公开(公告)号：US20080177055A1

公开(公告)日：2008-07-24

申请号：US11975080

申请日：2007-10-17

申请人： Iain F. Pickersgill ,  Edward H. Cheesman

发明人： Iain F. Pickersgill ,  Edward H. Cheesman

IPC分类号： C07H19/16

CPC分类号： C07H19/16

摘要： Disclosed are methods for preparing 2-alkynyladenosine derivatives of formula A: or a stereoisomer, pharmaceutically acceptable salt, hydrate, solvate, acid salt hydrate or isomorphic crystalline form thereof, the method comprising the step of: contacting 2-iodoadenosine-5′-N-ethyluronamide with a compound of formula B: wherein Z is —C(═O)OR or —CH2C(═O)R, where R is a C1 to C5 alkyl, preferably The methods are useful for preparing 2-alkynyladenosine derivatives that are, in certain embodiments, adenosine receptor agonists.

摘要翻译： 公开了制备式A的2-链炔基腺苷衍生物的方法：或其立体异构体，药学上可接受的盐，水合物，溶剂化物，酸盐水合物或同构晶体形式的方法，所述方法包括以下步骤：将2-碘腺嘌呤-5'-N - 乙基脲与式B化合物反应：其中Z是-C（-O）OR或-CH 2 C（-O）R，其中R是C 1〜 优选地，该方法可用于制备在某些实施方案中为腺苷受体激动剂的2-炔基腺苷衍生物。

公开(公告)号：US07671191B2

公开(公告)日：2010-03-02

申请号：US11975080

申请日：2007-10-17

申请人： Iain F. Pickersgill ,  Edward H. Cheesman

发明人： Iain F. Pickersgill ,  Edward H. Cheesman

IPC分类号： C07H21/00

CPC分类号： C07H19/16

摘要： Disclosed are methods for preparing 2-alkynyladenosine derivatives of formula A: or a stereoisomer, pharmaceutically acceptable salt, hydrate, solvate, acid salt hydrate or isomorphic crystalline form thereof, the method comprising the step of: contacting 2-iodoadenosine-5′-N-ethyluronamide with a compound of formula B: wherein Z is —C(═O)OR or —CH2C(═O)R, where R is a C1 to C5 alkyl, preferably The methods are useful for preparing 2-alkynyladenosine derivatives that are, in certain embodiments, adenosine receptor agonists.

摘要翻译： 公开了制备式A的2-链炔基腺苷衍生物的方法：或其立体异构体，药学上可接受的盐，水合物，溶剂化物，酸盐水合物或同构晶体形式的方法，所述方法包括以下步骤：将2-碘腺嘌呤-5'-N - 乙基脲与式B化合物反应：其中Z是-C（= O）OR或-CH 2 C（= O）R，其中R是C1至C5烷基，优选该方法可用于制备2-炔基腺苷衍生物， 在某些实施方案中，腺苷受体激动剂。

公开(公告)号：US20090252676A1

公开(公告)日：2009-10-08

申请号：US12350628

申请日：2009-01-08

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 ,  C07C229/36 ,  C07D257/02 ,  C07D213/56 ,  A61K51/04 ,  A61K49/04

CPC分类号： C07D257/02 ,  A61K49/103 ,  A61K49/106 ,  A61K51/04 ,  C07C53/18 ,  C07C259/06 ,  C07C259/14 ,  C07C271/22 ,  C07C2601/14 ,  C07D209/20 ,  C07D213/56 ,  C07D403/12

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。

公开(公告)号：US06558649B1

公开(公告)日：2003-05-06

申请号：US09466582

申请日：1999-12-17

申请人： Edward H. Cheesman ,  Michael Sworin ,  Milind Rajopadhye

发明人： Edward H. Cheesman ,  Michael Sworin ,  Milind Rajopadhye

IPC分类号： A61K5100

CPC分类号： C07K9/003 ,  A61K49/0002 ,  A61K51/0497 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07K5/0207 ,  C07K5/0806 ,  C07K5/0821 ,  C07K5/1008 ,  C07K5/1024 ,  C07K7/02 ,  C07K7/06 ,  C07K7/64

摘要： The present invention describes novel compounds of the formula: (Q)d—Ln—Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention further provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia and myocardial reperfusion injury. The present invention still further provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety. The imageable moiety is a gamma ray or positron emitting radioisotope, a magnetic resonance imaging contrast agent, an X-ray contrast agent, or an ultrasound contrast agent.

