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1. 发明授权

US07090828B2 Vitronectin receptor antagonist pharmaceuticals 失效
标题翻译： Vitronectin受体拮抗剂药物
公开(公告)号：US07090828B2
公开(公告)日：2006-08-15
申请号：US10348268
申请日：2003-01-21
申请人： Edward H. Cheesman , John A. Barrett , Alan P. Carpenter, Jr. , Milind Rajopadhye , Michael Sworin
发明人： Edward H. Cheesman , John A. Barrett , Alan P. Carpenter, Jr. , Milind Rajopadhye , Michael Sworin
IPC分类号： A61K5/00 , A61M36/14
CPC分类号： 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
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.
摘要翻译：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。

2. 发明授权

US06569402B1 Vitronectin receptor antagonist pharmaceuticals 失效
标题翻译： Vitronectin受体拮抗剂药物
公开(公告)号：US06569402B1
公开(公告)日：2003-05-27
申请号：US09599365
申请日：2000-06-21
申请人： Edward H. Cheesman , John A. Barrett , Alan P. Carpenter, Jr. , Milind Rajopadhye , Michael Sworin
发明人： Edward H. Cheesman , John A. Barrett , Alan P. Carpenter, Jr. , Milind Rajopadhye , Michael Sworin
IPC分类号： A61K500
CPC分类号： 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
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.
摘要翻译：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。

3. 发明授权

US07332149B1 Vitronectin receptor antagonist pharmaceuticals 失效
标题翻译： Vitronectin受体拮抗剂药物
公开(公告)号：US07332149B1
公开(公告)日：2008-02-19
申请号：US09599890
申请日：2000-06-21
申请人： Milind Rajopadhye , John A. Barrett , Alan P. Carpenter, Jr. , Edward H. Cheesman , Thomas D. Harris
发明人： Milind Rajopadhye , John A. Barrett , Alan P. Carpenter, Jr. , Edward H. Cheesman , Thomas D. Harris
IPC分类号： A61K51/00 , A61K51/04 , A61K51/06 , A61M36/00 , A61P35/00 , C07D231/54 , C07D259/00 , C07D403/14 , A61K31/416 , A61K31/33
CPC分类号： C07D401/14 , A61K49/0002 , C07D401/12 , C07K5/0205 , C07K5/0215 , C07K5/06139 , C07K5/06191
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 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.
摘要翻译：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。

4. 发明授权

US06416733B1 Radiopharmaceuticals for imaging infection and inflammation 失效
标题翻译：用于成像感染和炎症的放射性药物
公开(公告)号：US06416733B1
公开(公告)日：2002-07-09
申请号：US08943659
申请日：1997-10-03
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。

5. 发明授权

US07018611B2 Vitronectin receptor antagonist pharmaceuticals 失效
标题翻译： Vitronectin受体拮抗剂药物
公开(公告)号：US07018611B2
公开(公告)日：2006-03-28
申请号：US10281015
申请日：2002-10-26
申请人： Thomas D. Harris , John A. Barrett , Alan P. Carpenter, Jr. , Milind Rajopadhye
发明人： Thomas D. Harris , John A. Barrett , Alan P. Carpenter, Jr. , Milind Rajopadhye
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： A61K49/0002 , A61K49/04 , A61K49/085 , A61K49/10 , A61K49/223 , A61K51/0455 , A61K51/0459 , A61K51/0497 , C07D401/12 , C07D401/14
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.
摘要翻译：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。

6. 发明授权

US06511649B1 Vitronectin receptor antagonist pharmaceuticals 失效
标题翻译： Vitronectin受体拮抗剂药物
公开(公告)号：US06511649B1
公开(公告)日：2003-01-28
申请号：US09599364
申请日：2000-06-21
申请人： Thomas D. Harris , John A. Barrett , Alan P. Carpenter, Jr. , Milind Rajopadhye
发明人： Thomas D. Harris , John A. Barrett , Alan P. Carpenter, Jr. , Milind Rajopadhye
IPC分类号： A61K5100
CPC分类号： A61K49/0002 , A61K49/04 , A61K49/085 , A61K49/10 , A61K49/223 , A61K51/0455 , A61K51/0459 , A61K51/0497 , C07D401/12 , C07D401/14
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.
摘要翻译：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。

