公开(公告)号：US08329737B2

公开(公告)日：2012-12-11

申请号：US12895548

申请日：2010-09-30

申请人： Michelle Leanne Styles ,  Jun Zeng ,  Herbert Rudolf Treutlein ,  Andrew Frederick Wilks ,  Marcel Robert Kling ,  Xianyong Bu ,  Christopher John Burns

发明人： Michelle Leanne Styles ,  Jun Zeng ,  Herbert Rudolf Treutlein ,  Andrew Frederick Wilks ,  Marcel Robert Kling ,  Xianyong Bu ,  Christopher John Burns

IPC分类号： A61K31/415

CPC分类号： C07D403/04 ,  C07D235/30 ,  C07D241/20 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12

摘要： A compound of the general formula (I) or pharmaceutically acceptable prodrugs, salts, hydrates, solvates, crystal forms or diastereomers thereof, wherein A represents a variety of six membered nitrogen containing heterocyclic rings, Q is a bond, halogen, C1-4 alkyl, O, S, SO2, CO or CS and X1, X2, X3 and X4 are optionally substituted by 9 specific substituents or one can be nitrogen. Compositions comprising a carrier and at least one compound of formula (I) are also provided. Further provided are methods of treating tyrosine kinase-associated disease states by administering a compound of formula (I) and methods of suppressing the immune system of a subject by administering a compound of formula (I).

摘要翻译： 通式（I）的化合物或其药学上可接受的前药，盐，水合物，溶剂合物，结晶形式或非对映异构体，其中A代表多种六元含氮杂环，Q为键，卤素，C 1-4烷基 ，O，S，SO 2，CO或CS，X 1，X 2，X 3和X 4任选被9个特定取代基取代，或者可以是氮。 还提供了包含载体和至少一种式（I）化合物的组合物。 还提供了通过施用式（I）化合物和通过施用式（I）化合物来抑制受试者的免疫系统的方法来治疗酪氨酸激酶相关疾病状态的方法。

公开(公告)号：US20080207613A1

公开(公告)日：2008-08-28

申请号：US10585916

申请日：2005-01-12

申请人： Michelle Leanne Styles ,  Jun Zeng ,  Herbert Rudolf Treutlein ,  Andrew Frederick Wilks ,  Marcel Robert Kling ,  Christopher John Burns ,  Xianyong Bu

发明人： Michelle Leanne Styles ,  Jun Zeng ,  Herbert Rudolf Treutlein ,  Andrew Frederick Wilks ,  Marcel Robert Kling ,  Christopher John Burns ,  Xianyong Bu

IPC分类号： A61K31/5377 ,  C07D403/04 ,  C07D403/14 ,  C07D401/04 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  A61P37/06 ,  C07D401/14 ,  C07D235/04 ,  A61K31/497 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/4184

CPC分类号： C07D403/04 ,  C07D235/30 ,  C07D241/20 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12

摘要： A compound of the general formula (I) or pharmaceutically acceptable prodrugs, salts, hydrates, solvates, crystal forms or diastereomers thereof, wherein A represents a variety of six membered nitrogen containing heterocyclic rings, Q is a bond, halogen, C1-4 alkyl, O, S, SO2, CO or CS and X1, X2, X3 and X4 are optionally substituted by 9 specific substituents or one can be nitrogen. Compositions comprising a carrier and at least one compound of formula (I) are also provided. Further provided are methods of treating tyrosine kinase-associated disease states by administering a compound of formula (I) and methods of suppressing the immune system of a subject by administering a compound of formula (I).

摘要翻译： 通式（I）的化合物或其药学上可接受的前药，盐，水合物，溶剂合物，结晶形式或非对映异构体，其中A表示多种六元含氮杂环，Q为键，卤素， 1-4烷基，O，S，SO 2，CO或CS和X 1，X 2，X _{3和X 4任选被9个特定取代基取代，或者可以是氮。 还提供了包含载体和至少一种式（I）化合物的组合物。 还提供了通过施用式（I）化合物和通过施用式（I）化合物来抑制受试者的免疫系统的方法来治疗酪氨酸激酶相关疾病状态的方法。}

公开(公告)号：US07593820B2

公开(公告)日：2009-09-22

申请号：US11248478

申请日：2005-10-11

申请人： Andrew Frederick Wilks ,  Christopher John Burns ,  Emmanuelle Fantino ,  Isabelle Lucet ,  Jamie Rossjohn ,  Michelle Leanne Styles

发明人： Andrew Frederick Wilks ,  Christopher John Burns ,  Emmanuelle Fantino ,  Isabelle Lucet ,  Jamie Rossjohn ,  Michelle Leanne Styles

IPC分类号： G01N31/00 ,  C12N9/12 ,  G06G7/58

CPC分类号： C07D491/04 ,  C07D471/04 ,  C07K2299/00 ,  C12N9/1205 ,  Y02A90/26

摘要： The present invention relates to X-ray crystallography studies of a human Janus Kinase 2 (JAK2) domain. More particularly, it relates to the crystal structure of a JAK2 kinase domain bound to a inhibitor. The invention further relates to the use of the crystal and related structural information to select and screen for compounds that interact with JAK2 and related proteins and to compounds that could be used for the treatment of diseases mediated by inappropriate JAK2 activity.

摘要翻译： 本发明涉及人类Janus Kinase 2（JAK2）结构域的X射线晶体学研究。 更具体地，涉及与抑制剂结合的JAK2激酶结构域的晶体结构。 本发明还涉及晶体和相关结构信息用于选择和筛选与JAK2和相关蛋白相互作用的化合物以及可用于治疗由不适当的JAK2活性介导的疾病的化合物。