公开(公告)号：US08455651B2

公开(公告)日：2013-06-04

申请号：US13450003

申请日：2012-04-18

Applicant: Milind Rajopadhye ,  Narasimhachari Narayanan

Inventor： Milind Rajopadhye ,  Narasimhachari Narayanan

IPC: C07D401/06

CPC classification number: A61K49/0032 ,  A61K49/0021 ,  C07D401/06 ,  C07D401/14 ,  C07D417/06 ,  C09B23/0008 ,  C09B23/083

Abstract: This invention relates to new fluorescent chemical entities, including fluorescent molecules that comprise a carboxyl or carbonyl functionalized pyridine moiety. This invention also relates to the corresponding reactive versions of such molecules. This invention also relates to the corresponding conjugates with moieties such as peptides, proteins, various biomolecules, carbocyclic and heterocyclic compounds, sugars, and their uses thereof.

Abstract translation: 本发明涉及新的荧光化学实体，包括含有羧基或羰基官能化的吡啶部分的荧光分子。 本发明还涉及这种分子的相应的反应性形式。 本发明还涉及与诸如肽，蛋白质，各种生物分子，碳环和杂环化合物，糖等部分的相应缀合物及其用途。

公开(公告)号：US07947256B2

公开(公告)日：2011-05-24

申请号：US12065385

申请日：2006-09-01

Applicant: Milind Rajopadhye ,  Kevin Groves

Inventor： Milind Rajopadhye ,  Kevin Groves

IPC: A61K49/04

CPC classification number: G01N33/582 ,  A61K49/0032 ,  A61K49/0052 ,  C09B23/0008 ,  C09B23/0066 ,  C09B23/083 ,  C09B23/086 ,  G01N33/533

Abstract: This invention relates to new carbocyanine fluorophores comprising a biomolecule targeting moiety containing 1-6 aromatic moieties, wherein the targeting moiety is designed to attach to biocompatible molecules to form in vivo optical imaging agents.

Abstract translation: 本发明涉及包含含有1-6个芳族部分的生物分子靶向部分的新的碳代花青荧光团，其中靶向部分设计成附着于生物相容性分子以形成体内光学成像剂。

公开(公告)号：US20100172841A1

公开(公告)日：2010-07-08

申请号：US12555754

申请日：2009-09-08

Applicant: Jeffrey D. Peterson ,  Milind Rajopadhye

Inventor： Jeffrey D. Peterson ,  Milind Rajopadhye

IPC: A61K49/00 ,  C07H15/00 ,  C12N5/07

CPC classification number: A61B5/0059 ,  A61B5/411 ,  A61B5/415 ,  A61B5/418 ,  A61B5/4504 ,  A61B5/4528 ,  A61K49/0032 ,  A61K49/0097

Abstract: The invention provides viable near-infrared fluorochrome labeled cells and in vivo imaging methods for tracking, locating or determining the quantity of the viable cells once they have been administered to a subject.

Abstract translation: 本发明提供了可行的近红外荧光染料标记细胞和体内成像方法，用于跟踪，定位或确定活细胞一旦施用于受试者的数量。

公开(公告)号：US07018611B2

公开(公告)日：2006-03-28

申请号：US10281015

申请日：2002-10-26

Applicant: Thomas D. Harris ,  John A. Barrett ,  Alan P. Carpenter, Jr. ,  Milind Rajopadhye

Inventor： Thomas D. Harris ,  John A. Barrett ,  Alan P. Carpenter, Jr. ,  Milind Rajopadhye

IPC: A61K51/00 ,  A61M36/14

CPC classification number: A61K49/0002 ,  A61K49/04 ,  A61K49/085 ,  A61K49/10 ,  A61K49/223 ,  A61K51/0455 ,  A61K51/0459 ,  A61K51/0497 ,  C07D401/12 ,  C07D401/14

Abstract: 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.

