. Harris , Heike S. Radeke , Simon P. Robinson , Ming Yu , David S. Casebier , Michael T. Azure
IPC分类号： A61K51/00 , A61K51/04 , C07C279/06 , A01N47/44
CPC分类号： A61K51/04 , A61K51/0453 , A61K51/0459 , C07B59/001 , C07B2200/05 , C07C215/60 , C07C217/70 , C07C279/06 , C07C279/08
摘要： Novel compounds that find use as imaging agents within nuclear medicine applications (PET imaging) for imaging of cardiac innervation are disclosed. These PET based radiotracers may exhibit increased stability, decreased NE release (thereby reducing side effects), improved quantitative data, and/or high affinity for VMAT over prior radiotracers. Methods of using the compounds to image cardiac innervation are also provided. In some instances the compounds are developed by derivatizing certain compounds with 18F in a variety of positions: aryl, alkyl, a keto, benzylic, beta-alkylethers, gamma-propylalkylethers and beta-proplylalkylethers. Alternatively or additionally, a methyl group a is added to the amine, and/or the catechol functionality is either eliminated or masked as a way of making these compounds more stable.
摘要翻译： 公开了用于心脏神经支配成像的核医学应用（PET成像）中用作成像剂的新型化合物。 这些基于PET的放射性示踪剂可能表现出增加的稳定性，减少NE释放（从而减少副作用），改进的定量数据，和/或对先前的放射性示踪剂对VMAT的高亲和力。 还提供了使用化合物成像心脏神经支配的方法。 在某些情况下，化合物通过在各种位置上衍生化某些化合物而形成：芳基，烷基，酮基，苄基，β-烷基醚，γ-丙基烷基醚和β-丙基烷基醚。 或者或另外，将甲基a加入到胺中，和/或儿茶酚官能团被消除或掩蔽，作为使这些化合物更稳定的方式。
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公开(公告)号：US20110091374A1
公开(公告)日：2011-04-21
申请号：US12919600
申请日：2009-02-27
CPC分类号： A61K51/0459
摘要： The present invention is directed, in part, to compounds and methods for imaging the central nervous system or cancer, comprising administering to a subject a contrast agent which comprises a compound that binds MC-I, and an imaging moiety, and scanning the subject using diagnostic imaging.
摘要翻译： 本发明部分地涉及用于对中枢神经系统或癌症进行成像的化合物和方法，包括向受试者施用包含结合MC-1的化合物和成像部分的造影剂，并使用 诊断成像。
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6.发明申请COMPOSITIONS, METHODS, AND SYSTEMS FOR THE SYNTHESIS AND USE OF IMAGING AGENTS 有权用于合成和成像剂使用的组合物，方法和系统公开(公告)号：US20140328756A1
公开(公告)日：2014-11-06
申请号：US14343627
申请日：2012-09-07
申请人： Heike S. Radeke , Richard R. Cesati , Ajay Purohit , Thomas D. Harris , Simon P. Robinson , Ming Yu , David S. Casebier , Carol Hui Hu , Matthias Broekema , David C. Onthank
发明人： Heike S. Radeke , Richard R. Cesati , Ajay Purohit , Thomas D. Harris , Simon P. Robinson , Ming Yu , David S. Casebier , Carol Hui Hu , Matthias Broekema , David C. Onthank
IPC分类号： A61K51/04
CPC分类号： A61K51/0459 , A61K51/04 , A61K51/041 , A61K51/0453 , A61K51/0497 , C07B2200/05 , C07C217/70 , C07C257/14 , C07C279/04 , C07C279/06 , C07C279/08 , C07C279/12 , C07C279/14 , C07C281/18 , C07D209/14 , C07D233/46
摘要： The present invention relates to systems, compositions, and methods for the synthesis and use of imaging agents, or precursors thereof. An imaging agent precursor may be converted to an imaging agent using the methods described herein. In some cases, the imaging agent is enriched in 18F. In some cases, an imaging agent may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs. In some embodiments, methods and compositions for assessing perfusion and innervation mismatch in a portion of a subject are provided.
摘要翻译： 本发明涉及用于合成和使用成像剂或其前体的体系，组合物和方法。 成像剂前体可以使用本文所述的方法转化成成像剂。 在某些情况下，成像剂富集于18F。 在一些情况下，成像剂可用于对受试者感兴趣的区域进行成像，包括但不限于心脏，心血管系统，心脏血管，脑和其他器官。 在一些实施例中，提供了用于评估受试者的一部分中的灌注和神经支配失配的方法和组合物。
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公开(公告)号：US20120328514A1
公开(公告)日：2012-12-27
申请号：US13382689
申请日：2010-07-08
申请人： Richard R. Cesati , Thomas D. Harris , Simon P. Robinson , Richard J. Looby , Edward H. Cheesman , Padmaja Yalamanchili , David S. Casebier
发明人： Richard R. Cesati , Thomas D. Harris , Simon P. Robinson , Richard J. Looby , Edward H. Cheesman , Padmaja Yalamanchili , David S. Casebier
IPC分类号： A61K49/00 , A61K51/04 , C07D209/20 , C07D213/56 , C07C229/36 , C07D257/02
CPC分类号： A61K51/0497 , A61K49/085 , A61K49/10 , A61K51/0406 , C07C259/06 , C07C271/22 , C07D257/02
摘要： The present disclosure is directed to compounds, diagnostic agents, and related methods. In some cases, methods for treating patients are provided. More specifically, the disclosure provides compounds, diagnostic agents, and kits for detecting and/or imaging and/or monitoring elastin rich tissues. In addition, the disclosure provides methods of detecting and/or imaging and/or monitoring the presence of coronary plaque, carotid plaque, iliac/femoral plaque, aortic plaque, renal artery plaque, plaque of any arterial vessel, aneurism, vasculitis, other diseases of the arterial wall, and/or damage or structural changes in ligaments, uterus, lungs or skin, as indicated by changes in total vessel wall area, internal lumen size, and exterior arterial perimeter.
