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1. 发明申请

US20110312992A1 Inhibitors of C-Kit and Uses Thereof 审中-公开
标题翻译： C-Kit的抑制剂及其用途
公开(公告)号：US20110312992A1
公开(公告)日：2011-12-22
申请号：US13195825
申请日：2011-08-01
申请人： William Bornmann , David Maxwell , Ashutosh Pal , Zhenghong Peng , Zeev Estrov
发明人： William Bornmann , David Maxwell , Ashutosh Pal , Zhenghong Peng , Zeev Estrov
IPC分类号： A61K31/437 , A61P35/02 , A61P35/00 , C07D471/04 , C12N9/99
CPC分类号： C07D471/04
摘要： Compounds and methods useful as inhibitors of c-Kit are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of c-Kit and processes for synthesizing these compounds are also described herein.
摘要翻译：提出了可用作c-Kit抑制剂的化合物和方法。含有这些化合物的药物组合物，使用这些化合物作为c-Kit抑制剂的方法以及合成这些化合物的方法也在本文中描述。

2. 发明申请

US20100196273A1 NOVEL AGENT FOR IN VIVO PET IMAGING OF TUMOR PROLIFERATION 审中-公开
标题翻译：用于肿瘤增生的血管成像的新颖代理
公开(公告)号：US20100196273A1
公开(公告)日：2010-08-05
申请号：US12526688
申请日：2008-02-11
申请人： Mian M. Alauddin , Uday Mukhopadhyay , Juri Gelovani , Ashutosh Pal , William Bornmann
发明人： Mian M. Alauddin , Uday Mukhopadhyay , Juri Gelovani , Ashutosh Pal , William Bornmann
IPC分类号： A61K51/04 , C07H19/09 , A61P35/00
CPC分类号： A61K51/0491
摘要： Compounds for in vivo diagnostic imaging of cellular proliferation are provided. The compounds include L-nucleosides such as a 2′-deoxy-2′-fluoro-L-ara-binofuranosyl pyrimidine nucleoside analogue. These nucleosides are labeled with a positron emitting radioisotope. The present invention also provides a method for in vivo diagnostic imaging of cellular proliferation.
摘要翻译：提供了用于细胞增殖的体内诊断成像的化合物。化合物包括L-核苷，例如2'-脱氧-2'-氟-L-芳 - 二呋喃糖基嘧啶核苷类似物。这些核苷被正电子发射放射性同位素标记。本发明还提供了用于细胞增殖的体内诊断成像的方法。

3. 发明申请

US20080214491A1 Methods of Inhibiting the Interaction Between S100 and the Receptor for Advanced Glycation End-Products 审中-公开
标题翻译：抑制S100与高分子糖蛋白终产物受体相互作用的方法
公开(公告)号：US20080214491A1
公开(公告)日：2008-09-04
申请号：US12041112
申请日：2008-03-03
申请人： Craig D. Logsdon , William Bornmann
发明人： Craig D. Logsdon , William Bornmann
IPC分类号： A61K31/352 , A61K31/7068 , A61P35/00
CPC分类号： A61K31/352 , A61K31/7068 , A61K2300/00
摘要： A method of inhibiting an interaction between a S100 protein and the receptor for advanced glycation end-products is provided comprising administering to a subject a therapeutically effective amount of cromolyn, C5, or salt, hydrate, or solvate thereof. In some embodiments, the S100 protein is S100P. In some embodiments, the S100 protein is S100P. In addition, the present invention provides a method of treating a cancer comprising administering to a mammal a therapeutically effective amount of cromolyn, C5, or salt, hydrate, or solvate thereof. Additional methods are also provided.
摘要翻译：提供了抑制S100蛋白与用于晚期糖基化终产物的受体之间的相互作用的方法，包括向受试者施用治疗有效量的色甘酸，C5或其盐，水合物或溶剂合物。在一些实施方案中，S100蛋白是S100P。在一些实施方案中，S100蛋白是S100P。此外，本发明提供了一种治疗癌症的方法，包括向哺乳动物施用治疗有效量的色甘酸，C5或其盐，水合物或溶剂合物。还提供了附加的方法。

