公开(公告)号：WO2009109576A1

公开(公告)日：2009-09-11

申请号：PCT/EP2009/052506

申请日：2009-03-03

申请人： NOVARTIS AG ,  BURGER, Matthew ,  LAN, Jiong ,  LINDVALL, Mika ,  NISHIGUCHI, Gisele ,  TETALMAN, Michelle

发明人： BURGER, Matthew ,  LAN, Jiong ,  LINDVALL, Mika ,  NISHIGUCHI, Gisele ,  TETALMAN, Michelle

IPC分类号： C07D417/12 ,  C07D417/14 ,  A61K31/4439 ,  A61P35/00

CPC分类号： C07D417/12 ,  C07D417/14

摘要： The present invention relates to new compounds of Formulas (I) and (II), their tautomers, stereoisomers and polymorphs, and pharmaceutically acceptable salts, esters, metabolites or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the inhibition of Pirn kinase activity and/or the prophylaxis or treatment of cancer.

摘要翻译： 本发明涉及式（I）和（II）的新化合物，其互变异构体，立体异构体和多晶型物及其药学上可接受的盐，酯，代谢物或前药，新化合物与药学上可接受的载体的组合物，以及 新化合物单独或与至少一种另外的治疗剂联合用于抑制皮激素活性和/或预防或治疗癌症。

公开(公告)号：WO2008138889A8

公开(公告)日：2009-07-09

申请号：PCT/EP2008055751

申请日：2008-05-09

申请人： NOVARTIS AG ,  CAPRARO HANS-GEORG ,  CARAVATTI GIORGIO ,  FURET PASCAL ,  IMBACH PATRICIA ,  LAN JIONG ,  PECCHI SABINA ,  SCHOEPFER JOSEPH

发明人： CAPRARO HANS-GEORG ,  CARAVATTI GIORGIO ,  FURET PASCAL ,  IMBACH PATRICIA ,  LAN JIONG ,  PECCHI SABINA ,  SCHOEPFER JOSEPH

IPC分类号： A61K31/519 ,  A61K31/5025 ,  A61P11/00 ,  A61P11/06 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  C07D487/04

CPC分类号： C07D487/04

摘要： The present invention relates to compounds are of the formula I, processes for the preparation thereof, more generally these compounds for use in the treatment of the human or animal body, in the treatment of an inflammatory or obstructive airway disease, disorders commonly occurring in connection with transplantation, or a proliferative disease, which disease responds to an inhibition of kinases of the PI3-kinase-related protein kinase family.

摘要翻译： 本发明涉及式I化合物，其制备方法，更一般地，这些化合物用于治疗人体或动物体，用于治疗炎性或阻塞性气道疾病，连接中常见的病症 与移植或增殖性疾病相关，所述疾病对抑制PI3-激酶相关蛋白激酶家族的激酶起反应。

公开(公告)号：WO2006089076A2

公开(公告)日：2006-08-24

申请号：PCT/US2006005562

申请日：2006-02-16

申请人： NEUROGEN CORP ,  PRINGLE WALLACE C ,  PETERSON JOHN M ,  XIE LINGHONG ,  GE PING ,  GAO YANG ,  OCHTERSKI JOSEPH W ,  LAN JIONG

发明人： PRINGLE WALLACE C ,  PETERSON JOHN M ,  XIE LINGHONG ,  GE PING ,  GAO YANG ,  OCHTERSKI JOSEPH W ,  LAN JIONG

IPC分类号： A61K31/426

CPC分类号： C07D231/14 ,  C07D233/64 ,  C07D233/90 ,  C07D277/28 ,  C07D277/30 ,  C07D401/06 ,  C07D403/06 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D451/04 ,  C07D471/04

摘要： Thiazole amides, imidazole amides and related analogues of the Formula: are provided, in which variables are as described herein. Such compounds may be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) and other disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).

