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11.发明授权Piperazine substituted 6-phenyldihydro-3(2H)-pyridazinones, and pharmaceutical preparations containing these 失效哌嗪取代的6-苯基二氢-3（2H） - 哒嗪酮，以及含有它们的药物制剂
公开(公告)号：US4954501A
公开(公告)日：1990-09-04
申请号：US247868
申请日：1988-09-21
申请人： Rolf Herter , Peter Morsdorf , Volker Pfahlert , Heidrun Engler , Helmut Schickaneder , Kurt-Henning Ahrens
发明人： Rolf Herter , Peter Morsdorf , Volker Pfahlert , Heidrun Engler , Helmut Schickaneder , Kurt-Henning Ahrens
IPC分类号： A61K31/50 , A61K31/505 , A61P9/04 , A61P9/12 , C07D237/04 , C07D401/10 , C07D403/12 , C07D417/12
CPC分类号： C07D401/10 , C07D237/04 , C07D403/12 , C07D417/12
摘要： New 6-phenyldihydro-3(2H)-pyridazinones corresponding to the following general formula ##STR1## are described. These compounds are readily prepared in a form suitable for oral administration and are distinguished by a high positive inotropic action and have only a slight effect on blood pressure and cardiac frequency. A process for their preparation and pharmaceutical preparations containing these compounds are also described.
摘要翻译： 描述对应于以下通式
的新的6-苯基二氢-3（2H） - 哒嗪酮。 这些化合物容易地以适于口服给药的形式制备，并且通过高的正性肌力作用区分，并且对血压和心脏频率仅具有轻微的影响。 还描述了其制备方法和含有这些化合物的药物制剂。 -
12.发明授权Thiomethylpyridine derivatives and their use for eliciting a bronchosecretolytic or mucolytic response 失效硫代甲基吡啶衍生物及其用于引发支气管解吸或溶血反应的用途
公开(公告)号：US4866066A
公开(公告)日：1989-09-12
申请号：US015007
申请日：1987-02-17
IPC分类号： A61K31/325 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/505 , A61P11/10 , C07D213/32 , C07D213/61 , C07D213/70 , C07D401/12 , C07D413/12 , C07D487/04 , C07D498/04
CPC分类号： C07D213/70 , C07D213/32 , C07D401/12 , C07D487/04
摘要： Thiomethylpyridine derivatives having bronchosecretolytic and mucolytic activity according to the formula: ##STR1## wherein R is a group attached in the 2-, 3- or 4-position of the pyridine ring which corresponds to the following general formula:Q--S--CH.sub.2 -- (II)wherein Q is a substituted or unsubstituted aryl group or a 5- or 6-membered heterocyclic group which may optionally contain one or more substituents and/or which may be condensed with an optionally substituted phenyl group or with an optionally substituted heterocycle; R' is a lower alkyl group, a halogen atom or an aminoalkyl group; and n is 0 or an integer of from 1 to 4; and the therapeutically-acceptable acid addition salts thereof.The new compounds are distinguished by surprising activity compared with known compounds, such as "Ambroxol".
摘要翻译： 具有下列通式的其中R是连接在吡啶环的2-，3-或4-位的基团的具有支气管解吸和溶血活性的硫代甲基吡啶衍生物，其对应于下列通式：QS-CH2 - （II）其中Q是取代或未取代的芳基或可以任选地含有一个或多个取代基和/或可以与任选取代的苯基或任选取代的杂环稠合的5-或6-元杂环基 ; R'是低级烷基，卤素原子或氨基烷基; n为0或1〜4的整数， 及其治疗上可接受的酸加成盐。 与已知化合物（例如“Ambroxol”）相比，新化合物的特征在于惊人的活性。
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13.发明授权Imidazoyl-substituted thiomethylpyridine derivatives, method of administration thereof and medicaments containing them 失效咪唑酰基取代的硫代甲基吡啶衍生物，其施用方法和含有它们的药物
公开(公告)号：US4810715A
公开(公告)日：1989-03-07
申请号：US26189
申请日：1987-03-16
IPC分类号： A61K31/325 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/505 , A61P11/10 , C07D213/32 , C07D213/61 , C07D213/70 , C07D401/12 , C07D413/12 , C07D487/04 , C07D498/04
CPC分类号： C07D213/70 , C07D213/32 , C07D401/12 , C07D487/04
摘要： Thiomethylpyridine derivatives having bronchosecretolytic and mucolytic activity according to the formula: ##STR1## wherein R is a group attached in the 2-, 3- or 4-position of the pyridine ring which corresponds to the following general formula:Q--S--CH.sub.2 -- (II) wherein Q is a substituted or unsubstituted aryl group or a 5- or 6-membered heterocyclic group which may optionally contain one or more substituents and/or which may be condensed with an optionally substituted phenyl group or with an optionally substituted heterocycle;R' is a lower alkyl group, a halogen atom or an aminoalkyl group; andn is 0 or an integer of from 1 to 4;and the therapeutically-acceptable acid addition salts thereof.The new compounds are distinguished by surprising activity compared with known compounds, such as "Ambroxol".
