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公开(公告)号：US20060128736A1
公开(公告)日：2006-06-15
申请号：US10519193
申请日：2003-06-26
申请人： Heinrich Haas , Brita Schulze , Uwe Michaelis , Michael Teifel , Birgitta Sauer , Thomas Fichert
发明人： Heinrich Haas , Brita Schulze , Uwe Michaelis , Michael Teifel , Birgitta Sauer , Thomas Fichert
IPC分类号： A61K31/4745
CPC分类号： A61K31/47 , A61K9/1272 , A61K31/335 , A61K31/4745 , A61K47/34 , A61K47/541 , A61K47/543 , A61K47/56 , A61K47/6911 , A61K49/1812 , B82Y5/00 , C07D471/14
摘要： The present invention relates to compositions, particularly colloidal nanoaggregates comprising the carboxylate form of a campothecin drug or a derivative thereof associated with at least one organic cationic molecule, which has a positive net charge. The composition or nanoaggregate may be present as an emulsion, droplet, mincelle, liposome, nanoparticle or nanocapsule.
摘要翻译： 本发明涉及组合物，特别是包含与至少一种有机阳离子分子缔合的营养不良的羧酸盐形式的氨基辛酸或其衍生物的胶体纳米聚集体，其具有正的净电荷。 组合物或纳米聚集体可以乳液，液滴，分解，脂质体，纳米颗粒或纳米胶囊存在。
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2.发明申请NOVEL TETRAHYDROCARBAZOLE DERIVATIVES AS LIGANDS OF G-PROTEIN COUPLED RECEPTORS 失效新型四氮唑衍生物作为G蛋白偶联受体的配体公开(公告)号：US20120122763A1
公开(公告)日：2012-05-17
申请号：US13358055
申请日：2012-01-25
申请人： Tilmann SCHUSTER , Klaus Paulini , Peter Schmidt , Silke Baasner , Emmanuel Polymeropoulos , Eckhard Guenther , Michael Teifel
发明人： Tilmann SCHUSTER , Klaus Paulini , Peter Schmidt , Silke Baasner , Emmanuel Polymeropoulos , Eckhard Guenther , Michael Teifel
IPC分类号： A61K38/05 , A61P35/00 , A61P5/00 , A61P17/00 , A61P25/00 , A61P25/28 , A61P1/08 , A61P29/00 , A61P25/06 , A61P25/22 , A61P11/14 , A61P11/06 , A61P9/12 , A61P1/00 , A61P25/24 , A61P19/02 , A61K38/06
CPC分类号： C07K5/06191 , A61K38/00 , C07K5/0827
摘要： The present invention provides novel tetrahydrocarbazole compounds according to formula (I) as ligands of G-protein coupled receptors (GPCR) which are useful in the treatment and/or prophylaxis of physiological and/or pathological conditions in mammals mediated by GPCR or of physiological and/or pathological conditions which can be treated by modulation of these receptors.
摘要翻译： 本发明提供了根据式（I）的新型四氢咔唑化合物作为G蛋白偶联受体（GPCR）的配体，其可用于治疗和/或预防由GPCR介导的哺乳动物的生理和/或病理状况或生理和/ /或可以通过调节这些受体来治疗的病理状况。
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3.发明申请Method of Producing A Cationic Liposomal Preparation Comprising A Lipophilic Compound 有权产生包含亲脂性化合物的阳离子脂质体制备方法公开(公告)号：US20120087975A1
公开(公告)日：2012-04-12
申请号：US13278801
申请日：2011-10-21
申请人： Carsten Mundus , Christian Welz , Oliver Schramel , Heinrich Haas , Thomas Fichert , Brita Schulze , Toralf Peymann , Uwe Michaelis , Michael Teifel , Friedrich Gruber , Gerhard Winter
发明人： Carsten Mundus , Christian Welz , Oliver Schramel , Heinrich Haas , Thomas Fichert , Brita Schulze , Toralf Peymann , Uwe Michaelis , Michael Teifel , Friedrich Gruber , Gerhard Winter
IPC分类号： A61K9/127 , A61K31/337 , A61K31/4375 , A61K31/427 , A61K31/685 , A61K31/56
CPC分类号： A61K31/337 , A61K9/127 , A61K9/1272 , A61K31/335 , A61K31/47 , A61K31/4745 , A61K47/34 , A61K47/543 , A61K47/56 , A61K47/6911 , A61K49/1812 , B82Y5/00 , C07D471/14
摘要： A method for producing a cationic liposomal preparation comprising a lipophilic active compound with physical and chemical stability during manufacturing, storing and reconstituting, and further a cationic liposomal preparation obtainable by this method as well as specific cationic liposomal preparations as well as pharmaceutical compositions are disclosed.
