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21. 发明授权

US06541476B1 Piperazine derivatives and their use as anti-inflammatory agents 失效
标题翻译：哌嗪衍生物及其作为抗炎剂的用途
公开(公告)号：US06541476B1
公开(公告)日：2003-04-01
申请号：US09713606
申请日：2000-11-14
申请人： John G. Bauman , Brad O. Buckman , Ameen F. Ghannam , Joseph E. Hesselgesser , Richard Horuk , Imadul Islam , Meina Liang , Karen B. May , Sean D. Monahan , Michael M. Morrissey , Howard P. Ng , Kenneth J. Shaw , Guo Ping Wei , Wei Xu , Zuchun Zhao , Wei Zheng
发明人： John G. Bauman , Brad O. Buckman , Ameen F. Ghannam , Joseph E. Hesselgesser , Richard Horuk , Imadul Islam , Meina Liang , Karen B. May , Sean D. Monahan , Michael M. Morrissey , Howard P. Ng , Kenneth J. Shaw , Guo Ping Wei , Wei Xu , Zuchun Zhao , Wei Zheng
IPC分类号： A61K31496
CPC分类号： C07D295/185 , C07D215/18 , C07D241/04 , C07D241/38 , C07D261/14 , C07D295/192 , C07D307/52 , C07D403/06 , C07D403/12 , C07D405/12 , C07D413/12
摘要： This invention is directed to acyl piperazine derivatives, for example, of the following formula (Ia): wherein R1a, R2, R3, R4, R5, and R6 are described herein. These derivatives are useful anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the derivatives, and methods of using the derivatives to treat inflammatory disorders in humans.
摘要翻译：本发明涉及例如下式（Ia）的酰基哌嗪衍生物：其中R1a，R2，R3，R4，R5和R6如本文所述。这些衍生物是有用的抗炎剂。本发明还涉及含有衍生物的药物组合物，以及使用该衍生物治疗人类炎性疾病的方法。

22. 发明授权

US06379966B2 Intravascular delivery of non-viral nucleic acid 有权
标题翻译：非病毒核酸的血管内递送
公开(公告)号：US06379966B2
公开(公告)日：2002-04-30
申请号：US09450315
申请日：1999-11-29
申请人： Sean D. Monahan , Jon A. Wolff , Paul M. Slattum , James E. Hagstrom , Vladimir G. Budker , David B. Rozema
发明人： Sean D. Monahan , Jon A. Wolff , Paul M. Slattum , James E. Hagstrom , Vladimir G. Budker , David B. Rozema
IPC分类号： C12N1585
CPC分类号： A61K48/0041 , A61K48/0008 , A61K48/0083
摘要： Disclosed is a complex for providing nucleic acid expression in a cell. A polynucleotide and a polymer are mixed together to form the complex wherein the zeta potential of the complex is not positive. Then the complex is delivered to the cell wherein the nucleic acid is expressed.
摘要翻译：公开了用于在细胞中提供核酸表达的复合物。将多核苷酸和聚合物混合在一起形成复合物，其中络合物的ζ电位不是正的。然后将复合物递送到其中表达核酸的细胞。

23. 发明授权

US5178791A Halogenated diphenyldiacetylene liquid crystals 失效
标题翻译：卤化二苯基二乙炔液晶
公开(公告)号：US5178791A
公开(公告)日：1993-01-12
申请号：US667668
申请日：1991-03-11
申请人： Michael D. Wand , Sean D. Monahan
发明人： Michael D. Wand , Sean D. Monahan
IPC分类号： C07C43/225 , C09K19/18
CPC分类号： C07C43/225 , C09K19/18
摘要： The present invention provides liquid crystals that are 3,3'-dihalogenated diphenyldiacetylenes of the general formula: ##STR1## where X and Y are, independently of one another, a halogen atom and T.sub.1 and T.sub.2, independently of one another are alkyl or alkenyl or alkoxy tail groups, R.sub.1, R.sub.2, or OR.sub.3, respectively, wherein R.sub.1 and R.sub.3, independently of one another, are straight-chain or branched alkyl groups having three to twenty carbon atoms and R.sub.2 is a mono or diene which may be branched or straight-chain having three to twenty carbon atoms. R.sub.1, R.sub.2, or R.sub.3 may be substituted with one or more halogens, particularly fluorines, except that the C-1 carbon of an OR.sub.3 tail may not be halogenated. One or two non-neighboring CH.sub.2 groups of R.sub.1 or R.sub.3 may be substituted with an O atom, except that the C-1 CH.sub.2 group of an OR.sub.3 tail may not be substituted with an O atom. Liquid crystals in which X=Y=fluorine and T.sub.1 =T.sub.2 are more preferred. Compounds in which R.sub.1, R.sub.2 and R.sub.3 are straight-chain alkyl groups or .omega.-monoene groups are more preferred.
摘要翻译：本发明提供了具有以下通式的3,3'-二卤代二苯基二乙炔的液晶：其中X和Y彼此独立地为卤素原子，且T1和T2彼此独立地为烷基或烯基或烷氧基尾基，R1，R2或OR3，其中R1和R3彼此独立地是具有3-20个碳原子的直链或支链烷基，R2是可以是支链的单或二烯或具有3-20个碳原子的直链。 R1，R2或R3可以被一个或多个卤素，特别是氟取代，除了OR3尾部的C-1碳不能被卤化。 R 1或R 3的一个或两个不相邻的CH 2基团可以被O原子取代，除了OR 3尾部的C-1 CH 2基团可以不被O原子取代。更优选X = Y =氟且T1 = T2的液晶。 R1，R2和R3是直链烷基或ω-单烯基的化合物是更优选的。

