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1. 发明授权

US5756825A Hydroxamic acid-based bifunctional chelating compounds 失效
标题翻译：羟基恶唑基双功能螯合化合物
公开(公告)号：US5756825A
公开(公告)日：1998-05-26
申请号：US48869
申请日：1993-04-16
申请人： Ahmad Safavy , Donald J. Buchsbaum , Mohammad Bagher Kazaeli
发明人： Ahmad Safavy , Donald J. Buchsbaum , Mohammad Bagher Kazaeli
IPC分类号： A61K51/10 , C07C259/06 , C07K5/02 , C07C229/00 , C07C239/00
CPC分类号： C07C259/06 , A61K51/1093 , C07K5/022 , A61K2121/00 , A61K2123/00
摘要： The present disclosure details the preparation of hydroxamic-acid based bifunctional chelators and their use in conjugating metal ions to proteins and nucleic acids for tumor or tissue imaging or therapy purposes. Some preferred aspects of the disclosure involve the preparation of trisuccin, chemical name N-�tris(2-N- benzyloxyaminocarbonylethyl)! methylsuccinamic acid, which is a hydroxamic acid/succinate based structure that is particularly useful for binding radionuclides such as .sup.99m Tc, .sup.186 Re and .sup.67 Cu.
摘要翻译：本公开详细描述了基于异羟肟酸的双功能螯合剂的制备及其在将金属离子与用于肿瘤或组织成像或治疗目的的蛋白质和核酸结合的用途。本公开的一些优选方面涉及三琥珀，化学名称N- [三（2-N-苄氧基氨基羰基乙基）]甲基琥珀酸，其是特异可用于结合放射性核素如99mTc，186Re的异羟肟酸/琥珀酸酯基结构和67Cu。

2. 发明申请

US20110293515A1 HETEROFUNCTIONAL SEGMENT-POLY (ETHYLENE GLYCOL) POLYMERS AS DELIVERY VEHICLES 审中-公开
标题翻译：交联聚乙烯（乙烯甘油）聚合物
公开(公告)号：US20110293515A1
公开(公告)日：2011-12-01
申请号：US13144440
申请日：2010-01-12
申请人： Ahmad Safavy , James A. Bonner , Donald J. Buchsbaum
发明人： Ahmad Safavy , James A. Bonner , Donald J. Buchsbaum
IPC分类号： A61K51/06 , A61P35/00 , A61K49/00 , C08G69/48 , A61K47/48
CPC分类号： C08G69/44 , A61B5/055 , A61B5/411 , A61K47/59 , A61K47/60 , A61K47/645 , C08G69/10 , C08G69/40
摘要： Heterofunctional segment-poly(ethylene glycol) polymers, conjugates of these molecules with therapeutic and/or imaging agents, and methods for their use are disclosed. The heterofunctional segment-poly(ethylene glycol) polymers are useful as drug delivery conjugates, i.e., the heterofunctional segment-poly(ethylene glycol) polymers can be covalently attached to therapeutic agents (e.g., pharmaceutically active agents) and serve as delivery vehicles for the therapeutic agents. The heterofunctional segment-poly(ethylene glycol) polymers are also useful as imaging agent conjugates, i.e. the heterofunctional segment-poly(ethylene glycol) polymers can be covalently attached to imaging agents (e.g., tracers, imaging atoms, and imaging molecules) and serve as delivery vehicles for the imaging agents. Also disclosed are methods for treating a subject by administering to the subject an effective amount of the polymers conjugated to a therapeutic agent, an imaging agent, or a mixture thereof.
摘要翻译：公开了异功能段 - 聚（乙二醇）聚合物，这些分子与治疗和/或显像剂的缀合物及其使用方法。异源功能区段 - 聚（乙二醇）聚合物可用作药物递送缀合物，即异功能区段 - 聚（乙二醇）聚合物可以共价连接到治疗剂（例如药物活性剂）上，并用作治疗剂。异源功能片段 - 聚（乙二醇）聚合物也可用作显影剂缀合物，即异功能片段 - 聚（乙二醇）聚合物可以共价连接到成像剂（例如，示踪剂，成像原子和成像分子）并且用于作为成像剂的递送载体。还公开了通过向受试者施用有效量的与治疗剂，显像剂或其混合物缀合的聚合物来治疗受试者的方法。

3. 发明申请

US20110054037A1 BIS-AROMATIC ANTICANCER AGENTS 失效
标题翻译：双酚A反应剂代理
公开(公告)号：US20110054037A1
公开(公告)日：2011-03-03
申请号：US12936608
申请日：2009-04-06
申请人： Ahmad Safavy
发明人： Ahmad Safavy
IPC分类号： A61K31/135 , A61K31/095 , A61K31/075 , C12N5/00 , C07C381/00 , A61P35/00
CPC分类号： C07C323/16 , A61K31/047 , A61K31/09 , A61K31/095 , A61K31/10
摘要： Treatment of cancer includes administering a compound of formula (I) to a subject. In particular, treatment of colorectal cancer is described.
摘要翻译：治疗癌症包括向受试者施用式（I）化合物。特别地，描述了结肠直肠癌的治疗。

