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1. 发明申请

US20060204442A1 Magnetically targetable particles comprising magnetic components and biocompatible polymers for site-specific delivery of biologically active agents 审中-公开
标题翻译：包含磁性组分和生物相容性聚合物的可磁性靶向颗粒用于生物活性剂的位点特异性递送
公开(公告)号：US20060204442A1
公开(公告)日：2006-09-14
申请号：US10571210
申请日：2004-09-11
申请人： Gilles Tapolsky , Yuhua Li , Yuyuan Jiao
发明人： Gilles Tapolsky , Yuhua Li , Yuyuan Jiao
IPC分类号： A61K49/10 , A61K9/14
CPC分类号： A61K41/00 , A61K9/5094 , A61K31/282 , A61K31/40 , A61K31/555 , A61K33/26 , A61K45/06 , A61K47/593 , A61K47/62 , A61K47/6923 , A61K47/6929 , A61K49/0002 , A61K2300/00
摘要： The invention relates to magnetically targetable particles comprising at least one magnetic component The particles are capable of delivering selectively to a site or organ a biologically active substance for in vivo medical diagnosis and/or treatment. The particles are prepared by many processes such as encapsulation processes. Also described are methods for making the particles, methods for localized in vivo delivery of a biologically active agent utilizing the particles, a kit for the administration of the particles, as well as a method for sterilizing the particles.
摘要翻译：本发明涉及包含至少一种磁性组分的可磁性靶向颗粒。颗粒能够选择性地递送至位点或器官用于体内医学诊断和/或治疗的生物活性物质。颗粒通过许多方法制备，例如封装方法。还描述了制备颗粒的方法，利用颗粒的生物活性剂的局部体内递送方法，用于施用颗粒的试剂盒以及用于对颗粒进行灭菌的方法。

2. 发明申请

US20070274907A1 Magnetically Targetable Mitomycin C Compositions and Methods of Their Use 审中-公开
标题翻译：磁性靶向丝裂霉素C组合物及其使用方法
公开(公告)号：US20070274907A1
公开(公告)日：2007-11-29
申请号：US10593045
申请日：2004-05-12
申请人： Yuhua Li , Caryn Peterson , Scott Rudge , Suzanne Stevens , Gilles Tapolsky
发明人： Yuhua Li , Caryn Peterson , Scott Rudge , Suzanne Stevens , Gilles Tapolsky
IPC分类号： A61K51/00 , A61K49/10 , A61K9/14 , A61K31/407
CPC分类号： A61K9/1611 , A61K9/0019 , A61K9/5094
摘要： The present embodiments are directed to compositions and methods of delivering the compositions that comprise mitomycin C and superior magnetically targetable carrier particles. As the compositions are magnetically targetable, their use allows the localization of mitomycin C to particular locations within a patient. This allows for an increase in the effective concentration or a decrease in systemic exposure of mitomycin C in a patient.
摘要翻译：本实施方案涉及递送包含丝裂霉素C和优异的可磁性靶向载体颗粒的组合物的组合物和方法。由于组合物是可磁性靶向的，它们的用途允许将丝裂霉素C定位在患者体内的特定位置。这可以增加患者中丝裂霉素C的有效浓度或全身暴露的减少。

3. 发明申请

US20120177749A1 FAMILY OF PFKFB3 INHIBITORS WITH ANTI-NEOPLASTIC ACTIVITIES 有权
标题翻译：具有抗神经活性的PFKFB3抑制剂家族
公开(公告)号：US20120177749A1
公开(公告)日：2012-07-12
申请号：US13307552
申请日：2011-11-30
申请人： Gilles Tapolsky , Pooran Chand , John O. Trent , Sucheta Telang , Brian F. Clem , Jason A. Chesney
发明人： Gilles Tapolsky , Pooran Chand , John O. Trent , Sucheta Telang , Brian F. Clem , Jason A. Chesney
IPC分类号： A61K31/4709 , C07D215/14 , C12N5/02 , A61K33/24 , A61P35/00 , C07D401/06 , A61K31/47
CPC分类号： A61K31/00 , A61K31/12 , A61K31/121
摘要： A methods and compounds for inhibiting 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3) are described. Also described are methods of inhibiting cell proliferation, treating cancer, and screening compounds to determine their ability to inhibit PFKFB3.
摘要翻译：描述了用于抑制6-磷酸果糖-2-激酶/果糖-2,6-二磷酸酶3（PFKFB3）的方法和化合物。还描述了抑制细胞增殖，治疗癌症和筛选化合物以确定其抑制PFKFB3的能力的方法。

