公开(公告)号：WO2011005322A3

公开(公告)日：2011-01-13

申请号：PCT/US2010/001926

申请日：2010-07-08

申请人： LANTHEUS MEDICAL IMAGING, INC. ,  CESATI, Richard, R. ,  HARRIS, Thomas, D. ,  ROBINSON, Simon, P. ,  LOOBY, Richard, J. ,  CHEESMAN, Edward, H. ,  YALAMANCHILI, Padmaja ,  CASEBIER, David, S.

发明人： CESATI, Richard, R. ,  HARRIS, Thomas, D. ,  ROBINSON, Simon, P. ,  LOOBY, Richard, J. ,  CHEESMAN, Edward, H. ,  YALAMANCHILI, Padmaja ,  CASEBIER, David, S.

IPC分类号： C07C271/22 ,  C07D257/02 ,  A61K49/10

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.

公开(公告)号：WO2008083054A2

公开(公告)日：2008-07-10

申请号：PCT/US2007/088495

申请日：2007-12-21

申请人： BRISTOL-MYERS SQUIBB PHARMA COMPANY ,  PUROHIT, Ajay ,  HARRIS, Thomas D. ,  ROBINSON, Simon P. ,  YALAMANCHILI, Padmaja ,  AZURE, Michael T. ,  CASEBIER, David S.

发明人： PUROHIT, Ajay ,  HARRIS, Thomas D. ,  ROBINSON, Simon P. ,  YALAMANCHILI, Padmaja ,  AZURE, Michael T. ,  CASEBIER, David S.

IPC分类号： A61K51/04 ,  C07D213/75 ,  C07C275/34 ,  A61K101/02

CPC分类号： A61K51/04 ,  C07B59/001 ,  C07B2200/05 ,  C07C255/54 ,  C07C275/34 ,  C07C275/42 ,  C07D213/75 ,  C07D231/20 ,  C07D295/215

摘要： Novel β 1 adrenoreceptor ligands that find use as imaging agents within nuclear medicine applications (e.g., PET imaging and SPECT imaging) are provided. Methods of imaging, including methods of imaging congestive heart failure, are also provided. The novel compounds may exhibit high affinity and selectivity, minimal metabolism, minimal non-specific binding and have a favorable log P value ( 1 -AR selective ligands are conjugated to an imaging moiety in such a way that it does not impact the antagonist affinity and their use. In other instances, the conjugation may be directly to the antagonist at several sites that will not impact affinity. In further instances, the conjugation may be by means of a linking group, which can be used to alter the pharmacokinetics and clearance of the complex.

摘要翻译： 提供了在核医学应用（例如，PET成像和SPECT成像）中用作成像剂的新型β1肾上腺素受体配体。 还提供了成像方法，包括充血性心力衰竭成像方法。 新化合物可表现出高亲和力和选择性，最小的代谢，最小的非特异性结合，并且具有良好的对数P值（<0）。 在某些情况下，β1 -AR选择性配体以不影响拮抗剂亲合力及其用途的方式与成像部分缀合。 在其他情况下，缀合可以在不影响亲和力的几个位点处直接与拮抗剂结合。 在另外的情况下，缀合可以通过连接基团，其可用于改变复合物的药代动力学和清除率。

公开(公告)号：WO2007005491A1

公开(公告)日：2007-01-11

申请号：PCT/US2006/025298

申请日：2006-06-28

申请人： BRISTOL-MYERS SQUIBB PHARMA COMPANY ,  HARRIS, Thomas, D. ,  ROBINSON, Simon, P. ,  CESATI, Richard, R. ,  YALAMANCHILI, Padmaja

发明人： HARRIS, Thomas, D. ,  ROBINSON, Simon, P. ,  CESATI, Richard, R. ,  YALAMANCHILI, Padmaja

IPC分类号： A61K51/08 ,  A61K49/00 ,  C07K1/13

CPC分类号： A61K49/085 ,  A61K49/0002 ,  A61K49/10 ,  A61K51/088 ,  C07C243/38 ,  C07C271/22 ,  C07D209/16 ,  C07D213/82 ,  C07D257/02 ,  C07K7/02

摘要： The present disclosure is directed to diagnostic agents. More specifically, the disclosure is directed to compounds, diagnostic agents, compositions, and kits for detecting and/or imaging and/or monitoring a pathological disorder associated with coronary plaque, carotid plaque, aortic plaque, plaque of the arterial vessel, aneurism, vasculitis, and other diseases of the arterial wall. In addition, the disclosure is directed to methods of detecting and/or imaging and/or monitoring changes in the arterial wall, including expansive and constrictive remodeling, total vessel wall area, internal lumen size, and exterior artery perimeter.

