公开(公告)号：US08354408B2

公开(公告)日：2013-01-15

申请号：US12739704

申请日：2008-11-14

申请人： David Gerard Bourke ,  Christopher John Burns ,  Anthony Nicholas Cuzzupe ,  John Thomas Feutrill ,  Marcel Robert Kling ,  Tracy Leah Nero

发明人： David Gerard Bourke ,  Christopher John Burns ,  Anthony Nicholas Cuzzupe ,  John Thomas Feutrill ,  Marcel Robert Kling ,  Tracy Leah Nero

IPC分类号： A61K31/52 ,  A61K31/519 ,  A61P31/18 ,  C07D473/30 ,  C07D487/04

CPC分类号： C07D495/04 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

摘要： The present invention relates to N-containing heterocyclic compounds that are inhibitors of protein kinases including JAK kinases. In particular, the compounds are selective for JAK1, JAK2, JAK3 or TYK2 kinases and combinations thereof such as JAK1 and JAK2. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.

摘要翻译： 本发明涉及作为包括JAK激酶的蛋白激酶抑制剂的含氮杂环化合物。 特别地，这些化合物对JAK1，JAK2，JAK3或TYK2激酶及其组合如JAK1和JAK2是选择性的。 激酶抑制剂可用于治疗激酶相关疾病，例如免疫学和炎性疾病，包括器官移植物; 过度增生性疾病，包括癌症和骨髓增生性疾病; 病毒性疾病 代谢疾病; 和血管疾病。

公开(公告)号：US08846704B2

公开(公告)日：2014-09-30

申请号：US12524849

申请日：2008-01-31

申请人： David Gerard Bourke ,  Xianyong Bu ,  Christopher John Burns ,  Anthony Nicholas Cuzzupe ,  John Thomas Feutrill ,  Tracy Leah Nero ,  Beata Maria Blannin ,  Jun Zeng ,  Shaun Patrick Gaynor

发明人： David Gerard Bourke ,  Xianyong Bu ,  Christopher John Burns ,  Anthony Nicholas Cuzzupe ,  John Thomas Feutrill ,  Tracy Leah Nero ,  Beata Maria Blannin ,  Jun Zeng ,  Shaun Patrick Gaynor

IPC分类号： A01N43/54 ,  A61K31/505 ,  C07D239/02

CPC分类号： C07D413/12 ,  A61K31/505 ,  A61K31/506 ,  C07D239/38 ,  C07D239/47 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D487/00 ,  C07D487/02

摘要： The present invention relates to thiopyrimidine-based compounds that are inhibitors of protein kinases including JAK kinases. In particular, the compounds are selective for JAK1, JAK2 or JAK3 kinases and combinations thereof such as JAK1 and JAK2. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases and vascular diseases.

摘要翻译： 本发明涉及作为包括JAK激酶在内的蛋白激酶抑制剂的硫嘧啶类化合物。 特别地，这些化合物对JAK1，JAK2或JAK3激酶及其组合如JAK1和JAK2是选择性的。 激酶抑制剂可用于治疗激酶相关疾病，例如免疫学和炎性疾病，包括器官移植物; 过度增生性疾病，包括癌症和骨髓增生性疾病; 病毒性疾病 代谢疾病和血管疾病。

公开(公告)号：US20100239631A1

公开(公告)日：2010-09-23

申请号：US12524849

申请日：2008-01-31

申请人： David Gerard Bourke ,  Xianyong Bu ,  Christopher John Burns ,  Anthony Nicholas Cuzzupe ,  John Thomas Feutrill ,  Tracy Leah Nero ,  Beata Maria Blannin ,  Jun Zeng ,  Shaun Patrick Gaynor

发明人： David Gerard Bourke ,  Xianyong Bu ,  Christopher John Burns ,  Anthony Nicholas Cuzzupe ,  John Thomas Feutrill ,  Tracy Leah Nero ,  Beata Maria Blannin ,  Jun Zeng ,  Shaun Patrick Gaynor

IPC分类号： A61K9/00 ,  C07D239/28 ,  C07D239/24 ,  C07D413/06 ,  A61K31/495 ,  A61K31/505 ,  A61K31/5377 ,  A61P35/00 ,  A61P25/00 ,  A61P37/02

CPC分类号： C07D413/12 ,  A61K31/505 ,  A61K31/506 ,  C07D239/38 ,  C07D239/47 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D487/00 ,  C07D487/02

摘要： The present invention relates to thiopyrimidine-based compounds that are inhibitors of protein kinases including JAK kinases. In particular, the compounds are selective for JAK1, JAK2 or JAK3 kinases and combinations thereof such as JAK1 and JAK2. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases and vascular diseases.

摘要翻译： 本发明涉及作为包括JAK激酶在内的蛋白激酶抑制剂的硫嘧啶类化合物。 特别地，这些化合物对JAK1，JAK2或JAK3激酶及其组合如JAK1和JAK2是选择性的。 激酶抑制剂可用于治疗激酶相关疾病，例如免疫学和炎性疾病，包括器官移植物; 过度增生性疾病，包括癌症和骨髓增生性疾病; 病毒性疾病 代谢疾病和血管疾病。