摘要翻译： 提供噻唑酰胺，咪唑酰胺和式的相关类似物：其中变量如本文所述。 这样的化合物可用于在体内或体外调节配体与组胺H3受体的结合，并且特别可用于治疗人，家养伴侣动物和家畜中的各种中枢神经系统（CNS）和其他疾病。 本文提供的化合物可以单独施用或与一种或多种其它CNS剂组合施用，以增强其它CNS剂的作用。 提供了用于治疗这种病症的药物组合物和方法，以及使用这种配体检测组胺H3受体的方法（例如受体定位研究）。

公开(公告)号：WO2008138889A3

公开(公告)日：2009-04-30

申请号：PCT/EP2008055751

申请日：2008-05-09

申请人： NOVARTIS AG ,  CAPRARO HANS-GEORG ,  CARAVATTI GIORGIO ,  FURET PASCAL ,  IMBACH PATRICIA ,  LAN JIONG ,  PECCHI SABINA ,  SCHOEPFER JOSEPH

发明人： CAPRARO HANS-GEORG ,  CARAVATTI GIORGIO ,  FURET PASCAL ,  IMBACH PATRICIA ,  LAN JIONG ,  PECCHI SABINA ,  SCHOEPFER JOSEPH

IPC分类号： A61K31/519 ,  A61K31/5025 ,  A61P11/00 ,  A61P11/06 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  C07D487/04

CPC分类号： C07D487/04

摘要： The present invention relates to compounds are of the formula I, processes for the preparation thereof, more generally these compounds for use in the treatment of the human or animal body, in the treatment of an inflammatory or obstructive airway disease, disorders commonly occurring in connection with transplantation, or a proliferative disease, which disease responds to an inhibition of kinases of the PI3-kinase-related protein kinase family.

摘要翻译： 本发明涉及式I化合物，其制备方法，更一般地，这些用于治疗人或动物体的化合物，用于治疗炎性或阻塞性气道疾病，通常在连接中发生的疾病 移植或增殖性疾病，该疾病对PI3激酶相关蛋白激酶家族的激酶的抑制作出反应。

公开(公告)号：WO2008138889A2

公开(公告)日：2008-11-20

申请号：PCT/EP2008/055751

申请日：2008-05-09

申请人： NOVARTIS AG ,  CAPRARO, Hans-Georg ,  CARAVATTI, Giorgio ,  FURET, Pascal ,  IMBACH, Patricia ,  LAN, Jiong ,  PECCHI, Sabina ,  SCHOEPFER, Joseph

发明人： CAPRARO, Hans-Georg ,  CARAVATTI, Giorgio ,  FURET, Pascal ,  IMBACH, Patricia ,  LAN, Jiong ,  PECCHI, Sabina ,  SCHOEPFER, Joseph

IPC分类号： A61K31/5025 ,  A61K31/519 ,  A61P29/00 ,  A61P37/00 ,  A61P35/00 ,  A61P11/00 ,  A61P11/06 ,  C07D487/04

CPC分类号： C07D487/04

摘要： The present invention relates to compounds are of the formula I, processes for the preparation thereof, more generally these compounds for use in the treatment of the human or animal body, in the treatment of an inflammatory or obstructive airway disease, disorders commonly occurring in connection with transplantation, or a proliferative disease, which disease responds to an inhibition of kinases of the PI3-kinase-related protein kinase family.

摘要翻译： 本发明涉及式I化合物，其制备方法，更一般地，这些用于治疗人或动物体的化合物，用于治疗炎性或阻塞性气道疾病，通常在连接中发生的疾病 移植或增殖性疾病，该疾病对PI3激酶相关蛋白激酶家族的激酶的抑制作出反应。

公开(公告)号：WO2008106692B1

公开(公告)日：2008-10-30

申请号：PCT/US2008055724

申请日：2008-03-03

申请人： NOVARTIS VACCINES & DIAGNOSTIC ,  BURGER MATTHEW ,  LINDVALL MIKA ,  HAN WOOSEOK ,  LAN JIONG ,  NISHIGUCHI GISELE ,  SHAFER CYNTHIA ,  BELLAMACINA CORNELIA ,  HUH KAY ,  ATALLAH GORDANA ,  MCBRIDE CHRISTOPHER ,  ANTONIOS-MCCREA WILLIAM JR ,  ZAVOROTINSKAYA TATIANA ,  WALTER ANNETTE ,  GARCIA PABLO