公开(公告)号：US06254852B1

公开(公告)日：2001-07-03

申请号：US09356178

申请日：1999-07-16

申请人： Joseph L Glajch ,  Alan P. Carpenter, Jr. ,  Edward H. Cheesman

发明人： Joseph L Glajch ,  Alan P. Carpenter, Jr. ,  Edward H. Cheesman

IPC分类号： A61B800

CPC分类号： A61K49/225

摘要： Targeted ultrasound contrast agents are described. The contrast agents are porous particles of an inorganic material containing an entrapped gas or liquid and having an average particle diameter of about 0.05 to 500 microns. The outer surfaces of the particles incorporate a targeting ligand to target delivery of the contrast agent.

摘要翻译： 描述了靶向超声造影剂。 造影剂是含有截留气体或液体并且平均粒径为约0.05至500微米的无机材料的多孔颗粒。 颗粒的外表面包含靶向配体以靶向造影剂的递送。

公开(公告)号：US5279811A

公开(公告)日：1994-01-18

申请号：US143561

申请日：1988-01-26

申请人： Paul L. Bergstein ,  Edward H. Cheesman ,  Alan D. Watson

发明人： Paul L. Bergstein ,  Edward H. Cheesman ,  Alan D. Watson

IPC分类号： A61K51/00 ,  A61K51/04 ,  C07B59/00 ,  C07C67/00 ,  C07C313/00 ,  C07C323/25 ,  C07C323/34 ,  C07C323/58 ,  C07C323/62 ,  C07D521/00 ,  C07F11/00 ,  C07F13/00 ,  C07F15/00 ,  A61K49/02 ,  A61K43/00

CPC分类号： C07F13/005 ,  A61K51/04 ,  A61K2123/00

摘要： Radiopharmaceuticals consisting essentially of a lipophilic, charge neutral radionuclide complex of a diaminedithiol ligand having 1-4 ester groups of the formula --A--COOR where A is a straight or branched chain alkylene of 0-10 carbon atoms and R is an alkyl group of 1-10 carbon atoms are useful in radioimaging brain perfusion in primates. Ester-substituted diaminedithiols in sterile, pharmaceutically acceptable form, and kits of the diaminedithiols and sterile, non-pyrogenic reducing agents for reducing preselected radionuclides are also provided. Technetium-99m is a preferred radionuclide.

摘要翻译： 基本上由具有1-4个式-A-COOR的酯基的二硫代二醇配体的亲脂性电荷中性放射性核素复合物组成的放射性药物，其中A是0-10个碳原子的直链或支链亚烷基，R是 1-10个碳原子可用于放射性成像在灵长类动物中的脑灌注。 还提供了无菌，药学上可接受的形式的酯取代的二硫代二醇和用于还原预选的放射性核素的二硫代二醇和无菌非致热原还原剂的试剂盒。 锝-99m是优选的放射性核素。

公开(公告)号：US20130064769A1

公开(公告)日：2013-03-14

申请号：US13577674

申请日：2011-02-08

申请人： Richard R. Cesati ,  Edward H. Cheesman ,  Joel Lazewatsky ,  Heike S. Radeke ,  James F. Castner ,  Enrico Mongeau ,  Dianne D. Zdankiewicz ,  Robert Wilburn Siegler ,  Marybeth Devine

发明人： Richard R. Cesati ,  Edward H. Cheesman ,  Joel Lazewatsky ,  Heike S. Radeke ,  James F. Castner ,  Enrico Mongeau ,  Dianne D. Zdankiewicz ,  Robert Wilburn Siegler ,  Marybeth Devine

IPC分类号： A61K51/04 ,  B01J19/00 ,  C07D237/16

CPC分类号： A61K51/0459 ,  C07D237/16 ,  C07D407/12

摘要： The present invention generally relates to methods and system for the synthesis of imaging agents, and precursors thereof. The methods may exhibit improved yields and may allow for the large-scale synthesis of imaging agents, including imaging agents comprising a radioisotope (e.g., 18F). Various embodiments of the invention may be useful as sensors, diagnostic tools, and the like. In some cases, methods for evaluating perfusion, including myocardial perfusion, are provided. Synthetic methods of the invention have also been incorporated into an automated synthesis unit to prepare and purify imaging agents that comprise a radioisotope. In some embodiments, the present invention provides a novel methods and systems comprising imaging agent 1, including methods of imaging in a subject comprising administering a composition comprising imaging agent 1 to a subject by injection, infusion, or any other known method, and imaging the area of the subject wherein the event of interest is located.

