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1. 发明授权

US09150561B2 Thiazole derivatives and use thereof 有权
标题翻译：噻唑衍生物及其用途
公开(公告)号：US09150561B2
公开(公告)日：2015-10-06
申请号：US14175751
申请日：2014-02-07
申请人： Merck Serono S.A.
发明人： Anna Quattropani , Thomas Rueckle , Matthias Schwarz , Jerome Dorbais , Wolfgang Sauer , Christophe Cleva , Gwenaelle Desforges
IPC分类号： C07D417/14 , C07D417/04 , C07D277/46
CPC分类号： C07D417/04 , C07D277/46 , C07D417/14
摘要： The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neturodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
摘要翻译：本发明涉及式（I）的噻唑衍生物，特别是用于治疗和/或预防自身免疫疾病和/或炎性疾病，心血管疾病，神经变性疾病，细菌或病毒感染，肾脏疾病，血小板聚集，癌症，移植，移植排斥或肺部损伤。

2. 发明授权

US08796280B2 2,3-disubstituted pyrazinesulfonamides as CRTH2 inhibitors 有权
标题翻译： 2,3-二取代吡嗪磺酰胺作为CRTH2抑制剂
公开(公告)号：US08796280B2
公开(公告)日：2014-08-05
申请号：US11918294
申请日：2006-04-20
申请人： Patrick Page , Matthias Schwarz , Eric Sebille , Christophe Cleva , Cedric Merlot , Maurizio Maio
发明人： Patrick Page , Matthias Schwarz , Eric Sebille , Christophe Cleva , Cedric Merlot , Maurizio Maio
IPC分类号： A61K31/4965 , C07D409/12 , C07D401/10 , C07D241/22 , C07D413/10 , C07D405/12 , C07D403/10 , C07D401/12
CPC分类号： C07D241/22 , C07D241/20 , C07D401/10 , C07D401/12 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D411/14 , C07D413/10 , C07D413/12 , C07D417/10 , C07D417/12
摘要： The present invention is related to the use of 2,3 substituted pyrazine sulfonamides of formula (I) for the treatment and/or prevention of allergic diseases, inflammatory dermatoses and other diseases with an inflammatory component. Specifically, the present invention is related to the use of 2,3 substituted pyrazine sulfonamides for the modulation, notably the inhibition, of CRTH2 activity.
摘要翻译：本发明涉及式（I）的2,3-取代吡嗪磺酰胺在治疗和/或预防过敏性疾病，炎性皮肤病和其它具有炎性成分的疾病中的应用。具体地说，本发明涉及2,3取代吡嗪磺酰胺用于调节，特别是抑制CRTH2活性的用途。

3. 发明申请

US20140011213A1 MEMBRANE BOUND REPORTER MOLECULES AND THEIR USE IN CELL SORTING 审中-公开
标题翻译：膜结合报告分子及其在细胞分选中的应用
公开(公告)号：US20140011213A1
公开(公告)日：2014-01-09
申请号：US13995716
申请日：2011-12-19
申请人： Daniel Helman , Mira Toister-Achituv , Meirav Bar-Shimon , Moshe Smolarsky
发明人： Daniel Helman , Mira Toister-Achituv , Meirav Bar-Shimon , Moshe Smolarsky
IPC分类号： G01N33/569
CPC分类号： G01N33/56966 , C07K2319/035 , C07K2319/20 , C12N15/85 , C12N2830/20 , C12N2830/40 , C12Q1/6897 , C12Q2563/131
摘要： The present invention relates to nucleic acid molecules comprising a nucleic acid sequence encoding a membrane-bound biotin mimetic peptide (BMP) or biotin acceptor peptide (BAP). The invention also relates to a method for selection of high producer cells secreting a protein of interest.
摘要翻译：本发明涉及包含编码膜结合生物素模拟肽（BMP）或生物素受体肽（BAP）的核酸序列的核酸分子。本发明还涉及用于选择分泌目的蛋白质的高生产细胞的方法。

