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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

WO2010065756A3 USIRNA COMPLEXES 审中-公开
标题翻译： USIRNA配合物
公开(公告)号：WO2010065756A3
公开(公告)日：2010-11-25
申请号：PCT/US2009066610
申请日：2009-12-03
申请人： MDRNA INC , TEMPLIN MICHAEL V , VAISH NARENDRA K , POLISKY BARRY A , HOUSTON MICHAEL E
发明人： TEMPLIN MICHAEL V , VAISH NARENDRA K , POLISKY BARRY A , HOUSTON MICHAEL E
IPC分类号： C12N15/113 , A61K31/7088
CPC分类号： C12N15/1138 , C12N15/113 , C12N15/1131 , C12N2310/14 , C12N2310/32 , C12N2310/323 , C12N2320/30
摘要： This disclosure provides double-stranded RNA complexes having one or more hydroxymethyl substituted nucleomonomer(s) in the passenger strand (or sense strand) of an RNA complex. RNA complexes of the disclosure may be useful for therapeutic applications, diagnostic applications or research applications. RNA complexes include short interfering RNA complexes (siRNA) capable of modulating gene expression comprising an antisense strand and a continuous or a discontinuous passenger strand ("sense strand"). Further, one or more hydroxymethyl substituted nucleomonomer(s) of this disclosure may be positioned at the 3 '-end, at the 5 '-end, at both the 3 '-end and 5 'end.
摘要翻译：本公开提供了在RNA复合物的过客链（或有义链）中具有一个或多个羟甲基取代的核苷酸单体的双链RNA复合物。本公开的RNA复合物可用于治疗应用，诊断应用或研究应用。 RNA复合物包括能够调节基因表达的短干扰RNA复合物（siRNA），其包含反义链和连续或不连续的过客链（“有义链”）。此外，本公开内容的一种或多种羟甲基取代的核苷酸单体可位于3'末端，5'末端，3'末端和5'末端。

3. 发明申请

WO2007014391A2 TIGHT JUNCTION MODULATING PEPTIDE COMPONENTS FOR ENHANCING MUCOSAL DELIVERY 审中-公开
标题翻译：用于增强粘膜递送的轻度连接调节肽组分
公开(公告)号：WO2007014391A2
公开(公告)日：2007-02-01
申请号：PCT/US2006029768
申请日：2006-07-27
申请人： NASTECH PHARM CO , QUAY STEVEN C , QUAY SHU-CHIH CHEN , CUI KUNYUAN , SILENO ANTHONY P , JOHNSON PAUL HICKOK , HOUSTON MICHAEL E , COSTANTINO HENRY R , TEMPLIN MICHAEL V , LAMHARZI NAJIB
发明人： QUAY STEVEN C , QUAY SHU-CHIH CHEN , CUI KUNYUAN , SILENO ANTHONY P , JOHNSON PAUL HICKOK , HOUSTON MICHAEL E , COSTANTINO HENRY R , TEMPLIN MICHAEL V , LAMHARZI NAJIB
IPC分类号： C07K14/435 , A61K38/00
CPC分类号： C07K14/00 , A61K9/0043 , A61K31/55 , A61K38/12 , A61K38/22 , A61K38/23 , A61K45/06 , A61K47/42 , A61K47/60 , A61K2300/00
摘要： Compounds and components including sequences for mucosal epithelial transport of an active agent are given. Tight junction modulating peptide components are described for use in transport and delivery. Permeability can be enhanced with reversibility. Compounds and components for enhanced delivery may be peptide or protein variants, conjugates, or other analog types and structures.
摘要翻译：给出了包括活性剂粘膜上皮转运序列的化合物和组分。描述了紧密连接调节肽组分用于运输和递送。渗透性可以提高可逆性。用于增强递送的化合物和组分可以是肽或蛋白质变体，缀合物或其它类似物和结构。

