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公开(公告)号：US20060008830A1
公开(公告)日：2006-01-12
申请号：US11176405
申请日：2005-07-06
申请人： Paul Slattum , Vladimir Budker , Andrei Blokhin
发明人： Paul Slattum , Vladimir Budker , Andrei Blokhin
CPC分类号： C07H21/04
摘要： Compounds and methods are provided for covalent end-labeling of polynucleotides. Incorporation of a nucleic acid affinity group improves the efficiency of reaction of aldehyde reactive groups with the nucleic acid leading to more efficient labeling.
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公开(公告)号：US20060115848A1
公开(公告)日：2006-06-01
申请号：US11290802
申请日：2005-11-29
申请人： Andrei Blokhin , Paul Slattum , Vladimir Budker
发明人： Andrei Blokhin , Paul Slattum , Vladimir Budker
IPC分类号： C12Q1/68 , C07K14/435 , C07H21/04 , C07D403/02 , A61K38/16
CPC分类号： C07D495/04 , C07D209/18
摘要： Compounds and methods are provided for covalent end-labeling of polynucleotides. Incorporation of a nucleic acid affinity group improves the efficiency of reaction of aldehyde reactive groups with the nucleic acid leading to more efficient labeling.
摘要翻译： 化合物和方法用于多核苷酸的共价末端标记。 掺入核酸亲和基团提高醛反应性基团与核酸的反应效率，从而导致更有效的标记。
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公开(公告)号：US20080152661A1
公开(公告)日：2008-06-26
申请号：US11840468
申请日：2007-08-17
申请人： David B. Rozema , Darren H. Wakefield , Jason Klein , So Wong , Jon A. Wolff , David L. Lewis , James E. Hagstrom , Andrei Blokhin , Vladimir Trubetskoy , Hans Herweijer
发明人： David B. Rozema , Darren H. Wakefield , Jason Klein , So Wong , Jon A. Wolff , David L. Lewis , James E. Hagstrom , Andrei Blokhin , Vladimir Trubetskoy , Hans Herweijer
IPC分类号： A61K31/70 , A61K39/395 , C12N5/00 , A61K38/00
CPC分类号： C12N15/87 , A01K2217/058 , A01K2267/0362 , A61K47/58 , A61K48/0041
摘要： The present invention is directed to compounds, compositions, and methods useful for delivering polynucleotides or other cell-impermeable molecules to mammalian cells. Described are polyconjugates systems that incorporate targeting, anti-opsonization, anti-aggregation, and transfection activities into small biocompatible in vivo delivery vehicles. The use of multiple reversible linkages connecting component parts provides for physiologically responsive activity modulation.
摘要翻译： 本发明涉及可用于将多核苷酸或其它细胞不可渗透分子递送至哺乳动物细胞的化合物，组合物和方法。 描述了将靶向，抗调理作用，抗聚集和转染活性结合到小的生物相容性体内递送载体中的多偶联体系。 连接组成部分的多个可逆连接的使用提供了生理响应活性调节。
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4.发明申请Cycloalkyl substituted polyamines for cancer therapy and methods of synthesis therefor 失效用于癌症治疗的环烷基取代多胺及其合成方法公开(公告)号：US20070287754A1
公开(公告)日：2007-12-13
申请号：US11810409
申请日：2007-06-04
申请人： Benjamin Frydman , Linda Clifford , Aldonia Valasinas , Andrei Blokhin , Aparajita Sarkar , Hirak Basu , Venodhar Reddy , Laurence Marton , Yu Wang
发明人： Benjamin Frydman , Linda Clifford , Aldonia Valasinas , Andrei Blokhin , Aparajita Sarkar , Hirak Basu , Venodhar Reddy , Laurence Marton , Yu Wang
IPC分类号： A61K31/13 , A61P35/00 , C07C211/13
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.
