公开(公告)号：US20060217562A1

公开(公告)日：2006-09-28

申请号：US10535345

申请日：2004-10-29

申请人： Graeme Semple ,  Thomas Schrader ,  Philip Skinner ,  Steven Colletti ,  Tawfik Gharbaoui ,  Jason Imbriglio ,  Jae-Kyu Jung ,  Rui Liang ,  Subharekha Raghavan ,  Darby Schmidt ,  James Tata

发明人： Graeme Semple ,  Thomas Schrader ,  Philip Skinner ,  Steven Colletti ,  Tawfik Gharbaoui ,  Jason Imbriglio ,  Jae-Kyu Jung ,  Rui Liang ,  Subharekha Raghavan ,  Darby Schmidt ,  James Tata

IPC分类号： A61K31/416 ,  C07D403/02

CPC分类号： C07D491/04 ,  C07D403/04 ,  C07D495/04

摘要： The present invention relates to certain tetrazole derivatives of Formula (I), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers and the like.

摘要翻译： 本发明涉及式（I）的某些四唑衍生物及其药学上可接受的盐，其表现出有用的药理学性质，例如作为RUP25受体的激动剂。 本发明还提供含有本发明化合物的药物组合物，以及使用本发明化合物和组合物治疗代谢相关疾病包括血脂异常，动脉粥样硬化，冠心病，胰岛素抵抗，2型糖尿病的方法 ，综合征-X等。 此外，本发明还提供本发明化合物与其它活性剂如属于α-葡糖苷酶抑制剂类，醛糖还原酶抑制剂，双胍类，HMG-CoA还原酶抑制剂，角鲨烯合成 抑制剂，贝特类，LDL分解代谢增强剂，血管紧张素转换酶（ACE）抑制剂，胰岛素分泌增强剂等。

公开(公告)号：US20070072924A1

公开(公告)日：2007-03-29

申请号：US11601252

申请日：2006-11-17

申请人： Graeme Semple ,  Thomas Schrader ,  Philip Skinner ,  Steven Colletti ,  Tawfik Gharbaoui ,  Jason Imbriglio ,  Jae-Kyu Jung ,  Rui Liang ,  Subharekha Raghavan ,  Darby Schmidt ,  James Tata

发明人： Graeme Semple ,  Thomas Schrader ,  Philip Skinner ,  Steven Colletti ,  Tawfik Gharbaoui ,  Jason Imbriglio ,  Jae-Kyu Jung ,  Rui Liang ,  Subharekha Raghavan ,  Darby Schmidt ,  James Tata

IPC分类号： A61K31/416 ,  C07D403/04

CPC分类号： C07D491/04 ,  C07D403/04 ,  C07D495/04

摘要： The present invention relates to certain tetrazole derivatives of Formula (I), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers and the like.

摘要翻译： 本发明涉及式（I）的某些四唑衍生物及其药学上可接受的盐，其表现出有用的药理学性质，例如作为RUP25受体的激动剂。 本发明还提供含有本发明化合物的药物组合物，以及使用本发明化合物和组合物治疗代谢相关疾病包括血脂异常，动脉粥样硬化，冠心病，胰岛素抵抗，2型糖尿病 ，综合征-X等。 此外，本发明还提供本发明化合物与其它活性剂如属于α-葡糖苷酶抑制剂类，醛糖还原酶抑制剂，双胍类，HMG-CoA还原酶抑制剂，角鲨烯合成 抑制剂，贝特类，LDL分解代谢增强剂，血管紧张素转换酶（ACE）抑制剂，胰岛素分泌增强剂等。

公开(公告)号：US08637555B2

公开(公告)日：2014-01-28

申请号：US10535345

申请日：2004-10-29

申请人： Graeme Semple ,  Thomas Schrader ,  Philip J. Skinner ,  Steven L. Colletti ,  Tawfik Gharbaoui ,  Jason E. Imbriglio ,  Jae-Kyu Jung ,  Rui Liang ,  Subharekha Raghavan ,  Darby Schmidt ,  James R. Tata

发明人： Graeme Semple ,  Thomas Schrader ,  Philip J. Skinner ,  Steven L. Colletti ,  Tawfik Gharbaoui ,  Jason E. Imbriglio ,  Jae-Kyu Jung ,  Rui Liang ,  Subharekha Raghavan ,  Darby Schmidt ,  James R. Tata

IPC分类号： A61K31/407 ,  C07D231/54

CPC分类号： C07D491/04 ,  C07D403/04 ,  C07D495/04

摘要： The present invention relates to certain tetrazole derivatives of Formula (I), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers and the like.