4. 发明申请

WO2011133584A3 NUCLEIC ACID COMPOUNDS FOR INHIBITING HRAS GENE EXPRESSION AND USES THEREOF 审中-公开
标题翻译：用于抑制人源基因表达的核酸化合物及其用途
公开(公告)号：WO2011133584A3
公开(公告)日：2012-01-12
申请号：PCT/US2011033102
申请日：2011-04-19
申请人： MARINA BIOTECH INC , VAISH NARENDRA K , SETH SHAGUNA , FOSNAUGH KATHY L , HOUSTON MICHAEL E , TEMPLIN MICHAEL V
发明人： VAISH NARENDRA K , SETH SHAGUNA , FOSNAUGH KATHY L , HOUSTON MICHAEL E , TEMPLIN MICHAEL V
IPC分类号： C12N15/113 , A61P35/00
CPC分类号： C12N15/1135 , C12N2310/14 , C12N2310/321 , C12N2310/344 , C12N2310/3521
摘要： This disclosure provides double- stranded nucleic acid complexes having one or more hydroxymethyl substituted nucleomonomer(s) and wherein one strand is complementary to a HRAS mRNA. Nucleic acid complexes of the disclosure may be useful for therapeutic applications, diagnostic applications or research applications. Nucleic complexes include short interfering RNA complexes (siRNA) capable of modulating gene expression comprising an antisense strand and a continuous or a discontinuous passenger strand ("sense strand"). Further, one or more hydroxymethyl substituted nucleomonomer(s) of this disclosure may be positioned at the 3 '-end, at the 5 '-end, at both the 3 '-end and 5 'end, and/or in a double-stranded region of a nucleic acid complex. Also provided are methods of decreasing expression of a HRAS gene in a cell or in a subject to treat a HRAS-related disease.
摘要翻译：本公开提供了具有一个或多个羟甲基取代的核小体单体的双链核酸复合物，其中一条链与HRAS mRNA互补。本公开的核酸复合物可用于治疗应用，诊断应用或研究应用。核复合物包括能够调节包含反义链和连续或不连续乘客链（“有义链”）的基因表达的短干扰RNA复合物（siRNA）。此外，本公开的一个或多个羟甲基取代的核小体单体可以位于3'端，5“端，3”端和5“端，和/ 核酸复合物的双链区。还提供减少细胞或受试者中HRAS基因表达以治疗HRAS相关疾病的方法。

5. 发明申请

WO2011139842A3 NUCLEIC ACID COMPOUNDS FOR INHIBITING FGFR3 GENE EXPRESSION AND USES THEREOF 审中-公开
标题翻译：用于抑制FGFR3基因表达的核酸化合物及其用途
公开(公告)号：WO2011139842A3
公开(公告)日：2012-01-26
申请号：PCT/US2011034352
申请日：2011-04-28
申请人： MARINA BIOTECH INC , VAISH NARENDRA K , SETH SHAGUNA , FOSNAUGH KATHY L , HOUSTON MICHAEL E , TEMPLIN MICHAEL V
发明人： VAISH NARENDRA K , SETH SHAGUNA , FOSNAUGH KATHY L , HOUSTON MICHAEL E , TEMPLIN MICHAEL V
IPC分类号： C12N15/113 , A61P35/00
CPC分类号： C12N15/1138 , C12N2310/14 , C12N2310/321 , C12N2310/323 , C12N2310/533 , C12N2310/3521
摘要： This disclosure provides double- stranded nucleic acid complexes having one or more hydroxymethyl substituted nucleomonomer(s) and wherein one strand is complementary to a FGFR3 mRNA. Nucleic acid complexes of the disclosure may be useful for therapeutic applications, diagnostic applications or research applications. Nucleic complexes include short interfering RNA complexes (siRNA) capable of modulating gene expression comprising an antisense strand and a continuous or a discontinuous passenger strand ("sense strand"). Further, one or more hydroxymethyl substituted nucleomonomer(s) of this disclosure may be positioned at the 3 '-end, at the 5 '-end, at both the 3 '-end and 5 'end, and/or in a double- stranded region of a nucleic acid complex. Also provided are methods of decreasing expression of a FGFR3 gene in a cell or in a subject to treat a FGFR3-related disease.
摘要翻译：本公开提供了具有一个或多个羟甲基取代的核小体单体的双链核酸复合物，其中一条链与FGFR3 mRNA互补。本公开的核酸复合物可用于治疗应用，诊断应用或研究应用。核复合物包括能够调节包含反义链和连续或不连续乘客链（“有义链”）的基因表达的短干扰RNA复合物（siRNA）。此外，本公开的一个或多个羟甲基取代的核小体单体可以位于3'端，5“端，3”端和5“端，和/ 核酸复合物的双链区。还提供减少细胞或受试者中FGFR3基因表达以治疗FGFR3相关疾病的方法。

