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1.发明申请公开(公告)号：US20120172412A1
公开(公告)日：2012-07-05
申请号：US13336028
申请日：2011-12-23
申请人： David B. Rozema , Darren H. Wakefield , David L. Lewis , Jon A. Wolff , Andrei V. Blokhin , Jonathan D. Benson , Jeffrey C. Carlson , Philipp Hadwiger , Eric A. Kitas , Torsten Hoffmann , Kerstin Jahn-Hofmann , Peter Mohr , Hans Martin Mueller , Guenther Ott , Ingo Roehl
发明人： David B. Rozema , Darren H. Wakefield , David L. Lewis , Jon A. Wolff , Andrei V. Blokhin , Jonathan D. Benson , Jeffrey C. Carlson , Philipp Hadwiger , Eric A. Kitas , Torsten Hoffmann , Kerstin Jahn-Hofmann , Peter Mohr , Hans Martin Mueller , Guenther Ott , Ingo Roehl
CPC分类号： A61K38/00 , A61K31/7088 , A61K47/60 , A61K47/65 , A61K48/00 , C07C69/96 , C07C271/20 , C07H15/04 , C07H15/20 , C07H15/26 , C07K7/02 , C07K2317/77 , C12N15/1138 , C12N15/87 , C12N2310/14 , C12N2310/321 , C12N2310/322 , C12N2310/351 , C12N2320/30
摘要： The present invention is directed compositions for delivery of RNA interference (RNAi) polynucleotides to cells in vivo. The compositions comprise amphipathic membrane active polyamines reversibly modified with enzyme cleavable dipeptide-amidobenzyl-carbonate masking agents. Modification masks membrane activity of the polymer while reversibility provides physiological responsiveness. The reversibly modified polyamines (dynamic polyconjugate or DPC) are further covalently linked to an RNAi polynucleotide or co-administered with a targeted RNAi polynucleotide-targeting molecule conjugate.
摘要翻译： 本发明涉及用于将RNA干扰（RNAi）多核苷酸递送至细胞体内的组合物。 组合物包含用酶切割二肽 - 氨基苄基 - 碳酸酯掩蔽剂可逆地修饰的两亲膜活性多胺。 改性掩盖聚合物的膜活性，而可逆性提供生理反应性。 可逆修饰的多胺（动态多偶联物或DPC）进一步共价连接到RNAi多核苷酸或与靶向RNAi多核苷酸靶向分子缀合物共同施用。
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公开(公告)号：US08501930B2
公开(公告)日：2013-08-06
申请号：US13326433
申请日：2011-12-15
申请人： David B. Rozema , Darren H. Wakefield , David L. Lewis , Jon A. Wolff , Andrei V. Blokhin , Jonathan D. Benson , Jeffrey C. Carlson , Philipp Hadwiger , Eric A. Kitas , Torsten Hoffmann , Kerstin Jahn-Hofmann , Peter Mohr , Hans Martin Mueller , Guenther Ott , Ingo Roehl
发明人： David B. Rozema , Darren H. Wakefield , David L. Lewis , Jon A. Wolff , Andrei V. Blokhin , Jonathan D. Benson , Jeffrey C. Carlson , Philipp Hadwiger , Eric A. Kitas , Torsten Hoffmann , Kerstin Jahn-Hofmann , Peter Mohr , Hans Martin Mueller , Guenther Ott , Ingo Roehl
CPC分类号： A61K47/48261 , A61K47/549 , A61K47/64 , A61K47/6415 , C12N15/111 , C12N2310/14 , C12N2310/351 , C12N2310/3515 , C12N2320/32
摘要： The present invention is directed compositions for targeted delivery of RNA interference (RNAi) polynucleotides to hepatocytes in vivo. Targeted RNAi polynucleotides are administered together with co-targeted melittin delivery peptides. Delivery peptides provide membrane penetration function for movement of the RNAi polynucleotides from outside the cell to inside the cell. Reversible modification provides physiological responsiveness to the delivery peptides.