摘要翻译： 本发明涉及式（I）的某些四唑衍生物及其药学上可接受的盐，其表现出有用的药理学性质，例如作为RUP25受体的激动剂。 本发明还提供含有本发明化合物的药物组合物，以及使用本发明化合物和组合物治疗代谢相关疾病包括血脂异常，动脉粥样硬化，冠心病，胰岛素抵抗，2型糖尿病 ，综合征-X等。 此外，本发明还提供本发明化合物与其它活性剂如属于α-葡糖苷酶抑制剂类，醛糖还原酶抑制剂，双胍类，HMG-CoA还原酶抑制剂，角鲨烯合成 抑制剂，贝特类，LDL分解代谢增强剂，血管紧张素转换酶（ACE）抑制剂，胰岛素分泌增强剂等。

公开(公告)号：US20060205955A1

公开(公告)日：2006-09-14

申请号：US11315753

申请日：2005-12-22

申请人： P. Boatman ,  Thomas Schrader ,  Graeme Semple ,  Philip Skinner ,  Jae-Kyu Jung

发明人： P. Boatman ,  Thomas Schrader ,  Graeme Semple ,  Philip Skinner ,  Jae-Kyu Jung

IPC分类号： C07D231/54

CPC分类号： C07D403/04 ,  C07D209/80 ,  C07D209/88 ,  C07D231/54 ,  C07D265/36 ,  C07D471/04 ,  C07D471/14

摘要： The present invention relates to certain fused pyrazole derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, DP receptor antagonists, and the like.

公开(公告)号：US20070073062A1

公开(公告)日：2007-03-29

申请号：US11601184

申请日：2006-11-17

申请人： P. Boatman ,  Thomas Schrader ,  Graeme Semple ,  Philip Skinner ,  Jae-Kyu Jung

发明人： P. Boatman ,  Thomas Schrader ,  Graeme Semple ,  Philip Skinner ,  Jae-Kyu Jung

IPC分类号： C07D231/54 ,  C07D403/02

CPC分类号： C07D403/04 ,  C07D209/80 ,  C07D209/88 ,  C07D231/54 ,  C07D265/36 ,  C07D471/04 ,  C07D471/14

摘要： The present invention relates to certain fused pyrazole derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, DP receptor antagonists, and the like.

公开(公告)号：US20050200276A1

公开(公告)日：2005-09-15

申请号：US11019452

申请日：2004-12-23

申请人： Albrecht Uhlig ,  Kerstin Nolte ,  Thomas Schrader

发明人： Albrecht Uhlig ,  Kerstin Nolte ,  Thomas Schrader

IPC分类号： H05B33/28 ,  C09K11/06 ,  H01J1/62 ,  H01L51/50 ,  H05B33/04 ,  H05B33/14 ,  H05B33/20 ,  H05B33/22 ,  H05B33/26

CPC分类号： H01L51/5088 ,  H01L51/5206 ,  H01L51/5215

摘要： An organic electroluminescence device and display having high efficiency and improved durability. A layer formed of polysiloxane, fluorinated hydrocarbon, and/or derivatives thereof is interposed between an anode and a hole injection layer/hole transport layer, thus improving the durability of the organic electroluminescence device.