7. 发明授权

US07052673B2 Pharmaceuticals for the imaging of angiogenic disorders 失效
标题翻译：用于血管生成障碍成像的药物
公开(公告)号：US07052673B2
公开(公告)日：2006-05-30
申请号：US10622246
申请日：2003-07-18
申请人： Milind Rajopadhye , D. Scott Edwards , John A. Barrett , Alan P. Carpenter, Jr. , Thomas D Harris , Stuart D Heminway , Shuang Liu , Singh R Prahlad
发明人： Milind Rajopadhye , D. Scott Edwards , John A. Barrett , Alan P. Carpenter, Jr. , Thomas D Harris , Stuart D Heminway , Shuang Liu , Singh R Prahlad
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： C07D401/14 , A61K38/00 , A61K45/06 , A61K49/0002 , A61K49/227 , A61K51/082 , A61K51/088 , C07D401/12 , C07K7/06 , C07K7/08 , 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 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.
摘要翻译：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。

8. 发明授权

US06800273B2 Pharmaceuticals for the imaging of angiogenic disorders 失效
标题翻译：用于血管生成障碍成像的药物
公开(公告)号：US06800273B2
公开(公告)日：2004-10-05
申请号：US10342081
申请日：2003-01-14
申请人： Milind Rajopadhye , D. Scott Edwards , John A. Barrett , Alan P. Carpenter, Jr. , Thomas D. Harris , Stuart J. Heminway , Shuang Liu , Prahlad R. Singh
发明人： Milind Rajopadhye , D. Scott Edwards , John A. Barrett , Alan P. Carpenter, Jr. , Thomas D. Harris , Stuart J. Heminway , Shuang Liu , Prahlad R. Singh
IPC分类号： A61K5100
CPC分类号： C07D401/14 , A61K38/00 , A61K45/06 , A61K49/0002 , A61K49/227 , A61K51/082 , A61K51/088 , C07D401/12 , C07K7/06 , C07K7/08 , 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 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.
摘要翻译：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。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。

9. 发明授权

US06537520B1 Pharmaceuticals for the imaging of angiogenic disorders 失效
标题翻译：用于血管生成障碍成像的药物
公开(公告)号：US06537520B1
公开(公告)日：2003-03-25
申请号：US09599295
申请日：2000-06-21
申请人： Milind Rajopadhye , D. Scott Edwards , John A. Barrett , Alan P. Carpenter, Jr. , Thomas D. Harris , Stuart J. Heminway , Shuang Liu , Prahlad R. Singh
发明人： Milind Rajopadhye , D. Scott Edwards , John A. Barrett , Alan P. Carpenter, Jr. , Thomas D. Harris , Stuart J. Heminway , Shuang Liu , Prahlad R. Singh
IPC分类号： A61K5100
CPC分类号： C07D401/14 , A61K38/00 , A61K45/06 , A61K49/0002 , A61K49/227 , A61K51/082 , A61K51/088 , C07D401/12 , C07K7/06 , C07K7/08 , 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 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.
摘要翻译：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。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。

10. 发明授权

US06989139B2 Matrix metalloproteinase inhibitors 失效
标题翻译：基质金属蛋白酶抑制剂
公开(公告)号：US06989139B2
公开(公告)日：2006-01-24
申请号：US09783248
申请日：2001-02-14
申请人： Carl P. Decicco , David J. Nelson , John A. Barrett , Alan P. Carpenter Jr. , Jingwu Duan , Milind Rajopadhye
发明人： Carl P. Decicco , David J. Nelson , John A. Barrett , Alan P. Carpenter Jr. , Jingwu Duan , Milind Rajopadhye
IPC分类号： A61K31/395 , C07D267/00 , C07D401/12 , C07D413/12 , C07F9/6527
CPC分类号： A61K49/14 , A61K49/0002 , A61K49/085 , A61K49/10 , A61K51/088 , C07D207/26 , C07D213/82 , C07D267/00 , C07D401/12 , C07D401/14 , C07D413/12 , C07F9/6527
摘要： 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.
摘要翻译：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。

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