Abstract translation: 本发明描述了新的下式化合物：<？in-line-formula description =“In-line Formulas”end =“lead”？>（Q） 对于癌症的诊断和治疗有用的<？in-line-formula description =“在线公式”end =“tail”？>，肿瘤成像方法 患者，以及在患者中治疗癌症的方法。 本发明还提供了可用于监测治疗性血管生成治疗和破坏新的血管生成脉管系统的新型化合物。 本发明还提供可用于成像动脉粥样硬化，再狭窄，心脏缺血和心肌再灌注损伤的新型化合物。 本发明还提供了可用于治疗类风湿性关节炎的新化合物。 药物由与血管发生期间上调的受体结合的靶向部分，任选的连接基团和治疗有效的放射性同位素或诊断上有效的可成像部分组成。 可成像部分是伽马射线或正电子发射放射性同位素，磁共振成像造影剂，X射线造影剂或超声造影剂。

公开(公告)号：US20050287074A1

公开(公告)日：2005-12-29

申请号：US11194845

申请日：2005-08-01

Applicant: Alan Carpenter ,  Milind Rajopadhye

Inventor： Alan Carpenter ,  Milind Rajopadhye

IPC: A61K38/00 ,  A61K47/48 ,  A61K49/00 ,  A61K49/04 ,  A61K49/08 ,  A61K51/00 ,  A61K51/04 ,  C07F5/00 ,  C07F9/6527 ,  C07K5/06 ,  C07K5/065

CPC classification number: A61K49/00 ,  A61K38/00 ,  A61K49/0002 ,  A61K49/085 ,  A61K49/10 ,  A61K49/223 ,  A61K51/0497 ,  C07F9/6527 ,  C07K5/06026 ,  C07K5/06078 ,  C07K5/06191

Abstract: Thus the present invention describes diagnostic agents comprising a diagnostic metal and a compound, wherein the compound comprises: 1-10 targeting moieties; a chelator; and 0-1 linking groups between the targeting moiety and chelator; wherein the targeting moiety is a matrix metalloproteinase inhibitor; and wherein the chelator is capable of conjugating to the diagnostic metal. The present invention also provides novel compositions of the compounds of the invention, kits, and their uses in diagnosis of diseases associated with MMPs.

Abstract translation: 因此，本发明描述了包含诊断金属和化合物的诊断剂，其中所述化合物包含：1-10个靶向部分; 螯合剂 和靶向部分和螯合剂之间的0-1个连接基团; 其中靶向部分是基质金属蛋白酶抑制剂; 并且其中螯合剂能够与诊断金属共轭。 本发明还提供本发明化合物，试剂盒及其在诊断与MMP相关的疾病中的用途的新组合物。

公开(公告)号：US20050154185A1

公开(公告)日：2005-07-14

申请号：US10770380

申请日：2004-02-02

Applicant: Milind Rajopadhye ,  Thomas Harris ,  Edward Cheesman

Inventor： Milind Rajopadhye ,  Thomas Harris ,  Edward Cheesman

IPC: A61K49/00 ,  C07D401/12 ,  C07D401/14 ,  C07K5/02 ,  C07K5/06 ,  C07K5/078 ,  C07K5/12 ,  C07D471/02 ,  C07D487/02

CPC classification number: C07D401/14 ,  A61K49/0002 ,  C07D401/12 ,  C07K5/0205 ,  C07K5/0215 ,  C07K5/06139 ,  C07K5/06191

Abstract: 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 also provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia, and myocardial reperfusion injury. The present invention also 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.

Abstract translation: 本发明描述了新的下式化合物：<？in-line-formula description =“In-line Formulas”end =“lead”？>（Q） 对于癌症的诊断和治疗有用的<？in-line-formula description =“在线公式”end =“tail”？>，肿瘤成像方法 患者，以及在患者中治疗癌症的方法。 本发明还提供了可用于监测治疗性血管生成治疗和破坏新的血管生成脉管系统的新型化合物。 本发明还提供了用于成像动脉粥样硬化，再狭窄，心脏缺血和心肌再灌注损伤的新型化合物。 本发明还提供了可用于治疗类风湿性关节炎的新化合物。 药物由与血管发生期间上调的受体结合的靶向部分，任选的连接基团和治疗有效的放射性同位素或诊断上有效的可成像部分组成。 可成像部分是伽马射线或正电子发射放射性同位素，磁共振成像造影剂，X射线造影剂或超声造影剂。

公开(公告)号：US20050025702A1

公开(公告)日：2005-02-03

申请号：US09783248

申请日：2001-02-14

Applicant: Carl Decicco ,  David Nelson ,  John Barrett ,  Alan Carpenter ,  Jingwu Duan ,  Milind Rajopadhye

Inventor： Carl Decicco ,  David Nelson ,  John Barrett ,  Alan Carpenter ,  Jingwu Duan ,  Milind Rajopadhye

IPC: A61K49/00 ,  A61K49/14 ,  A61K51/08 ,  C07D207/26 ,  C07D213/82 ,  C07D267/00 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07F9/6527 ,  A61K51/00