摘要翻译： 本公开涉及诊断剂。 更具体地，本公开涉及用于检测和/或成像和/或监测与冠状动脉斑块，颈动脉斑块，主动脉斑块，动脉血管斑块，动脉瘤，血管炎相关的病理学障碍的化合物，诊断剂，组合物和试剂盒 ，以及其他动脉壁疾病。 此外，本公开涉及检测和/或成像和/或监测动脉壁变化的方法，包括扩张和收缩性重建，总血管壁面积，内腔尺寸和外周动脉周长。

公开(公告)号：WO2011005322A2

公开(公告)日：2011-01-13

申请号：PCT/US2010001926

申请日：2010-07-08

申请人： LANTHEUS MEDICAL IMAGING INC ,  CESATI RICHARD R ,  HARRIS THOMAS D ,  ROBINSON SIMON P ,  LOOBY RICHARD J ,  CHEESMAN EDWARD H ,  YALAMANCHILI PADMAJA ,  CASEBIER DAVID S

发明人： CESATI RICHARD R ,  HARRIS THOMAS D ,  ROBINSON SIMON P ,  LOOBY RICHARD J ,  CHEESMAN EDWARD H ,  YALAMANCHILI PADMAJA ,  CASEBIER DAVID S

IPC分类号： C07C271/22 ,  A61K49/10 ,  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。 更具体而言，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/股动脉斑块，主动脉斑块，肾动脉斑块，任何动脉血管斑块，动脉瘤，血管炎，其他疾病 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，内腔尺寸和外动脉周长的变化所指示的。

公开(公告)号：WO2005023314A1

公开(公告)日：2005-03-17

申请号：PCT/US2004/028660

申请日：2004-09-02

申请人： BRISTOL-MYERS SQUIBB COMPANY ,  HARRIS, Thomas D. ,  YALAMANCHILI, Padmaja

发明人： HARRIS, Thomas D. ,  YALAMANCHILI, Padmaja

IPC分类号： A61K49/00

CPC分类号： A61K51/0495 ,  A61K49/0002 ,  A61K51/08

摘要： Compounds for use in a diagnostic agent for detecting, imaging, and/or monitoring a pathological disorder associated with matrix metalloproteinase activity at a site of interest in a patient are disclosed. Compositions and kits containing the compounds are also disclosed. In addition, methods of detecting, imaging, and/or monitoring the presence of matrix metalloproteinase or a pathological disorder associated with matrix metalloproteinase activity in a patient are disclosed.

摘要翻译： 公开了用于诊断用于检测，成像和/或监测与患者感兴趣部位的基质金属蛋白酶活性相关的病理学障碍的化合物。 还公开了含有这些化合物的组合物和试剂盒。 此外，公开了检测，成像和/或监测基质金属蛋白酶的存在或与患者中的基质金属蛋白酶活性相关的病理学障碍的方法。

公开(公告)号：WO2009089022A1

公开(公告)日：2009-07-16

申请号：PCT/US2009/000096

申请日：2009-01-08

申请人： LANTHEUS MEDICAL IMAGING, INC. ,  CESATI, Richard, R. ,  HARRIS, Thomas, D. ,  ROBINSON, Simon, P. ,  LOOBY, Richard, J. ,  CHEESMAN, Edward, H. ,  YALAMANCHILI, Padmaja ,  CASEBIER, David, S.

发明人： CESATI, Richard, R. ,  HARRIS, Thomas, D. ,  ROBINSON, Simon, P. ,  LOOBY, Richard, J. ,  CHEESMAN, Edward, H. ,  YALAMANCHILI, Padmaja ,  CASEBIER, David, S.