摘要翻译： 公开了一种阳离子脂质体制剂的制备方法，其包括在制造，储存和重构过程中具有物理和化学稳定性的亲脂性活性化合物，以及可通过该方法获得的阳离子脂质体制剂以及特定的阳离子脂质体制剂以及药物组合物。
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公开(公告)号：US20110038926A1
公开(公告)日：2011-02-17
申请号：US12859000
申请日：2010-08-18
申请人： Carsten Mundus , Christain Welz , Oliver Schramel , Heinrich Haas , Thomas Fichert , Brita Schulze , Toralf Peymann , Uwe Michaelis , Michael Teifel , Friedrich Gruber , Gerhard Winter
发明人： Carsten Mundus , Christain Welz , Oliver Schramel , Heinrich Haas , Thomas Fichert , Brita Schulze , Toralf Peymann , Uwe Michaelis , Michael Teifel , Friedrich Gruber , Gerhard Winter
IPC分类号： A61K9/127 , A61K31/337 , A61P35/00
CPC分类号： A61K31/337 , A61K9/127 , A61K9/1272 , A61K31/335 , A61K31/47 , A61K31/4745 , A61K47/34 , A61K47/543 , A61K47/56 , A61K47/6911 , A61K49/1812 , B82Y5/00 , C07D471/14
摘要： A method for producing a cationic liposomal preparation comprising a lipophilic active compound with physical and chemical stability during manufacturing, storing and reconstituting, and further a cationic liposomal preparation obtainable by this method as well as specific cationic liposomal preparations as well as pharmaceutical compositions are disclosed.
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5.发明授权Pyridopyrazines as highly selective ras-Raf-Mek-Erk signal transduction pathway inhibitors 有权吡吡嗪作为高选择性ras-Raf-Mek-Erk信号转导途径抑制剂公开(公告)号：US08791118B2
公开(公告)日：2014-07-29
申请号：US13439150
申请日：2012-04-04
申请人： Matthias Gerlach , Irene Seipelt , Lars Blumenstein , Gilbert Mueller , Eckhard Guenther , Tilmann Schuster , Michael Teifel
发明人： Matthias Gerlach , Irene Seipelt , Lars Blumenstein , Gilbert Mueller , Eckhard Guenther , Tilmann Schuster , Michael Teifel
IPC分类号： A61K31/4985 , C07D487/04
CPC分类号： A61K31/4985 , A61K31/501 , A61K31/5377 , C07D471/04
摘要： The invention provides new pyridopyrazine compounds according to formula (I) which are highly selective as Ras-Raf-Mek-Erk signal transduction pathway inhibitors and in particular are highly selective Erk inhibitors.
摘要翻译： 本发明提供了根据式（I）的新的吡啶并吡嗪化合物，其作为Ras-Raf-Mek-Erk信号转导途径抑制剂具有高选择性，特别是高度选择性的Erk抑制剂。
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6.发明授权Conjugates of disorazoles and their derivatives with cell-binding molecules, novel disorazole derivatives, processes of manufacturing and uses thereof 有权异恶唑及其衍生物与细胞结合分子的结合物，新型二唑衍生物，制造方法及其用途公开(公告)号：US08470776B2
公开(公告)日：2013-06-25
申请号：US12728050
申请日：2010-03-19
申请人： Eckhard Guenther , Olaf Schaefer , Michael Teifel , Klaus Paulini
发明人： Eckhard Guenther , Olaf Schaefer , Michael Teifel , Klaus Paulini
CPC分类号： C12P17/188 , C07D498/18 , C07D498/22 , C07K7/23 , C07K14/6555
摘要： The present invention provides conjugates of disorazoles and their derivatives with cell-binding molecules, such as peptides, proteins, hormones, blood proteins and antibodies. The present invention further provides novel disorazole derivatives and processes of manufacturing such conjugates and disorazole derivatives. These compounds can be used as medicaments for the treatment of physiological and/or pathophysiological conditions in mammals, in particular for the treatment of various tumors.
