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公开(公告)号：US06558649B1
公开(公告)日：2003-05-06
申请号：US09466582
申请日：1999-12-17
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.
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公开(公告)号：US06254852B1
公开(公告)日：2001-07-03
申请号：US09356178
申请日：1999-07-16
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。
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13.发明授权
公开(公告)号：US5279811A
公开(公告)日：1994-01-18
申请号：US143561
申请日：1988-01-26
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。
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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。
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公开(公告)号：US07321045B2
公开(公告)日：2008-01-22
申请号：US10770380
申请日：2004-02-02
IPC分类号： C07D231/54 , C07D259/00 , A61K51/00 , 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.
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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。
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公开(公告)号：US06794518B1
公开(公告)日：2004-09-21
申请号：US09466588
申请日：1999-12-17
IPC分类号： C07D23154
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：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。
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18.发明授权
公开(公告)号：US5431900A
公开(公告)日：1995-07-11
申请号：US139894
申请日：1993-10-20
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 , C07C321/00
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。
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公开(公告)号：US07671191B2
公开(公告)日：2010-03-02
申请号：US11975080
申请日：2007-10-17
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。
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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
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。
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