摘要翻译： 一种具有高效率和改善的耐久性的有机电致发光器件和显示器。 由聚硅氧烷，氟化烃和/或其衍生物形成的层插入在阳极和空穴注入层/空穴传输层之间，从而提高了有机电致发光器件的耐久性。

公开(公告)号：US20050058785A1

公开(公告)日：2005-03-17

申请号：US10936708

申请日：2004-09-09

申请人： Albrecht Uhlig ,  Michael Redecker ,  Marcus Schaedig ,  Thomas Schrader ,  Werner Humbs

发明人： Albrecht Uhlig ,  Michael Redecker ,  Marcus Schaedig ,  Thomas Schrader ,  Werner Humbs

IPC分类号： G03F7/40 ,  B41M3/00 ,  B41M5/52 ,  H01L21/027 ,  H01L51/00 ,  H01L51/40 ,  H01L51/50 ,  H05B33/02 ,  H05B33/10 ,  H05B33/12 ,  H05B33/22 ,  B41M5/00

CPC分类号： H01L51/0005 ,  B41M5/506 ,  B41M5/52 ,  Y10S428/917 ,  Y10T428/24851 ,  Y10T428/24942

摘要： A substrate for inkjet printing, which includes a photoresist layer structure on a base substrate, and a method of manufacturing the same are provided. The substrate, which has high surface tension variation and slight thickness variation, may be manufactured at a low cost. The substrate includes a discontinuous organic layer structure made of a fluorinated hydrocarbon or a polysiloxane on the photoresist layer structure.

摘要翻译： 提供了一种用于喷墨印刷的基板，其包括在基底基板上的光致抗蚀剂层结构及其制造方法。 可以以低成本制造具有高表面张力变化和轻微厚度变化的基材。 基板包括在光致抗蚀剂层结构上由氟化烃或聚硅氧烷制成的不连续的有机层结构。

公开(公告)号：US08791092B2

公开(公告)日：2014-07-29

申请号：US13203962

申请日：2010-03-05

申请人： Gal Bitan ,  Akila Shanmugam ,  Aleksey Lomakin ,  Thomas Schrader ,  Frank Gerrit Klarner ,  Peter Talbiersky ,  Jolanta Polkowska ,  Frank Bastkowski ,  Sharmistha Sinha ,  Sally Frautschy

发明人： Gal Bitan ,  Akila Shanmugam ,  Aleksey Lomakin ,  Thomas Schrader ,  Frank Gerrit Klarner ,  Peter Talbiersky ,  Jolanta Polkowska ,  Frank Bastkowski ,  Sharmistha Sinha ,  Sally Frautschy

IPC分类号： A61K31/6615 ,  A61K31/663 ,  C07K14/47 ,  C07F9/40 ,  C07F9/12

CPC分类号： C07F9/12 ,  A61K31/661 ,  A61K31/663 ,  A61K49/0052 ,  C07F9/4084

摘要： This invention provides novel compositions to inhibit the aggregation of amyloid proteins. In various embodiments the compositions comprise a molecular tweezers that binds lysine and/or arginine and thereby inhibits the aggregation of amyloidogenic proteins.

摘要翻译： 本发明提供抑制淀粉样蛋白聚集的新型组合物。 在各种实施方案中，组合物包含结合赖氨酸和/或精氨酸并由此抑制淀粉样蛋白形成蛋白质聚集的分子镊子。

公开(公告)号：US20050239808A1

公开(公告)日：2005-10-27

申请号：US10514015

申请日：2003-05-09

申请人： Thomas Schrader ,  Detlev Riesner ,  Petra Rzepecki ,  Luitgard Nagel-Steger ,  Mark Wehner ,  Christian Kirsten ,  Oliver Molt ,  Reza Zadmard ,  Katja Aschermann

发明人： Thomas Schrader ,  Detlev Riesner ,  Petra Rzepecki ,  Luitgard Nagel-Steger ,  Mark Wehner ,  Christian Kirsten ,  Oliver Molt ,  Reza Zadmard ,  Katja Aschermann

IPC分类号： A61P25/28 ,  C07D231/40 ,  C07D401/14 ,  A61K31/522 ,  A61K31/416 ,  A61K31/4196 ,  A61K31/4709 ,  C07D473/02 ,  C07D43/02

