专利号:US-6096874-A 优先权日:1990-10-01 标 题:High affinity tamoxifen derivatives 发明人:WALLACE SIDNEY; YANG DAVID; DELPASSAND EBRAHIM; CHERIF ABDALLAH; QUADRI SYED M 权利人:UNIV TEXAS 摘要:The synthesis of tamoxifen derivatives, most particularly halo, halo alkyl, hydroxy, and amino tamoxifen derivatives is disclosed. The native tamoxifen molecule includes a substituted chemical group positioned on the aliphatic chain of the tamoxifen molecule. Particular tamoxifen derivatives of the invention include chloro, bromo, iodo, fluoro, amino and DTPA tamoxifen derivatives, and corresponding lower alkyl halogenated forms. The halogenated tamoxifen derivatives possess superior binding affinities for estrogen receptor rich tissues, such as uterine tissue and breast tissue, relative to unsubstituted native tamoxifen. Radiolabeled forms of the tamoxifen derivatives may be used as highly specific imaging agents for estrogen receptor rich tissues. The fluoro and bromo tamoxifen derivatives are particularly useful for imaging estrogen receptors by PET whereas the iodinated tamoxifens are particularly useful in imaging estrogen receptors by SPECT. Rapid and efficient methods of preparing the tamoxifen derivatives having high specific activity (>6 Ci/μmol) are also disclosed. Aliphatic chain substituted tamoxifen derivatives are shown to possess greater estrogen receptor binding affinity and more potent tumor cell inhibition than tamoxifen or tamoxifen derivatives substituted at other locations on the molecule (i.e., non-aliphatic chain substituted tamoxifen). The tanioxifen derivatives of the present invention may advantageously be used as anti-cancer therapeutic agents to halt estrogen-receptor positive tumors, such as those of breast and uterine tissue. The present invention also provides a hydrophilic DTPA-tamnoxifen analogue, and uses thereof in imaging estrogen receptor positive ER+ lesions.
专利号:US-2011104052-A1 优先权日:2007-12-03 标 题 :Methods of synthesis and use of chemospheres 发明人:BARNETT BRADLEY POWERS; GESCHWIND JEFFREY 权利人:UNIV JOHNS HOPKINS 摘要:The present invention provides, in general, compositions comprising a hydrogel and an agent, for example a therapeutic agent or an imaging agent, for locoregional delivery. In certain preferred embodiments of the invention, the hydrogel compositions are detectable by Magnetic Responance and CT Scan and are used for locoregional delivery of therapeutic agents, for example chemotherapeutic agents. The invention also features polymer matrix compositions comprising nanoparticles that can be loaded after polymerization with bioactive agents, for example a diagnostic agent or therapeutic agent.
专利号:US-9186422-B2 优先权日:2003-08-11 标题 :Radio-opaque compounds, compositions containing same and methods of their synthesis and use 发明人:PATHAK CHANDRASHEKHAR P; THIGLE SANJAY M 权利人:PATHAK CHANDRASHEKHAR P; THIGLE SANJAY M; PATHAK HOLDINGS LLC 摘要:Radio-opaque biodegradable compositions are formed by modifying terminal groups of synthetic and natural biodegradable polymers such as polylactones with iodinated moieties. The biodegradable property of the compositions renders them suitable for use in medical field such as drug delivery, imaging. Compounds disclosed in this invention exist as neat liquid. Certain compositions disclosed in this invention form hydrophobic iodine rich domains when dissolved in water, such domains provide better contrasting properties as well as ability to dissolve hydrophobic bioactive drugs. Certain iodinated moieties disclosed in the invention are capable of cross linking natural proteins in situ in presence of suitable catalysts and co-catalysts.
专利号:US-12343191-B2 优先权日:2019-12-02 标题 :Medical image synthesis for motion correction using generative adversarial networks 发明人:CRABB BRENDAN THOMAS; NOO FREDERIC NICOLAS FIRMIN; FINE GABRIEL CHAIM 权利人:UNIV UTAH RES FOUND 摘要:A computer system is configured to remove motion artifacts in medical images using a generative adversarial network (GAN). The computer system instantiates the GAN having one or more generative network(s) and one or more discriminative network(s) that are pitted against each other to train a generative model and a discriminative model. The training uses a training dataset including a plurality of medical images that are previously classified as without significant motion artifacts for diagnostic purposes. The discriminative model is trained to classify medical images as real or artificial. The generative model is trained to enhance the quality of a medical image and remove motion artifacts by producing a medical image directly from a post-contrast image, without using a pre-contrast mask.
专利号:US-7790141-B2 优先权日:2003-08-11 标题 :Radio-opaque compounds, compositions containing same and methods of their synthesis and use
专利号:US-2010290995-A1 优先权日:2003-08-11 标 题:Radio-opaque compounds, compositions containing same and methods of their synthesis and use
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合成参考文献
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