IPC分类号： A61K49/10 ,  C07C271/22 ,  C07D257/02

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：WO2007005491B1

公开(公告)日：2007-04-12

申请号：PCT/US2006025298

申请日：2006-06-28

申请人： BRISTOL MYERS SQUIBB PHARMA CO ,  HARRIS THOMAS D ,  ROBINSON SIMON P ,  CESATI RICHARD R ,  YALAMANCHILI PADMAJA

发明人： HARRIS THOMAS D ,  ROBINSON SIMON P ,  CESATI RICHARD R ,  YALAMANCHILI PADMAJA

IPC分类号： A61K51/08 ,  A61K49/00 ,  C07K1/13

CPC分类号： A61K49/085 ,  A61K49/0002 ,  A61K49/10 ,  A61K51/088 ,  C07C243/38 ,  C07C271/22 ,  C07D209/16 ,  C07D213/82 ,  C07D257/02 ,  C07K7/02

摘要： The present disclosure is directed to diagnostic agents. More specifically, the disclosure is directed to compounds, diagnostic agents, compositions, and kits for detecting and/or imaging and/or monitoring a pathological disorder associated with coronary plaque, carotid plaque, aortic plaque, plaque of the arterial vessel, aneurism, vasculitis, and other diseases of the arterial wall. In addition, the disclosure is directed to methods of detecting and/or imaging and/or monitoring changes in the arterial wall, including expansive and constrictive remodeling, total vessel wall area, internal lumen size, and exterior artery perimeter.

摘要翻译： 本公开涉及诊断剂。 更具体地说，本公开涉及用于检测和/或成像和/或监测与冠状动脉斑块，颈动脉斑块，主动脉斑块，动脉血管斑块，动脉瘤，血管炎相关的病理性疾病的化合物，诊断剂，组合物和试剂盒 和其他动脉壁疾病。 另外，本公开涉及检测和/或成像和/或监测动脉壁中的变化的方法，包括膨胀和收缩性重塑，总血管壁面积，内腔尺寸和外动脉周长。

公开(公告)号：WO2008083054A3

公开(公告)日：2010-01-28

申请号：PCT/US2007088495

申请日：2007-12-21

申请人： BRISTOL MYERS SQUIBB PHARMA CO ,  PUROHIT AJAY ,  HARRIS THOMAS D ,  ROBINSON SIMON P ,  YALAMANCHILI PADMAJA ,  AZURE MICHAEL T ,  CASEBIER DAVID S

发明人： PUROHIT AJAY ,  HARRIS THOMAS D ,  ROBINSON SIMON P ,  YALAMANCHILI PADMAJA ,  AZURE MICHAEL T ,  CASEBIER DAVID S

IPC分类号： A61K51/04 ,  A61K101/02 ,  C07B59/00 ,  C07C255/54 ,  C07C275/34 ,  C07C275/42 ,  C07D213/75 ,  C07D231/20 ,  C07D295/215

CPC分类号： A61K51/04 ,  C07B59/001 ,  C07B2200/05 ,  C07C255/54 ,  C07C275/34 ,  C07C275/42 ,  C07D213/75 ,  C07D231/20 ,  C07D295/215

摘要： Novel ß1 adrenoreceptor ligands that find use as imaging agents within nuclear medicine applications (e.g., PET imaging and SPECT imaging) are provided. Methods of imaging, including methods of imaging congestive heart failure, are also provided. The novel compounds may exhibit high affinity and selectivity, minimal metabolism, minimal non-specific binding and have a favorable log P value (1-AR selective ligands are conjugated to an imaging moiety in such a way that it does not impact the antagonist affinity and their use. In other instances, the conjugation may be directly to the antagonist at several sites that will not impact affinity. In further instances, the conjugation may be by means of a linking group, which can be used to alter the pharmacokinetics and clearance of the complex.

摘要翻译： 提供了在核医学应用（例如，PET成像和SPECT成像）中用作成像剂的新型β1肾上腺素受体配体。 还提供了成像方法，包括充血性心力衰竭成像方法。 新化合物可以表现出高亲和力和选择性，最小的代谢，最小的非特异性结合并且具有良好的对数P值（1-AR选择性配体与成像部分缀合，使得其不影响拮抗剂亲和力， 在其他情况下，缀合可以在不影响亲和力的几个位点处直接与拮抗剂结合。在另外的情况下，缀合可以是连接基团，其可用于改变药代动力学和清除率 的复合体。