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1.发明授权Compounds related to the amidinium family, pharmaceutical compositions containing same, and uses thereof 失效与idin族有关的化合物，含有它们的药物组合物及其用途公开(公告)号：US06316422B1
公开(公告)日：2001-11-13
申请号：US09706619
申请日：2000-11-06
IPC分类号： A01N4304
CPC分类号： C07J41/0055 , A61K9/1272
摘要： Novel amidinium derivatives of formula (I), wherein R1 is a cholesterol derivative or an alkylamino-NR′R″ grouping, and each of R2 and R3 is independently a hydrogen atom or a grouping of formula (II), wherein each of R4 and R5 is independently a hydrogen atom or a grouping of formula (III), are disclosed. The corresponding pharmaceutical compositions, which are particularly useful in gene therapy for transferring therapeutic genes into cells, are also disclosed.
摘要翻译： 式（I）的新型脒鎓衍生物，其中R1是胆固醇衍生物或烷基氨基-NR'R“基团，R2和R3各自独立地是氢原子或式（II）的基团，其中R4 和R 5独立地为氢原子或式（III）的基团。 还公开了相应的药物组合物，其特别可用于将治疗基因转移到细胞中的基因治疗。
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公开(公告)号：US07772003B2
公开(公告)日：2010-08-10
申请号：US10228959
申请日：2002-08-28
CPC分类号： C07J41/0055
摘要： Transfecting compounds which include an aminoglycoside linked to a lipid via a spacer, and their polyguanidylated derivatives are provided. These compounds are useful for the in vitro, ex vivo, or in vivo transfection of nucleic acids into various cell types.
摘要翻译： 提供了包括通过间隔基与脂质连接的氨基糖苷类及其聚胍基化衍生物的化合物。 这些化合物可用于核酸进入各种细胞类型的体外，离体或体内转染。
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3.发明授权Compounds related to the amidinium family, pharmaceutical compositions containing same, and uses thereof 有权与idin族有关的化合物，含有它们的药物组合物及其用途
公开(公告)号：US6143729A
公开(公告)日：2000-11-07
申请号：US125825
申请日：1998-09-11
IPC分类号： C12N15/09 , A61K9/127 , A61K31/575 , C07C271/60 , C07J41/00 , C12N15/88 , A61K48/00 , A61K31/70 , A61K51/00 , B01J13/02 , B01J13/04 , C12N5/00
CPC分类号： C07J41/0055 , A61K9/1272
摘要： Novel amidinium derivatives of formula (I), wherein R1 is a cholesterol derivative or an alkylamino-NR'R" grouping, and each of R2 and R3 is independently a hydrogen atom or a grouping of formula (II), wherein each of R4 and R5 is independently a hydrogen atom or a grouping of formula (III), are disclosed. The corresponding pharmaceutical compositions, which are particularly useful in gene therapy for transferring therapeutic genes into cells, are also disclosed. ##STR1##
摘要翻译： PCT No.PCT / FR97 / 00364 Sec。 371日期：1998年9月11日 102（e）1998年9月11日PCT PCT 1997年2月28日提交PCT公布。 第WO97 / 31935号公报 日期1997年9月4日，式（I）的新型脒鎓衍生物，其中R1为胆固醇衍生物或烷基氨基-NR'R“基，R2和R3各自独立地为氢原子或式（Ⅱ） ，其中R 4和R 5各自独立地为氢原子或式（III）的基团。 还公开了相应的药物组合物，其特别可用于将治疗基因转移到细胞中的基因治疗。
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4.发明申请COMPOSITIONS COMPRISING A SIRNA AND LIPIDIC 4,5-DISUBSTITUTED 2-DEOXYSTREPTAMINE RING AMINOGLYCOSIDE DERIVATIVES AND USES THEREOF 审中-公开包含SIRNA和脂质的4-dis取代的2-脱氧蛋白环环氨基酰胺衍生物的组合物及其用途公开(公告)号：US20100035974A1
公开(公告)日：2010-02-11
申请号：US12444390
申请日：2007-10-04
IPC分类号： A61K31/7008 , A61K38/02 , C12N5/08
CPC分类号： C12N15/111 , A61K31/713 , A61K48/0025 , C12N2310/14 , C12N2320/32
摘要： The present invention relates to a composition comprising a siRNA and a transfecting compound consisting of an aminoglycoside of the class of 4,5-disubstituted 2-deoxystreptamine ring linked via a spacer molecule to a lipid moiety of formula —(R1)R2 wherein R1 and R2 represent, independently of one another, a hydrogen atom or a fatty aliphatic chain or R1 or R2 is absent, with the proviso that at least one of R1 and R2 represents a fatty aliphatic chain; or —OR3 or —NR3 wherein R3 represents a steroidal derivative. The invention also concerns in vitro and in vivo applications of these compositions.