4. 发明申请

US20130131076A1 METHODS AND COMPOSITIONS RELATED TO WRAPPING OF DEHYDRONS 失效
标题翻译：与DEHYDRONS包裹相关的方法和组合物
公开(公告)号：US20130131076A1
公开(公告)日：2013-05-23
申请号：US11927329
申请日：2007-10-29
申请人： Ariel Fernandez , William Bornmann , Gabriel Lopez-Berestein , Angela Sanguino , Zheng-Hong Peng , Anil K. Sood
发明人： Ariel Fernandez , William Bornmann , Gabriel Lopez-Berestein , Angela Sanguino , Zheng-Hong Peng , Anil K. Sood
IPC分类号： A61K31/506
CPC分类号： A61K31/506 , C07D401/04
摘要： This application describes a novel technology in drug discovery and drug-based imaging/detection: the wrapping technology. This technology is based on identified singularities in the structure of soluble proteins. In contrast with drug-design approaches based on standard structural considerations, the packing of a protein, or more precisely, its dehydron pattern, may be used as a selectivity filter to design small-molecule inhibitors. The wrapping technology described herein is a novel form of rational drug design for avoiding side effects in drug therapy and sharpening the inhibitory impact of drugs on the oncokinome.
摘要翻译：该应用描述了药物发现和药物成像/检测中的新技术：包装技术。该技术基于可溶性蛋白质结构中确定的奇异点。与基于标准结构考虑的药物设计方法相比，蛋白质的包装，或更准确地说，其脱水剂图案可以用作选择性过滤器来设计小分子抑制剂。本文描述的包装技术是用于避免药物治疗中的副作用并且锐化药物对肿瘤细胞的抑制作用的合理药物设计的新型形式。

5. 发明授权

US08252807B2 Methods of inhibiting the interaction between S100 and the receptor for advanced glycation end-products 失效
标题翻译：抑制S100与晚期糖基化终产物受体相互作用的方法
公开(公告)号：US08252807B2
公开(公告)日：2012-08-28
申请号：US12247635
申请日：2008-10-08
申请人： Craig D. Logsdon , William Bornmann
发明人： Craig D. Logsdon , William Bornmann
IPC分类号： A61K31/353 , A61K31/513
CPC分类号： A61K31/352 , A61K31/7068 , A61K2300/00
摘要： A method of inhibiting an interaction between a S100 protein and the receptor for advanced glycation end-products is provided comprising administering to a subject a therapeutically effective amount of cromolyn, C5, or salt, hydrate, or solvate thereof. In some embodiments, the S100 protein is S100P. In some embodiments, the S100 protein is S100P. In addition, the present invention provides a method of treating a cancer comprising administering to a mammal a therapeutically effective amount of cromolyn, C5, or salt, hydrate, or solvate thereof. Additional methods are also provided.
摘要翻译：提供了抑制S100蛋白与用于晚期糖基化终产物的受体之间的相互作用的方法，包括向受试者施用治疗有效量的色甘酸，C5或其盐，水合物或溶剂合物。在一些实施方案中，S100蛋白是S100P。在一些实施方案中，S100蛋白是S100P。此外，本发明提供了一种治疗癌症的方法，包括向哺乳动物施用治疗有效量的色甘酸，C5或其盐，水合物或溶剂合物。还提供了附加的方法。

6. 发明申请

US20110195924A1 Methods of Inhibiting the Interaction Between S100P and the Receptor for Advanced Glycation End-Products 审中-公开
标题翻译：抑制S100P与受体之间高级糖基化终产物相互作用的方法
公开(公告)号：US20110195924A1
公开(公告)日：2011-08-11
申请号：US13122814
申请日：2009-10-06
申请人： Craig D. Logsdon , William Bornmann
发明人： Craig D. Logsdon , William Bornmann
IPC分类号： A61K31/7068 , A61K31/352 , A61P35/00
CPC分类号： A61K31/352
摘要： A method of inhibiting an interaction between a S100 protein and the receptor for advanced glycation end-products is provided comprising administering to a subject a therapeutically effective amount of cromolyn, C5, and/or other analogs, or salts, hydrates, or solvates thereof. In addition, provided herein are methods of treating a cancer comprising administering to a mammal a therapeutically effective amount of cromolyn, C5, and/or other analogs, or salts, hydrates, or solvates thereof.
摘要翻译：提供抑制S100蛋白与晚期糖基化终产物的受体之间的相互作用的方法，包括向受试者施用治疗有效量的色甘酸，C5和/或其它类似物或其盐，水合物或溶剂合物。此外，本文提供了治疗癌症的方法，包括向哺乳动物施用治疗有效量的色甘酸，C5和/或其它类似物或其盐，水合物或溶剂化物。

7. 发明申请

US20110097268A1 RADIOHALOIMATINIBS AND METHODS OF THEIR SYNTHESIS AND USE IN PET IMAGING OF CANCERS 审中-公开
标题翻译：放射性蛋白酶及其合成及其在PET成像中的应用
公开(公告)号：US20110097268A1
公开(公告)日：2011-04-28
申请号：US12310333
申请日：2007-08-22
申请人： William Bornmann , Mian Alauddin , Juri Gelovani , Pradip Ghosh , Liwei Guo , Dongmei Han , David Maxwell , Uday Mukhopadhyay , Zhenghong Peng , Aleksandr Shavrin , Yunming Ying
发明人： William Bornmann , Mian Alauddin , Juri Gelovani , Pradip Ghosh , Liwei Guo , Dongmei Han , David Maxwell , Uday Mukhopadhyay , Zhenghong Peng , Aleksandr Shavrin , Yunming Ying
IPC分类号： A61K51/04 , C07D403/14 , A61P35/00
CPC分类号： A61K51/0491
摘要： We disclose methods of synthesizing radiohalidated organic compounds and their use in positron emission tomography (PET) imaging of cancer cells.
摘要翻译：我们公开了合成放射性有机化合物的方法及其在癌细胞正电子发射断层扫描（PET）成像中的应用。