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3.发明授权公开(公告)号：US08426554B2
公开(公告)日：2013-04-23
申请号：US13336028
申请日：2011-12-23
申请人： David B. Rozema , Darren H. Wakefield , David L. Lewis , Jon A. Wolff , Andrei V. Blokhin , Jonathan D. Benson , Jeffrey C. Carlson , Philipp Hadwiger , Eric A. Kitas , Torsten Hoffmann , Kerstin Jahn-Hoffmann , Peter Mohr , Hans Martin Mueller , Guenther Ott , Ingo Roehl
发明人： David B. Rozema , Darren H. Wakefield , David L. Lewis , Jon A. Wolff , Andrei V. Blokhin , Jonathan D. Benson , Jeffrey C. Carlson , Philipp Hadwiger , Eric A. Kitas , Torsten Hoffmann , Kerstin Jahn-Hoffmann , Peter Mohr , Hans Martin Mueller , Guenther Ott , Ingo Roehl
IPC分类号： C07K16/00
CPC分类号： A61K38/00 , A61K31/7088 , A61K47/60 , A61K47/65 , A61K48/00 , C07C69/96 , C07C271/20 , C07H15/04 , C07H15/20 , C07H15/26 , C07K7/02 , C07K2317/77 , C12N15/1138 , C12N15/87 , C12N2310/14 , C12N2310/321 , C12N2310/322 , C12N2310/351 , C12N2320/30
摘要： The present invention is directed compositions for delivery of RNA interference (RNAi) polynucleotides to cells in vivo. The compositions comprise amphipathic membrane active polyamines reversibly modified with enzyme cleavable dipeptide-amidobenzyl-carbonate masking agents. Modification masks membrane activity of the polymer while reversibility provides physiological responsiveness. The reversibly modified polyamines (dynamic polyconjugate or DPC) are further covalently linked to an RNAi polynucleotide or co-administered with a targeted RNAi polynucleotide-targeting molecule conjugate.
摘要翻译： 本发明涉及用于将RNA干扰（RNAi）多核苷酸递送至细胞体内的组合物。 组合物包含用酶切割二肽 - 氨基苄基 - 碳酸酯掩蔽剂可逆地修饰的两亲膜活性多胺。 改性掩盖聚合物的膜活性，而可逆性提供生理反应性。 可逆修饰的多胺（动态多偶联物或DPC）进一步与RNAi多核苷酸共价连接，或与靶向RNAi多核苷酸靶向分子缀合物共同施用。
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公开(公告)号：US20140128584A1
公开(公告)日：2014-05-08
申请号：US14119074
申请日：2012-05-31
IPC分类号： C07D307/89 , C07D307/60 , C07H15/26
CPC分类号： C07D307/89 , C07D307/60 , C07D307/66 , C07D307/88 , C07H15/08 , C07H15/26
摘要： We describe anhydride compounds suitable for physiologically labile modification of amine-containing molecules. The described anhydrides form reversible linkages having desirable kinetics for in vivo delivery of biologically active molecules. Also described are endosomolytic polymers formed by modification of membrane active polyamines with the described anhydrides.
