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1. 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。

2. 发明授权

US5324827A Optionally oriented, monomeric and polymeric nonlinearly optically active materials and derivatives thereof 失效
标题翻译：任选取向的单体和聚合物非线性光学活性材料及其衍生物
公开(公告)号：US5324827A
公开(公告)日：1994-06-28
申请号：US118286
申请日：1993-09-09
申请人： Yves Camberlin , Gerard Mignani , Remi Meyrueix , Gilles Tapolsky
发明人： Yves Camberlin , Gerard Mignani , Remi Meyrueix , Gilles Tapolsky
IPC分类号： C08F20/60 , C07D207/44 , C07D207/452 , C07D207/456 , C08F20/52 , C08F22/36 , C08F22/40 , C08G73/10 , C08G73/14 , G02F1/35 , G02F1/355 , G02F1/361 , G03F7/027 , C07C245/06
CPC分类号： C07D207/452 , C07D207/456 , C08G73/1067 , C08G73/14 , G02F1/361 , G03F7/027
摘要： Nonlinearly optically active monomer species comprising at least two carbon-carbon activated double bonds, i.e., the polymerization of which is facilitated by the presence of an electron attracting function, and a non-centrosymmetric system of pi (.pi.) conjugated bonds bearing at least one electron attracting group on one terminal thereof and at least one electron donor group on the other terminal, are readily (co)polymerized and optionally oriented and crosslinked into shaped articles well adopted for the manufacture of a variety of electrooptical devices; such monomer species can have, for example, the following structural formula (I): ##STR1##
摘要翻译：包含至少两个碳 - 碳活化双键的非线性光学活性单体物质，即其聚合通过存在吸电子功能而促进，以及带有至少一个的π（π）共轭键的非中心对称体系其一端上的吸电子基团和另一个末端上的至少一个电子给体基团容易（共）聚合并任选取向并交联成良好地用于制造各种电光器件的成形制品; 这样的单体物质可以具有例如以下结构式（I）：其中（I）

3. 发明授权

US5444136A Optionally oriented, monomeric and polymeric nonlinearly optically active materials and derivatives thereof 失效
标题翻译：任选取向的单体和聚合物非线性光学活性材料及其衍生物
公开(公告)号：US5444136A
公开(公告)日：1995-08-22
申请号：US213090
申请日：1994-03-15
申请人： Yves Camberlin , Gerard Mignani , Remi Meyrueix , Gilles Tapolsky
发明人： Yves Camberlin , Gerard Mignani , Remi Meyrueix , Gilles Tapolsky
IPC分类号： C08F20/60 , C07D207/44 , C07D207/452 , C07D207/456 , C08F20/52 , C08F22/36 , C08F22/40 , C08G73/10 , C08G73/14 , G02F1/35 , G02F1/355 , G02F1/361 , G03F7/027 , C08F226/06
CPC分类号： C07D207/452 , C07D207/456 , C08G73/1067 , C08G73/14 , G02F1/361 , G03F7/027
摘要： Nonlinearly optically active monomer species comprising at least two carbon-carbon activated double bonds, i.e., the polymerization of which is facilitated by the presence of an electron attracting function, and a non-centrosymmetric system of pi (.pi.) conjugated bonds bearing at least one electron attracting group on one terminal thereof and at least one electron donor group on the other terminal, are readily (co)polymerized and optionally oriented and crosslinked into shaped articles well adopted for the manufacture of a variety of electrooptical devices; such monomer species can have, for example, the following structural formula (I): ##STR1##
摘要翻译：包含至少两个碳 - 碳活化双键的非线性光学活性单体物质，即其聚合通过存在吸电子功能而促进，以及带有至少一个的π（π）共轭键的非中心对称体系其一端上的吸电子基团和另一个末端上的至少一个电子给体基团容易（共）聚合并任选取向并交联成良好地用于制造各种电光器件的成形制品; 这样的单体物质可以具有例如以下结构式（I）：

4. 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。

5. 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。

6. 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。

7. 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.

8. 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。

9. 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。

10. 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。

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