4. 发明申请

US20100166654A1 Single-Drug Multi-Ligand Conjugates for Targeted Drug Delivery 审中-公开
标题翻译：单药多配体结合物用于靶向药物递送
公开(公告)号：US20100166654A1
公开(公告)日：2010-07-01
申请号：US11792329
申请日：2005-12-02
申请人： Ahmad Safavy
发明人： Ahmad Safavy
IPC分类号： A61K47/48 , C07K7/06 , C07D305/14 , A61K51/08 , A61K49/14 , A61P37/06 , A61P29/00 , A61P35/00 , A61P9/10 , A61P31/00 , C12N9/96
CPC分类号： A61K49/0056 , A61K47/60 , A61K47/61 , A61K47/62 , A61K47/6425
摘要： An adhesive is provided containing at least one synthetic polymer with receptor sites that enable the selective capture or release of a target molecule. A polymer is synthesized by polymerizing and cross-linking a functional monomer or functional copolymers in the presence of a target or template molecule allowing for reversible interactions between the polymer and the target molecule. The target molecule may be extracted from the polymer creating receptor sites complimentary to the target molecule. Alternatively, the target molecule may remain in the polymer network and be controllably released. The molecularly imprinted polymer is formulated into an adhesive. The adhesive can be used as a component in an in-vitro diagnostic device to release template molecules or to capture target molecules in vacated receptor sites in the synthetic polymer.
摘要翻译：提供了含有至少一种具有能够选择性捕获或释放靶分子的受体位点的合成聚合物的粘合剂。聚合物通过使聚合物和靶分子之间的可逆相互作用在靶或模板分子存在下聚合和交联官能单体或官能共聚物来合成。可以从产生与靶分子互补的受体位点的聚合物中提取靶分子。或者，靶分子可以保留在聚合物网络中并被可控地释放。将分子印迹聚合物配制成粘合剂。粘合剂可以用作体外诊断装置中的组分以释放模板分子或捕获合成聚合物中空的受体位点中的靶分子。

5. 发明申请

US20080167370A1 MULTIDRUG MULTILIGAND CONJUGATES FOR TARGETED DRUG DELIVERY 失效
标题翻译：多剂量多药联合用于定向药物递送
公开(公告)号：US20080167370A1
公开(公告)日：2008-07-10
申请号：US11959947
申请日：2007-12-19
申请人： Ahmad Safavy
发明人： Ahmad Safavy
IPC分类号： A61K31/335
CPC分类号： B82Y5/00 , A61K47/60 , A61K47/6425 , A61K47/665 , A61K47/6811 , A61K51/088
摘要： Described is a multi drug multiligand conjugate for targeted drug delivery. The MDML conjugate contains a plurality of tripartite molecules linked to a central scaffold moiety, with each tripartite molecule comprising a targeting molecule, a therapeutic agent and a scaffold binding element. The MDML conjugate allows for more efficient delivery of therapeutic agents to the cells resulting in enhanced therapeutic efficiency. A model MDL conjugate is disclosed as well as method for the synthesis of the model conjugate.
摘要翻译：描述了用于靶向药物递送的多药物多配体缀合物。 MDML缀合物包含连接到中心支架部分的多个三分子分子，其中每个三分子包含靶向分子，治疗剂和支架结合元件。 MDML结合物可以更有效地将治疗剂递送至细胞，从而提高治疗效率。公开了一种模型MDL缀合物以及合成模型缀合物的方法。

6. 发明授权

US08686190B2 Bis-aromatic anticancer agents 失效
标题翻译：双芳族抗癌剂
公开(公告)号：US08686190B2
公开(公告)日：2014-04-01
申请号：US12936608
申请日：2009-04-06
申请人： Ahmad Safavy
发明人： Ahmad Safavy
IPC分类号： C07C319/00 , C07C321/00
CPC分类号： C07C323/16 , A61K31/047 , A61K31/09 , A61K31/095 , A61K31/10
摘要： Treatment of cancer includes administering a compound of formula (I) to a subject. In particular, treatment of colorectal cancer is described.
摘要翻译：治疗癌症包括向受试者施用式（I）化合物。特别地，描述了结肠直肠癌的治疗。

