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1. 发明申请

WO2010045512A3 PROCESSES AND COMPOSITIONS FOR LIPOSOMAL AND EFFICIENT DELIVERY OF GENE SILENCING THERAPEUTICS 审中-公开
标题翻译：用于脂质和有效递送基因沉默治疗的方法和组合物
公开(公告)号：WO2010045512A3
公开(公告)日：2011-01-27
申请号：PCT/US2009060930
申请日：2009-10-16
申请人： MDRNA INC , POLISKY BARRY A , ADAMI ROGER C , TEMPLIN MICHAEL V , HARVIE PIERROT , JOHNS RACHEL E , GIYANANI JAYA S , HOUSTON MICHAEL E
发明人： POLISKY BARRY A , ADAMI ROGER C , TEMPLIN MICHAEL V , HARVIE PIERROT , JOHNS RACHEL E , GIYANANI JAYA S , HOUSTON MICHAEL E
IPC分类号： A61K9/127 , A61K48/00 , C12N15/11 , C12N15/88
CPC分类号： A61K9/127 , A61K9/1271 , A61K9/1277 , C12N15/111 , C12N15/113 , C12N15/88 , C12N2310/14 , C12N2320/32
摘要： Processes and compositions for liposomal delivery of therapeuticals prepared by contacting an aqueous solution of an active agent with a solution of liposome-forming components containing one or more DILA2 amino acid compounds or lipids in organic solvent to form an impinging stream. A protocol including flow rates, pH, and an incubation period are used to control formation of liposomal components for therapeutic applications. The impinging stream may be collected and incubated to prepare a liposomal formulation which encapsulates the active agent. The composition can be quenched with buffer and filtered by tangential flow and diafiltration and other means for finishing as a pharmaceutical composition. An efficiency for delivering a drug cargo is provided. Compositions can include a liposome containing one or more carrier particles, each carrier particle having an active agent and a peptide, wherein the ratio of the mass of the peptide plus the mass of the liposome to the mass of the active agent is less than about 15.
摘要翻译：通过使活性剂的水溶液与含有一种或多种DILA2氨基酸化合物或脂质的脂质体形成成分的溶液在有机溶剂中接触形成冲击流而制备的治疗剂的脂质体递送的方法和组合物。使用包括流速，pH和潜伏期的方案来控制用于治疗应用的脂质体组分的形成。可以收集冲击流并将其温育以制备封装活性剂的脂质体制剂。组合物可以用缓冲液淬火并通过切向流动和渗滤过滤，以及用作药物组合物的其它装置。提供了提供药物的效率。组合物可包括含有一种或多种载体颗粒的脂质体，每种载体颗粒具有活性剂和肽，其中肽的质量与脂质体的质量与活性剂的质量之比小于约15 。

2. 发明申请

WO2009046220A2 LIPOPEPTIDES FOR DELIVERY OF NUCLEIC ACIDS 审中-公开
标题翻译：用于输送核酸的脂质体
公开(公告)号：WO2009046220A2
公开(公告)日：2009-04-09
申请号：PCT/US2008078627
申请日：2008-10-02
申请人： MDRNA INC , ADAMI ROGER C , HOUSTON MICHAEL E , JOHNS RACHEL E
发明人： ADAMI ROGER C , HOUSTON MICHAEL E , JOHNS RACHEL E
IPC分类号： A61K47/48 , A61P3/00 , A61P29/00 , A61P31/12 , A61P35/00 , C12N15/87
CPC分类号： A61K47/42 , A61K31/713 , A61K47/543 , A61K47/544 , A61K47/6455 , A61K48/00 , A61K48/0033 , A61K48/0041 , C07K7/08 , C07K14/00 , C07K14/001 , C12N15/113 , C12N15/87 , C12N2310/14
摘要： Lipopeptide compounds comprising a peptide having 2 to 100 amino acid residues, and having a lipophilic group attached to at least one terminus of the peptide or to at least one amino acid residue of the peptide, and salts and uses thereof. The lipophilic group may be attached to the N-terminus, C-terminus or both termini of the peptide. The lipophilic group may be attached to at least one interal amino acid residue (i.e., an amino acid residue that is not the N-terminus or the C-terminus amino acid residue of the peptide). The lipophilic group may be attached to either termini or both and at least one internal amino acid residue.
摘要翻译：包含具有2至100个氨基酸残基并且具有连接至该肽的至少一个末端或该肽的至少一个氨基酸残基的亲脂基团的脂肽化合物及其盐和用途。亲脂基团可以连接到肽的N末端，C末端或两个末端。亲脂基团可以连接到至少一个间氨基酸残基（即，不是肽的N-末端或C末端氨基酸残基的氨基酸残基）。亲油基团可以连接到末端或两者和至少一个内部氨基酸残基。