24. 发明授权

US07498017B2 Compositions for delivering nucleic acids to cells 失效
标题翻译：用于将核酸递送至细胞的组合物
公开(公告)号：US07498017B2
公开(公告)日：2009-03-03
申请号：US11154494
申请日：2005-06-16
申请人： Sean D. Monahan , Vladimir Trubetskoy
发明人： Sean D. Monahan , Vladimir Trubetskoy
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： A61K48/0041 , C12N15/87
摘要： Cyclic amidinium containing compounds and their methods of preparation are described. Compositions containing these compounds facilitate delivery of biologically active polymers to cells in vitro and in vivo.
摘要翻译：描述了含有环脒的化合物及其制备方法。含有这些化合物的组合物有助于将体内和体内的生物活性聚合物递送至细胞。

25. 发明授权

US07091041B2 Micellar systems 失效
公开(公告)号：US07091041B2
公开(公告)日：2006-08-15
申请号：US10627247
申请日：2003-07-25
申请人： Sean D. Monahan , Jon A. Wolff , Paul M. Slattum , James E. Hagstrom , Vladimir G. Budker
发明人： Sean D. Monahan , Jon A. Wolff , Paul M. Slattum , James E. Hagstrom , Vladimir G. Budker
IPC分类号： C12N15/88 , A61K48/00
CPC分类号： A61K48/0025 , A61K9/1075
摘要： A complex is described that is deliverable to a cell comprising inserting a nucleic acid or other cargo into a reverse micelle. The reverse micelle has the property to compact the nucleic acid for easier delivery.

26. 发明授权

US06897068B2 Polynucleotide complex delivery 有权
标题翻译：多核苷酸复合物递送
公开(公告)号：US06897068B2
公开(公告)日：2005-05-24
申请号：US10085378
申请日：2002-02-27
申请人： Sean D. Monahan , Jon A. Wolff , James E. Hagstrom , Vladimir G. Budker , DAvid B. Rozema , Paul M. Slattum
发明人： Sean D. Monahan , Jon A. Wolff , James E. Hagstrom , Vladimir G. Budker , DAvid B. Rozema , Paul M. Slattum
IPC分类号： A61K48/00 , C12N5/08 , C12N15/64
CPC分类号： A61K48/0008 , A61K48/0041 , A61K48/0083
摘要： Disclosed is a complex for providing nucleic acid expression in a cell. A polynucleotide and a polymer are mixed together to form the complex wherein the zeta potential of the complex is not positive. Then the complex is delivered to the cell wherein the nucleic acid is expressed.
摘要翻译：公开了用于在细胞中提供核酸表达的复合物。将多核苷酸和聚合物混合在一起形成复合物，其中络合物的ζ电位不是正的。然后将复合物递送到其中表达核酸的细胞。

27. 发明授权

US06867196B1 Process for delivering nucleic acids to cardiac tissue 失效
公开(公告)号：US06867196B1
公开(公告)日：2005-03-15
申请号：US09330909
申请日：1999-06-11
申请人： Jon A. Wolff , Hans Herweijer , Larry F. Whitesell , Matthew R. Wolff , Sean D. Monahan , Paul M. Slattum , James E. Hagstrom , Vladimir G. Budker , David B. Rozema
发明人： Jon A. Wolff , Hans Herweijer , Larry F. Whitesell , Matthew R. Wolff , Sean D. Monahan , Paul M. Slattum , James E. Hagstrom , Vladimir G. Budker , David B. Rozema
IPC分类号： A01N43/04 , A61K31/70 , A61K48/00
CPC分类号： A61K48/0008 , A61K48/0075
摘要： A process for delivering a nucleic acid to a cardiac tissue cell in a mammal is described, comprising introducing a composition consisting of a nucleic acid to a blood vessel, which subsequently delivers the nucleic acid to the cardiac tissue cell. The nucleic acid can be DNA or RNA or plasmid DNA or viral. This process is for purposes of gene therapy, and research.