发明人： BURGER MATTHEW ,  LINDVALL MIKA ,  HAN WOOSEOK ,  LAN JIONG ,  NISHIGUCHI GISELE ,  SHAFER CYNTHIA ,  BELLAMACINA CORNELIA ,  HUH KAY ,  ATALLAH GORDANA ,  MCBRIDE CHRISTOPHER ,  ANTONIOS-MCCREA WILLIAM JR ,  ZAVOROTINSKAYA TATIANA ,  WALTER ANNETTE ,  GARCIA PABLO

IPC分类号： C07D213/78 ,  A61K31/44 ,  A61P35/00 ,  C07D239/28 ,  C07D401/12

CPC分类号： C07D401/12 ,  C07D213/78 ,  C07D239/28

摘要： New compounds, compositions and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase- mediated disorder, such as cancer.

摘要翻译： 提供了在人或动物受试者中抑制与肿瘤发生相关的激酶活性的新化合物，组合物和方法。 在某些实施方案中，化合物和组合物有效地抑制至少一种丝氨酸/苏氨酸激酶或受体酪氨酸激酶的活性。 新化合物和组合物可以单独使用或与至少一种另外的药物组合使用，用于治疗丝氨酸/苏氨酸激酶或受体酪氨酸激酶介导的病症，例如癌症。

公开(公告)号：WO2007095588A1

公开(公告)日：2007-08-23

申请号：PCT/US2007/062157

申请日：2007-02-14

申请人： NOVARTIS AG ,  NI, Zhi-jie ,  PECCHI, Sabina ,  BURGER, Matthew ,  HAN, Wooseok ,  SMITH, Aaron ,  ATALLAH, Gordana ,  BARTULIS, Sarah ,  FRAZIER, Kelly ,  VERHAGEN, Joelle ,  ZHANG, Yanchen ,  IWANOWICZ, Ed ,  HENDRICKSON, Tom ,  KNAPP, Mark ,  MERRITT, Hanne ,  VOLIVA, Charles ,  WIESMANN, Marion ,  LEGRAND, Darren Mark ,  BRUCE, Ian ,  DALE, James ,  LAN, Jiong ,  LEVINE, Barry ,  COSTALES, Abran ,  LIU, Jie ,  PICK, Teresa ,  MENEZES, Daniel

发明人： NI, Zhi-jie ,  PECCHI, Sabina ,  BURGER, Matthew ,  HAN, Wooseok ,  SMITH, Aaron ,  ATALLAH, Gordana ,  BARTULIS, Sarah ,  FRAZIER, Kelly ,  VERHAGEN, Joelle ,  ZHANG, Yanchen ,  IWANOWICZ, Ed ,  HENDRICKSON, Tom ,  KNAPP, Mark ,  MERRITT, Hanne ,  VOLIVA, Charles ,  WIESMANN, Marion ,  LEGRAND, Darren Mark ,  BRUCE, Ian ,  DALE, James ,  LAN, Jiong ,  LEVINE, Barry ,  COSTALES, Abran ,  LIU, Jie ,  PICK, Teresa ,  MENEZES, Daniel

IPC分类号： C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  A61K31/437 ,  A61K31/5025 ,  A61K31/428 ,  A61P35/00

CPC分类号： C07D487/04 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04

摘要： Phosphatidylinositol (PI) 3 kinase inhibitor compounds, their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, phospholipid kinases, G-protein coupled receptors, and phosphatases.

