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61. 发明申请

US20090324495A1 COMPOUNDS AND METHODS FOR ENZYME-MEDIATED TUMOR IMAGING AND THERAPY 有权
标题翻译：用于酶介导的肿瘤成像和治疗的化合物和方法
公开(公告)号：US20090324495A1
公开(公告)日：2009-12-31
申请号：US12476102
申请日：2009-06-01
申请人： Amin I. Kassis
发明人： Amin I. Kassis
IPC分类号： A61K51/00 , C07D239/72 , A61K31/517 , A61K38/16 , C07K7/00
CPC分类号： A61K51/0459 , C07D239/74 , C07D239/86 , C07D239/91 , C07D239/94
摘要： The invention provides methods and compositions, e.g., for tumor imaging and therapy.
摘要翻译：本发明提供了方法和组合物，例如用于肿瘤成像和治疗。

62. 发明申请

US20090185975A1 DIAGNOSTIC PROBE FOR CONFORMATION DISEASE 审中-公开
标题翻译：诊断疾病诊断探针
公开(公告)号：US20090185975A1
公开(公告)日：2009-07-23
申请号：US12097842
申请日：2006-12-25
申请人： Yukitsuka Kudo , Hiroyuki Arai , Nobuyuki Okamura , Masahiro Maruyama , Syozo Furumoto , Katsumi Doh-Ura
发明人： Yukitsuka Kudo , Hiroyuki Arai , Nobuyuki Okamura , Masahiro Maruyama , Syozo Furumoto , Katsumi Doh-Ura
IPC分类号： A61K49/00 , C12Q1/00 , A61K31/553 , A61K31/535 , A61K31/505 , C07D471/04
CPC分类号： C07D417/06 , A61K51/04 , A61K51/0431 , A61K51/0446 , A61K51/0453 , A61K51/0455 , A61K51/0459 , A61K51/0463 , A61K51/0465 , A61K51/0468
摘要： The invention provides a probe compound useful for early diagnosis of conformation disease, a composition and a kit comprising it for diagnosis for conformation disease, and a medical composition for treatment and/or prevention of conformation disease.
摘要翻译：本发明提供了可用于构象疾病早期诊断的探针化合物，组合物和包含其用于构象疾病诊断的试剂盒，以及用于治疗和/或预防构象疾病的医药组合物。

63. 发明授权

US07470698B2 Adenosine A3 receptor modulators 有权
标题翻译：腺苷A3受体调节剂
公开(公告)号：US07470698B2
公开(公告)日：2008-12-30
申请号：US11774784
申请日：2007-07-09
申请人： Pier Giovanni Baraldi , Pier Andrea Borea
发明人： Pier Giovanni Baraldi , Pier Andrea Borea
IPC分类号： A01N43/54 , A61K31/505 , C07D239/00 , C07D471/00 , C07D487/00 , C07D491/00
CPC分类号： A61K49/0052 , A61K31/519 , A61K49/0021 , A61K51/0459 , A61K51/0491 , C07B2200/05 , C07D471/14 , C07D487/14 , G01N33/57492 , G01N2333/726 , G01N2500/00
摘要： The compounds of the following formula: wherein R, R2, R3 and A have the meanings given in the specification, are endowed with selective A3 adenosine receptor antagonist activity. These compounds can be used in a pharmaceutical composition to treat disorders caused by excessive activation of the A3 receptor, or can be used in a diagnostic application to determine the relative binding of other compounds to the A3 receptor. The compounds can be labeled, for example with fluorescent or radiolabels, and the labels used in vivo or in vitro to determine the presence of tumor cells which possess a high concentration of adenosine A3 receptors.
摘要翻译：下式的化合物：其中R，R2，R3和A具有说明书中给出的含义，具有选择性的A3腺苷受体拮抗剂活性。这些化合物可用于药物组合物中以治疗由A3受体的过度活化引起的疾病，或可用于诊断应用以确定其它化合物与A3受体的相对结合。化合物可以用例如荧光或放射性标记物标记，以及在体内或体外用于测定具有高浓度腺苷A3受体的肿瘤细胞的存在的标记物。