6. 发明申请

WO2007014391B1 TIGHT JUNCTION MODULATING PEPTIDE COMPONENTS FOR ENHANCING MUCOSAL DELIVERY OF THERAPEUTIC AGENTS 审中-公开
标题翻译：用于增强治疗药物的粘膜递送的轻度结节调节肽组分
公开(公告)号：WO2007014391B1
公开(公告)日：2007-08-16
申请号：PCT/US2006029768
申请日：2006-07-27
申请人： NASTECH PHARM CO , QUAY STEVEN C , QUAY SHU-CHIH CHEN , CUI KUNYUAN , SILENO ANTHONY P , JOHNSON PAUL HICKOK , HOUSTON MICHAEL E , COSTANTINO HENRY R , TEMPLIN MICHAEL V , LAMHARZI NAJIB
发明人： QUAY STEVEN C , QUAY SHU-CHIH CHEN , CUI KUNYUAN , SILENO ANTHONY P , JOHNSON PAUL HICKOK , HOUSTON MICHAEL E , COSTANTINO HENRY R , TEMPLIN MICHAEL V , LAMHARZI NAJIB
IPC分类号： C07K14/435 , A61K38/00
CPC分类号： C07K14/00 , A61K9/0043 , A61K31/55 , A61K38/12 , A61K38/22 , A61K38/23 , A61K45/06 , A61K47/42 , A61K47/60 , A61K2300/00
摘要： Compounds and components including sequences for mucosal epithelial transport of an active agent are given. Tight junction modulating peptide components are described for use in transport and delivery. Permeability can be enhanced with reversibility. Compounds and components for enhanced delivery may be peptide or protein variants, conjugates, or other analog types and structures.
摘要翻译：给出了包括活性剂粘膜上皮转运序列的化合物和组分。描述了紧密连接调节肽组分用于运输和递送。渗透性可以提高可逆性。用于增强递送的化合物和组分可以是肽或蛋白质变体，缀合物或其它类似物和结构。

7. 发明申请

WO2007061434B1 A PHARMACEUTICAL FORMULATION OF GLP-1 AND ITS USE FOR TREATING A METABOLIC SYNDROME 审中-公开
标题翻译： GLP-1的药物制剂及其用于治疗代谢综合症的用途
公开(公告)号：WO2007061434B1
公开(公告)日：2007-10-11
申请号：PCT/US2006008928
申请日：2006-03-10
申请人： NASTECH PHARM CO , KLEPPE MARY S , TEMPLIN MICHAEL V , QUAY STEVEN C
发明人： KLEPPE MARY S , TEMPLIN MICHAEL V , QUAY STEVEN C
IPC分类号： A61K38/26
CPC分类号： A61K38/12 , A61K9/0043 , A61K38/00 , A61K38/26 , A61K45/06 , A61K2300/00
摘要： What is described is a pharmaceutical formulation for intranasal delivery of glucagon-like protein- 1 (GLP-1), comprising an aqueous mixture of GLP-1 and a dipeptidyl aminopeptidase (DPP) IV inhibitor, and a method of treating a metabolic syndrome in a mammal, comprising intranasally administering a pharmaceutical formulation comprising a pharmaceutically effective amount of GLP-1.
摘要翻译：所描述的是用于鼻内递送胰高血糖素样蛋白-1（GLP-1）的药物制剂，其包含GLP-1和二肽氨基肽酶（DPP）IV抑制剂的含水混合物，以及治疗代谢综合征的方法包括鼻内施用包含药学有效量的GLP-1的药物制剂。

8. 发明申请

WO2007044375A2 PTH FORMULATIONS AND METHODS OF USE 审中-公开
标题翻译： PTH配方及使用方法
公开(公告)号：WO2007044375A2
公开(公告)日：2007-04-19
申请号：PCT/US2006038735
申请日：2006-10-03
申请人： NASTECH PHARM CO , COSTANTINO HENRY R , QUAY STEVEN C , TEMPLIN MICHAEL V , LI CHING-YUAN , SILENO ANTHONY P , PRINN KRISTIN B
发明人： COSTANTINO HENRY R , QUAY STEVEN C , TEMPLIN MICHAEL V , LI CHING-YUAN , SILENO ANTHONY P , PRINN KRISTIN B
IPC分类号： A61K38/29 , A61K47/18 , A61K47/24 , A61K47/26 , A61K47/40 , A61P19/10
CPC分类号： A61K9/0043 , A61K38/29 , A61K47/183 , A61K47/24 , A61K47/26 , A61K47/40
摘要： What is described is an aqueous pharmaceutical formulation of PTH, comprising a therapeutically effective amount of PTH(l-34) and one or more excipients selected from the group consisting of a solubilizing agent, a chelating agent, one or more polyols, and a nonionic surface active agent, a method of using such formulation for treating osteoporosis in a mammal by intranasal administration, and use of PTH(I -34) in the manufacture of such formulation for treating osteoporosis in a mammal.
摘要翻译：描述的是PTH的水性药物制剂，其包含治疗有效量的PTH（1-34）和一种或多种赋形剂，其选自增溶剂，螯合剂，一种或多种多元醇和非离子表面活性剂表面活性剂，使用这种制剂通过鼻内给药治疗哺乳动物的骨质疏松症的方法，以及在制备用于治疗哺乳动物骨质疏松症的制剂中使用PTH（I-34）。

