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公开(公告)号：US20120149761A1
公开(公告)日：2012-06-14
申请号：US13392042
申请日：2010-08-27
申请人： Steven C. Quay
发明人： Steven C. Quay
IPC分类号： A61K31/713 , A61P35/00
CPC分类号： A61K31/713 , A61K9/0019 , A61K31/7105 , C12N15/111 , C12N2310/14 , C12N2310/3231 , C12N2320/52 , C12N2320/53
摘要： Provided in this application are formulations of double stranded RNA molecules and Krebs Cycle analogs that improving ribonuclease stability, reducing off-target effects of a double stranded siRNA molecule, or of reducing interferon responsiveness of a double stranded siRNA molecule using such dsRNA. Also disclosed are methods of treating a primary tumor or a metastasis by contacting circulating tumor cells, a primary tumor, or a metastasis with a described formulation.
摘要翻译： 本申请中提供了双链RNA分子和Krebs Cycle类似物的制剂，其使用这种dsRNA改善了核糖核酸酶稳定性，减少了双链siRNA分子的脱靶效应，或降低了双链siRNA分子的干扰素响应性。 还公开了通过使循环肿瘤细胞，原发性肿瘤或转移与所述制剂接触来治疗原发性肿瘤或转移的方法。
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92.发明申请TIGHT JUNCTION MODULATOR PEPTIDES FOR ENHANCED MUCOSAL DELIVERY OF THERAPEUTIC COMPOUNDS 审中-公开用于增强治疗化学物质输送的轻度结节调节剂肽公开(公告)号：US20100247482A1
公开(公告)日：2010-09-30
申请号：US12108452
申请日：2008-04-23
IPC分类号： A61K38/20 , C07K14/435 , C07K7/08 , A61K38/17 , A61K38/21 , A61K39/00 , A61K39/395 , A61P31/12 , A61P35/00 , A61P37/02 , A61P19/10 , A61P29/00 , A61P13/12 , A61P11/00 , A61P9/00 , A61P7/12 , A61P5/00 , A61P3/00 , A61K38/46 , A61K38/44 , A61K38/48
CPC分类号： A61K9/0043
摘要： Compositions and methods are provided that include a biologically active agent and a permeabilizing agent effective to enhance mucosal delivery of the biologically active agent in a mammalian subject, in which the permeabilizing peptide is a PN159 analog or conjugate.
摘要翻译： 提供的组合物和方法包括有效增强哺乳动物受试者中的生物活性剂的粘膜递送的生物活性剂和渗透剂，其中透化肽是PN159类似物或缀合物。
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93.发明申请NUCLEIC ACID COMPOUNDS FOR INHIBITING RAS GENE EXPRESSION AND USES THEREOF 审中-公开用于抑制RAS基因表达的核酸化合物及其用途公开(公告)号：US20100055783A1
公开(公告)日：2010-03-04
申请号：US12529302
申请日：2008-03-03
CPC分类号： C12N15/1135 , C12N2310/14 , C12N2310/321 , C12N2310/3231 , C12N2310/33 , C12N2310/53 , C12N2310/3521
摘要： The present disclosure provides meroduplex ribonucleic acid molecules (mdRNA) capable of decreasing or silencing RAS (e.g., HRAS, KRAS, NRAS) gene expression. An mdRNA of this disclosure comprises at least three strands that combine to form at least two non-overlapping double-stranded regions separated by a nick or gap wherein one strand is complementary to an HRAS, KRAS, or NRAS mRNA. In addition, the meroduplex may have at least one uridine is a 5-methyluridine, a nucleoside is a locked nucleic acid, or optionally other modifications, and any combination thereof. Also provided are methods of decreasing expression of a RAS gene in a cell or in a subject to treat a RAS-related disease.
摘要翻译： 本公开提供能够降低或沉默RAS（例如，HRAS，KRAS，NRAS）基因表达的meroduplex核糖核酸分子（mdRNA）。 本公开的mdRNA包含至少三条链，其组合形成由切口或间隙隔开的至少两个不重叠的双链区域，其中一条链与HRAS，KRAS或NRAS mRNA互补。 此外，meroduplex可以具有至少一个尿苷是5-甲基尿苷，核苷是锁定的核酸或任选的其它修饰，以及它们的任何组合。 还提供减少细胞或受试者中RAS基因表达以治疗RAS相关疾病的方法。
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公开(公告)号：US20080318861A1
公开(公告)日：2008-12-25
申请号：US12096650
申请日：2006-12-07
CPC分类号： A61K9/0043 , A61K9/006 , A61K38/2278 , A61K47/40
摘要： What is described is a pharmaceutical formulation for intranasal administration of exendin to a mammal, wherein the formulation comprises a therapeutically effective amount of an exendin, a viscosity enhancer, methyl-β-cyclodextrin, a surfactant, tartrate buffer to control pH and a chelating agent for cations, and wherein such exendin dosage form exhibits at least 95% exenatide recovery after storage for at least 365 days at 5° C.