64. 发明授权

US07425318B2 Amyloid plaque aggregation inhibitors and diagnostic imaging agents 有权
标题翻译：淀粉样蛋白斑块聚集抑制剂和诊断显像剂
公开(公告)号：US07425318B2
公开(公告)日：2008-09-16
申请号：US11203429
申请日：2005-08-15
申请人： Hank F. Kung , Mei-Ping Kung , Zhi-Ping Zhuang
发明人： Hank F. Kung , Mei-Ping Kung , Zhi-Ping Zhuang
IPC分类号： A61K49/00
CPC分类号： C07F13/005 , A61K51/0453 , A61K51/0455 , A61K51/0459 , A61K51/0468 , A61K51/0478 , A61K51/0497 , C07D471/04 , C07F7/2208
摘要： This invention relates to a method of imaging amyloid deposits and to labeled compounds, and methods of making labeled compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.
摘要翻译：本发明涉及成像淀粉样沉积物和标记化合物的方法，以及制备用于成像淀粉样沉积物的标记化合物的方法。本发明还涉及化合物和制备用于抑制淀粉样蛋白聚集以形成淀粉样沉积物的化合物的方法，以及将治疗剂递送至淀粉样沉积物的方法。

65. 发明申请

US20080219922A1 Alzheimer's Disease Imaging Agents 审中-公开
标题翻译：阿尔茨海默病成像剂
公开(公告)号：US20080219922A1
公开(公告)日：2008-09-11
申请号：US12066042
申请日：2006-09-11
申请人： Mark M. Goodman , Fanxing Zeng
发明人： Mark M. Goodman , Fanxing Zeng
IPC分类号： A61K51/04 , C07D237/26 , A61K31/5025 , A61P25/28 , C07D471/04 , A61K31/437
CPC分类号： C07D487/04 , A61K51/0455 , A61K51/0459 , A61K51/0461 , C07B2200/05
摘要： This invention provides compounds and methods of imaging amyloid deposits using radiolabeled compounds. This invention also provides a method of inhibiting the aggregation of amyloid proteins to form amyloid plaques or deposits, a method of determining a therapeutic compound's ability to inhibit aggregation of amyloid protein, and a method of delivering a therapeutic agent to amyloid deposits.
摘要翻译：本发明提供使用放射性标记的化合物成像淀粉样沉积物的化合物和方法。本发明还提供了抑制淀粉样蛋白聚集以形成淀粉样蛋白斑或沉积物的方法，确定治疗化合物抑制淀粉样蛋白聚集的能力的方法以及将治疗剂递送至淀粉样沉积物的方法。