3. 发明申请

WO2010059829A3 COMPOSITIONS AND METHODS FOR TRIGGERED RELEASE RNA THERAPEUTICS 审中-公开
标题翻译：用于触发释放RNA治疗的组合物和方法
公开(公告)号：WO2010059829A3
公开(公告)日：2010-09-30
申请号：PCT/US2009065153
申请日：2009-11-19
申请人： MDRNA INC , ADAMI ROGER C , JOHNS RACHEL E
发明人： ADAMI ROGER C , JOHNS RACHEL E
IPC分类号： A61K48/00
CPC分类号： A61K47/51
摘要： Provided are compositions for delivery of an active agent including a ribonucleic acid, an RNAi-inducing agent, or an antisense agent, comprising a DILA2 amino acid compound and an intracellularly-cleavable peptide of from six to 100 amino acid residues in length, the intracellularly-cleavable peptide comprising two or more nucleic acid-binding region amino acid sequences connected by one or more intracellularly-cleavable linker amino acid sequences, wherein the nucleic acid-binding regions each contain two or more positively-charged amino acid residues. Further provided are methods of using the compositions to efficiently deliver an active agent such as a nucleic acid.
摘要翻译：提供了用于递送包括核糖核酸，RNAi诱导剂或反义剂的活性剂的组合物，其包含长度为6至100个氨基酸残基的DILA2氨基酸化合物和细胞内可裂解肽，细胞内包含由一个或多个细胞内可切割的连接氨基酸序列连接的两个或多个核酸结合区氨基酸序列的可切除肽，其中所述核酸结合区各自含有两个或多个带正电荷的氨基酸残基。还提供了使用组合物有效递送活性剂如核酸的方法。

4. 发明专利

CA2701274A1 LIPOPEPTIDES FOR DELIVERY OF NUCLEIC ACIDS 未知
公开(公告)号：CA2701274A1
公开(公告)日：2009-04-09
申请号：CA2701274
申请日：2008-10-02
申请人： MDRNA INC
发明人： ADAMI ROGER C , HOUSTON MICHAEL E , JOHNS RACHEL E
IPC分类号： A61K47/48 , A61P3/00 , A61P29/00 , A61P31/12 , A61P35/00 , C12N15/87
摘要： Lipopeptide compounds comprising a peptide having 2 to 100 amino acid residues, and having a lipophilic group attached to at least one terminus of the peptide or to at least one amino acid residue of the peptide, and salts and uses thereof. The lipophilic group may be attached to the N-terminus, C-terminus or both termini of the peptide. The lipophilic group may be attached to at least one interal amino acid residue (i.e., an amino acid residue that is not the N-terminus or the C-terminus amino acid residue of the peptide). The lipophilic group may be attached to either termini or both and at least one internal amino acid residue.

5. 发明专利

AU2008308679A1 Lipopeptides for delivery of nucleic acids 未知
公开(公告)号：AU2008308679A1
公开(公告)日：2009-04-09
申请号：AU2008308679
申请日：2008-10-02
申请人： MDRNA INC
发明人： JOHNS RACHEL E , HOUSTON MICHAEL E , ADAMI ROGER C
IPC分类号： A61K47/48 , A61P3/00 , A61P29/00 , A61P31/12 , A61P35/00 , C12N15/87

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