摘要翻译： 本发明提供了disorazole及其衍生物与细胞结合分子如肽，蛋白质，激素，血液蛋白和抗体的缀合物。 本发明还提供了新的二唑衍生物和制备这种缀合物和二唑衍生物的方法。 这些化合物可以用作治疗哺乳动物的生理和/或病理生理状况的药物，特别是用于治疗各种肿瘤。
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公开(公告)号：US20120258080A1
公开(公告)日：2012-10-11
申请号：US13439150
申请日：2012-04-04
申请人： Matthias GERLACH , Irene SEIPELT , Lars BLUMENSTEIN , Gilbert MUELLER , Eckhard GUENTHER , Tilmann SCHUSTER , Michael TEIFEL
发明人： Matthias GERLACH , Irene SEIPELT , Lars BLUMENSTEIN , Gilbert MUELLER , Eckhard GUENTHER , Tilmann SCHUSTER , Michael TEIFEL
IPC分类号： A61K31/4985 , A61K31/5377 , C07F9/6561 , A61K31/675 , A61P29/00 , A61P35/00 , A61P19/02 , A61P37/00 , A61P31/18 , A61P25/00 , A61P25/28 , A61P17/06 , A61P17/02 , A61P3/10 , A61P35/02 , A61P7/02 , A61P37/06 , A61P3/00 , A61P27/02 , A61P11/06 , A61P37/08 , A61P11/00 , A61P9/00 , A61P1/00 , A61P9/10 , A61P13/12 , A61P5/14 , A61P9/04 , A61P9/08 , A61P3/04 , A61P3/08 , A61P9/12 , A61K38/50 , A61K38/14 , A61K33/24 , A61K31/7048 , A61K39/395 , A61K38/21 , A61K31/704 , A61N5/00 , C07D471/04
CPC分类号： A61K31/4985 , A61K31/501 , A61K31/5377 , C07D471/04
摘要： The present invention provides new pyridopyrazine compounds which are suitable for the treatment or prevention of physiological and/or pathophysiological states mediated and/or modulated by signal transduction pathways and/or enzymes in mammals and in particular in humans.
摘要翻译： 本发明提供了适用于治疗或预防由哺乳动物，特别是人类中的信号转导途径和/或酶介导和/或调节的生理和/或病理生理状态的新的吡啶并吡嗪化合物。
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8.发明申请CONJUGATES OF DISORAZOLES AND THEIR DERIVATIVES WITH CELL-BINDING MOLECULES, NOVEL DISORAZOLE DERIVATIVES, PROCESSES OF MANUFACTURING AND USES THEREOF 审中-公开异恶唑及其衍生物与细胞结合分子的结合，新型异唑衍生物，制造方法及其用途公开(公告)号：US20100323963A1
公开(公告)日：2010-12-23
申请号：US12728075
申请日：2010-03-19
申请人： Eckhard GUENTHER , Olaf Schaefer , Michael Teifel , Klaus Paulini
发明人： Eckhard GUENTHER , Olaf Schaefer , Michael Teifel , Klaus Paulini
IPC分类号： A61K38/09 , C07D498/22 , C07D498/16 , C07K7/23 , C07K14/655 , A61K31/424 , A61K38/31 , A61P35/00 , A61P35/02
CPC分类号： C12P17/188 , C07D498/18 , C07D498/22 , C07K7/23 , C07K14/6555
摘要： The present invention provides conjugates of disorazoles and their derivatives with cell-binding molecules, such as peptides, proteins, hormones, blood proteins and antibodies. The present invention further provides novel disorazole derivatives and processes of manufacturing such conjugates and disorazole derivatives. These compounds can be used as medicaments for the treatment of physiological and/or pathophysiological conditions in mammals, in particular for the treatment of various tumors.