摘要翻译： 公开了可用于治疗由异常细胞增殖表现的癌症和其它疾病的构象限制性多胺化合物。 还公开了合成这些化合物的改进方法。 在本发明的一种方法中，含有含碳或含碳原子的化合物与烯烃化合物的双键反应形成环丙基环作为合成中的第一步。
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公开(公告)号：US20050080144A1
公开(公告)日：2005-04-14
申请号：US10957105
申请日：2004-10-01
IPC分类号： A61K31/785 , A61K31/132 , A61P35/00 , C07B61/00 , C07C209/26 , C07C211/14 , C07C213/00 , C07C215/18 , C08G73/02 , A61K31/13 , C07C211/13
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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6.发明申请公开(公告)号：US20130190484A1
公开(公告)日：2013-07-25
申请号：US13833814
申请日：2013-03-15
申请人： David Rozema , David Lewis , Darren Wakefield , Eric Kitas , Philipp Hadwiger , Jon Wolff , Ingo Roehl , Peter Mohr , Torsten Hoffmann , Kerstin Jahn-Hofmann , Hans Martin Mueller , Guenther Ott , Andrei Blokhin , Jeffrey Carlson , Jonathan Benson
发明人： David Rozema , David Lewis , Darren Wakefield , Eric Kitas , Philipp Hadwiger , Jon Wolff , Ingo Roehl , Peter Mohr , Torsten Hoffmann , Kerstin Jahn-Hofmann , Hans Martin Mueller , Guenther Ott , Andrei Blokhin , Jeffrey Carlson , Jonathan Benson
IPC分类号： C12N15/113 , C07C271/20 , C07C69/96
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：US20080269450A1
公开(公告)日：2008-10-30
申请号：US12140741
申请日：2008-06-17
申请人： Darren H. Wakefield , David B. Rozema , Sean D. Monahan , Andrei Blokhin , Lori Higgs , Jon A. Wolff , James E. Hagstrom
发明人： Darren H. Wakefield , David B. Rozema , Sean D. Monahan , Andrei Blokhin , Lori Higgs , Jon A. Wolff , James E. Hagstrom
IPC分类号： C08G69/02 , C08F251/00
CPC分类号： C12N15/87 , A01K2217/058 , A01K2267/0362 , A61K47/58 , A61K48/0041
摘要： The present invention is directed to membrane active polymers useful for cellular delivery of compounds. Described are polyconjugates systems that incorporate targeting, anti-opsonization, anti-aggregation, and transfection activities into small biocompatible in vivo delivery conjugates. The use of reversible modification provides for physiologically responsive activity modulation.
摘要翻译： 本发明涉及可用于细胞递送化合物的膜活性聚合物。 描述了将靶向，抗调理作用，抗聚集和转染活性结合到小的生物相容性体内递送缀合物中的多偶联体系。 使用可逆修饰提供了生理反应活性调节。
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公开(公告)号：US20060030735A1
公开(公告)日：2006-02-09
申请号：US11205341
申请日：2005-08-16
申请人： Benjamin Frydman , Linda Clifford , Aldonia Valasinas , Andrei Blokhin , Aparajita Sarkar , Hirak Basu , Venodhar Reddy , Laurence Marton , Yu Wang
发明人： Benjamin Frydman , Linda Clifford , Aldonia Valasinas , Andrei Blokhin , Aparajita Sarkar , Hirak Basu , Venodhar Reddy , Laurence Marton , Yu Wang
IPC分类号： C07C211/34
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：US20070161692A1
公开(公告)日：2007-07-12
申请号：US11643592
申请日：2006-12-20
申请人： Benjamin Frydman , Linda Clifford , Laurence Marton , Venodhar Reddy , Aldonia Valasinas , Andrei Blokhin , Hirak Basu
发明人： Benjamin Frydman , Linda Clifford , Laurence Marton , Venodhar Reddy , Aldonia Valasinas , Andrei Blokhin , Hirak Basu
IPC分类号： A61K31/409 , A61K31/13 , C07D487/22 , C07C211/13 , C07C211/17
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.
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公开(公告)号：US20060276444A1
公开(公告)日：2006-12-07
申请号：US11350308
申请日：2006-02-07
申请人： Benjamin Frydman , Linda Clifford , Aldonia Valasinas , Venodhar Reddy , Hirak Basu , Aparajita Sarkar , Subhra Bhattacharya , Yu Wang , Laurence Marton , Andrei Blokhin
发明人： Benjamin Frydman , Linda Clifford , Aldonia Valasinas , Venodhar Reddy , Hirak Basu , Aparajita Sarkar , Subhra Bhattacharya , Yu Wang , Laurence Marton , Andrei Blokhin
IPC分类号： A61K31/409 , A61K31/555
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.
摘要翻译： 公开了具有抗癌和抗肿瘤作用的卟啉 - 多胺缀合物。 卟啉部分选择性定位在肿瘤中，而多胺部分用作细胞毒性剂。 还公开了制备和使用卟啉 - 多胺缀合物的方法。
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