8. 发明申请

US20100322858A1 Radiohaloimatinibs and Methods of Their Synthesis and Use in PET Imaging of Cancers 审中-公开
标题翻译：他们合成和应用于PET成像的放射性卤代西他滨及其方法
公开(公告)号：US20100322858A1
公开(公告)日：2010-12-23
申请号：US12438045
申请日：2007-08-22
申请人： William Bornmann , Mian Alauddin , Juri Gelovani , Pradip Ghosh , Liwei Guo , Dongmei Han , David Maxwell , Uday Mukhopadhyay , Zhenghong Peng , Aleksandr Shavrin , Yunming Ying
发明人： William Bornmann , Mian Alauddin , Juri Gelovani , Pradip Ghosh , Liwei Guo , Dongmei Han , David Maxwell , Uday Mukhopadhyay , Zhenghong Peng , Aleksandr Shavrin , Yunming Ying
IPC分类号： A61K49/04 , C07H5/02
CPC分类号： A61K51/0491
摘要： We disclose methods of synthesizing radiohalidated organic compounds and their use in positron emission tomography (PET) imaging of cancer cells.
摘要翻译：我们公开了合成放射性有机化合物的方法及其在癌细胞正电子发射断层扫描（PET）成像中的应用。

9. 发明申请

US20100152140A1 Method of Cancer Treatment with Naphthol Analogs 审中-公开
标题翻译：萘酚类似物治疗癌症的方法
公开(公告)号：US20100152140A1
公开(公告)日：2010-06-17
申请号：US12529252
申请日：2008-01-18
申请人： Ja Seok Koo , William Bornmann , David Maxwell
发明人： Ja Seok Koo , William Bornmann , David Maxwell
IPC分类号： A61K31/66
CPC分类号： A61K31/661
摘要： In one embodiment, the present invention relates to a method of treating a cancer characterized by overexpression of cyclic adenosine monophosphate response element-binding protein (CREB) or phosphorylated CREB (p-CREB) by administering to a patient suffering from the cancer a pharmaceutically-effective amount of a composition comprising a compound selected from the group consisting of 2-{1-[3-(Amidinothio)propyl]-1H-indol-3-yl}-3-(1-methylindol-3-yl)maleimide, naphthol analogs having the structure (I), wherein R1 is selected from the group consisting of —H, —F, —Cl, —Br, and —I; R2 is selected from the group consisting of —H, —F, —Cl, —Br, —I, —C1-6 alkyl, —C1-6alkenyl, and —C1-6 alkynyl; R3 is selected from the group consisting of —H and —NO2; and R4 is selected from the group consisting of —H, —C1-6 alkyl, —C1-6 alkenyl, —C1-6 alkynyl, —OC1-6 alkyl, —OC1-6 alkenyl, and —OC1-6 alkynyl; and salts and esters thereof.
摘要翻译：在一个实施方案中，本发明涉及一种治疗癌症的方法，其特征在于通过向患有癌症的患者施用药学上可接受的方法来过表达环腺苷一磷酸应答元件结合蛋白（CREB）或磷酸化CREB（p-CREB）有效量的包含选自2- {1- [3-（脒基硫代）丙基] -1H-吲哚-3-基} -3-（1-甲基吲哚-3-基）马来酰亚胺的化合物的组合物，具有结构（I）的萘酚类似物，其中R 1选自-H，-F，-Cl，-Br和-I; R 2选自-H，-F，-Cl，-Br，-I，-C 1-6烷基，-C 1-6烯基和-C 1-6炔基; R3选自-H和-NO 2; 并且R 4选自-H，-C 1-6烷基，-C 1-6烯基，-C 1-6炔基，-OC 1-6烷基，-OC 1-6链烯基和-OC 1-6苯基; 及其盐和酯。

10. 发明申请

US20090281115A1 INHIBITORS OF C-KIT AND USES THEREOF 审中-公开
标题翻译： C-kit及其用途的抑制剂
公开(公告)号：US20090281115A1
公开(公告)日：2009-11-12
申请号：US12307001
申请日：2007-06-29
申请人： William Bornmann , David Maxwell , Ashutosh Pal , Zhenghong Peng , Zeev Estrov
发明人： William Bornmann , David Maxwell , Ashutosh Pal , Zhenghong Peng , Zeev Estrov
IPC分类号： A61K31/496 , C07D471/04 , A61K31/437 , A61P35/00 , C12N9/99
CPC分类号： C07D471/04
摘要： Compounds and methods useful as inhibitors of c-Kit are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of c-Kit and processes for synthesizing these compounds are also described herein.
摘要翻译：提出了可用作c-Kit抑制剂的化合物和方法。含有这些化合物的药物组合物，使用这些化合物作为c-Kit抑制剂的方法以及合成这些化合物的方法也在本文中描述。

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