CPC classification number: A61K49/14 ,  A61K49/0002 ,  A61K49/085 ,  A61K49/10 ,  A61K51/088 ,  C07D207/26 ,  C07D213/82 ,  C07D267/00 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07F9/6527

Abstract: Thus the present invention describes novel compounds comprising: 1-10 targeting moieties; a chelator (Ch); and 0-1 linking groups (Ln) between the targeting moiety and chelator; wherein the targeting moiety is a matrix metalloproteinase inhibitor; and wherein the chelator is capable of conjugating to a cytotoxic radioisotope. The present invention also provides novel compositions of the compounds of the invention, kits, and their uses in treatment of diseases associated with MMPs.

Abstract translation: 因此，本发明描述了新的化合物，其包含：1-10个靶向部分; 螯合剂（Ch）; 和靶向部分和螯合剂之间的0-1个连接基团（Ln）; 其中靶向部分是基质金属蛋白酶抑制剂; 并且其中所述螯合剂能够缀合到细胞毒性放射性同位素。 本发明还提供本发明化合物，试剂盒及其用于治疗与MMP相关的疾病的新型组合物。

公开(公告)号：US06416733B1

公开(公告)日：2002-07-09

申请号：US08943659

申请日：1997-10-03

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

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

IPC: A61K5100

CPC classification number: 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

Abstract: 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.

Abstract translation: 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：US6015904A

公开(公告)日：2000-01-18

申请号：US956313

申请日：1997-10-23

Applicant: Michael Sworin ,  Milind Rajopadhye ,  Thomas David Harris ,  David Scott Edwards ,  Edward Hollister Cheesman ,  Shuang Liu

Inventor： Michael Sworin ,  Milind Rajopadhye ,  Thomas David Harris ,  David Scott Edwards ,  Edward Hollister Cheesman ,  Shuang Liu

IPC: A61K31/00 ,  A61K38/12 ,  A61K49/04 ,  A61K51/00 ,  A61K51/04 ,  A61K51/08 ,  C07B59/00 ,  C07D213/82 ,  C07D257/00 ,  C07D259/00 ,  C07D277/60 ,  C07D401/00 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07K5/10 ,  C07K5/103 ,  C07K7/64 ,  C07K14/75 ,  C07K17/02

CPC classification number: C07D213/82 ,  A61K51/04 ,  A61K51/082 ,  A61K51/088 ,  C07B59/008 ,  C07D401/12 ,  C07D401/14 ,  C07K14/75 ,  A61K2123/00

Abstract: This invention provides novel reagents for the preparation of radiopharmaceuticals useful as imaging agents for the diagnosis of cardiovascular disorders, infection, inflammation and cancer, diagnostic kits comprising said reagents and intermediate compounds useful for the preparation of said reagents. The reagents are comprised of stable hydrazone modified biologically active molecules that react with gamma emitting radioisotopes to form radiopharmaceuticals that selectively localize at sites of disease and thus allow an image to be obtained of the loci using gamma scintigraphy.

Abstract translation: 本发明提供用于制备用作诊断心血管疾病，感染，炎症和癌症的成像剂的放射性药物的新型试剂，包含所述试剂的诊断试剂和可用于制备所述试剂的中间体化合物。 试剂由稳定的腙修饰的生物活性分子组成，其与γ发射放射性同位素反应形成放射性药物，其选择性地定位在疾病部位，从而允许使用γ闪烁扫描获得基因座的图像。

公开(公告)号：US5961952A

公开(公告)日：1999-10-05

申请号：US785399

申请日：1997-01-23

Applicant: Paul David Crane ,  David Charles Onthank ,  Milind Rajopadhye

Inventor： Paul David Crane ,  David Charles Onthank ,  Milind Rajopadhye

IPC: A61K51/04 ,  A61K51/00 ,  A61M36/14

CPC classification number: A61K51/0476

Abstract: A novel method of diagnosing or radioimaging breast tumors using .sup.99m Tc- or .sup.186/188 Re-tertiary-butyl isonitrile complex and a kit for diagnosing or radioimaging breast tumors containing tertiary-butyl isonitrile and a solubilization aid are presented.

Abstract translation: 提出了使用99mTc-或186 / 188Re-叔丁基异腈络合物诊断或放射成像乳腺肿瘤的新方法，以及用于诊断或放射成像包含叔丁基异腈和增溶助剂的乳腺肿瘤的试剂盒。