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。

公开(公告)号：US06416733B1

公开(公告)日：2002-07-09

申请号：US08943659

申请日：1997-10-03

申请人： John A. Barrett ,  Edward H. Cheesman ,  Thomas D. Harris ,  Shuang Liu ,  Milind Rajopadhye ,  Michael Sworin

发明人： John A. Barrett ,  Edward H. Cheesman ,  Thomas D. Harris ,  Shuang Liu ,  Milind Rajopadhye ,  Michael Sworin

IPC分类号： A61K5100

CPC分类号： A61K51/0497 ,  A61K51/0455 ,  A61K51/0478 ,  C07C59/90 ,  C07D213/64 ,  C07D213/71 ,  C07D213/77 ,  C07D213/82 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07F13/005

摘要： The present invention provides novel radiopharmaceuticals useful for the diagnosis of infection and inflammation, reagents and kits useful for preparing the radiopharmaceuticals, methods of imaging sites of infection and/or inflammation in a patient, and methods of diagnosing diseases associated with infection or inflammation in patients in need of such diagnosis. The radiopharmaceuticals bind in vivo to the leukotriene B4 (LTB4) receptor on the surface of leukocytes which accumulate at the site of infection and inflammation. The reagents provided by this invention are also useful for the treatment of diseases associated with infection and inflammation.

摘要翻译： 本发明提供了可用于诊断感染和炎症的新型放射性药物，可用于制备放射性药物的试剂和试剂盒，成像患者感染和/或炎症部位成像方法以及诊断患者感染或炎症相关疾病的方法 需要这样的诊断。 放射性药物在体内结合白细胞表面的白细胞三烯B4（LTB4）受体，其在感染和炎症部位积聚。 本发明提供的试剂也可用于治疗与感染和炎症相关的疾病。

公开(公告)号：US09388125B2

公开(公告)日：2016-07-12

申请号：US13697287

申请日：2011-05-11

申请人： Ajay Purohit ,  Pedro Benites ,  Edward H. Cheesman ,  Joel Lazewatsky ,  L. Veronica Lee ,  Richard R. Cesati ,  Richard J. Looby ,  Heike S. Radeke

发明人： Ajay Purohit ,  Pedro Benites ,  Edward H. Cheesman ,  Joel Lazewatsky ,  L. Veronica Lee ,  Richard R. Cesati ,  Richard J. Looby ,  Heike S. Radeke

IPC分类号： A61K51/00 ,  A61M36/14 ,  C07C277/08 ,  A61K51/04 ,  C07B59/00 ,  C07C53/06 ,  C07C217/58 ,  C07C255/54 ,  C07C279/10 ,  C07C279/24 ,  C07C309/65 ,  C07C309/66 ,  C07C309/73 ,  C07C53/10 ,  C07C53/18 ,  C07C63/08 ,  C07C213/02 ,  C07C303/28 ,  C07C303/30 ,  C07C309/04 ,  C07C309/30 ,  C07C277/00

CPC分类号： C07C303/30 ,  A61K51/00 ,  A61K51/04 ,  A61K51/0406 ,  C07B59/001 ,  C07B2200/05 ,  C07C53/06 ,  C07C53/10 ,  C07C53/18 ,  C07C63/08 ,  C07C213/02 ,  C07C217/58 ,  C07C255/54 ,  C07C277/00 ,  C07C277/08 ,  C07C279/10 ,  C07C279/24 ,  C07C303/28 ,  C07C309/04 ,  C07C309/30 ,  C07C309/65 ,  C07C309/66 ,  C07C309/73 ,  C07C279/08

摘要： The present invention generally relates to novel synthetic methods, systems, kits, salts, and precursors useful in medical imaging. In some embodiments, the present invention provides compositions comprising an imaging agent precursor, which may be formed using the synthetic methods described herein. An imaging agent 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 including salt forms (e.g., ascorbate salt) 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.

摘要翻译： 本发明一般涉及可用于医学成像的新型合成方法，系统，试剂盒，盐和前体。 在一些实施方案中，本发明提供了包含可以使用本文所述的合成方法形成的成像剂前体的组合物。 可以使用本文所述的方法将成像剂转化成成像剂。 在某些情况下，成像剂富集于18F。 在一些情况下，包括盐形式的成像剂（例如抗坏血酸盐）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 。