摘要翻译： 本发明提供了disorazole及其衍生物与细胞结合分子如肽，蛋白质，激素，血液蛋白和抗体的缀合物。 本发明还提供了新的二唑衍生物和制备这种缀合物和二唑衍生物的方法。 这些化合物可以用作治疗哺乳动物的生理和/或病理生理状况的药物，特别是用于治疗各种肿瘤。
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9.发明申请NOVEL TETRAHYDROCARBAZOLE DERIVATIVES AS LIGANDS OF G-PROTEIN COUPLED RECEPTORS 有权新型四氮唑衍生物作为G蛋白偶联受体的配体公开(公告)号：US20090170783A1
公开(公告)日：2009-07-02
申请号：US12109479
申请日：2008-04-25
申请人： Tilmann Schuster , Klaus Paulini , Peter Schmidt , Silke Baasner , Emmanuel Polymeropoulos , Eckhard Guenther , Michael Teifel
发明人： Tilmann Schuster , Klaus Paulini , Peter Schmidt , Silke Baasner , Emmanuel Polymeropoulos , Eckhard Guenther , Michael Teifel
CPC分类号： C07K5/06191 , A61K38/00 , C07K5/0827
摘要： The present invention provides novel tetrahydrocarbazole compounds according to formula (I) as ligands of G-protein coupled receptors (GPCR) which are useful in the treatment and/or prophylaxis of physiological and/or pathological conditions in mammals mediated by GPCR or of physiological and/or pathological conditions which can be treated by modulation of these receptors.
摘要翻译： 本发明提供了根据式（I）的新型四氢咔唑化合物作为G蛋白偶联受体（GPCR）的配体，其可用于治疗和/或预防由GPCR介导的哺乳动物的生理和/或病理状况或生理和/ /或可以通过调节这些受体来治疗的病理状况。
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10.发明申请Novel method of stabilizing diagnostic and therapeutic compounds in a cationic carrier system 审中-公开在阳离子载体体系中稳定诊断和治疗化合物的新方法公开(公告)号：US20050181038A1
公开(公告)日：2005-08-18
申请号：US11018575
申请日：2004-12-22
申请人： Heinrich Haas , Thomas Fichert , Brita Schulze , Toralf Peymann , Uwe Michaelis , Michael Teifel
发明人： Heinrich Haas , Thomas Fichert , Brita Schulze , Toralf Peymann , Uwe Michaelis , Michael Teifel
IPC分类号： A61K47/18 , A61K9/127 , A61K31/00 , A61K31/335 , A61K31/337 , A61K31/47 , A61K31/4745 , A61K47/24 , A61K47/28 , A61K47/34 , A61K47/48 , A61K49/00 , A61K49/18 , A61K51/12 , A61P9/00 , A61P11/06 , A61P17/02 , A61P19/02 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00
CPC分类号： A61K9/1271 , A61K9/1272 , A61K31/00 , A61K31/335 , A61K31/47 , A61K31/4745 , A61K47/186 , A61K47/34 , A61K47/543 , A61K47/56 , A61K47/6911 , A61K49/1812 , B82Y5/00
摘要： The present invention relates to a method of stabilizing a low molecular weight compound in a cationic liposome, wherein said compound has a low solubility in a lipid membrane and/or a low permeability across a lipid membrane. Preferrably, the compound is modified in order to increase lipid membrane solubility and/or lipid membrane permeability. After delivery of the cationic liposome to a target site, particularly a target site in an organism, the modification is reversed and the low molecular weight compound may enact its desired activity.
摘要翻译： 本发明涉及在阳离子脂质体中稳定低分子量化合物的方法，其中所述化合物在脂质膜中的溶解度低，和/或脂质膜上的低渗透性。 优选地，化合物被修饰以增加脂质膜溶解度和/或脂质膜渗透性。 将阳离子脂质体递送到靶位点，特别是生物体中的靶位点后，修饰被逆转，低分子量化合物可以产生其所需的活性。
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