摘要翻译： 描述了用于鼻内给予哺乳动物毒蜥外泌肽的药物制剂，其中所述制剂包含治疗有效量的毒蜥外泌肽，粘度增强剂，甲基-β-环糊精，表面活性剂，控制pH的酒石酸盐缓冲剂和螯合剂 对于阳离子，并且其中这种毒蜥外泌肽剂型在5℃下储存至少365天后显示出至少95％的艾塞那肽恢复。
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95.发明申请Pharmaceutical Formation For Increased Epithelial Permeability of Glucose-Regulating Peptide 审中-公开药物形成用于增加葡萄糖调节肽的上皮通透性公开(公告)号：US20080318837A1
公开(公告)日：2008-12-25
申请号：US12095801
申请日：2006-12-01
申请人： Steven C. Quay , Henry R. Costantino , Michael V. Templin , Alexis Kays Leonard , Mary S. Kleppe , Joshua O. Sestak
发明人： Steven C. Quay , Henry R. Costantino , Michael V. Templin , Alexis Kays Leonard , Mary S. Kleppe , Joshua O. Sestak
IPC分类号： A61K38/00
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.
摘要翻译： 描述的是包含药学有效量的葡萄糖调节肽（GRP）和增强剂的混合物的药物制剂，其中药物制剂用于治疗代谢综合征。
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96.发明申请NUCLEIC ACID COMPOUNDS FOR INHIBITING APOB GENE EXPRESSION AND USES THEREOF 审中-公开用于抑制APOB基因表达的核酸化合物及其用途公开(公告)号：US20080299659A1
公开(公告)日：2008-12-04
申请号：US12039668
申请日：2008-02-28
CPC分类号： C12N15/113 , C12N2310/14 , C12N2310/3231
摘要： The present disclosure provides meroduplex ribonucleic acid molecules (mdRNA) capable of decreasing or silencing ApoB gene expression. An mdRNA of this disclosure comprises at least three strands that combine to form at least two non-overlapping double-stranded regions separated by a nick or gap wherein one strand is complementary to an ApoB mRNA. In addition, the meroduplex may have at least one uridine substituted with a 5-methyluridine, a nucleoside replaced with a locked nucleic acid, or optionally other modifications, and any combination thereof. Also provided are methods of decreasing expression of an ApoB gene in a cell or in a subject to treat an ApoB-related disease.
摘要翻译： 本公开提供能够降低或沉默ApoB基因表达的meroduplex核糖核酸分子（mdRNA）。 本公开的mdRNA包含至少三条链，其组合形成由切口或间隙分开的至少两个不重叠的双链区域，其中一条链与ApoB mRNA互补。 此外，meroduplex可以具有至少一个用5-甲基尿苷取代的尿苷，被锁定的核酸替代的核苷，或任选的其它修饰，以及它们的任何组合。 还提供减少细胞或受试者中ApoB基因表达以治疗ApoB相关疾病的方法。
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97.发明申请NUCLEIC ACID COMPOUNDS FOR INHIBITING AKT GENE EXPRESSION AND USES THEREOF 审中-公开用于抑制AKT基因表达的核酸化合物及其用途公开(公告)号：US20080293136A1
公开(公告)日：2008-11-27
申请号：US12039662
申请日：2008-02-28
CPC分类号： C12N15/1137 , C12N2310/111 , C12N2310/14 , C12N2310/321 , C12N2310/3231 , C12N2310/53 , C12N2310/3521
摘要： The present disclosure provides meroduplex ribonucleic acid molecules (mdRNA) capable of decreasing or silencing AKT gene expression. An mdRNA of this disclosure comprises at least three strands that combine to form at least two non-overlapping double-stranded regions separated by a nick or gap wherein one strand is complementary to an AKT mRNA. In addition, the meroduplex may have at least one uridine substituted with a 5-methyluridine, a nucleoside replaced with a locked nucleic acid, or optionally other modifications, and any combination thereof. Also provided are methods of decreasing expression of an AKT gene in a cell or in a subject to treat an AKT-related disease.