4. 发明申请

US20140005368A1 Low Fucose Cell Lines And Uses Thereof 有权
标题翻译：低岩藻糖细胞系及其用途
公开(公告)号：US20140005368A1
公开(公告)日：2014-01-02
申请号：US14003767
申请日：2012-03-05
申请人： Daniel Helman , Meirav Barshimon , Mira Toister-Achituv
发明人： Daniel Helman , Meirav Barshimon , Mira Toister-Achituv
IPC分类号： C07K16/28 , C12N15/85
CPC分类号： C07K16/2863 , C07K16/00 , C07K2317/41 , C07K2319/30 , C12N9/0006 , C12N9/1051 , C12N9/88 , C12N15/01 , C12N15/85 , C12Y101/01271 , C12Y204/01068 , C12Y402/01047
摘要： A method of selecting cells having zero fucose level useful as host cells for expressing recombinant proteins is disclosed. The method comprises: (d) introducing genetic mutations into a population of CHO cells by contacting the cells with a methotrexate (MTX), (e) contacting the population of CHO cells comprising mutated cells with a non-toxic fucose binding agent for an amount of time that allows binding of the fucose binding agent to a fucose moiety on a cell membrane of the population of cells, wherein the amount of time does not allow killing of the cells; and (f) depleting from the population of cells comprising mutated cells, a subpopulation of cells which bind the fucose binding agent, thereby selecting cells useful as host cells for expressing recombinant proteins, the selected cells having zero fucose content. There are also disclosed cells and cell lines useful as host cells for expressing recombinant proteins.
摘要翻译：公开了选择具有用作表达重组蛋白的宿主细胞的零岩藻糖水平的细胞的方法。该方法包括：（d）通过使细胞与甲氨蝶呤（MTX）接触，将遗传突变引入CHO细胞群体;（e）将含有突变细胞的CHO细胞群与无毒岩藻糖结合剂接触，的时间，其允许岩藻糖结合剂与细胞群的细胞膜上的岩藻糖部分结合，其中所述时间量不允许杀死细胞; 和（f）从包含突变细胞的细胞群体中消耗，结合岩藻糖结合剂的细胞亚群，从而选择可用作表达重组蛋白质的宿主细胞的细胞，所选择的细胞具有零岩藻糖含量。还公开了可用作表达重组蛋白的宿主细胞的细胞和细胞系。

5. 发明申请

US20130157952A1 GENOMIC MARKERS FOR PREDICTION OF LONG-TERM RESPONSE TO GROWTH HORMONE (GH) THERAPY 有权
标题翻译：用于预测长期应对生长激素（GH）治疗的基因标记
公开(公告)号：US20130157952A1
公开(公告)日：2013-06-20
申请号：US13819058
申请日：2011-08-31
申请人： Pascal Croteau , John Raelson , Jerome Wojcik , Benoît Destenaves , Clement Olivier , Sonia Schnieper-Samec
发明人： Pascal Croteau , John Raelson , Jerome Wojcik , Benoît Destenaves , Clement Olivier , Sonia Schnieper-Samec
IPC分类号： C12Q1/68
CPC分类号： C12Q1/6883 , C12Q1/6876 , C12Q1/6886 , C12Q2600/106 , C12Q2600/156 , G01N2800/38 , G01N2800/52
摘要： The present invention relates to the use of genetic markers to identify the response to growth hormone treatment in Growth Hormone Deficiency (GHD) or Turner Syndrome (TS) patients as well as a method of treating GHD or TS patients and kits for genotyping.
摘要翻译：本发明涉及遗传标记物用于鉴定生长激素缺乏（GHD）或特纳综合征（TS）患者中对生长激素治疗的应答以及治疗GHD或TS患者和用于基因分型的试剂盒的方法。

