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公开(公告)号：US20110229581A1
公开(公告)日：2011-09-22
申请号：US13129611
申请日：2009-11-17
申请人： Hong Zhao , Weili Yan , Lianjun Shi , Dechun Wu , Maksim Royzen
发明人： Hong Zhao , Weili Yan , Lianjun Shi , Dechun Wu , Maksim Royzen
IPC分类号： A61K9/14 , C12N5/071 , C12N5/09 , C07J31/00 , C07J43/00 , A61K47/20 , A61K47/24 , A61K47/22 , A61K31/7088 , A61K31/713 , A61K38/14 , A61P35/00 , A61P29/00 , A61P31/12 , B82Y5/00
CPC分类号： C07J41/0055 , C07J51/00
摘要： The present invention is directed to releasable cationic lipids and nanoparticle compositions for the delivery of nucleic acids and methods of modulating an expression of a target gene using the same. In particular, the invention relates to cationic lipids including an acid labile linker, and nanoparticle compositions containing the same.
摘要翻译： 本发明涉及用于递送核酸的可释放阳离子脂质和纳米颗粒组合物以及使用其调节靶基因表达的方法。 特别地，本发明涉及包括酸不稳定接头的阳离子脂质和含有它的纳米颗粒组合物。
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公开(公告)号：US20110223257A1
公开(公告)日：2011-09-15
申请号：US13129546
申请日：2009-11-17
申请人： Hong Zhao , Weili Yan , Lianjun Shi , Dechun Wu , Maksim Royzen
发明人： Hong Zhao , Weili Yan , Lianjun Shi , Dechun Wu , Maksim Royzen
IPC分类号： A61K9/50 , C07C229/34 , C07C233/87 , C07F9/02 , C12N5/00 , A61K47/00 , A61K31/7088 , A61K31/56 , B82Y5/00
CPC分类号： A61K9/1272
摘要： The present invention relates to releasable fusogenic lipids and nanoparticle compositions containing the same for the delivery of oligonucleotides and methods of modulating gene expression using the same. In particular, this invention relates to releasable fusogenic lipids containing an imine linker and a zwitterionic moiety.
摘要翻译： 本发明涉及可释放的融合脂质和含有其的用于递送寡核苷酸的纳米颗粒组合物和使用其衍生调节基因表达的方法。 特别地，本发明涉及含有亚胺接头和两性离子部分的可释放的融合脂质。
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公开(公告)号：US20110305769A1
公开(公告)日：2011-12-15
申请号：US13129495
申请日：2009-07-31
申请人： Hong Zhao , Weili Yan , Lianjun Shi , Dechun Wu
发明人： Hong Zhao , Weili Yan , Lianjun Shi , Dechun Wu
IPC分类号： A61K9/14 , A61K31/7088 , A61K31/713 , C12N5/071 , A61P35/00 , A61P35/04 , A61P31/12 , A61P29/00 , C07J9/00 , C12N5/09 , B82Y5/00
CPC分类号： C12N15/88 , A61K9/1272 , A61K31/7088 , C07J41/0055 , C12N15/111 , C12N15/113 , C12N15/1138 , C12N2310/11 , C12N2310/315 , C12N2310/3231 , C12N2310/3341 , C12N2320/32
摘要： The present invention is directed to cationic lipid for the delivery of oligonucleotides and methods of modulating an expression of a targeted gene using the nanoparticle compositions. In particular, the invention relates to cholesterol and its derivatives having multiple positively charged moieties via branching spacers, and nanoparticle compositions of oligonucleotides encapsulated in a mixture of a cationic lipid, a fusogenic lipid and a PEG lipid.