摘要翻译： 我们描述适用于含胺分子的生理不稳定修饰的酸酐化合物。 所述的酸酐形成具有用于体内递送生物活性分子的所需动力学的可逆连接。 还描述了通过用所述酸酐修饰膜活性多胺而形成的内体分解聚合物。
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公开(公告)号：US20120165393A1
公开(公告)日：2012-06-28
申请号：US13326433
申请日：2011-12-15
申请人： David B. Rozema , Darren H. Wakefield , David L. Lewis , Jon A. Wolff , Andrei V. Blokhin , Jonathan D. Benson , Jeffrey C. Carlson , Philipp Hadwiger , Eric A. Kitas , Torsten Hoffman , Kerstin Jahn-Hofmann , Peter Mohr , Hans Martin Mueller , Guenther Ott , Ingo Roehl
发明人： David B. Rozema , Darren H. Wakefield , David L. Lewis , Jon A. Wolff , Andrei V. Blokhin , Jonathan D. Benson , Jeffrey C. Carlson , Philipp Hadwiger , Eric A. Kitas , Torsten Hoffman , Kerstin Jahn-Hofmann , Peter Mohr , Hans Martin Mueller , Guenther Ott , Ingo Roehl
CPC分类号： A61K47/48261 , A61K47/549 , A61K47/64 , A61K47/6415 , C12N15/111 , C12N2310/14 , C12N2310/351 , C12N2310/3515 , C12N2320/32
摘要： The present invention is directed compositions for targeted delivery of RNA interference (RNAi) polynucleotides to hepatocytes in vivo. Targeted RNAi polynucleotides are administered together with co-targeted melittin delivery peptides. Delivery peptides provide membrane penetration function for movement of the RNAi polynucleotides from outside the cell to inside the cell. Reversible modification provides physiological responsiveness to the delivery peptides.
摘要翻译： 本发明涉及用于将体内RNA干扰（RNAi）多核苷酸靶向递送至肝细胞的组合物。 靶向的RNAi多核苷酸与共靶向的蜂毒肽递送肽一起施用。 递送肽提供膜穿透功能，用于将RNAi多核苷酸从细胞外部移动到细胞内。 可逆修饰提供对递送肽的生理反应性。
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公开(公告)号：US07026347B2
公开(公告)日：2006-04-11
申请号：US10606016
申请日：2003-06-24
申请人： Benjamin Frydman , Aldonia L. Valasinas , Venodhar K. Reddy , Hirak S. Basu , Aparajita Sarkar , Subhra Bhattacharya , Yu Wang , Laurence J. Marton , Andrei V. Blokhin
发明人： Benjamin Frydman , Aldonia L. Valasinas , Venodhar K. Reddy , Hirak S. Basu , Aparajita Sarkar , Subhra Bhattacharya , Yu Wang , Laurence J. Marton , Andrei V. Blokhin
IPC分类号： A61K31/40 , A61K31/555 , A61B5/055 , A61B10/00 , C07B47/00
CPC分类号： C07D487/22
摘要： Porphyrin-polyamine conjugate compounds are disclosed which have anticancer and antitumor effects. The porphyrin moiety selectively localizes in tumors, while the polyamine moiety serves as a cytotoxic agent. Methods of making and using the porphyrin-polyamine conjugate compounds are also disclosed.
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公开(公告)号：US07253207B2
公开(公告)日：2007-08-07
申请号：US10909978
申请日：2004-08-02
申请人： Andrei V. Blokhin , Benjamin Frydman , Laurence J. Marton , Karen M. Neder , Jerry Shunneng Sun
发明人： Andrei V. Blokhin , Benjamin Frydman , Laurence J. Marton , Karen M. Neder , Jerry Shunneng Sun
IPC分类号： A61K31/35 , C07D311/92
CPC分类号： C07D295/185 , A61K38/00 , A61K47/65 , C07C45/00 , C07C45/46 , C07C46/00 , C07C50/32 , C07C67/343 , C07C69/708 , C07C69/96 , C07C229/22 , C07C233/31 , C07C237/22 , C07C255/54 , C07C305/20 , C07D207/34 , C07D219/10 , C07D235/18 , C07D307/79 , C07D307/92 , C07D311/92 , C07D317/70 , C07D493/04 , C07F9/12 , C07F9/65517 , C07F9/65522 , C07K5/1013 , C07K7/06 , C07C47/575 , C07C69/734
摘要： Novel quinones are provided, as well as compositions comprising these novel quinones. Methods of using the novel quinones in treatment of various indications including cancer are also provided.