4. 发明申请

US20050048102A1 Pharmaceutical carrier device suitable for delivery of pharmaceutical compounds to mucosal surfaces 审中-公开
标题翻译：适用于将药物化合物输送到粘膜表面的药物载体装置
公开(公告)号：US20050048102A1
公开(公告)日：2005-03-03
申请号：US10962833
申请日：2004-10-12
申请人： Gilles Tapolsky , David Osborne
发明人： Gilles Tapolsky , David Osborne
IPC分类号： A61K9/00 , A61K9/70 , A61K9/14
CPC分类号： A61K9/006 , A61K9/7023
摘要： The present invention relates to a pharmaceutical delivery device for application of a pharmaceutical to mucosal surfaces. The device comprises an adhesive layer and a non-adhesive backing layer, and the pharmaceutical may be provided in either or both layers. Upon application, the device adheres to the mucosal surface, providing localized drug delivery and protection to the treatment site. The kinetics of erodability are easily adjusted by varying the number of layers and/or the components.
摘要翻译：本发明涉及用于将药物施用于粘膜表面的药物递送装置。该装置包括粘合剂层和非粘性背衬层，并且药物可以在两层或两层中提供。应用后，该装置粘附于粘膜表面，为治疗部位提供局部药物输送和保护。可以通过改变层数和/或组分来容易地调节可蚀性的动力学。

5. 发明授权

US08409574B2 Taxane analogs for the treatment of brain cancer 有权
公开(公告)号：US08409574B2
公开(公告)日：2013-04-02
申请号：US12859990
申请日：2010-08-20
申请人： James D. McChesney , Gilles Tapolsky , David E. Emerson , John Marshall , Tauseef Ahmed , Allen Cohn , Michael Kurman , Manuel Modiano
发明人： James D. McChesney , Gilles Tapolsky , David E. Emerson , John Marshall , Tauseef Ahmed , Allen Cohn , Michael Kurman , Manuel Modiano
IPC分类号： A61K39/00 , A61K31/415 , A61K31/335 , A01N43/52 , A01N43/32 , C07D309/00
CPC分类号： A61K31/357 , A61K31/337 , A61K31/4188 , A61K31/495 , A61K39/3955 , A61K45/06 , C07D493/04 , A61K2300/00
摘要： Provided herein are compounds and methods for the treatment of brain cancer in a mammal, wherein the method comprises the administration to the mammal a compound that stabilizes tubulin dimers or microtubles at G2-M interface during mitosis but is not a substrate for MDR protein. In particular, the present application relates to the use of an orally effective abeo-taxane, alone or in combination with temozolomide or bevacizumab, for the treatment of brain cancer.

6. 发明授权

US08552056B2 Biologically active taxane analogs and methods of treatment by oral administration 有权
标题翻译：生物活性紫杉烷类似物和口服治疗方法
公开(公告)号：US08552056B2
公开(公告)日：2013-10-08
申请号：US13620852
申请日：2012-09-15
申请人： James D. McChesney , Gilles Tapolsky , David E. Emerson , John Marshall , Tauseef Ahmed , Allen Cohn , Michael Kurman , Manuel Modiano
发明人： James D. McChesney , Gilles Tapolsky , David E. Emerson , John Marshall , Tauseef Ahmed , Allen Cohn , Michael Kurman , Manuel Modiano
IPC分类号： A61K31/335 , A61K31/44 , C07D407/00 , C07D309/00
CPC分类号： C07D493/06 , A61K31/357 , A61K31/495 , A61K39/3955 , A61K45/06
摘要： The present invention relates to a novel chemical compound of formula S-(1): for use in the treatment of cancer, to compositions containing said compound, methods of manufacture and combinations with other therapeutic agents.
摘要翻译：本发明涉及式S-（1）的新型化合物：用于治疗癌症的组合物，含有所述化合物的组合物，制备方法和与其它治疗剂的组合。

7. 发明授权

US08273789B2 Biologically active taxane analogs and methods of treatment by oral administration 有权
标题翻译：生物活性紫杉烷类似物和口服治疗方法
公开(公告)号：US08273789B2
公开(公告)日：2012-09-25
申请号：US12873477
申请日：2010-09-01
申请人： James D. McChesney , Gilles Tapolsky , David L. Emerson , John Marshall , Tauseef Ahmed , Allen Cohn , Michael Kurman , Manuel Modiano
发明人： James D. McChesney , Gilles Tapolsky , David L. Emerson , John Marshall , Tauseef Ahmed , Allen Cohn , Michael Kurman , Manuel Modiano
IPC分类号： A61K31/35 , A61K31/335 , C07D309/00 , C07D407/00
CPC分类号： C07D493/06 , A61K31/357 , A61K31/495 , A61K39/3955 , A61K45/06
摘要： The present invention relates to a novel chemical compound of formula S-(1): for use in the treatment of cancer, to compositions containing said compound, methods of manufacture and combinations with other therapeutic agents.
摘要翻译：本发明涉及式S-（1）的新型化合物：用于治疗癌症的组合物，含有所述化合物的组合物，制备方法和与其它治疗剂的组合。