7. 发明授权

US07311892B2 Multidrug multiligand conjugates for targeted drug delivery 失效
标题翻译：用于靶向药物递送的多药物多配体缀合物
公开(公告)号：US07311892B2
公开(公告)日：2007-12-25
申请号：US10281840
申请日：2002-10-28
申请人： Ahmad Safavy
发明人： Ahmad Safavy
IPC分类号： A61K39/00 , A61K39/385 , A61K47/08 , A61K51/08 , C07K17/18
CPC分类号： B82Y5/00 , A61K47/60 , A61K47/6425 , A61K47/665 , A61K47/6811 , A61K51/088
摘要： Described is a multi drug multiligand conjugate for targeted drug delivery. The MDML conjugate contains a plurality of tripartite molecules linked to a central scaffold moiety, with each tripartite molecule comprising a targeting molecule, a therapeutic agent and a scaffold binding element. The MDML conjugate allows for more efficient delivery of therapeutic agents to the cells resulting in enhanced therapeutic efficiency. A model MDL conjugate is disclosed as well as method for the synthesis of the model conjugate.
摘要翻译：描述了用于靶向药物递送的多药物多配体缀合物。 MDML缀合物包含连接到中心支架部分的多个三分子分子，其中每个三分子包含靶向分子，治疗剂和支架结合元件。 MDML结合物可以更有效地将治疗剂递送至细胞，从而提高治疗效率。公开了一种模型MDL缀合物以及合成模型缀合物的方法。

8. 发明申请

US20100316631A1 Water Soluble Curcumin-Based Compounds 审中-公开
标题翻译：水溶性姜黄素类化合物
公开(公告)号：US20100316631A1
公开(公告)日：2010-12-16
申请号：US12446375
申请日：2007-10-19
申请人： Ahmad Safavy
发明人： Ahmad Safavy
IPC分类号： A61K39/395 , C07C57/42 , C07C49/255 , C07D317/54 , C07C49/172 , C07H15/203 , C07K2/00 , C07C229/34 , C07K16/00 , A61K31/36 , A61K31/192 , A61K31/197 , A61K31/12 , A61K31/7034 , A61P35/00 , A61P29/00 , C08G73/06
CPC分类号： A61K36/9066
摘要： The present disclosure describes the design and synthesis of a novel class of water soluble curcumin-based compounds. These water soluble curcumin-based compounds are shown to provide superior cell killing activity and exhibit increased and cell internalization solubility in aqueous solutions as compared to the free (unconjugated) curcumin. The present disclosure provides compositions for the treatment or prevention of a variety of disease states or conditions, such as but not limited to, cancer, other cell hyperproliferative disorders and chronic inflammatory conditions, said compositions comprising a water soluble curcumin-based compound.
摘要翻译：本公开描述了一类新型水溶性姜黄素类化合物的设计和合成。与游离（非共轭）姜黄素相比，这些水溶性姜黄素类化合物显示出提供优异的细胞杀伤活性，并且在水溶液中表现出增加的细胞内化溶解度。本公开提供了用于治疗或预防各种疾病状态或病症（例如但不限于癌症，其他细胞过度增殖性病症和慢性炎性病症）的组合物，所述组合物包含水溶性姜黄素基化合物。

9. 发明授权

US07807134B2 Multidrug multiligand conjugates for targeted drug delivery 失效
标题翻译：用于靶向药物递送的多药物多配体缀合物
公开(公告)号：US07807134B2
公开(公告)日：2010-10-05
申请号：US11959947
申请日：2007-12-19
申请人： Ahmad Safavy
发明人： Ahmad Safavy
IPC分类号： A61K51/06 , A61K38/08 , A61K38/04 , A61K39/00 , A61K39/385
CPC分类号： B82Y5/00 , A61K47/60 , A61K47/6425 , A61K47/665 , A61K47/6811 , A61K51/088
摘要： Described is a multi drug multiligand conjugate for targeted drug delivery. The MDML conjugate contains a plurality of tripartite molecules linked to a central scaffold moiety, with each tripartite molecule comprising a targeting molecule, a therapeutic agent and a scaffold binding element. The MDML conjugate allows for more efficient delivery of therapeutic agents to the cells resulting in enhanced therapeutic efficiency. A model MDL conjugate is disclosed as well as method for the synthesis of the model conjugate.
摘要翻译：描述了用于靶向药物递送的多药物多配体缀合物。 MDML缀合物包含连接到中心支架部分的多个三分子分子，其中每个三分子包含靶向分子，治疗剂和支架结合元件。 MDML结合物可以更有效地将治疗剂递送至细胞，从而提高治疗效率。公开了一种模型MDL缀合物以及合成模型缀合物的方法。

10. 发明授权

US06191290B1 Taxane derivatives for targeted therapy of cancer 有权
标题翻译：用于靶向治疗癌症的紫杉烷衍生物
公开(公告)号：US06191290B1
公开(公告)日：2001-02-20
申请号：US09510896
申请日：2000-02-23
申请人： Ahmad Safavy
发明人： Ahmad Safavy
IPC分类号： C07D30514
CPC分类号： A61K47/6425
摘要： The present invention describes for the first time the design and synthesis of a soluble tumor-directed paclitaxel prodrug which may establish a new mode of utilization of the taxane class of anticancer agents in cancer therapy.
摘要翻译：本发明首次描述了可以建立抗癌剂类紫杉烷类在癌症治疗中的新方式的可溶性肿瘤指导性紫杉醇前药的设计和合成。

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