公开(公告)号：US06689337B2

公开(公告)日：2004-02-10

申请号：US09948390

申请日：2001-09-07

Applicant: Thomas D. Harris ,  Milind Rajopadhye

Inventor： Thomas D. Harris ,  Milind Rajopadhye

IPC: A61K5100

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

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.

公开(公告)号：US06656448B1

公开(公告)日：2003-12-02

申请号：US09783249

申请日：2001-02-14

Applicant: Alan P. Carpenter, Jr. ,  Milind Rajopadhye

Inventor： Alan P. Carpenter, Jr. ,  Milind Rajopadhye

IPC: A61K4900

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：US6022523A

公开(公告)日：2000-02-08

申请号：US999400

申请日：1997-12-29

Applicant: William Frank DeGrado ,  Shaker Ahmed Mousa ,  Michael Sworin ,  John Andrew Barrett ,  Scott David Edwards ,  Thomas David Harris ,  Milind Rajopadhye ,  Shuang Liu

Inventor： William Frank DeGrado ,  Shaker Ahmed Mousa ,  Michael Sworin ,  John Andrew Barrett ,  Scott David Edwards ,  Thomas David Harris ,  Milind Rajopadhye ,  Shuang Liu

IPC: 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: C07K14/75 ,  A61K51/04 ,  A61K51/0482 ,  A61K51/082 ,  A61K51/088 ,  C07B59/008 ,  C07D213/82 ,  C07D401/12 ,  C07D401/14 ,  A61K2123/00

Abstract: This invention provides novel radiopharmaceuticals that are radiolabeled cyclic compounds containing carbocyclic or heterocyclic ring systems which act as antagonists of the platelet glycoprotein IIb/IIIa complex; to methods of using said radiopharmaceuticals as imaging agents for the diagnosis of arterial and venous thrombi; to novel reagents for the preparation of said radiopharmaceuticals; and to kits comprising said reagents.

Abstract translation: 本发明提供新的放射性药物，其是放射性标记的环状化合物，其含有作为血小板糖蛋白IIb / IIIa复合物拮抗剂的碳环或杂环系统; 使用所述放射性药物作为诊断动脉和静脉血栓的显像剂的方法; 用于制备所述放射性药物的新型试剂; 以及包含所述试剂的试剂盒。

公开(公告)号：US5879657A

公开(公告)日：1999-03-09

申请号：US218861

申请日：1994-03-28

Applicant: William Frank DeGrado ,  Shaker Ahmed Mousa ,  Michael Sworin ,  John Andrew Barrett ,  Scott David Edwards ,  Thomas David Harris ,  Milind Rajopadhye ,  Shuang Liu

Inventor： William Frank DeGrado ,  Shaker Ahmed Mousa ,  Michael Sworin ,  John Andrew Barrett ,  Scott David Edwards ,  Thomas David Harris ,  Milind Rajopadhye ,  Shuang Liu

IPC: 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 ,  A61M36/14

CPC classification number: C07K14/75 ,  A61K51/04 ,  A61K51/0482 ,  A61K51/082 ,  A61K51/088 ,  C07B59/008 ,  C07D213/82 ,  C07D401/12 ,  C07D401/14 ,  A61K2123/00

Abstract: This invention provides novel radiopharmaceuticals that are radiolabeled cyclic compounds containing carbocyclic or heterocyclic ring systems which act as antagonists of the platelet glycoprotein IIb/IIIa complex; to methods of using said radiopharmaceuticals as imaging agents for the diagnosis of arterial and venous thrombi; to novel reagents for the preparation of said radiopharmaceuticals; and to kits comprising said reagents.

