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1. 发明申请

US20130143909A1 Acid Salt Forms of Polymer-Drug Conjugates and Alkoxylation Methods 审中-公开
标题翻译：聚合物 - 药物偶联物的酸盐形式和烷氧基化方法
公开(公告)号：US20130143909A1
公开(公告)日：2013-06-06
申请号：US13510555
申请日：2010-11-18
申请人： Anthony O. Chong , Seoju Lee , Bhalchandra V. Joshi , Brian Bray , Shaoyong Nie , Patrick L. Spence , Antoni Kozlowski , Samuel P. McManus , Sachin Tipnis , Greg Lavaty , David Swallow , John R. Handley , Anthony G. Schaefer
发明人： Anthony O. Chong , Seoju Lee , Bhalchandra V. Joshi , Brian Bray , Shaoyong Nie , Patrick L. Spence , Antoni Kozlowski , Samuel P. McManus , Sachin Tipnis , Greg Lavaty , David Swallow , John R. Handley , Anthony G. Schaefer
IPC分类号： C08G65/48 , A61K47/48 , C07C51/41 , C07C53/18
摘要： Among other aspects, provided herein is a mixed-acid salt of a water-soluble polymer-drug conjugate, along with related methods of making and using the same. The mixed-salt acid salt is stably formed, and appears to be more resistant to hydrolytic degradation than the corresponding predominantly pure acid salt or free base forms of the polymer-drug conjugate. The mixed acid salt is reproducibly prepared and recovered, and provides surprising advantages over non-mixed acid salt forms of the water-soluble polymer drug conjugate.
摘要翻译：除了其它方面之外，本文提供了水溶性聚合物 - 药物偶联物的混合酸盐以及其制备和使用相关方法。混合盐酸盐稳定地形成，并且似乎比聚合物 - 药物缀合物的相应的主要纯的酸盐或游离碱形式更耐水解降解。混合酸盐可重复制备和回收，并且相对于水溶性聚合物药物缀合物的非混合酸盐形式提供了惊人的优点。

2. 发明授权

US08039579B2 Intermediates useful in the preparation of maleimide functionalized polymers 有权
标题翻译：用于制备马来酰亚胺官能化聚合物的中间体
公开(公告)号：US08039579B2
公开(公告)日：2011-10-18
申请号：US12822148
申请日：2010-06-23
申请人： Samuel P. McManus , Antoni Kozlowski , Tracy L. Hutchison , Brian Bray , Xiaoming Shen
发明人： Samuel P. McManus , Antoni Kozlowski , Tracy L. Hutchison , Brian Bray , Xiaoming Shen
IPC分类号： C08G69/08
CPC分类号： C07D403/12 , A61K47/60 , C08G65/33337 , C08G69/08
摘要： Methods for forming maleimide functionalized polymers are provided. In one such embodiment, a maleimide functionalized polymer is prepared in a method that includes a step of carrying out a reverse Diels-Alder reaction. Intermediates useful in the methods, as well as methods for preparing the intermediates, are also provided. Also provided are polymeric reagents, methods of using polymeric reagents, compounds and conjugates.
摘要翻译：提供了形成马来酰亚胺官能化聚合物的方法。在一个这样的实施方案中，马来酰亚胺官能化聚合物在包括进行反向Diels-Alder反应的步骤的方法中制备。还提供了可用于该方法的中间体以及制备中间体的方法。还提供了聚合物试剂，使用聚合物试剂，化合物和共轭物的方法。