摘要翻译： 本发明涉及一种组合物，其包含siRNA和由间隔分子连接到式 - （R1）R2的脂质部分的4,5-二取代的2-脱氧链霉胺环类的氨基糖苷组成的转染化合物，其中R 1和 R2彼此独立地表示氢原子或脂肪族脂肪链，或者R1或R2不存在，条件是R1和R2中的至少一个表示脂肪族脂肪链; 或-OR 3或-NR 3，其中R 3表示甾体衍生物。 本发明还涉及这些组合物的体外和体内应用。
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公开(公告)号：US4677218A
公开(公告)日：1987-06-30
申请号：US755486
申请日：1985-07-16
IPC分类号： C07C67/48 , C07C51/15 , C07C67/00 , C07C67/31 , C07C67/317 , C07C67/327 , C07C69/747 , C07C69/757 , C07C325/00 , C07C329/04 , C07C329/20 , C07D307/33 , C07D307/58 , C07D491/04 , C07D491/048 , C07C154/00
CPC分类号： C07D307/33 , C07C51/15 , C07D491/04
摘要： A process for the preparation of racemic or optically active isomers of alkyl esters of cis chrysanthemic of the formula ##STR1## wherein R is alkyl of 1 to 6 carbon atoms comprising reacting a racemic or optically active cis compound of the formula ##STR2## wherein R has the above definition with an aryl halothioformate of the formula ##STR3## wherein Hal is a halogen and Ar is aryl of 6 to 12 carbon atoms optionally substituted with at least one alkyl of 1 to 3 carbon atoms to obtain a compound of the formula ##STR4## of cis configuration and heating the latter optionally in an organic solvent to obtain the compound of formula I and novel intermediates.
摘要翻译： 制备式I的顺式菊花的烷基酯的外消旋或旋光异构体的方法，其中R是1至6个碳原子的烷基，包括使下式的外消旋或光学活性的顺式化合物 其中R具有上述定义，其中Hal为卤素，Ar为任选被至少一个1至3个碳原子的烷基取代的6至12个碳原子的芳基，得到式 顺式构型的配方＆lt; IMAGE＆gt; IV＆gt;任选地在有机溶剂中加热，得到式I化合物和新型中间体。
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公开(公告)号：US20130205493A1
公开(公告)日：2013-08-15
申请号：US13814666
申请日：2011-07-01
IPC分类号： E03C1/02
CPC分类号： E03C1/02 , E03B1/04 , E03B1/042 , E03B1/048 , E03B2001/045 , E03C1/00 , E03C1/0408 , E03C2001/005 , Y02A20/148
摘要： Device for recirculating shower water: a mixing device is connected directly to the hot and cold water inlets, the cold water inlet is connected to a recirculation system; a pump is actuated while the cold water inlet is cut off. In such a device, the hot water flow rate is kept by the mixing device just high enough to compensate for the thermal losses of the water circulating through the system. Water losses are thus minimized to the strict requirement. Advantage: partial continual renewal of the shower water, unlike systems involving full recirculation.
摘要翻译： 用于循环淋浴水的装置：混合装置直接连接到冷热水入口，冷水入口连接到再循环系统; 当冷水入口被切断时，泵被致动。 在这种装置中，热水流量由混合装置保持足够高以补偿循环通过系统的水的热损失。 因此，水损失被最小化到严格的要求。 优点：部分不断更新淋浴水，不同于涉及完全再循环的系统。
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公开(公告)号：US4551545A
公开(公告)日：1985-11-05
申请号：US632203
申请日：1984-07-18
IPC分类号： C07C67/48 , C07C51/15 , C07C67/00 , C07C67/31 , C07C67/317 , C07C67/327 , C07C69/747 , C07C69/757 , C07C325/00 , C07C329/04 , C07C329/20 , C07D307/33 , C07D307/58 , C07D491/04 , C07D491/048
CPC分类号： C07D307/33 , C07C51/15 , C07D491/04
摘要： A process for the preparation of racemic or optically active isomers of alkyl esters of cis chrysanthemic of the formula ##STR1## wherein R is alkyl of 1 to 6 carbon atoms comprising reacting a racemic or optically active cis compound of the formula ##STR2## wherein R has the above definition with an aryl halothioformate of the formula ##STR3## wherein Hal is a halogen and Ar is aryl of 6 to 12 carbon atoms optionally substituted with at least one alkyl of 1 to 3 carbon atoms to obtain a compound of the formula ##STR4## of cis configuration and heating the latter optionally in an organic solvent to obtain the compound of formula I and novel intermediates.
摘要翻译： 制备式I的顺式菊花的烷基酯的外消旋或旋光异构体的方法，其中R是1至6个碳原子的烷基，包括使下式的外消旋或光学活性的顺式化合物 其中R具有上述定义，其中Hal为卤素，Ar为任选被至少一个1至3个碳原子的烷基取代的6至12个碳原子的芳基，得到式 顺式构型的配方＆lt; IMAGE＆gt; IV＆gt;任选地在有机溶剂中加热，得到式I化合物和新型中间体。
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