公开(公告)号：US07090828B2

公开(公告)日：2006-08-15

申请号：US10348268

申请日：2003-01-21

Applicant: Edward H. Cheesman ,  John A. Barrett ,  Alan P. Carpenter, Jr. ,  Milind Rajopadhye ,  Michael Sworin

Inventor： Edward H. Cheesman ,  John A. Barrett ,  Alan P. Carpenter, Jr. ,  Milind Rajopadhye ,  Michael Sworin

IPC: A61K5/00 ,  A61M36/14

CPC classification number: 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 ,  C07K9/003

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：US06989139B2

公开(公告)日：2006-01-24

申请号：US09783248

申请日：2001-02-14

Applicant: Carl P. Decicco ,  David J. Nelson ,  John A. Barrett ,  Alan P. Carpenter Jr. ,  Jingwu Duan ,  Milind Rajopadhye

Inventor： Carl P. Decicco ,  David J. Nelson ,  John A. Barrett ,  Alan P. Carpenter Jr. ,  Jingwu Duan ,  Milind Rajopadhye

IPC: A61K31/395 ,  C07D267/00 ,  C07D401/12 ,  C07D413/12 ,  C07F9/6527

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，本发明描述了包含1-10个靶向部分的新化合物; 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的新组合物，试剂盒及其在治疗与MMP相关的疾病中的用途。

公开(公告)号：US20060003926A1

公开(公告)日：2006-01-05

申请号：US10622246

申请日：2003-07-18

Applicant: Milind Rajopadhye ,  D. Edwards ,  John Barrett ,  Alan Carpenter ,  Thomas Harris ,  Stuart Heminway ,  Shuang Liu ,  Singh Prahlad

Inventor： Milind Rajopadhye ,  D. Edwards ,  John Barrett ,  Alan Carpenter ,  Thomas Harris ,  Stuart Heminway ,  Shuang Liu ,  Singh Prahlad

IPC: A61K38/12 ,  C07K7/64

CPC classification number: C07D401/14 ,  A61K38/00 ,  A61K45/06 ,  A61K49/0002 ,  A61K49/227 ,  A61K51/082 ,  A61K51/088 ,  C07D401/12 ,  C07K7/06 ,  C07K7/08 ,  C07K7/64

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 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。 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：US06818201B2

公开(公告)日：2004-11-16

申请号：US10306244

申请日：2002-11-26

Applicant: Edward H. Cheesman ,  Michael Sworin ,  Milind Rajopadhye

Inventor： Edward H. Cheesman ,  Michael Sworin ,  Milind Rajopadhye

IPC: A61K4900

CPC classification number: 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

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：可用于癌症的诊断和治疗，对患者肿瘤成像的方法，以及治疗患者癌症的方法。 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：US06569402B1

公开(公告)日：2003-05-27

申请号：US09599365

申请日：2000-06-21

Applicant: Edward H. Cheesman ,  John A. Barrett ,  Alan P. Carpenter, Jr. ,  Milind Rajopadhye ,  Michael Sworin

Inventor： Edward H. Cheesman ,  John A. Barrett ,  Alan P. Carpenter, Jr. ,  Milind Rajopadhye ,  Michael Sworin

IPC: A61K500

CPC classification number: 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 ,  C07K9/003

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：可用于癌症的诊断和治疗，对患者肿瘤成像的方法，以及治疗患者癌症的方法。 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：US06524554B1

公开(公告)日：2003-02-25

申请号：US09285280

申请日：1999-04-02

Applicant: David Scott Edwards ,  Milind Rajopadhye

Inventor： David Scott Edwards ,  Milind Rajopadhye

IPC: A61K4904

CPC classification number: C07K7/06 ,  A61K51/088

Abstract: The present invention provides novel radiopharmaceuticals comprising one to three pentapeptides, X1X2X3X4X5, independently attached to a metal chelator or bonding moiety, Ch, to which is attached a Tc-99m, Re-186, or Re-188, optionally further comprising a linking group, Ln, between-the peptides and the chelator or bonding moiety. The pentapeptide sequence binds to the tuftsin receptor and is attached at the N-terminus to Ln or Ch. These radiopharmaceuticals are 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.

Abstract translation: 本发明提供了包含一至三个五肽X1X2X3X4X5的新型放射性药物，其独立地连接到金属螯合剂或结合部分Ch上，其连接有Tc-99m，Re-186或Re-188，任选地还包含连接基团 ，Ln，肽与螯合剂或结合部分之间。 五肽序列与簇绒蛋白受体结合，并在N末端连接至Ln或Ch。 这些放射性药物可用于感染和炎症的诊断，可用于制备放射性药物的试剂和试剂盒，成像患者感染和/或炎症部位的成像方法，以及诊断与感染或炎症有关的疾病的方法 这样的诊断。