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公开(公告)号：US20090042852A1
公开(公告)日：2009-02-12
申请号：US11813289
申请日：2006-01-04
申请人： Peter Bach , Jonas Bostrom , Kay Brickmann , Leifeng Cheng , Fabrizio Giordanetto , Robert D. Groneberg , Darren Martin Harvey , Michael F. O'Sullivan , Fredrik Zetterberg , Krister Osterlund
发明人： Peter Bach , Jonas Bostrom , Kay Brickmann , Leifeng Cheng , Fabrizio Giordanetto , Robert D. Groneberg , Darren Martin Harvey , Michael F. O'Sullivan , Fredrik Zetterberg , Krister Osterlund
IPC分类号： A61K31/496 , C07D487/04 , A61K31/4439 , C07D401/04 , C12N5/06 , A61K31/551 , A61K31/4545
CPC分类号： C07D413/14 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/14
摘要： The present invention relates to certain novel pyridin compounds of Formula (I) to processes for preparing such compounds, to their utility as P2Y12 inhibitors and as anti-trombotic agents etc, and processes for their preparation, their use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing them.
摘要翻译： 本发明涉及式（I）的某些新颖的吡啶化合物，用于制备这些化合物的方法，其用途为P2Y12抑制剂和抗血栓形成剂等，及其制备方法，它们用作心血管疾病中的药物 作为含有它们的药物组合物。
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公开(公告)号：US20090143422A1
公开(公告)日：2009-06-04
申请号：US12364330
申请日：2009-02-02
申请人： Mark Munson , David A. Mareska , Youngboo Kim , Robert D. Groneberg , James Rizzi , Martha Rodriguez , Ganghyeok Kim , Guy Vigers , Chang Rao , Devan Balachari , Darren Harvey
发明人： Mark Munson , David A. Mareska , Youngboo Kim , Robert D. Groneberg , James Rizzi , Martha Rodriguez , Ganghyeok Kim , Guy Vigers , Chang Rao , Devan Balachari , Darren Harvey
IPC分类号： A61K31/4375 , C07D231/54 , A61K31/416 , C07D261/20 , A61K31/42 , C07D471/04
CPC分类号： C07D401/14 , C07D231/56 , C07D261/20 , C07D403/04 , C07D403/12 , C07D405/12 , C07D413/12 , C07D471/04
摘要： This invention relates to inhibitors of p38 and methods of utilizing the inhibitors and pharmaceutical compositions thereof in the treatment and prevention of various disorders mediated by p38.
摘要翻译： 本发明涉及p38的抑制剂和利用该抑制剂及其药物组合物治疗和预防由p38介导的各种疾病的方法。
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![5,7-substituted-imidazo[1,2-C]pyrimidines as inhibitors of JAK kinases](/abs-image/US/2015/02/24/US08962596B2/abs.jpg.150x150.jpg)
3.发明授权5,7-substituted-imidazo[1,2-C]pyrimidines as inhibitors of JAK kinases 有权5,7-取代 - 咪唑并[1,2-C]嘧啶作为JAK激酶抑制剂公开(公告)号：US08962596B2
公开(公告)日：2015-02-24
申请号：US13640099
申请日：2011-04-11
申请人： Laurence E. Burgess , Mark Laurence Boys , Robert D. Groneberg , Darren M. Harvey , Timothy Kercher , Christopher F. Kraser , Ellen Laird , Eugene Tarlton , Qian Zhao , Lily Huang
发明人： Laurence E. Burgess , Mark Laurence Boys , Robert D. Groneberg , Darren M. Harvey , Timothy Kercher , Christopher F. Kraser , Ellen Laird , Eugene Tarlton , Qian Zhao , Lily Huang
IPC分类号： C07D487/04 , A61K31/519 , A61P29/00 , A61P35/00 , A61P37/06 , C07D498/04
CPC分类号： C07D487/04 , C07D498/04
摘要： Compounds of Formula I: and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3, R4, R5, R6, R7, X1 and X2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.