摘要翻译： 磷脂酰肌醇（PI）3激酶抑制剂化合物，其药学上可接受的盐和前药; 单独或与至少一种另外的治疗剂组合的新化合物与药学上可接受的载体的组合物; 以及单独或与至少一种另外的治疗剂联合使用的新化合物在预防或治疗以生长因子，蛋白丝氨酸/苏氨酸激酶，磷脂激酶，G蛋白偶联的异常活性为特征的增殖性疾病中的用途 受体和磷酸酶。

公开(公告)号：WO2006089076A3

公开(公告)日：2006-08-24

申请号：PCT/US2006/005562

申请日：2006-02-16

申请人： NEUROGEN CORPORATION ,  PRINGLE, Wallace C. ,  PETERSON, John M. ,  XIE, Linghong ,  GE, Ping ,  GAO, Yang ,  OCHTERSKI, Joseph W. ,  LAN, Jiong

发明人： PRINGLE, Wallace C. ,  PETERSON, John M. ,  XIE, Linghong ,  GE, Ping ,  GAO, Yang ,  OCHTERSKI, Joseph W. ,  LAN, Jiong

IPC分类号： A61K31/426 ,  C07D277/24 ,  C07D277/28

摘要： Thiazole amides, imidazole amides and related analogues of the Formula: are provided, in which variables are as described herein. Such compounds may be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro , and are particularly useful in the treatment of a variety of central nervous system (CNS) and other disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting histamine H3 receptors ( e.g ., receptor localization studies).

公开(公告)号：WO2005063766A3

公开(公告)日：2005-09-09

申请号：PCT/US2004043682

申请日：2004-12-23

申请人： NOVARTIS PHARMA AG ,  DONG QING ,  WANG JIANQIANG ,  LAN JIONG ,  LANG HENGYUAN

发明人： DONG QING ,  WANG JIANQIANG ,  LAN JIONG ,  LANG HENGYUAN

IPC分类号： C07D473/00 ,  C07D487/04 ,  A61K31/437 ,  A61P29/00

CPC分类号： C07D473/00 ,  C07D473/28 ,  C07D473/30 ,  C07D473/34 ,  C07D487/04

摘要： Provided are bicyclic heterocycle-based p38 kinase, including p38alpha and p38beta kinase, inhibitors. Pharmaceutical compositions containing the compounds are also provided. Methods of use of the compounds and compositions are also provided, including methods of treatment, prevention, or amehoration of one or more symptoms of p38 kinase mediated diseases and disorders, including, but not limited to, inflammatory diseases and disorders.

摘要翻译： 提供了基于双环杂环的p38激酶，包括p38α和p38β激酶抑制剂。 还提供了含有这些化合物的药物组合物。 还提供了使用所述化合物和组合物的方法，包括治疗，预防，或p38激酶介导的疾病和病症，包括的一种或多种症状的amehoration方法，但不限于，炎性疾病和病症。

公开(公告)号：WO2005063766A2

公开(公告)日：2005-07-14

申请号：PCT/US2004/043682

申请日：2004-12-23

申请人： TRIAD THERAPEUTICS, INC. ,  DONG, Qing ,  WANG, Jianqiang ,  LAN, Jiong ,  LANG, Hengyuan

发明人： DONG, Qing ,  WANG, Jianqiang ,  LAN, Jiong ,  LANG, Hengyuan

IPC分类号： C07D487/04

CPC分类号： C07D473/00 ,  C07D473/28 ,  C07D473/30 ,  C07D473/34 ,  C07D487/04

摘要： Provided are bicyclic heterocycle-based p38 kinase, including p38α and p38β kinase, inhibitors. Pharmaceutical compositions containing the compounds are also provided. Methods of use of the compounds and compositions are also provided, including methods of treatment, prevention, or amehoration of one or more symptoms of p38 kinase mediated diseases and disorders, including, but not limited to, inflammatory diseases and disorders.

摘要翻译： 提供基于双环杂环的p38激酶，包括p38alpha和p38beta激酶抑制剂。 还提供了含有这些化合物的药物组合物。 还提供了使用化合物和组合物的方法，包括治疗，预防或发生p38激酶介导的疾病和病症的一种或多种症状的方法，包括但不限于炎性疾病和病症。