9. 发明申请

WO2007065156B1 PHARMACEUTICAL FORMULATION FOR INCREASED EPITHELIAL PERMEABILITY OF GLUCOSE-REGULATING PEPTIDE 审中-公开
公开(公告)号：WO2007065156B1
公开(公告)日：2007-09-13
申请号：PCT/US2006061503
申请日：2006-12-01
申请人： NASTECH PHARM CO , QUAY STEVEN C , COSTANTINO HENRY R , TEMPLIN MICHAEL V , LEONARD ALEXIS KAYS , KLEPPE MARY S , SESTAK JOSHUA O
发明人： QUAY STEVEN C , COSTANTINO HENRY R , TEMPLIN MICHAEL V , LEONARD ALEXIS KAYS , KLEPPE MARY S , SESTAK JOSHUA O
IPC分类号： A61K38/26
CPC分类号： A61K38/26 , A61K9/0043
摘要： What is described is a pharmaceutical formulation comprising a mixture of a pharmaceutically effective amount of glucose-regulating peptide (GRP) and enhancers, wherein the pharmaceutical formulation is used in the treatment of a metabolic syndrome.

10. 发明申请

WO2007044069A3 PTH FORMULATIONS AND METHODS OF USE 审中-公开
标题翻译： PTH配方及使用方法
公开(公告)号：WO2007044069A3
公开(公告)日：2009-08-27
申请号：PCT/US2006013377
申请日：2006-04-10
申请人： NASTECH PHARM CO , COSTANTINO HENRY R , QUAY STEVEN C , TEMPLIN MICHAEL V , LI CHING-YUAN , SILENO ANTHONY
发明人： COSTANTINO HENRY R , QUAY STEVEN C , TEMPLIN MICHAEL V , LI CHING-YUAN , SILENO ANTHONY
IPC分类号： A61K38/29 , A61K47/18 , A61K47/24 , A61K47/26 , A61K47/40 , A61P19/10
CPC分类号： A61K9/0043 , A61K38/29 , A61K47/26 , A61K47/40
摘要： What is described is an aqueous pharmaceutical formulation of PTH, comprising PTH(I -34) and a nonionic surface active agent, a dosage form comprising the formulation, a system of delivering PTH to a human, comprising exposing a layer of mucosal cells to the formulation, and a method of using such formulation for treating osteoporosis in a mammal, preferably wherein a time to maximum plasma concentration, Tmax, of PTH(I -34) following administration is less than 30 minutes. Also described is a method for treating osteoporosis in a mammal comprising administering intranasally a PTH formulation comprises a therapeutically effective amount of PTH(I -34) and one or more excipients selected from the group consisting of a solubilizing agent, a chelating agent, and one or more polyols. Comprising PTH(l-34) and a nonionic surface active agent. Also described is a use of PTH(l-34) in the manufacture of a medicament for treating osteoporosis in a mammal, wherein the medicament comprises a therapeutically effective amount of PTH(I -34) and one or more excipients selected from the group consisting of a nonionic surface active agent, a solubilizing agent, a chelating agent, and one or more polyols.
摘要翻译：描述的是含有PTH（I-34）和非离子表面活性剂的PTH水性药物制剂，包含该制剂的剂型，将PTH递送给人的系统，包括将粘膜细胞层暴露于制剂和使用这种制剂治疗哺乳动物骨质疏松症的方法，优选其中施用后PTH（I-34）的时间至最大血浆浓度T max小于30分钟。还描述了一种治疗哺乳动物骨质疏松症的方法，其包括鼻内施用PTH制剂，其包含治疗有效量的PTH（I-34）和一种或多种赋形剂，其选自增溶剂，螯合剂和一种或更多的多元醇。包括PTH（1-34）和非离子表面活性剂。还描述了PTH（1-34）在制备用于治疗哺乳动物的骨质疏松症的药物中的用途，其中所述药物包含治疗有效量的PTH（I-34）和一种或多种选自以下的赋形剂：的非离子表面活性剂，增溶剂，螯合剂和一种或多种多元醇。

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