CPC分类号： C07D231/40 ,  C07D401/14

摘要： The invention on hand refers to diseases associated with abnormal protein structures, including Alzheimer's disease, Creutzfeldt-Jakob's disease, BSE and other prion-associated diseases. It is the task of the invention on hand to provide new active agents preventing the formation of amyloid plaques and to dissolve existing plaques, such agents being convenient for therapy, diagnosis and prophylaxis of diseases that are associated with abnormal protein structures. This task is performed in terms of the current invention by heterocyclic or aromatic agents with a rigid structure and a donor-acceptor-donor pattern (DAD), the latter being formed by donors and acceptors of hydrogen bridge linkages which comply with the β-sheet structure of the peptide or protein and thus fit as binding partners. The heterocyclic or aromatic agents are available at least as dimers. They recognise peptides and proteins with a β-sheet structure, form stable complexes with them and inhibit their aggregation to β-amyloid plaques. Furthermore, the new active agents are able to dissolve β-amyloid plaques that already exist. Another task of the current invention is to provide methods for the synthesis of said heterocyclic or aromatic compounds.

摘要翻译： 手头的发明是指与异常蛋白质结构相关的疾病，包括阿尔茨海默病，克雅氏病，疯牛病和其他朊病毒相关疾病。 本发明的任务是提供防止淀粉样蛋白斑块形成和溶解现有斑块的新的活性剂，所述药剂便于治疗，诊断和预防与异常蛋白质结构相关的疾病。 根据本发明，通过具有刚性结构和供体 - 受体 - 给体模式（DAD）的杂环或芳族化合物来执行该任务，后者由供体和符合β-折叠板的氢桥连接体的受体形成 肽或蛋白质的结构，因此适合作为结合配偶体。 杂环或芳族试剂至少可以作为二聚体获得。 它们识别具有β-折叠结构的肽和蛋白质，与它们形成稳定的复合物并抑制它们与β-淀粉样蛋白斑的聚集。 此外，新的活性剂能够溶解已经存在的β-淀粉样斑块。 本发明的另一个任务是提供合成所述杂环或芳族化合物的方法。

公开(公告)号：US08481494B2

公开(公告)日：2013-07-09

申请号：US13504325

申请日：2010-01-26

申请人： Thomas Schrader ,  Katrin Hochdörffer ,  Julia März-Berberich ,  Luitgard Nagel-Steger ,  Gal Bitan ,  Sharmistha Sinha

发明人： Thomas Schrader ,  Katrin Hochdörffer ,  Julia März-Berberich ,  Luitgard Nagel-Steger ,  Gal Bitan ,  Sharmistha Sinha

IPC分类号： A61K38/00 ,  A61K38/04 ,  A61K38/08 ,  A61K38/10 ,  A61K31/4155 ,  C07K5/00 ,  C07K7/00 ,  C07D403/14

CPC分类号： C07D231/38 ,  A61K38/00

摘要： The present invention relates to the field of protein misfolding diseases and thus to diseases which are associated with or induced by abnormal or pathogenic three-dimensional folding of proteins and/or peptides or which are linked to pathogenic conformational changes of proteins and/or peptides, such as Alzheimer's disease. Particularly, the present invention provides novel trimeric pyrazole compounds, which exhibit a therapeutic effectiveness in regard to the aforementioned protein misfolding diseases, and refers to their use for the treatment of such protein misfolding diseases, especially neurodegenerative diseases as well as to medicaments or pharmaceutical compositions comprising these compounds.

摘要翻译： 本发明涉及蛋白质错误折叠疾病的领域，因此涉及与蛋白质和/或肽的异常或致病性三维折叠相关或由其引起的或与蛋白质和/或肽的致病性构象变化相关的疾病， 如阿尔茨海默病。 特别地，本发明提供了新颖的三聚吡唑化合物，其对上述蛋白质错误折叠疾病具有治疗效果，并且是指其用于治疗这种蛋白质错折叠疾病，特别是神经变性疾病以及药物或药物组合物的用途 包括这些化合物。