公开(公告)号：EP1761540B1

公开(公告)日：2016-09-28

申请号：EP05752122.1

申请日：2005-05-12

申请人： ICOS CORPORATION

发明人： FOWLER, Kerry, W. ,  HUANG, Danwen ,  KESICKI, Edward, A. ,  OOI, Hua Chee ,  OLIVER, Amy, R. ,  RUAN, Fuqiang ,  TREIBERG, Jennifer ,  PURI, Kamal, Deep

IPC分类号： C07D487/04 ,  A61K31/517 ,  A61K31/519 ,  A61P37/00 ,  A61P29/00

CPC分类号： C07D473/34 ,  A61K31/52 ,  C07D239/91 ,  C07D473/16 ,  C07D487/04

摘要： Compounds that inhibit PI3K´ activity, including compounds that selectively inhibit PI3K´ activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K´) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3K´ plays a role in leukocyte function, using the compounds also are disclosed.

公开(公告)号：EP1438052A1

公开(公告)日：2004-07-21

申请号：EP02757407.8

申请日：2002-08-27

申请人： ICOS CORPORATION

发明人： SADHU, Chanchal ,  DICK, Kenneth, O. ,  TREIBERG, Jennifer ,  SOWELL, C., Gregory ,  KESICKI, Edward, A. ,  OLIVER, Amy

IPC分类号： A61K31/505 ,  A61K31/53 ,  C07D473/34 ,  C07D473/38 ,  C07D473/24 ,  C07D473/16 ,  C07D473/00 ,  C07D473/40 ,  C07D403/12 ,  C07D487/04

CPC分类号： A61K31/506 ,  C07D403/12 ,  C07D473/00 ,  C07D473/16 ,  C07D473/24 ,  C07D473/30 ,  C07D473/32 ,  C07D473/34 ,  C07D473/38 ,  C07D473/40 ,  C07D487/04 ,  C12N9/1205 ,  C12N9/99 ,  C12Y207/01137

摘要： Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kdelta) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kdelta plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3Kdelta, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3Kdelta activity, including compounds that selectively inhibit PI3Kdelta activity. Methods of using PI3Kdelta inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3Kdelta inhibitory compounds to inhibit PI3Kdelta-mediated processes in vitro and in vivo.

公开(公告)号：EP3943494A1

公开(公告)日：2022-01-26

申请号：EP21169213.2

申请日：2005-05-12

申请人： ICOS CORPORATION

发明人： FOWLER, Kerry, W. ,  HUANG, Danwen ,  KESICKI, Edward, A. ,  OOI, Hua Chee ,  OLIVER, Amy R. ,  RUAN, Fuqiang ,  TREIBERG, Jennifer ,  PURI, Kamal, Deep

IPC分类号： C07D473/34 ,  C07D239/91

摘要： Compounds that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3Kδ plays a role in leukocyte function, using the compounds also are disclosed.

公开(公告)号：EP1869020B1

公开(公告)日：2010-12-01

申请号：EP06748900.5

申请日：2006-03-29

申请人： ICOS Corporation

发明人： DIAZ, Frank ,  FAROUZ, Francine, S. ,  HOLCOMB, Ryan ,  KESICKI, Edward, A. ,  OOI, Hua, Chee ,  RUDOLPH, Alexander ,  STAPPENBECK, Frank ,  THORSETT, Eugene ,  GAUDINO, John, Joseph ,  FISHER, Kimba, L. ,  COOK, Adam, Wade

IPC分类号： C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  A61K31/497 ,  A61K31/5355 ,  A61K31/541 ,  A61P35/00

CPC分类号： C07D413/12 ,  C07D403/12 ,  C07D417/12

摘要： Substituted urea compounds useful in the treatment of diseases and conditions related to DNA damage or lesions in DNA replication are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating cancer and other diseases characterized by defects in DNA replication, chromosome segregation, or cell division, also are disclosed.

摘要翻译： 公开了可用于治疗与DNA复制中的DNA损伤或病变有关的疾病和病症的取代脲化合物。 还公开了制备这些化合物的方法以及它们作为治疗剂的用途，例如用于治疗癌症和其他以DNA复制，染色体分离或细胞分裂缺陷为特征的疾病。

公开(公告)号：EP1242400B1

公开(公告)日：2006-05-03

申请号：EP00987999.0

申请日：2000-11-28

申请人： ICOS Corporation

发明人： MARTINS, Timothy, J. ,  FOWLER, Kerry, W. ,  ODINGO, Joshua ,  KESICKI, Edward, A. ,  OLIVER, Amy ,  BURGESS, Laurence, E. ,  GAUDINO, John, J. ,  JONES, Zachary, S. ,  NEWHOUSE, Bradley, J. ,  SCHLACHTER, Stephen

IPC分类号： C07D295/20 ,  C07D295/18 ,  C07D417/06 ,  C07D401/12 ,  C07D295/14 ,  C07D405/06 ,  C07D401/04 ,  C07D417/12 ,  C07D403/12 ,  C07D401/06 ,  C07D407/12 ,  C07D413/12 ,  C07D407/06 ,  C07D409/12 ,  A61K31/40

CPC分类号： C07D207/08 ,  A61K31/40 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/06 ,  C07D417/12 ,  Y02A50/411

摘要： Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.