摘要翻译： 式I化合物及其其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，X 1和X 2具有本说明书中给出的含义的立体异构体及其药学上可接受的盐和溶剂化物是一种或多种JAK激酶的抑制剂， 可用于治疗自身免疫性疾病，炎性疾病，移植器官，组织和细胞排斥，以及血液系统疾病和恶性肿瘤及其并发症。
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公开(公告)号：US08304407B2
公开(公告)日：2012-11-06
申请号：US13414579
申请日：2012-03-07
IPC分类号： A61P37/00 , A61K31/55 , C07D223/16 , C07D403/10
CPC分类号： C07D223/16
摘要： Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency.
摘要翻译： 提供了可用于通过Toll样受体TLR7和/或TLR8调节信号传导的组合物和方法。 组合物和方法用于治疗自身免疫，炎症过敏，哮喘，移植物排斥，移植物抗宿主病，感染，败血症，癌症和免疫缺陷。
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公开(公告)号：US20120165317A1
公开(公告)日：2012-06-28
申请号：US13414579
申请日：2012-03-07
CPC分类号： C07D223/16
摘要： Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency.
摘要翻译： 提供了可用于通过Toll样受体TLR7和/或TLR8调节信号传导的组合物和方法。 组合物和方法用于治疗自身免疫，炎症过敏，哮喘，移植物排斥，移植物抗宿主病，感染，败血症，癌症和免疫缺陷。
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公开(公告)号：US08153622B2
公开(公告)日：2012-04-10
申请号：US12064193
申请日：2006-08-17
IPC分类号： A61P37/00 , A61K31/55 , C07D223/16 , C07D403/10
CPC分类号： C07D223/16
摘要： Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency.
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公开(公告)号：US20090149459A1
公开(公告)日：2009-06-11
申请号：US12364310
申请日：2009-02-02
申请人： Mark Munson , David A. Mareska , Youngboo Kim , Robert D. Groneberg , James Rizzi , Martha Rodriguez , Ganghyeok Kim , Guy Vigers , Chang Rao , Devan Balachari , Darren Harvey
发明人： Mark Munson , David A. Mareska , Youngboo Kim , Robert D. Groneberg , James Rizzi , Martha Rodriguez , Ganghyeok Kim , Guy Vigers , Chang Rao , Devan Balachari , Darren Harvey
IPC分类号： A61K31/416 , C07D471/04 , C07D413/02 , C07D231/56 , A61P37/00 , A61P31/00 , A61P25/28 , A61P19/08 , A61P29/00 , A61K31/437 , A61K31/5377
CPC分类号： C07D401/14 , C07D231/56 , C07D261/20 , C07D403/04 , C07D403/12 , C07D405/12 , C07D413/12 , C07D471/04
摘要： This invention relates to inhibitors of p38 and methods of utilizing the inhibitors and pharmaceutical compositions thereof in the treatment and prevention of various disorders mediated by p38.
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公开(公告)号：US07005440B1
公开(公告)日：2006-02-28
申请号：US09724496
申请日：2000-11-28
申请人： Zaid Jayyosi , Gerard M. McGeehan , Michael F. Kelley , Richard F. Labaudiniere , Litao Zhang , Robert D. Groneberg , Daniel G. McGarry , Thomas J. Caulfield , Anne Minnich , Mark Bobko , Robert Morris
发明人： Zaid Jayyosi , Gerard M. McGeehan , Michael F. Kelley , Richard F. Labaudiniere , Litao Zhang , Robert D. Groneberg , Daniel G. McGarry , Thomas J. Caulfield , Anne Minnich , Mark Bobko , Robert Morris
IPC分类号： A01N43/76
CPC分类号： C07D213/30 , C07C65/24 , C07D213/61 , C07D215/14 , C07D215/18 , C07D215/20 , C07D215/38 , C07D215/60 , C07D239/74 , C07D241/42 , C07D261/08 , C07D263/32 , C07D263/58 , C07D271/06 , C07D277/24 , C07D277/64 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/04
摘要： The use of triaryl acid derivatives of formula (I) and their pharmaceutical compositions as PPAR ligand receptor binders. The PPAR ligand receptor binders of this invention are useful as agonists or antagonists of the PPAR receptor.