28. 发明授权

US06627616B2 Intravascular delivery of non-viral nucleic acid 有权
公开(公告)号：US06627616B2
公开(公告)日：2003-09-30
申请号：US09447966
申请日：1999-11-23
申请人： Sean D. Monahan , Jon A. Wolff , Paul M. Slattum , James E. Hagstrom , Vladimir G. Budker , David B. Rozema
发明人： Sean D. Monahan , Jon A. Wolff , Paul M. Slattum , James E. Hagstrom , Vladimir G. Budker , David B. Rozema
IPC分类号： C12N1500
CPC分类号： C12N15/113 , A61K31/70 , A61K47/58 , A61K47/59 , A61K47/593 , A61K47/62 , A61K47/6455 , A61K48/00 , A61K48/0008 , A61K48/0041 , A61K48/0083 , C07H21/00 , C12N15/87 , C12N2320/32 , A61K2300/00
摘要： Disclosed is a process for transfecting genetic material into a mammalian cell to alter endogenous properties of the cell. The process comprises designing a polynucleotide for transfection. Then the polynucleotide is inserted into a mammalian vessel such as a tail vein or artery. Prior to insertion, subsequent to insertion, or concurrent with insertion the permeability of the vessel is increased thereby the genetic material is delivered to the parenchymal cell altering endogenous properties of the cell.

29. 发明授权

US5457235A Halogenated diphenyldiacetylene liquid crystals 失效
标题翻译：卤化二苯基二乙炔液晶
公开(公告)号：US5457235A
公开(公告)日：1995-10-10
申请号：US3019
申请日：1993-01-11
申请人： Michael D. Wand , Sean D. Monahan , William N. Thurmes , Kundalika M. More
发明人： Michael D. Wand , Sean D. Monahan , William N. Thurmes , Kundalika M. More
IPC分类号： C07C43/225 , C09K19/18 , C07C319/00 , C07C17/00 , C07C41/00 , C09K19/06
CPC分类号： C07C43/225 , C09K19/18
摘要： The present invention provides liquid crystals that are diphenyldiacetylenes of the general formulas: ##STR1## where W, X, Y and Z are, independently of one another, a halogen atom, a hydrogen atom or a trihalomethyl group, T.sub.1 and T.sub.2, independently of one another can be an alkyl, alkene, alkoxy, alkenoxy, ether, thioalkyl, thioalkenyl, haloalkyl, haloalkoxy or haloalkylether groups having from three to twenty carbon atoms or a silylalkyl, silylalkenyl, silylalkoxy or silylthioalkyl group having from three to twenty-eight carbon atoms and wherein M.sub.1 and M.sub.2 can both be single bonds or one of M.sub.1 or M.sub.2 can be a trans-1,4-cyclohexylene or a --CH.sub.2 CH.sub.2 -trans-1,4-cyclohexylene.
摘要翻译：本发明提供了以下通式的二苯基二乙炔的液晶：其中W，X，Y和Z彼此独立地为卤素原子，氢原子或三卤甲基，T1和具有3至20个碳原子的烷基，烯烃，烷氧基，链烯氧基，醚，硫代烷基，硫代链烯基，卤代烷基，卤代烷氧基或卤代烷基醚，或具有三至二个碳原子的甲硅烷基烷基，甲硅烷基烯基，甲硅烷基烷氧基或甲硅烷基硫代烷基二十八个碳原子，其中M1和M2都可以是单键或M1或M2中的一个可以是反式-1,4-亚环己基或-CH2CH2反式-1,4-亚环己基。

30. 发明授权

US07985406B2 Membrane active heteropolymers 有权
标题翻译：膜活性杂聚物
公开(公告)号：US07985406B2
公开(公告)日：2011-07-26
申请号：US12123124
申请日：2008-05-19
申请人： Sean D. Monahan , Darren H. Wakefield , David B. Rozema , Lori Higgs , Jon A. Wolff , James E. Hagstrom
发明人： Sean D. Monahan , Darren H. Wakefield , David B. Rozema , Lori Higgs , Jon A. Wolff , James E. Hagstrom
IPC分类号： A61K31/74
CPC分类号： C12N15/87 , A01K2217/058 , A01K2267/0362 , A61K47/58 , A61K48/0041
摘要： The present invention is directed to a class of membrane active polymers useful for cellular delivery of compounds. Conjugation of the described membrane active polymers to targeting, anti-opsonization, and anti-aggregation agents provides polymers suitable for in vivo delivery. The use of multiple reversible linkages connecting component parts provides for physiologically responsive activity modulation.
摘要翻译：本发明涉及一类可用于细胞递送化合物的膜活性聚合物。所述膜活性聚合物与靶向，抗调理作用和抗聚集剂的结合提供了适合于体内递送的聚合物。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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