3. 发明授权

US07790835B2 Method of preparing maleimide functionalized polymers 有权
标题翻译：制备马来酰亚胺官能化聚合物的方法
公开(公告)号：US07790835B2
公开(公告)日：2010-09-07
申请号：US11004631
申请日：2004-12-03
申请人： Samuel P. McManus , Antoni Kozlowski , Tracy L. Hutchison , Brian Bray , Xiaoming Shen
发明人： Samuel P. McManus , Antoni Kozlowski , Tracy L. Hutchison , Brian Bray , Xiaoming Shen
IPC分类号： C08G69/08
CPC分类号： C07D403/12 , A61K47/60 , C08G65/33337 , C08G69/08
摘要： Methods for forming maleimide functionalized polymers are provided. In one such embodiment, a maleimide functionalized polymer is prepared in a method that includes a step of carrying out a reverse Diels-Alder reaction. Intermediates useful in the methods, as well as methods for preparing the intermediates, are also provided. Also provided are polymeric reagents, methods of using polymeric reagents, compounds and conjugates.
摘要翻译：提供了形成马来酰亚胺官能化聚合物的方法。在一个这样的实施方案中，马来酰亚胺官能化聚合物在包括进行反向Diels-Alder反应的步骤的方法中制备。还提供了可用于该方法的中间体以及制备中间体的方法。还提供了聚合物试剂，使用聚合物试剂，化合物和共轭物的方法。

4. 发明授权

US6015881A Methods and compositions for peptide synthesis 失效
标题翻译：肽合成的方法和组合物
公开(公告)号：US6015881A
公开(公告)日：2000-01-18
申请号：US71877
申请日：1998-05-01
申请人： Myung-Chol Kang , Brian Bray , Maynard Lichty , Catherine Mader , Gene Merutka
发明人： Myung-Chol Kang , Brian Bray , Maynard Lichty , Catherine Mader , Gene Merutka
IPC分类号： C07K14/16 , A61K38/00 , C07K5/00
CPC分类号： C07K14/005 , C12N2740/16122
摘要： The present invention relates, first, to methods for the synthesis of peptides, in particular T-20 (also referred to as "DP-178"; SEQ ID NO:1) and T-20-like peptides. Such methods utilize solid and liquid phase synthesis procedures to synthesize and combine groups of specific peptide fragments to yield the peptide of interest. The present invention further relates to individual peptide fragments which act as intermediates in the synthesis of the peptides of interest (e.g., T-20). The present invention still further relates to groups of such peptide intermediate fragments which can be utilized together to produce full length T-20 and T-20-like peptides.
摘要翻译：本发明首先涉及合成肽，特别是T-20（也称为“DP-178”; SEQ ID NO：1）和T-20样肽的方法。这些方法利用固相和液相合成方法来合成和组合特定肽片段的组合以产生感兴趣的肽。本发明还涉及在合成目标肽（例如T-20）中充当中间体的单个肽片段。本发明还涉及可以一起用于产生全长T-20和T-20样肽的这种肽中间体片段的基团。

5. 发明申请

US20120302761A1 INTERMEDIATES USEFUL IN THE PREPARATION OF MALEIMIDE FUNCTIONALIZED POLYMERS 有权
标题翻译：中间体用于制备马来酰亚胺官能化聚合物
公开(公告)号：US20120302761A1
公开(公告)日：2012-11-29
申请号：US13568518
申请日：2012-08-07
申请人： Samuel P. McManus , Antoni Kozlowski , Tracy L. Hutchison , Brian Bray , Xiaoming Shen
发明人： Samuel P. McManus , Antoni Kozlowski , Tracy L. Hutchison , Brian Bray , Xiaoming Shen
IPC分类号： C07D491/18
CPC分类号： C07D403/12 , A61K47/60 , C08G65/33337 , C08G69/08
摘要： Methods for forming maleimide functionalized polymers are provided. In one such embodiment, a maleimide functionalized polymer is prepared in a method that includes a step of carrying out a reverse Diels-Alder reaction. Intermediates useful in the methods, as well as methods for preparing the intermediates, are also provided. Also provided are polymeric reagents, methods of using polymeric reagents, compounds and conjugates.
摘要翻译：提供了形成马来酰亚胺官能化聚合物的方法。在一个这样的实施方案中，马来酰亚胺官能化聚合物在包括进行反向Diels-Alder反应的步骤的方法中制备。还提供了可用于该方法的中间体以及制备中间体的方法。还提供了聚合物试剂，使用聚合物试剂，化合物和共轭物的方法。