摘要翻译： 具有下列通式的其中R是连接在吡啶环的2-，3-或4-位的基团的具有支气管解吸和溶血活性的硫代甲基吡啶衍生物，其对应于下列通式：QS-CH2 - （II）其中Q是取代或未取代的芳基或可以任选地含有一个或多个取代基和/或可以与任选取代的苯基或任选取代的杂环稠合的5-或6-元杂环基 ; R'是低级烷基，卤素原子或氨基烷基; n为0或1〜4的整数， 及其治疗上可接受的酸加成盐。 与已知化合物如“Ambroxol”相比，新化合物的特征在于惊人的活性。
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公开(公告)号：US20110104118A1
公开(公告)日：2011-05-05
申请号：US12912496
申请日：2010-10-26
CPC分类号： A61K47/186 , A61K9/0019 , A61K38/1709 , A61K47/10 , A61K48/00 , C07K14/4736 , C07K14/4746 , C12N15/87 , C12N2799/022
摘要： A method and pharmaceutical composition for the treatment of cancer using a gene delivery system, such as a viral vector delivery system, comprising a therapeutic gene such as p53 or a retinoblastoma tumor suppressor gene wherein the gene delivery system is formulated in a buffer comprising a delivery-enhancing agent such as ethanol or a detergent.
摘要翻译： 一种用于使用基因递送系统（例如病毒载体递送系统）治疗癌症的方法和药物组合物，其包含治疗性基因如p53或成视网膜细胞瘤肿瘤抑制基因，其中所述基因递送系统配制在包含递送 - 增强剂如乙醇或洗涤剂。
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公开(公告)号：US07002027B1
公开(公告)日：2006-02-21
申请号：US08889355
申请日：1997-07-08
CPC分类号： A61K48/00
摘要： The present invention is directed to compositions and methods of treating cancer by gene therapy using a therapeutic gene formulated in a buffer comprising a delivery-enhancing agent. The delivery-enhancing agents of the invention can be used to formulate therapeutic or diagnostic agents, such as proteins, nucleic acids, antisense RNA, small molecules, etc., for administration to any tissue or organ having an epithelial membrane. The delivery-enhancing agents include detergents, alcohols, surfactants and other molecules.
摘要翻译： 本发明涉及通过使用配制在包含递送增强剂的缓冲液中的治疗基因进行基因治疗来治疗癌症的组合物和方法。 本发明的递送增强剂可用于配制治疗或诊断试剂，例如蛋白质，核酸，反义RNA，小分子等，用于给予具有上皮膜的任何组织或器官。 递送增强剂包括洗涤剂，醇，表面活性剂和其它分子。
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公开(公告)号：US20100028431A1
公开(公告)日：2010-02-04
申请号：US12422807
申请日：2009-04-13
IPC分类号： A61K9/10 , A61K31/70 , A61K31/7016 , A61K38/16 , A61K31/7088 , C08B37/00 , A61P35/00
CPC分类号： A61K48/00
摘要： A method and pharmaceutical composition for the enhancement of transfer of a therapeutic agent to a cell wherein the therapeutic agent is formulated in a buffer comprising a compound of Formula I: wherein: n is an integer from 2-8; X1 is a cholic acid group or deoxycholic acid group; and X2 and X3 are each independently selected from the group consisting of a cholic acid group, a deoxycholic acid group, and a saccharide group, wherein the saccharide group is selected from the group consisting of pentose monosaccharide groups, hexose monosaccharide groups, pentose-pentose disaccharide groups, hexose-hexose disaccharide groups, pentose-hexose disaccharide groups, and hexose-pentose disaccharide groups; and wherein at least one of X2 and X3 is a saccharide group.
摘要翻译： 一种用于增强治疗剂转移至细胞的方法和药物组合物，其中所述治疗剂配制在包含式I化合物的缓冲液中：其中：n为2-8的整数; X1是胆酸基或脱氧胆酸基; X2和X3各自独立地选自胆酸基，脱氧胆酸基和糖基，其中所述糖基选自戊糖单糖基，己糖单糖基，戊糖 - 戊糖基 二糖基团，己糖 - 己糖二糖基团，戊糖 - 己糖二糖基团和己糖 - 六糖二糖基团; 并且其中X 2和X 3中的至少一个是糖基团。
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公开(公告)号：US20050025742A1
公开(公告)日：2005-02-03
申请号：US10861654
申请日：2004-06-04
IPC分类号： A61K20060101 , A61K9/00 , A61K38/21 , A61K48/00
CPC分类号： A61K9/0034 , A61K38/21
摘要： Methods and pharmaceutical compositions for administering protein or gene therapy to tissues or organs having an epithelial cell layer are provided. A protein or nucleic acid encoding the protein is administered to the target tissue or organ in combination with treatment with a delivery enhancing agent which increases the delivery of the interferon or nucleic acid to the cells of the target tissues or organs. The methods and combinations are particularly useful in the treatment of cancers and other conditions responsive to interferon therapy. An exemplary method comprises the transurethral intravesical administration to the bladder of a therapeutically effective amount of a pharmaceutical composition comprising an alpha-interferon or a gene delivery system encoding the interferon and SYN3 or a SYN3 homolog or analog. In the urinary bladder, as much as a 10 to 1000 fold increased in interferon levels and activity may be observed with the use of a SYN3 formulation as opposed to a PBS formulation of the same interferon protein or interferon gene delivery system.