公开(公告)号：EP1379510B1

公开(公告)日：2011-06-01

申请号：EP02728396.9

申请日：2002-03-01

申请人： ICOS Corporation

发明人： KEEGAN, Kathleen, S. ,  KESICKI, Edward, A. ,  GAUDINO, John, Joseph ,  COOK, Adam Wade ,  COWEN, Scott, Douglas ,  BURGESS, Laurence, Edward

IPC分类号： C07D241/20 ,  C07D401/12 ,  C07D403/12 ,  C07D241/54 ,  A61K31/4965 ,  A61K31/498 ,  A61P35/00 ,  C07D405/12 ,  C07D251/22 ,  C07D231/40 ,  C07D239/46 ,  C07D253/06 ,  C07D239/42 ,  C07D257/06 ,  C07D213/75 ,  C07D277/48

CPC分类号： A61K45/06 ,  A61K31/4965 ,  A61K31/498 ,  C07D213/30 ,  C07D213/40 ,  C07D213/75 ,  C07D213/77 ,  C07D215/34 ,  C07D231/12 ,  C07D231/40 ,  C07D233/56 ,  C07D239/42 ,  C07D239/47 ,  C07D241/12 ,  C07D241/20 ,  C07D241/44 ,  C07D249/08 ,  C07D251/22 ,  C07D253/07 ,  C07D257/06 ,  C07D277/48 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D453/02 ,  A61K2300/00

摘要： Aryl- and heteroaryl substituted urea compounds useful in the treatment of diseases and conditions related to DNA damage or lesions in DNA replication are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating cancer and other diseases characterized by defects in DNA replication, chromosome segregation, or cell division also are disclosed. Wherein W' is a six-membered aromatic ring containing at least 2 introgen atoms and optionally substitutedas defined in the claims, Z' is a five- or six membered aromatic or heteraromatic ring as defined in the claims, Y' is O or S.

公开(公告)号：EP1761540A1

公开(公告)日：2007-03-14

申请号：EP05752122.1

申请日：2005-05-12

申请人： ICOS CORPORATION

发明人： FOWLER, Kerry, W. ,  HUANG, Danwen ,  KESICKI, Edward, A. ,  OOI, Hua Chee ,  OLIVER, Amy, R. ,  RUAN, Fuqiang ,  TREIBERG, Jennifer ,  PURI, Kamal, Deep

IPC分类号： C07D487/04 ,  A61K31/517 ,  A61K31/519 ,  A61P37/00 ,  A61P29/00

CPC分类号： C07D473/34 ,  A61K31/52 ,  C07D239/91 ,  C07D473/16 ,  C07D487/04

摘要： Compounds that inhibit PI3K´ activity, including compounds that selectively inhibit PI3K´ activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K´) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3K´ plays a role in leukocyte function, using the compounds also are disclosed.

摘要翻译： 公开了抑制PI3K活性的化合物，包括选择性抑制PI3K活性的化合物。 公开了抑制磷脂酰肌醇3-激酶δ同种型（PI3K'）活性的方法，以及使用该化合物治疗PI3K'在白细胞功能中起作用的免疫力和炎症疾病等疾病的方法。

公开(公告)号：EP1242400A1

公开(公告)日：2002-09-25

申请号：EP00987999.0

申请日：2000-11-28

申请人： ICOS CORPORATION

发明人： MARTINS, Timothy, J. ,  FOWLER, Kerry, W. ,  ODINGO, Joshua ,  KESICKI, Edward, A. ,  OLIVER, Amy ,  BURGESS, Laurence, E. ,  GAUDINO, John, J. ,  JONES, Zachary, S. ,  NEWHOUSE, Bradley, J. ,  SCHLACHTER, Stephen

IPC分类号： C07D295/20 ,  C07D295/18 ,  C07D417/06 ,  C07D401/12 ,  C07D295/14 ,  C07D405/06 ,  C07D401/04 ,  C07D417/12 ,  C07D403/12 ,  C07D401/06 ,  C07D407/12 ,  C07D413/12 ,  C07D407/06 ,  C07D409/12 ,  A61K31/40

CPC分类号： C07D207/08 ,  A61K31/40 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/06 ,  C07D417/12 ,  Y02A50/411

摘要： Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.

公开(公告)号：EP1278748B1

公开(公告)日：2011-03-23

申请号：EP01928855.4

申请日：2001-04-24

申请人： ICOS Corporation

发明人： SADHU, Chanchal ,  DICK, Ken ,  TREIBERG, Jennifer ,  SOWELL, C., Gregory ,  KESICKI, Edward, A. ,  OLIVER, Amy

IPC分类号： C07D473/38 ,  C07D473/34 ,  C07D473/00 ,  C07D473/24 ,  C07D473/16 ,  C07D473/40 ,  C07D473/30 ,  C07D403/12 ,  C07D487/04 ,  A61K31/517 ,  A61K31/52 ,  A61P7/00 ,  A61P29/00 ,  A61P19/10

CPC分类号： C07D473/00 ,  C07D403/12 ,  C07D473/16 ,  C07D473/24 ,  C07D473/30 ,  C07D473/34 ,  C07D473/38 ,  C07D473/40 ,  C07D487/04

摘要： Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3Kδ, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity. Methods of using PI3Kδ inhibitory compound s to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3Kδ inhibitory compounds to inhibit PI3Kδ-mediated processes in vitro and in vivo.

公开(公告)号：EP2220089A2

公开(公告)日：2010-08-25

申请号：EP08850176.2

申请日：2008-11-12

申请人： ICOS CORPORATION

发明人： WHITE, Stephen, L. ,  RUAN, Fuqiang ,  KESICKI, Edward, A. ,  THORSETT, Eugene ,  FAROUZ, Francine

IPC分类号： C07D487/04 ,  C07D487/02 ,  C07D403/08 ,  C07D403/12

CPC分类号： C07D519/00

摘要： Compounds that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3Kδ plays a role in leukocyte function, using the compounds also are disclosed.