6. 发明申请

US20100016225A1 CONJUGATES COMPRISED OF POLYMER AND HIV gp-41-DERIVED PEPTIDES AND THEIR USE IN THERAPY 审中-公开
标题翻译：聚合物和HIV gp-41衍生肽及其在治疗中的应用
公开(公告)号：US20100016225A1
公开(公告)日：2010-01-21
申请号：US12478310
申请日：2009-06-04
申请人： Brian Bray , Myung-Chol kang , Nicolai Tvermoes , Daniel Kinder , John William Lackey , Huyi Zhang
发明人： Brian Bray , Myung-Chol kang , Nicolai Tvermoes , Daniel Kinder , John William Lackey , Huyi Zhang
IPC分类号： C07K14/16 , C12N7/02 , A61K38/10 , A61K38/16 , C07K7/08 , A61P31/18
CPC分类号： C07K14/005 , A61K38/00 , A61K47/60 , C12N2740/16122
摘要： Provided are conjugates comprising a polymer having operably bound thereto no less than two molecules of synthetic peptide derived from HIV gp41; methods of using these conjugates to inhibit transmission of HIV to a target cell by adding an amount of effective to inhibit infection of the cell by the virus; and methods of producing the conjugates by operably binding each molecule of synthetic peptide, via a reactive functionality, to the polymer.
摘要翻译：提供了包含具有可操作地结合有不少于两个来自HIV gp41的合成肽的两分子的聚合物的缀合物; 使用这些缀合物通过添加有效抑制病毒感染的量来抑制HIV向目标细胞传播的方法; 以及通过将每个分子的合成肽通过反应性官能团可操作地结合到聚合物来生产缀合物的方法。

7. 发明申请

US20090068243A1 Novel formulations for delivery of antiviral peptide therapeutics 审中-公开
标题翻译：用于递送抗病毒肽治疗剂的新型制剂
公开(公告)号：US20090068243A1
公开(公告)日：2009-03-12
申请号：US12080404
申请日：2008-04-02
申请人： Brian Bray , Jie Di , David Heilman , Peter Silinski , Scott Webb
发明人： Brian Bray , Jie Di , David Heilman , Peter Silinski , Scott Webb
IPC分类号： A61K9/10 , A61K38/16
CPC分类号： A61K38/162 , A61K9/0024 , A61K38/19 , A61K47/26 , A61K47/34 , A61K2300/00
摘要： Provided herein are compositions and methods for their administration as therapeutic agents. In particular, provided herein are compositions and their use for the administration of antiviral peptide therapeutics.
摘要翻译：本文提供了作为治疗剂施用的组合物和方法。特别地，本文提供了组合物及其用于施用抗病毒肽治疗剂的用途。

8. 发明申请

US20070049688A1 Method for preparing polymer maleimides 有权
标题翻译：聚合物马来酰亚胺的制备方法
公开(公告)号：US20070049688A1
公开(公告)日：2007-03-01
申请号：US11490268
申请日：2006-07-19
申请人： Antoni Kozlowski , John Handley , Anthony Schaefer , Brian Bray , Ryan Odom , Tony Sander
发明人： Antoni Kozlowski , John Handley , Anthony Schaefer , Brian Bray , Ryan Odom , Tony Sander
IPC分类号： C07D403/02 , C08G63/91
CPC分类号： C08G73/121 , A61K47/60 , C07D207/452 , C08G65/329 , C08G65/33331
摘要： Methods for preparing polymeric reagents bearing a maleimide are provided. Also provided are compositions comprising the polymeric reagents, and conjugates prepared by polymeric reagents obtained by the described methods.
摘要翻译：提供了制备含有马来酰亚胺的聚合物的方法。还提供了包含聚合物试剂的组合物和通过所述方法获得的聚合物试剂制备的共轭物。