66. 发明申请

US20080193380A1 Radiolabeled selective androgen receptor modulators and their use in prostate cancer imaging and therapy 审中-公开
标题翻译：放射性标记的选择性雄激素受体调节剂及其在前列腺癌成像和治疗中的应用
公开(公告)号：US20080193380A1
公开(公告)日：2008-08-14
申请号：US11984838
申请日：2007-11-21
申请人： James T. Dalton , Duane D. Miller , Leonid I. Kirkovsky , Arnab Mukherjee
发明人： James T. Dalton , Duane D. Miller , Leonid I. Kirkovsky , Arnab Mukherjee
IPC分类号： A61K51/04 , C07C233/07
CPC分类号： A61K51/04 , A61K51/0402 , A61K51/0406 , A61K51/0446 , A61K51/0455 , A61K51/0459
摘要： Provided is a class of radiolabeled androgen receptor targeting agents (ARTA), useful for prostate cancer imaging and in treating or preventing prostate cancer. The agents define a new subclass of radiolabeled compounds, which are selective androgen receptor modulators (SARM), which demonstrate antiandrogenic activity of a nonsteroidal ligand for the androgen receptor, and/or which bind irreversibly to the androgen receptor. The present invention further provides methods for a) imaging of cancer in a subject, b) imaging an androgen receptor-containing tissue in a subject, c) in-vivo imaging in a subject, d) treating a subject suffering from prostate cancer, e) delaying the progression of prostate cancer in a subject suffering from prostate cancer, f) preventing the recurrence of prostate cancer in a subject suffering from prostate cancer, and g) treating the recurrence of prostate cancer in a subject suffering from prostate cancer, which comprise using the radiolabeled compounds of the present invention. The present invention further provides a method of producing the radiolabeled SARM compounds, and precursor compounds useful in the preparation of the radiolabeled SARM compounds.
摘要翻译：提供了一类用于前列腺癌成像和治疗或预防前列腺癌的放射性标记的雄激素受体靶向剂（ARTA）。这些试剂定义了一种放射性标记化合物的新亚类，它们是选择性雄激素受体调节剂（SARM），其表现出非甾类配体对雄激素受体的抗雄激素活性和/或不依赖于雄激素受体的结合。本发明进一步提供a）用于a）成像受试者中的癌症的方法，b）使受试者中含有雄激素受体的组织成像，c）受试者体内成像，d）治疗患有前列腺癌的受试者，e ）延迟患有前列腺癌的受试者的前列腺癌的进展，f）预防患有前列腺癌的受试者中前列腺癌的复发，以及g）治疗患有前列腺癌的受试者中前列腺癌的复发，其包括使用本发明的放射性标记的化合物。本发明还提供了一种制备放射性标记的SARM化合物的方法，以及可用于制备放射性标记的SARM化合物的前体化合物。

67. 发明申请

US20080056990A1 Polyalkylene glycol derivatives of inhibitors of epidermal growth factor receptor tyrosine kinase 有权
标题翻译：表皮生长因子受体酪氨酸激酶抑制剂的聚亚烷基二醇衍生物
公开(公告)号：US20080056990A1
公开(公告)日：2008-03-06
申请号：US11714760
申请日：2007-03-07
申请人： Eyal Mishani , Samar Dissoki , Galith Abourbeh , Alexander Levitzki
发明人： Eyal Mishani , Samar Dissoki , Galith Abourbeh , Alexander Levitzki
IPC分类号： A61K31/517 , A61B5/055 , A61K51/04 , A61P35/00 , C07D239/72 , C12N5/00
CPC分类号： C07D239/94 , A61K51/0459 , C07B2200/05
摘要： Novel epidermal growth factor receptor tyrosine kinase (EGFR-TK) inhibitors, pharmaceutical compositions including same and their use in the treatment of EGFR-TK related diseases or disorders are disclosed. Novel radiolabeled EGFR-TK inhibitors as their use as biomarkers for medicinal radioimaging such as Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) and as radiopharmaceuticals for radiotherapy are further disclosed. The disclosed EGFR-TK inhibitors comprise a polyalkylene glycol moiety and/or a hydroxy-containing moiety and are characterized by improved solubility, biostability and bioavailability. Processes of preparing the disclosed EGFR-TK inhibitors and of radiolabeling same, via, for example, one-step radiosyntheses, are also disclosed.
摘要翻译：公开了新型表皮生长因子受体酪氨酸激酶（EGFR-TK）抑制剂，包含其的药物组合物及其在治疗EGFR-TK相关疾病或病症中的用途。新型放射性标记的EGFR-TK抑制剂作为药物放射成像的生物标志物，如正电子发射断层扫描（PET）和单光子发射计算机断层扫描（SPECT）和放射治疗放射性药物的放射治疗进一步披露。所公开的EGFR-TK抑制剂包含聚亚烷基二醇部分和/或含羟基的部分，其特征在于改善的溶解度，生物稳定性和生物利用度。还公开了通过例如一步放射合成来制备所公开的EGFR-TK抑制剂和放射性标记相同的方法。