摘要翻译： 本发明涉及用于递送寡核苷酸的阳离子脂质和使用纳米颗粒组合物调节靶基因表达的方法。 具体地，本发明涉及通过支化间隔物具有多个带正电荷的部分的胆固醇及其衍生物，以及包封在阳离子脂质，融合脂质和PEG脂质的混合物中的寡核苷酸的纳米颗粒组合物。
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公开(公告)号：US20110305770A1
公开(公告)日：2011-12-15
申请号：US13129628
申请日：2009-11-17
申请人： Hong Zhao , Weili Yan , Lianjun Shi , Dechun Wu
发明人： Hong Zhao , Weili Yan , Lianjun Shi , Dechun Wu
IPC分类号： A61K9/14 , C07C237/32 , C07F9/24 , C07F9/09 , C07D207/09 , C07K5/11 , C07D475/04 , C07K14/475 , C07K14/79 , C07K14/655 , C07K14/68 , C07K14/745 , A61K47/44 , A61K31/7088 , A61K31/713 , A61K38/02 , C12N5/09 , A61P35/00 , A61P31/12 , A61P29/00 , C07C271/20 , B82Y5/00
CPC分类号： A61K31/785 , A61K47/6911 , C07C233/49 , C07C237/22 , C07C251/24
摘要： The present invention relates to polymer conjugated releasable lipids and nanoparticle compositions containing the same for the delivery of nucleic acids and methods of modulating gene expression using the same. In particular, this invention relates to releasable polymeric lipids containing an acid-labile linker based on a ketal or acetal-containing linker, or an imine-containing linker.
摘要翻译： 本发明涉及聚合物共轭的可释放脂质和含有该聚合物共轭的可释放脂质的纳米颗粒组合物，以及用于递送核酸的纳米颗粒组合物以及使用其调节基因表达的方法。 特别地，本发明涉及含有基于缩酮或含缩醛连接体的酸不稳定接头或含亚胺接头的可释放聚合物脂质。
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公开(公告)号：US08133707B2
公开(公告)日：2012-03-13
申请号：US11333072
申请日：2006-01-17
IPC分类号： C12P7/18
CPC分类号： C08G65/329 , C08G18/797 , C08G65/333
摘要： Methods for preparing substantially non-antigenic polymers having lone electron pair-containing moieties in high purity are disclosed. The polymers are useful as intermediates for synthesis of amine-based polymers and in the formation of activated polymers for conjugation with nucleophiles. Conjugates and methods of preparation and treatment with the conjugates are also disclosed. The resultant polymer-amines are of sufficient purity so that expensive and time consuming purification steps required for pharmaceutical grade polymers are avoided.
摘要翻译： 公开了制备基本上具有高纯度的含有电子对的部分的非抗原性聚合物的方法。 聚合物可用作合成基于胺的聚合物的中间体和用于与亲核试剂缀合的活化聚合物的形成。 还公开了共轭物的共轭物和制备和处理方法。 得到的聚合物胺具有足够的纯度，因此避免了医药级聚合物所需的昂贵且耗时的纯化步骤。
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6.发明授权Multi-arm polymeric conjugates of 7-ethyl-10-hydroxycamptothecin for treatment of breast, colorectal, pancreatic, ovarian and lung cancers 有权用于治疗乳腺癌，结肠直肠癌，胰腺癌，卵巢癌和肺癌的7-乙基-10-羟基喜树碱的多臂聚合物缀合物公开(公告)号：US07723351B2
公开(公告)日：2010-05-25
申请号：US12274474
申请日：2008-11-20
申请人： Hong Zhao , Maria Belen Rubio , Dechun Wu , Puja Sapra
发明人： Hong Zhao , Maria Belen Rubio , Dechun Wu , Puja Sapra
IPC分类号： A61K31/4745 , C07D491/22
CPC分类号： A61K31/121 , A61K31/4745 , A61K47/55 , A61K47/60 , C07D491/22 , C07D519/00
摘要： A four arm-polyethylene glycol-7-ethyl-10-hydroxycamptothecin conjugate, such as, is disclosed. Methods of making the conjugates and methods of treating mammals using the same are also disclosed.