摘要翻译： 本公开提供能够降低或沉默AKT基因表达的meroduplex核糖核酸分子（mdRNA）。 本公开的mdRNA包含至少三条链，其结合形成由切口或间隙分开的至少两个不重叠的双链区域，其中一条链与AKT mRNA互补。 此外，meroduplex可以具有至少一个用5-甲基尿苷取代的尿苷，被锁定的核酸替代的核苷，或任选的其它修饰，以及它们的任何组合。 还提供减少细胞或受试者中AKT基因表达以治疗AKT相关疾病的方法。
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公开(公告)号：US20080255067A1
公开(公告)日：2008-10-16
申请号：US12142240
申请日：2008-06-19
IPC分类号： A61K31/714
CPC分类号： A61K9/0043 , A61K9/08 , A61K31/7056 , A61K31/714 , A61K47/10 , A61K47/12 , A61K47/186
摘要： A stable pharmaceutical mercury-free aqueous solution of cyanocobalamin comprised of cyanocobalamin and water wherein said solution of cyanocobalamin is suitable for intranasal administration, has a viscosity less than about 1000 cPs, and wherein said solution of cyanocobalamin has a bioavailability of cyanocobalamin when administered intranasally of at least about 7% relative to an intramuscular injection of cyanocobalamin with the proviso that the solution is essentially free of mercury and mercury-containing compounds. The present invention is also directed towards a method for elevating the vitamin B12 levels in the cerebral spinal fluid (CSF) comprising administering intranasally a sufficient amount of a mercury-free cyanocobalamin solution so as to increase the average ratio of vitamin B12 in the CSF to that in the blood serum (B12 CSF/B12 Serum×100) to at least about 1.1 comprising intranasally administering an aqueous solution of a cyanocobalamin, wherein said solution of cyanocobalamin has a bioavailability of at least 7% relative to an intramuscular injection of a cyanocobalamin.
摘要翻译： 一种由氰钴胺素和水组成的稳定的药用无汞水溶液，其中所述氰钴胺溶液适合于鼻内给药，其粘度小于约1000cPs，其中所述氰钴胺溶液在鼻内给药时具有氰钴胺素的生物利用度 相对于肌内注射氰钴胺素至少约7％，条件是溶液基本上不含汞和含汞化合物。 本发明还涉及提高脑脊髓液（CSF）中维生素B12水平的方法，其包括向鼻内施用足够量的无汞氰钴胺溶液，以增加CSF中维生素B12的平均比例 在血清中（B12 CSF / B12 Serumx100）至少约1.1，包括鼻内施用氰钴胺水溶液，其中所述氰钴胺溶液相对于肌内注射氰钴胺素具有至少7％的生物利用度。
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99.发明授权Compositions and methods for enhanced mucosal delivery of parathyroid hormone 失效用于增强甲状旁腺激素粘膜递送的组合物和方法公开(公告)号：US07435720B2
公开(公告)日：2008-10-14
申请号：US11550051
申请日：2006-10-17
CPC分类号： A61K31/724 , A61K9/0043 , A61K38/29 , A61K47/183
摘要： Pharmaceutical compositions and methods are described comprising at least a parathyroid hormone peptide (PTH) preferably PTH1-34 and one or more mucosal delivery-enhancing agents for enhanced nasal mucosal delivery of PTH, for treating or preventing osteoporosis or osteopenia in a mammalian subject, preferably a human.
摘要翻译： 描述了药物组合物和方法，其至少包含甲状旁腺激素肽（PTH），优选PTH <1-34 和一种或多种用于增强鼻粘膜递送PTH的粘膜递送增强剂，用于治疗或预防骨质疏松症 或哺乳动物受试者，优选人类的骨质减少。
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公开(公告)号：US07404489B1
公开(公告)日：2008-07-29
申请号：US10814399
申请日：2004-03-31
IPC分类号： A61F13/00
CPC分类号： A61K9/0043 , A61K9/08 , A61K31/7056 , A61K31/714 , A61K47/10 , A61K47/12 , A61K47/186
摘要： A stable pharmaceutical mercury-free aqueous solution of cyanocobalamin comprised of cyanocobalamin and water wherein said solution of cyanocobalamin is suitable for intranasal administration, has a viscosity less than about 1000 cPs, and wherein said solution of cyanocobalamin has a bioavailability of cyanocobalamin when administered intranasally of at least about 7% relative to an intramuscular injection of cyanocobalamin with the proviso that the solution is essentially free of mercury and mercury-containing compounds. The present invention is also directed towards a method for elevating the vitamin B12 levels in the cerebral spinal fluid (CSF) comprising administering intranasally a sufficient amount of a mercury-free cyanocobalamin solution so as to increase the average ratio of vitamin B12 in the CSF to that in the blood serum (B12 CSF/B12 Serum×100) to at least about 1.1 comprising intranasally administering an aqueous solution of a cyanocobalamin, wherein said solution of cyanocobalamin has a bioavailability of at least 7% relative to an intramuscular injection of a cyanocobalamin.
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