6. 发明申请

US20120295889A1 3-Arylamino Pyridine Derivatives 有权
标题翻译： 3-芳基氨基吡啶衍生物
公开(公告)号：US20120295889A1
公开(公告)日：2012-11-22
申请号：US13472721
申请日：2012-05-16
申请人： Ulrich Abel , Holger Deppe , Achim Feurer , Ulrich Grädler , Kerstin Otte , Renate Sekul , Meinolf Thiemann , Andreas Goutopoulos , Matthias Schwarz , Xuliang Jiang
发明人： Ulrich Abel , Holger Deppe , Achim Feurer , Ulrich Grädler , Kerstin Otte , Renate Sekul , Meinolf Thiemann , Andreas Goutopoulos , Matthias Schwarz , Xuliang Jiang
IPC分类号： C07D213/81 , A61K31/5377 , A61K31/496 , A61K31/506 , A61K31/4709 , A61K31/4545 , A61K31/444 , A61K31/443 , A61K31/4439 , A61K31/44 , C07D413/12 , C07D401/12 , C07D413/04 , C07D405/12 , C07D213/79 , A61P9/10 , A61K31/4433 , C07D413/06 , C07D213/89 , C07D401/06 , A61P35/00 , A61P29/00 , A61P1/18 , A61P13/12 , A61P17/00 , A61P9/00 , A61P13/08 , A61P17/06 , A61P3/10 , A61P27/02 , A61P1/00 , A61K31/55
CPC分类号： C07D405/12 , C07D213/79 , C07D213/81 , C07D213/89 , C07D295/125 , C07D295/13 , C07D295/32 , C07D401/12
摘要： The invention provides novel, substituted 3-arylamino pyridine compounds pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.
摘要翻译：本发明提供新的取代的3-芳基氨基吡啶化合物其药学上可接受的盐，溶剂合物和前药化合物，其中W，R 1，R 2，R 9，R 10，R 11，R 12，R 13，R 14如说明书中所定义。这些化合物是MEK抑制剂，可用于治疗过度增殖性疾病，如癌症，再狭窄和炎症。还公开了这样的化合物在哺乳动物，特别是人类中过度增殖性疾病的治疗和含有这些化合物的药物组合物中的应用。

7. 发明申请

US20120115895A1 TRICYCLIC INDOLE-DERIVED SPIRO DERIVATIVES AS CRTH2 MODULATORS 审中-公开
标题翻译：作为CRTH2调节剂的TRICYCLIC INDOLE-DIVIVED SPIRO DERIVATIVES
公开(公告)号：US20120115895A1
公开(公告)日：2012-05-10
申请号：US13383857
申请日：2010-07-14
申请人： Stefano Crosignani , Catherine Jorand-Lebrun , Tania Grippi-Vallotton
发明人： Stefano Crosignani , Catherine Jorand-Lebrun , Tania Grippi-Vallotton
IPC分类号： A61K31/4439 , A61K31/422 , A61K31/4188 , C07D487/10 , A61P19/02 , A61P29/00 , A61P37/08 , A61P11/06 , A61P1/00 , A61K31/427 , A61P25/00
CPC分类号： C07D487/10
摘要： The present invention relates to compounds of formula (I) for use as pharmaceutical active compounds, as well as pharmaceutical formulations containing the same, for the treatment of allergic diseases. The compounds according to Formula (I) are suitable as modulators of CRTH2. The invention provides Spiro derivatives according to Formula (I) and related formulae that are useful in the treatment and/or prevention of diseases selected from allergic diseases such as allergic asthma, allergic rhinitis, allergic conjunctivitis, and inflammatory dermatoses such as atopic dermatitis, contact hypersensitivity, allergic contact dermatitis, chronic urticaria/chronic idiopathic/autoimmune urticaria, drag-induced exanthems (e.g., toxic epidermal necrolysis or Lyell's syndrome/Stevens-Johnson syndrome/drug hypersensitivity syndrome), photodermatosis or polymorphous light emption (e.g., photoirritant contact dermatitis, photoallergy contact dermatitis, chronic actinic dermatitis), and myositis neurodegenerative disorders such as neuropatic pain and other diseases with an inflammatory component such as rheumatoid arthritis, multiple sclerosis, osteoarthritis, and inflammatory bowel disease (IBD).
摘要翻译：本发明涉及用作药物活性化合物的式（I）化合物，以及含有该化合物的用于治疗过敏性疾病的药物制剂。根据式（I）的化合物适合作为CRTH2的调节剂。本发明提供了可用于治疗和/或预防选自过敏性疾病如过敏性哮喘，过敏性鼻炎，过敏性结膜炎和炎性皮肤病如特应性皮炎，接触的疾病的式（I）和相关配方的螺衍生物超敏反应，过敏性接触性皮炎，慢性荨麻疹/慢性特发性/自身免疫性荨麻疹，牵引性外阴（例如中毒性表皮坏死松解症或莱尔综合征/史蒂文斯 - 约翰逊综合征/药物过敏综合征），光照皮肤病或多形态光吸收（如光刺激性接触性皮炎，光敏性接触性皮炎，慢性光化性皮炎）和肌炎神经变性疾病如神经性疼痛和其它具有炎性成分的疾病，例如类风湿性关节炎，多发性硬化症，骨关节炎和炎症性肠病（IBD）。