9. 发明授权

US07045552B2 Pharmaceutical composition for improved administration of HIV gp41-derived peptides, and its use in therapy 有权
标题翻译：用于改善HIV gp41衍生肽的给药的药物组合物及其在治疗中的应用
公开(公告)号：US07045552B2
公开(公告)日：2006-05-16
申请号：US10663589
申请日：2003-09-16
申请人： David Heilman , Jie Di , Brian Bray
发明人： David Heilman , Jie Di , Brian Bray
IPC分类号： A61K47/30
CPC分类号： A61K9/0019 , A61K38/162 , A61K47/10 , A61K47/26
摘要： Provided is a pharmaceutical composition comprising a solution comprised of synthetic peptide in a final concentration of not less than 70 mg/ml in admixture with a polyol; wherein the synthetic peptide is an HIV fusion inhibitor, and wherein the polyol is in a final concentration of no less than 5 weight % and no more than 75 weight % of the pharmaceutical composition. Also provided is a synthetic peptide-containing pharmaceutical composition as a unit dose comprising an aqueous formulation comprised of synthetic peptide in a final concentration of not less than 70 mg/ml in admixture with a polyol; wherein the synthetic peptide is an HIV fusion inhibitor, and wherein the polyol is in a final concentration of no less than 5 weight % and no more than 75 weight % of the pharmaceutical composition. Further provided is a method of treating HIV infection by administering to an HIV-infected individual a pharmaceutical composition according to the present invention.
摘要翻译：本发明提供一种药物组合物，其包含与多元醇混合的终浓度不小于70mg / ml的合成肽的溶液; 其中所述合成肽是HIV融合抑制剂，并且其中所述多元醇的终浓度不低于所述药物组合物的5重量％且不大于75重量％。还提供了含合成肽的药物组合物作为单位剂量，其包含由多元醇混合而成的最终浓度不小于70mg / ml的合成肽的水性制剂; 其中所述合成肽是HIV融合抑制剂，并且其中所述多元醇的终浓度不低于所述药物组合物的5重量％且不大于75重量％。还提供了通过向HIV感染个体施用根据本发明的药物组合物来治疗HIV感染的方法。

10. 发明申请

US20130231359A1 Salt Form of a Multi-Arm Polymer-Drug Conjugate 有权
标题翻译：多臂聚合物 - 药物缀合物的盐形式
公开(公告)号：US20130231359A1
公开(公告)日：2013-09-05
申请号：US13510587
申请日：2010-11-18
申请人： Anthony O. Chong , Seoju Lee , Bhalchandra V. Joshi , Brian Bray , Shaoyong Nie , Patrick L. Spence , Antoni Kozlowski , Samuel P. McManus , Sachin Tipnis , Greg Lavaty , David Swallow , John R. Handley , Anthony G. Schaefer
发明人： Anthony O. Chong , Seoju Lee , Bhalchandra V. Joshi , Brian Bray , Shaoyong Nie , Patrick L. Spence , Antoni Kozlowski , Samuel P. McManus , Sachin Tipnis , Greg Lavaty , David Swallow , John R. Handley , Anthony G. Schaefer
IPC分类号： C07D491/22
CPC分类号： C08G65/331 , A61K31/4745 , A61K47/60 , C07C51/412 , C07C53/18 , C07D491/22 , C08G65/329 , C08G65/33396 , C08G65/48 , C08L2203/02
摘要： Among other aspects, provided herein is a hydrohalide salt of a multi-arm water-soluble polyethylene glycol-drug conjugate, along with related methods of making and using the same. The hydrohalide salt is stably formed, and appears to be more resistant to hydrolytic degradation than the corresponding free base form of the conjugate.
摘要翻译：在其它方面，本文提供了多臂水溶性聚乙二醇 - 药物偶联物的氢卤酸盐，以及制备和使用它们的相关方法。氢卤酸盐稳定地形成，似乎比结合物的相应游离碱形式更耐水解降解。

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