公开(公告)号：US07534769B2

公开(公告)日：2009-05-19

申请号：US10055863

申请日：2002-01-22

申请人： Heidrun Engler ,  Tattanahalli L. Nagabhushan ,  Stephen Kenneth Youngster

发明人： Heidrun Engler ,  Tattanahalli L. Nagabhushan ,  Stephen Kenneth Youngster

IPC分类号： A61K31/70 ,  A01N45/00 ,  C07J41/00

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.

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。

公开(公告)号：US5025016A

公开(公告)日：1991-06-18

申请号：US248927

申请日：1988-09-26

申请人： Kurt H. Ahrens ,  Helmut Schickaneder ,  Heidrun Engler ,  Istvan Szeleny

发明人： Kurt H. Ahrens ,  Helmut Schickaneder ,  Heidrun Engler ,  Istvan Szeleny

IPC分类号： A61K31/505 ,  A61P11/10 ,  A61P29/00 ,  C07D401/12

CPC分类号： C07D401/12

摘要： The invention relates to pyrimidine-thioalkyl pyridine derivatives corresponding to the following general formula ##STR1## in which R.sub.1 to R.sub.4, independently of one another, represent hydrogen, lower alkyl, halogen, amino or hydroxy groups, R.sub.5 represents a free electron pair or a lower alkyl group, a halogen atom, m has the value 0 or 1, the pyrimidine-thioalkyl group being bonded in the 2-, 3- or 4-position of the pyridine ring, and to therapeutically compatible acid addition salts thereof. The invention also relates to a process for producing the new pyrimidine-thioalkyl pyridine derivatives and to medicaments containing these compounds.

摘要翻译： 本发明涉及对应于以下通式（I）的嘧啶 - 硫代烷基吡啶衍生物，其中R 1至R 4彼此独立地表示氢，低级烷基，卤素，氨基或羟基，R 5表示自由电子 对或低级烷基，卤素原子，m具有值0或1，嘧啶硫代烷基键合在吡啶环的2-，3-或4-位，以及其治疗上相容的酸加成盐 。 本发明还涉及生产新的嘧啶 - 硫烷基吡啶衍生物的方法和含有这些化合物的药物。

公开(公告)号：US4833141A

公开(公告)日：1989-05-23

申请号：US69159

申请日：1987-07-02

申请人： Helmut Schickaneder ,  Rolf Herter ,  Hartmut Vergin ,  Heidrun Engler ,  Kurt H. Ahrens

发明人： Helmut Schickaneder ,  Rolf Herter ,  Hartmut Vergin ,  Heidrun Engler ,  Kurt H. Ahrens

IPC分类号： C07D413/06 ,  A61K31/41 ,  A61P31/04 ,  C07D521/00

CPC分类号： C07D249/08 ,  C07D231/12 ,  C07D233/56

摘要： The invention relates to new 1,4-piperazine compounds corresponding to the following general formula ##STR1## which show improved antimycotic activity in relation to the known compounds miconazol and ketoconazol.

摘要翻译： 本发明涉及对应于以下通式“IMAGE”的新的1,4-哌嗪化合物，其与已知的化合物咪康唑和酮康唑相比显示出改进的抗真菌活性。

公开(公告)号：US4757080A

公开(公告)日：1988-07-12

申请号：US51300

申请日：1987-05-19

申请人： Helmut Schickaneder ,  Peter Morsdorf ,  Armin Buschauer ,  Walter Schunack ,  Heidrun Engler ,  Hartmut Vergin ,  Kurt H. Ahrens

发明人： Helmut Schickaneder ,  Peter Morsdorf ,  Armin Buschauer ,  Walter Schunack ,  Heidrun Engler ,  Hartmut Vergin ,  Kurt H. Ahrens

IPC分类号： A61K31/4427 ,  A61K31/455 ,  A61P9/10 ,  A61P9/12 ,  C07D211/90 ,  C07D401/12 ,  C07D413/14 ,  A61K31/44

CPC分类号： C07D401/12 ,  C07D211/90 ,  C07D413/14

摘要： New compounds which act on the cardiac circulation and correspond to the general formula ##STR1## and may be used for the treatment of cardiac diseases, in certain forms of hypertension and in diseases of arterial occlusion are described.Methods of preparation for these compounds and medicaments containing these compounds are also described.

摘要翻译： 描述了作用于心脏循环并对应于通式并可用于治疗某些形式的高血压和动脉闭塞疾病的心脏疾病的新化合物。 还描述了这些化合物的制备方法和含有这些化合物的药物。

公开(公告)号：US20060199782A1

公开(公告)日：2006-09-07

申请号：US11359997

申请日：2006-02-21

申请人： Heidrun Engler ,  Tattanahalli Nagabhushan ,  Stephen Youngster

发明人： Heidrun Engler ,  Tattanahalli Nagabhushan ,  Stephen Youngster

IPC分类号： A61K48/00 ,  A61K31/704 ,  A61K31/56

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; X 1是胆酸基或脱氧胆酸基; X 2和X 3各自独立地选自胆酸基，脱氧胆酸基和糖基，其中选择糖基团 从戊糖单糖组，己糖单糖组，戊糖 - 戊糖二糖基团，己糖 - 六糖基团，戊糖 - 六糖二糖基团和己糖 - 戊糖二糖基团组成的组; 并且其中X 2和X 3中的至少一个是糖基团。

公开(公告)号：US06392069B1

公开(公告)日：2002-05-21

申请号：US09112074

申请日：1998-07-08

申请人： Heidrun Engler ,  Tattanahalli L. Nagabhushan ,  Stephen Kenneth Youngster

发明人： Heidrun Engler ,  Tattanahalli L. Nagabhushan ,  Stephen Kenneth Youngster

IPC分类号： C07J5300

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.

公开(公告)号：US5182294A

公开(公告)日：1993-01-26

申请号：US639511

申请日：1991-01-10

申请人： Peter Morsdorf ,  Heidrun Engler ,  Helmut Schickaneder ,  Kurt-Henning Ahrens

发明人： Peter Morsdorf ,  Heidrun Engler ,  Helmut Schickaneder ,  Kurt-Henning Ahrens

IPC分类号： A61K31/44 ,  A61K31/4427 ,  A61P9/00 ,  A61P9/04 ,  C07D401/12

CPC分类号： C07D401/12

摘要： A new imidazolyl propyl guanidine derivative corresponding to formula I ##STR1## is described, which is distinguished by a combination of particularly advantageous properties for the treatment of diseases of the heart and circulation.

摘要翻译： 描述了对应于式I的新的咪唑基丙基胍衍生物（I），其特征在于用于治疗心脏和循环疾病的特别有利的性质的组合。

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。

公开(公告)号：US4866066A

公开(公告)日：1989-09-12

申请号：US015007

申请日：1987-02-17

申请人： Helmut Schickaneder ,  Heidrun Engler ,  Istvan Szelenyi

发明人： Helmut Schickaneder ,  Heidrun Engler ,  Istvan Szelenyi

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。