8. 发明申请

US20110293564A1 2-MORPHOLINO-PYRIDO[3,2-D]PYRIMIDINES 有权
标题翻译： 2-吗啉代 - 吡啶并[3,2-D]嘧啶
公开(公告)号：US20110293564A1
公开(公告)日：2011-12-01
申请号：US13147449
申请日：2010-02-04
申请人： Cyril Montagne , Agnés Bombrun , Gwenaelle Desforges , Anna Quattropani , Pascale Gaillard
发明人： Cyril Montagne , Agnés Bombrun , Gwenaelle Desforges , Anna Quattropani , Pascale Gaillard
IPC分类号： A61K38/21 , A61K31/5377 , A61P25/00 , A61P35/00 , A61P37/00 , A61P19/04 , A61P29/00 , A61P1/00 , A61P17/06 , A61P17/00 , A61P37/06 , A61P5/14 , A61P21/04 , A61P27/02 , A61P7/06 , A61P35/02 , A61P9/10 , A61P9/00 , A61P35/04 , A61P31/14 , A61P1/16 , A61P25/16 , A61K39/395 , C07D413/14
CPC分类号： C07D471/04
摘要： This invention relates to compounds of Formula (I) as Pi3k inhibitors for treating autoimmune diseases, inflammatory disorders, multiple sclerosis and other deseases like cancers.
摘要翻译：本发明涉及作为用于治疗自身免疫疾病，炎症性疾病，多发性硬化和其它疾病如癌症的Pi3k抑制剂的式（I）化合物。

9. 发明授权

US08007797B2 Junctional adhesion molecule-C (JAM-C) binding compounds and methods of their use 有权
标题翻译：功能粘附分子-C（JAM-C）结合化合物及其使用方法
公开(公告)号：US08007797B2
公开(公告)日：2011-08-30
申请号：US12443231
申请日：2007-09-28
申请人： Pierre-Yves Dietrich , Mirna Tenan , Michel Aurrand-Lions , Beat Albert Imhof
发明人： Pierre-Yves Dietrich , Mirna Tenan , Michel Aurrand-Lions , Beat Albert Imhof
IPC分类号： A61K39/395
CPC分类号： C07K16/2803 , C07K2317/92
摘要： The present invention relates to the use of a compound that specifically binds to JAM-C or JAM-B for the treatment of gliomas. More specifically the invention relates to the use of an antagonist of JAM-B or JAM-C for the treatment of glioma, in particular astrocytoma.
摘要翻译：本发明涉及特异性结合JAM-C或JAM-B用于治疗神经胶质瘤的化合物的用途。更具体地，本发明涉及JAM-B或JAM-C拮抗剂用于治疗胶质瘤，特别是星形细胞瘤的用途。

10. 发明授权

US07998964B2 N-hydroxyamide derivatives and use thereof 有权
标题翻译： N-羟基酰胺衍生物及其用途
公开(公告)号：US07998964B2
公开(公告)日：2011-08-16
申请号：US12094921
申请日：2006-11-16
申请人： Dominique Swinnen , Jerome Gonzalez
发明人： Dominique Swinnen , Jerome Gonzalez
IPC分类号： A61K31/4965 , C07D241/04 , C07D295/00
CPC分类号： C07D241/04
摘要： The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.
摘要翻译：本发明涉及式（I）的N-羟基酰胺衍生物及其用途，特别是其用于治疗和/或预防自身免疫疾病，炎性疾病，心血管疾病，神经变性疾病，癌症，呼吸系统疾病和纤维化，包括多发性硬化症，关节炎，肺气肿，慢性阻塞性肺病，肝纤维化和肺纤维化。

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