摘要翻译： 提供了用于对具有上皮细胞层的组织或器官进行蛋白质或基因治疗的方法和药物组合物。 将编码蛋白质的蛋白质或核酸与目标组织或器官联合施用递送增强剂的组合施用，所述递送增强剂增加干扰素或核酸向靶组织或器官的细胞递送。 所述方法和组合在治疗癌症和其它对干扰素治疗有反应的病症方面特别有用。 示例性方法包括向膀胱经尿道膀胱内施用治疗有效量的药物组合物，其包含α-干扰素或编码干扰素和SYN3或SYN3同源物或类似物的基因递送系统。 在膀胱中，与使用相同干扰素蛋白或干扰素基因递送系统的PBS制剂相比，使用SYN3制剂可以观察到高达10至1000倍的干扰素水平和活性。
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公开(公告)号：US07538093B2
公开(公告)日：2009-05-26
申请号：US11359997
申请日：2006-02-21
CPC分类号： A61K48/00
摘要： A method and pharmaceutical composition for the enhancement of transfer of a therapeutic agent to a cell wherein the therapeutic agent is formulated in a buffer comprising a compound of Formula I: wherein: n is an integer from 2-8; X1 is a cholic acid group or deoxycholic acid group; and X2 and X3 are each independently selected from the group consisting of a cholic acid group, a deoxycholic acid group, and a saccharide group, wherein the saccharide group is selected from the group consisting of pentose monosaccharide groups, hexose monosaccharide groups, pentose-pentose disaccharide groups, hexose-hexose disaccharide groups, pentose-hexose disaccharide groups, and hexose-pentose disaccharide groups; and wherein at least one of X2 and X3 is a saccharide group.
摘要翻译： 一种用于增强治疗剂转移至细胞的方法和药物组合物，其中所述治疗剂配制在包含式I化合物的缓冲液中：其中：n为2-8的整数; X1是胆酸基或脱氧胆酸基; X2和X3各自独立地选自胆酸基，脱氧胆酸基和糖基，其中所述糖基选自戊糖单糖基，己糖单糖基，戊糖 - 戊糖基 二糖基团，己糖 - 己糖二糖基团，戊糖 - 己糖二糖基团和己糖 - 六糖二糖基团; 并且其中X 2和X 3中的至少一个是糖基团。
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公开(公告)号：US07534769B2
公开(公告)日：2009-05-19
申请号：US10055863
申请日：2002-01-22
CPC分类号： A61K31/56 , A61K31/7008 , A61K48/00 , C07J9/005 , C07J41/0061 , C12N15/87
摘要： This invention provides methods and compositions for enhancing transfer of an agent into a cell. The agents can include polypeptides, polynucleotides such as genes and antisense nucleic acids, and other molecules. In some embodiments, the agents are modulating agents that can modulate a cellular activity or function when introduced into the cell. The methods and compositions are useful for introducing agents into individual cells, as well as cells that are present as a tissue or organ.
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公开(公告)号：US20050014259A1
公开(公告)日：2005-01-20
申请号：US10913567
申请日：2004-08-06
申请人： Susan Conroy , Heidrun Engler , Daniel Maneval
发明人： Susan Conroy , Heidrun Engler , Daniel Maneval
IPC分类号： A61K31/715 , A61K31/724 , A61K48/00 , C12N15/87 , C12Q1/68 , C12N15/85
CPC分类号： C12N15/87 , A61K31/715 , A61K31/724 , A61K35/761 , A61K38/1758 , A61K48/00 , A61K48/0008 , C12N15/86 , C12N2710/10332 , C12N2710/10343 , Y10S435/932 , A61K2300/00
摘要： The present invention provides formulations and methods to enhance the delivery of nucleic acids to cells. Formulations comprising dextrin polymers in combination with sugars provide enhanced delivery of nucleic acids, particularly eucaryotic expression vectors, demonstrate enhanced delivery of nucleic acids to cells in vivo. The present invention also provides methods of treatment in combination with such formulations.
摘要翻译： 本发明提供了增强核酸向细胞递送的制剂和方法。 包含与糖组合的糊精聚合物的制剂提供增强的核酸递送，特别是真核表达载体，证明核酸在体内增强的细胞递送至细胞。 本发明还提供了与这些制剂组合的治疗方法。
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