68. 发明申请

US20070297976A1 Metal Ion-Labeled Bis-Aminoethanethiol-Targeting Ligand Conjugates, Compositions, and Methods for Tissue-Specific Imaging 有权
标题翻译：金属离子标记的双氨基乙硫醇靶向配体结合物，组合物和组织特异性成像方法
公开(公告)号：US20070297976A1
公开(公告)日：2007-12-27
申请号：US11760456
申请日：2007-06-08
申请人： DAVID YANG , Chun Liu , Dong-Fang Yu , E. Kim
发明人： DAVID YANG , Chun Liu , Dong-Fang Yu , E. Kim
IPC分类号： A61B5/055 , A61K51/00 , A61P43/00
CPC分类号： A61K51/0497 , A61K51/0453 , A61K51/0459 , A61K51/0491 , A61K51/087 , A61K51/088
摘要： The invention provides, in a general sense, a new labeling strategy employing 99mTc chelated with ethylenedicysteine (EC). EC is conjugated with a variety of ligands and chelated to 99mTc for use as an imaging agent for tissue-specific diseases. The drug conjugates of the invention may also be used as a prognostic tool or as a tool to deliver therapeutics to specific sites within a mammalian body. Kits for use in tissue-specific disease imaging are also provided.
摘要翻译：本发明在一般意义上提供了采用与乙二
氨酸（EC）螯合的99m Tc的新标记策略。 EC与各种配体缀合并螯合至99m Tc以用作组织特异性疾病的显像剂。本发明的药物缀合物也可用作预后工具或用作将治疗剂递送至哺乳动物体内特定部位的工具。还提供了用于组织特异性疾病成像的试剂盒。

69. 发明申请

US20070280880A1 Method for cell-specific targeting 有权
标题翻译：细胞特异性靶向的方法
公开(公告)号：US20070280880A1
公开(公告)日：2007-12-06
申请号：US11443442
申请日：2006-05-31
申请人： Rudolf Moser , Viola Groehn , Roger Schibli , Cristina Magdalena Mueller
发明人： Rudolf Moser , Viola Groehn , Roger Schibli , Cristina Magdalena Mueller
IPC分类号： A61N5/00 , A61K51/00 , A61K31/525 , A61K31/22 , A61K48/00 , A61K38/17
CPC分类号： A61K31/22 , A61K31/525 , A61K48/00 , A61K51/0459
摘要： Method for selective targeting of one or more effector moiety such as diagnostic or a therapeutic agent to a cell or population of cells expressing a folate-receptor comprising simultaneous or sequential administration of an antifolate with a folate- or pteroate-conjugate comprising said one or more effector moiety.
摘要翻译：将一种或多种效应部分例如诊断或治疗剂选择性靶向表达叶酸受体的细胞或群体的方法，其包括与叶酸或叶酸酯缀合物同时或顺序施用包含所述一种或多种效应部分。

70. 发明授权

US07172749B2 Radiolabeled irreversible inhibitors of epidermal growth factor receptor tyrosine kinase and their use in radioimaging and radiotherapy 失效
标题翻译：放射性标记的表皮生长因子受体酪氨酸激酶的不可逆抑制剂及其在放射成像和放射治疗中的应用
公开(公告)号：US07172749B2
公开(公告)日：2007-02-06
申请号：US10659747
申请日：2003-09-11
申请人： Alexander Levitzki , Eyal Mishani , Giuseppina Ortu , Iris Ben-David , Yulia Rozen
发明人： Alexander Levitzki , Eyal Mishani , Giuseppina Ortu , Iris Ben-David , Yulia Rozen
IPC分类号： A61K51/00
CPC分类号： A61K51/0459
摘要： Radiolabeled epidermal growth factor receptor tyrosine kinase (EGFR-TK) irreversible inhibitors and their use as biomarkers for medicinal radioimaging such as Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) and as radiopharmaceuticals for radiotherapy are disclosed.
摘要翻译：公开了放射性标记的表皮生长因子受体酪氨酸激酶（EGFR-TK）不可逆抑制剂及其作为药物放射成像的生物标志物，如正电子发射断层扫描（PET）和单光子发射计算机断层扫描（SPECT）以及放射治疗放射性药物。

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