摘要翻译： 使用式（I）的三芳基酸衍生物<化学id =“CHEM-US-00001”num =“000
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公开(公告)号：US06635655B1
公开(公告)日：2003-10-21
申请号：US09662649
申请日：2000-09-14
申请人： Zaid Jayyosi , Gerard M. McGeehan , Michael F. Kelley , Richard F. Labaudiniere , Litao Zhang , Robert D. Groneberg , Daniel G. McGarry , Thomas J. Caulfield , Anne Minnich , Mark Bobko
发明人： Zaid Jayyosi , Gerard M. McGeehan , Michael F. Kelley , Richard F. Labaudiniere , Litao Zhang , Robert D. Groneberg , Daniel G. McGarry , Thomas J. Caulfield , Anne Minnich , Mark Bobko
IPC分类号： A61K3147
CPC分类号： C07D403/12 , C07C59/66 , C07C59/68 , C07C65/24 , C07C69/94 , C07C233/11 , C07C235/06 , C07C235/34 , C07C311/51 , C07C323/12 , C07C323/52 , C07D209/18 , C07D209/34 , C07D213/643 , C07D215/12 , C07D215/14 , C07D215/18 , C07D215/233 , C07D215/38 , C07D215/60 , C07D217/04 , C07D231/56 , C07D239/90 , C07D241/44 , C07D257/04 , C07D263/32 , C07D307/81 , C07D333/28 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12 , Y10S514/824 , Y10S514/866 , Y10S514/884
摘要： The use of diaryl acid derivatives of formula (I) or pharmaceutically acceptable salts, N-oxides, hydrates or solvates thereof, wherein the variables shown are defined in the disclosure, and their pharmaceutical compositions as PPAR ligand receptor binders. The PPAR ligand receptor binders of this invention are useful as agonists or antagonists of the PPAR receptor.
摘要翻译： 使用式（I）的二芳基酸衍生物或其药学上可接受的盐，N-氧化物，水合物或溶剂化物，其中所示的变量在本公开内容中定义，其药物组合物作为PPAR配体受体结合剂。 本发明的PPAR配体受体结合物可用作PPAR受体的激动剂或拮抗剂。
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公开(公告)号：US08809538B2
公开(公告)日：2014-08-19
申请号：US13143998
申请日：2010-01-07
申请人： Martha E. Rodriguez , David A. Mareska , Jeremy J. Hans , Darren M. Harvey , Robert D. Groneberg , Michael O'Sullivan
发明人： Martha E. Rodriguez , David A. Mareska , Jeremy J. Hans , Darren M. Harvey , Robert D. Groneberg , Michael O'Sullivan
IPC分类号： C07D403/00 , C07D403/14 , A61K31/454 , A61K31/4545
CPC分类号： C07D413/14 , A61K31/445 , C07D401/12 , C07D401/14 , C07D409/06 , C07D409/14 , C07D413/06 , C07D417/14 , C07D471/04
摘要： A method for preventing and/or treating a metabolic disease, cerebrovascular disease, etc. which comprises administering to a mammal an effective amount of the compound of the formula (I): wherein all symbols have the same meanings as defined in the specification; a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof. And a novel compound of the formula (I-1): wherein all symbols have the same meanings as defined in the specification; a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof has an anti-diabetic effect and a neuroprotective effect. Accordingly, the compound of the formula (I) and the compound of the formula (I-1) are useful in a method for preventing and/or treating for a metabolic disease such as diabetes, cerebrovascular disease such as stroke, etc.
摘要翻译： 一种预防和/或治疗代谢性疾病，脑血管疾病等的方法，其包括向哺乳动物施用有效量的式（I）化合物：其中所有符号具有与说明书中定义的相同的含义; 其盐，其N-氧化物，其溶剂合物或其前药。 和式（I-1）的新化合物：其中所有符号具有与说明书中定义的相同的含义; 其盐，其N-氧化物，其溶剂化物或其前药具有抗糖尿病作用和神经保护作用。 因此，式（I）的化合物和式（I-1）的化合物可用于预防和/或治疗诸如糖尿病，脑血管疾病如中风等的代谢疾病的方法。
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