摘要翻译： 提供了新的醌，以及包含这些新型醌的组合物。 还提供了使用该类醌来治疗各种适应症（包括癌症）的方法。
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公开(公告)号：US20090124832A1
公开(公告)日：2009-05-14
申请号：US12357323
申请日：2009-01-21
申请人： Benjamin Frydman , Linda Clifford , Aldonia L. Valasinas , Andrei V. Blokhin , Hirak S. Basu , Laurence J. Marton , Venodhar K. Reddy
发明人： Benjamin Frydman , Linda Clifford , Aldonia L. Valasinas , Andrei V. Blokhin , Hirak S. Basu , Laurence J. Marton , Venodhar K. Reddy
IPC分类号： C07C237/06
CPC分类号： C07C215/18 , C07C211/14
摘要： Oligoamine compounds with anti-cancer and anti-proliferative activity are provided, as well as methods for making and using the compounds. The compounds are shown to be active against prostate cancer cell lines and against prostate cancer tumors in mice. The compounds are also useful in treatment of breast cancer and other cancers.
摘要翻译： 提供具有抗癌和抗增殖活性的寡胺化合物，以及制备和使用该化合物的方法。 该化合物显示出对前列腺癌细胞系和抗小鼠前列腺癌肿瘤的活性。 该化合物也可用于治疗乳腺癌和其它癌症。
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公开(公告)号：US07235695B2
公开(公告)日：2007-06-26
申请号：US11205341
申请日：2005-08-16
申请人： Benjamin Frydman , Aldonia L. Valasinas , Andrei V. Blokhin , Aparajita Sarkar , Hirak S. Basu , Venodhar K. Reddy , Laurence J. Marton , Yu Wang
发明人： Benjamin Frydman , Aldonia L. Valasinas , Andrei V. Blokhin , Aparajita Sarkar , Hirak S. Basu , Venodhar K. Reddy , Laurence J. Marton , Yu Wang
IPC分类号： C07C209/24 , C07C209/28 , C07C211/17
CPC分类号： A61K31/132 , C07C211/18 , C07C2601/02
摘要： Conformationally restricted polyamine compounds useful in treatment of cancer and other diseases marked by abnormal cell proliferation are disclosed. Improved methods of synthesizing such compounds are also disclosed. In one method of the invention, a carbene-bearing or carbene equivalent-bearing compound is reacted with the double bond of an alkene compound to form a cyclopropyl ring as the first step in the synthesis.
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公开(公告)号：US07186825B2
公开(公告)日：2007-03-06
申请号：US10873100
申请日：2004-06-21
申请人： Benjamin Frydman , Laurence J. Marton , Venodhar K. Reddy , Aldonia L. Valasinas , Andrei V. Blokhin , Hirak S. Basu
发明人： Benjamin Frydman , Laurence J. Marton , Venodhar K. Reddy , Aldonia L. Valasinas , Andrei V. Blokhin , Hirak S. Basu
IPC分类号： C07C47/00
CPC分类号： C07C211/09 , A61K38/00 , A61K47/65 , C07C45/46 , C07C67/343 , C07C211/18 , C07C211/22 , C07C211/23 , C07C211/36 , C07C215/14 , C07C257/18 , C07C2601/04 , C07C2601/08 , C07D207/34 , C07D219/10 , C07D235/18 , C07D295/185 , C07D307/79 , C07D307/92 , C07D311/92 , C07D317/70 , C07D487/22 , C07D493/04 , C07K5/1013 , C07K7/06 , C07C47/575 , C07C69/734
摘要： Novel conformationally restricted polyamine analogs are provided, as well as compositions comprising these novel polyamine analogs. Methods of using the novel polyamine analogs in treatment of diseases such as cancer are also provided. Also provided is a method of delivering these analogs specifically to tumor cells by covalently attaching polyamine analogs to porphyrin compounds, along with novel polyamine-porphyrin covalent conjugates.
摘要翻译： 提供新颖的构象限制性多胺类似物，以及包含这些新型多胺类似物的组合物。 还提供了将新型多胺类似物用于治疗诸如癌症的疾病的方法。 还提供了通过将多胺类似物共价连接到卟啉化合物以及新型多胺 - 卟啉共价缀合物将这些类似物特异性递送至肿瘤细胞的方法。
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