摘要翻译： 本公开涉及化合物，诊断剂和相关方法。 在某些情况下，提供了治疗患者的方法。 更具体地，本公开提供了用于检测和/或成像和/或监测富含弹性蛋白的组织的化合物，诊断剂和试剂盒。 此外，本公开提供了检测和/或成像和/或监测冠状动脉斑块，颈动脉斑块，髂骨/股骨斑块，主动脉斑块，肾动脉斑块，任何动脉血管的斑块，动脉瘤，血管炎，其他疾病的存在的方法 的动脉壁，和/或韧带，子宫，肺或皮肤的损伤或结构变化，如总血管壁面积，内腔大小和外动脉周长的变化所示。
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公开(公告)号：US07323587B2
公开(公告)日：2008-01-29
申请号：US11152891
申请日：2005-06-15
IPC分类号： A61K31/192 , C07C57/50
CPC分类号： C07D257/04 , C07C51/487 , C07C57/50 , C07C59/54 , C07C59/72 , C07C69/618 , C07C69/734 , C07C255/34 , C07C311/51 , C07C2601/10 , C07C2602/10 , C07C2602/12 , C07D277/80 , C07D311/58 , C07D333/34
摘要： The present invention provides, inter alia, triphenylethylene derivatives, such as, 3-{4-[6-(3-Methoxy-phenyl)-8,9-dihydro-7H-benzocyclohepten-5-yl]-phenyl}-acrylic acid, as selective estrogen receptor modulators. Also provided are methods for treating estrogen stimulated diseases in mammals including, but not limited to, for example, breast, uterine, ovarian, prostate and colon cancer; osteoporosis; endometriosis; uterine fibroid; Alzheimer's disease; macular degeneration; urinary incontinence; and type II diabetes, as well as, pharmaceutical compositions comprising at least one compound of the present invention.
摘要翻译： 本发明特别提供三苯基乙烯衍生物，例如3- {4- [6-（3-甲氧基 - 苯基）-8,9-二氢-7H-苯并环庚烯-5-基] - 苯基} - 丙烯酸 ，作为选择性雌激素受体调节剂。 还提供了用于治疗哺乳动物中雌激素刺激的疾病的方法，包括但不限于例如乳腺癌，子宫癌，卵巢癌，前列腺癌和结肠癌; 骨质疏松症 子宫内膜异位症 子宫肌瘤 阿尔茨海默氏病; 黄斑变性; 尿失禁 和II型糖尿病，以及包含至少一种本发明化合物的药物组合物。
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公开(公告)号：US09161997B2
公开(公告)日：2015-10-20
申请号：US13529756
申请日：2012-06-21
申请人： David S. Casebier , Simon P. Robinson , Ajay Purohit , Heike S. Radeke , Michael T. Azure , Douglas D. Dischino
发明人： David S. Casebier , Simon P. Robinson , Ajay Purohit , Heike S. Radeke , Michael T. Azure , Douglas D. Dischino
CPC分类号： C07D237/16 , A61K49/00 , A61K49/0002 , A61K49/0052 , A61K49/10 , A61K49/22 , A61K51/04 , A61K51/0421 , A61K51/0453 , A61K51/0459 , C07B59/002
摘要： The present disclosure is directed, in part, to compounds and methods for imaging myocardial perfusion, comprising administering to a patient a contrast agent which comprises a compound that binds MC-1, and an imaging moiety, and scanning the patient using diagnostic imaging.
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公开(公告)号：US08226929B2
公开(公告)日：2012-07-24
申请号：US12014161
申请日：2008-01-15
申请人： David S. Casebier , Simon P. Robinson , Ajay Purohit , Heike S. Radeke , Michael T. Azure , Douglas D. Dischino
发明人： David S. Casebier , Simon P. Robinson , Ajay Purohit , Heike S. Radeke , Michael T. Azure , Douglas D. Dischino
IPC分类号： A61K51/00 , A61M36/14 , A01N43/58 , C07D237/00 , A61B6/00
CPC分类号： C07D237/16 , A61K49/00 , A61K49/0002 , A61K49/0052 , A61K49/10 , A61K49/22 , A61K51/04 , A61K51/0421 , A61K51/0453 , A61K51/0459 , C07B59/002
摘要： The present disclosure is directed, in part, to compounds and methods for imaging myocardial perfusion, comprising administering to a patient a contrast agent which comprises a compound that binds MC-1, and an imaging moiety, and scanning the patient using diagnostic imaging.
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