8. 发明授权

US08557823B2 Family of PFKFB3 inhibitors with anti-neoplastic activities 有权
标题翻译：具有抗肿瘤活性的PFKFB3抑制剂家族
公开(公告)号：US08557823B2
公开(公告)日：2013-10-15
申请号：US13307552
申请日：2011-11-30
申请人： Gilles Tapolsky , Pooran Chand , John O. Trent , Sucheta Telang , Brian F. Clem , Jason A. Chesney
发明人： Gilles Tapolsky , Pooran Chand , John O. Trent , Sucheta Telang , Brian F. Clem , Jason A. Chesney
IPC分类号： A01N43/42 , A61K31/47 , A61K31/497 , C07D215/12 , C07D215/14
CPC分类号： A61K31/00 , A61K31/12 , A61K31/121
摘要： A methods and compounds for inhibiting 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3) are described. Also described are methods of inhibiting cell proliferation, treating cancer, and screening compounds to determine their ability to inhibit PFKFB3.
摘要翻译：描述了用于抑制6-磷酸果糖-2-激酶/果糖-2,6-二磷酸酶3（PFKFB3）的方法和化合物。还描述了抑制细胞增殖，治疗癌症和筛选化合物以确定其抑制PFKFB3的能力的方法。

9. 发明申请

US20050147658A1 Pharmaceutical carrier device suitable for delivery of pharmaceutical compounds to mucosal surfaces 有权
公开(公告)号：US20050147658A1
公开(公告)日：2005-07-07
申请号：US11069089
申请日：2005-03-01
申请人： Gilles Tapolsky , David Osborne
发明人： Gilles Tapolsky , David Osborne
IPC分类号： A61K9/00 , A61K9/22 , A61K9/70 , A61K31/716 , A61F13/02 , A61L15/16
CPC分类号： A61K9/7023 , A61K9/006 , A61K9/7069 , A61K31/137 , A61K31/245 , A61K31/4178 , A61K31/4515 , A61K31/568 , A61K47/10 , A61K47/32 , A61K47/38
摘要： The present invention relates to a pharmaceutical delivery device for application of a pharmaceutical to mucosal surfaces. The device comprises an adhesive layer and a non-adhesive backing layer, and the pharmaceutical may be provided in either or both layers. Upon application, the device adheres to the mucosal surface, providing localized drug delivery and protection to the treatment site. The kinetics of erodability are easily adjusted by varying the number of layers and/or the components.

10. 发明授权

US5811507A Polyesterimides for use in linear and/or non-linear optics, and one method for preparing same 失效
标题翻译：用于线性和/或非线性光学的聚酰亚胺及其制备方法
公开(公告)号：US5811507A
公开(公告)日：1998-09-22
申请号：US628639
申请日：1996-11-14
申请人： You-Ping Chan , Gilles Tapolsky , Remi Meyrueix , Jean-Pierre Lecomte , Michael Dickens
发明人： You-Ping Chan , Gilles Tapolsky , Remi Meyrueix , Jean-Pierre Lecomte , Michael Dickens
IPC分类号： G02F1/01 , C08G63/685 , C08G73/16 , G02F1/35 , G02F1/355 , G02F1/361
CPC分类号： G02F1/3617 , C08G63/6856 , C08G73/16
摘要： The present invention relates to a new polyesterimide of the type containing ester repeat functional groups E=--CO--O--, imide repeat functional groups I: ##STR1## and at least one chromophore, characterized in that it contains a quantity of recurrent amide functional groups capable of ring closure to imides which is smaller than or equal to 5 mol % relative to the sum of the imide functional groups and of the amide functional groups capable of ring closure to imides, which are present, and in that the polymerization functional groups consist essentially of E functional groups. This polyesterimide is preferably free from amide functional groups capable of ring closure to imides. One of the processes for obtaining this polyesterimide constitutes another subject-matter of the invention. Such a polymer is advantageously capable of behaving like a material that is transparent and/or active in nonlinear optics. It therefore constitutes a raw material of choice for producing LO and/or NLO devices: filters, polarizers, waveguides, a modulator, directional coupler, optical flip-flop and photoconductive film.
摘要翻译： PCT No.PCT / FR94 / 01219 Sec。 371日期：1996年11月14日 102（e）日期1996年11月14日PCT 1994年10月20日PCT PCT。第WO95 / 11476号公报日期：1995年04月27日本发明涉及含有酯重复官能团的类型的新的聚酯酰亚胺E = -CO-O-，酰亚胺重复官能团I：＆lt; IMAGE＆gt;和至少一种发色团，其特征在于它含有能够闭环的酰胺官能团的量相对于酰亚胺官能团和能够闭合的酰胺官能团的总和小于或等于5摩尔％，其存在和存在于酰亚胺中聚合官能团基本上由E官能团组成。该聚酯酰亚胺优选不含能够闭合成酰亚胺的酰胺官能团。获得该聚酯酰亚胺的方法之一构成本发明的另一主题。这种聚合物有利地能够表现得像非线性光学中透明和/或有活性的材料。因此，它构成了生产LO和/或NLO器件的首选材料：滤波器，偏振器，波导，调制器，定向耦合器，光学触发器和光电导膜。

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