摘要翻译： 公开了四臂聚乙二醇-7-乙基-10-羟基喜树碱缀合物。 还公开了制备缀合物的方法和使用其的治疗哺乳动物的方法。
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7.发明授权Multi-arm polymeric conjugates of 7-ethyl-10-hydroxycamptothecin for treatment of breast, colorectal, pancreatic, ovarian and lung cancers 失效用于治疗乳腺癌，结肠直肠癌，胰腺癌，卵巢癌和肺癌的7-乙基-10-羟基喜树碱的多臂聚合物缀合物公开(公告)号：US07462627B2
公开(公告)日：2008-12-09
申请号：US11704607
申请日：2007-02-09
申请人： Hong Zhao , Maria Belen Rubio , Dechun Wu , Puja Sapra
发明人： Hong Zhao , Maria Belen Rubio , Dechun Wu , Puja Sapra
IPC分类号： A61K31/4745 , C07D491/22
CPC分类号： A61K31/121 , A61K31/4745 , A61K47/55 , A61K47/60 , C07D491/22 , C07D519/00
摘要： A four arm-polyethylene glycol-7-ethyl-10-hydroxycamptothecin conjugate, such as, is disclosed. Methods of making the conjugates and methods of treating mammals using the same are also disclosed.
摘要翻译： 公开了四臂聚乙二醇-7-乙基-10-羟基喜树碱缀合物。 还公开了制备缀合物的方法和使用其的治疗哺乳动物的方法。
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公开(公告)号：US20060178474A1
公开(公告)日：2006-08-10
申请号：US11051009
申请日：2005-02-04
申请人： Dechun Wu , Hong Zhao , Richard Greenwald , Susan Adler
发明人： Dechun Wu , Hong Zhao , Richard Greenwald , Susan Adler
IPC分类号： A61K47/48
CPC分类号： A61K47/60
摘要： A process for efficiently preparing polymer conjugates such as branched PEG-polypeptide conjugates, in large scale without column chromatography clean up of the activated PEG linkers to remove impurities is disclosed.
摘要翻译： 公开了一种用于有效地制备聚合物缀合物如支链PEG-多肽缀合物的方法，其大规模没有柱色谱法清除活化的PEG接头以除去杂质。
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9.发明申请POLYMERIC CONJUGATES OF AROMATIC AMINE CONTAINING COMPOUNDS INCLUDING RELEASABLE UREA LINKER 审中-公开包含可释放尿素连接剂的芳香胺包含化合物的聚合物公开(公告)号：US20120289571A1
公开(公告)日：2012-11-15
申请号：US13520120
申请日：2010-12-30
申请人： Hong Zhao , Dechun Wu , Snehlata Tripathi , Jing Xia
发明人： Hong Zhao , Dechun Wu , Snehlata Tripathi , Jing Xia
IPC分类号： C07D403/14 , A61K31/404 , A61P35/00 , C07D403/06
CPC分类号： C07D403/06 , C07D403/14
摘要： The present invention relates to releasable urea linker systems involving amine-containing chemical compounds and biologically active agents. In particular, the present invention relates to reversibly releasable linkers based on intramolecular cyclization-assisted releasable urea linkages to aromatic amine-containing compounds. The present invention also relates to polymeric conjugates of indolinone-based tyrosine kinase inhibitors.
摘要翻译： 本发明涉及包含含胺化合物和生物活性剂的可释放的尿素连接体系。 特别地，本发明涉及基于分子内环化辅助的可释放脲键与含芳香胺的化合物的可逆释放接头。 本发明还涉及基于二氢吲哚酮的酪氨酸激酶抑制剂的聚合物缀合物。
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公开(公告)号：US20070166808A1
公开(公告)日：2007-07-19
申请号：US11333072
申请日：2006-01-17
CPC分类号： C08G65/329 , C08G18/797 , C08G65/333
摘要： Methods for preparing substantially non-antigenic polymers having lone electron pair-containing moieties in high purity are disclosed. The polymers are useful as intermediates for synthesis of amine-based polymers and in the formation of activated polymers for conjugation with nucleophiles. Conjugates and methods of preparation and treatment with the conjugates are also disclosed. The resultant polymer-amines are of sufficient purity so that expensive and time consuming purification steps required for pharmaceutical grade polymers are avoided.
摘要翻译： 公开了制备基本上具有高纯度的含有电子对的部分的非抗原性聚合物的方法。 聚合物可用作合成基于胺的聚合物的中间体和用于与亲核试剂缀合的活化聚合物的形成。 还公开了共轭物的共轭物和制备和处理方法。 得到的聚合物胺具有足够的纯度，因此避免了医药级聚合物所需的昂贵且耗时的纯化步骤。
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