公开(公告)号：US20110098274A1

公开(公告)日：2011-04-28

申请号：US12986951

申请日：2011-01-07

申请人： Dane Goff ,  Jing Zhang ,  Rajinder Singh ,  Sacha Holland ,  Jiaxin Yu ,  Thilo J. Heckrodt ,  Pingyu Ding ,  Joane Litvak

发明人： Dane Goff ,  Jing Zhang ,  Rajinder Singh ,  Sacha Holland ,  Jiaxin Yu ,  Thilo J. Heckrodt ,  Pingyu Ding ,  Joane Litvak

IPC分类号： A61K31/55 ,  C07D249/14 ,  C07D237/26 ,  C07D223/18 ,  C07D285/36 ,  A61K31/4196 ,  A61K31/502 ,  A61P35/00

CPC分类号： C07D401/14 ,  A61K31/502 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D417/04 ,  C07D417/14 ,  C07D451/04 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D491/04 ,  C07D491/20 ,  C07D495/04 ,  C07D519/00

摘要： Polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.

公开(公告)号：US20110071133A1

公开(公告)日：2011-03-24

申请号：US12957822

申请日：2010-12-01

申请人： Dane Goff ,  Jing Zhang ,  Rajinder Singh ,  Sacha Holland ,  Jiaxin Yu ,  Pingyu Ding ,  Thilo J. Heckrodt ,  Joane Litvak

发明人： Dane Goff ,  Jing Zhang ,  Rajinder Singh ,  Sacha Holland ,  Jiaxin Yu ,  Pingyu Ding ,  Thilo J. Heckrodt ,  Joane Litvak

IPC分类号： A61K31/551 ,  A61K31/502 ,  A61K31/496 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/55 ,  A61P29/00 ,  A61P9/00 ,  A61P17/06 ,  A61P19/10 ,  A61P35/00 ,  A61P13/12

CPC分类号： A61K31/519 ,  A61K31/395 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D417/14 ,  C07D495/04

摘要： Bicyclic aryl substituted triazoles or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.

摘要翻译： 公开了双环芳基取代的三唑或杂芳基取代的三唑和含有这些化合物的药物组合物可用于抑制受体蛋白酪氨酸激酶Ax1的活性。 还公开了使用该化合物治疗与Axl活性相关的疾病或病症的方法。

公开(公告)号：US20080188455A1

公开(公告)日：2008-08-07

申请号：US11967172

申请日：2007-12-29

申请人： Dane Goff ,  Jing Zhang ,  Rajinder Singh ,  Sacha Holland ,  Jiaxin Yu ,  Thilo J. Heckrodt ,  Pingyu Ding ,  Joane Litvak

发明人： Dane Goff ,  Jing Zhang ,  Rajinder Singh ,  Sacha Holland ,  Jiaxin Yu ,  Thilo J. Heckrodt ,  Pingyu Ding ,  Joane Litvak

IPC分类号： A61K31/4355 ,  C07D249/14 ,  C07D491/113 ,  A61K31/554 ,  A61P19/02 ,  A61P35/02 ,  A61P35/00 ,  A61P17/06 ,  C07D285/36 ,  A61K31/4196

CPC分类号： C07D401/14 ,  A61K31/502 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D417/04 ,  C07D417/14 ,  C07D451/04 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D491/04 ,  C07D491/20 ,  C07D495/04 ,  C07D519/00

摘要： Polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.

摘要翻译： 公开了多环杂芳基取代的三唑和含有这些化合物的药物组合物可用于抑制受体蛋白酪氨酸激酶Ax1的活性。 还公开了使用该化合物治疗与Axl活性相关的疾病或病症的方法。

公开(公告)号：US20080188454A1

公开(公告)日：2008-08-07

申请号：US11966585

申请日：2007-12-28

申请人： Dane Goff ,  Jing Zhang ,  Rajinder Singh ,  Sacha Holland ,  Jiaxin Yu ,  Pingyu Ding ,  Thilo J. Heckrodt ,  Joane Litvak

发明人： Dane Goff ,  Jing Zhang ,  Rajinder Singh ,  Sacha Holland ,  Jiaxin Yu ,  Pingyu Ding ,  Thilo J. Heckrodt ,  Joane Litvak

IPC分类号： A61K31/496 ,  C07D239/70 ,  A61K31/55 ,  A61P35/00 ,  A61P35/02 ,  A61K31/397 ,  C07D403/14

CPC分类号： A61K31/519 ,  A61K31/395 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D417/14 ,  C07D495/04

摘要： Bicyclic aryl substituted triazoles or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.

摘要翻译： 公开了双环芳基取代的三唑或杂芳基取代的三唑和含有这些化合物的药物组合物可用于抑制受体蛋白酪氨酸激酶Ax1的活性。 还公开了使用该化合物治疗与Axl活性相关的疾病或病症的方法。

公开(公告)号：US10710983B2

公开(公告)日：2020-07-14

申请号：US15633258

申请日：2017-06-26

申请人： Yan Chen ,  Rose Yen ,  Jiaxin Yu ,  Vanessa Taylor ,  Rajinder Singh

发明人： Yan Chen ,  Rose Yen ,  Jiaxin Yu ,  Vanessa Taylor ,  Rajinder Singh

IPC分类号： C07D401/14 ,  C07D403/12 ,  C07D239/48 ,  C07D405/14

摘要： Compounds within the scope of the present invention have a Formula 1 or a salt or prodrug thereof, where ring A is selected from cycloaliphatic; ring B is aryl; R1 is selected from (C1-C10)alkyl, (C3-C10)cycloalkyl, halo, aryl, and heteroaryl; and R2 and R3 are independently selected from hydrogen and (C1-C6)alkyl. Disclosed compounds may have an IRAK4 IC50 of from 0.003 μM to 3.7 μM; a TAK1 IC50 of from 0.008 μM to 132 μM; and/or an IRAK4/TAK1 selectivity of from 1 to 450. Particular compounds may have an IRAK4/TAK1 selectivity of from 100 to 500. Disclosed compositions may be formulated as pharmaceutical compositions. A method for using the compounds and/or compositions also are disclosed. The method may comprise administering to a subject an effective amount of a compound within the scope of the present invention, particularly to selectively inhibit IRAK 1 and/or IRAK4 over TAK1.

公开(公告)号：US08809364B2

公开(公告)日：2014-08-19

申请号：US13078759

申请日：2011-04-01

申请人： Rajinder Singh ,  Dane Goff ,  Jiaxin Yu ,  Sacha Holland ,  Thilo J. Heckrodt ,  Pingyu Ding ,  Joane Litvak ,  Jing Zhang

发明人： Rajinder Singh ,  Dane Goff ,  Jiaxin Yu ,  Sacha Holland ,  Thilo J. Heckrodt ,  Pingyu Ding ,  Joane Litvak ,  Jing Zhang

IPC分类号： A61K31/4439 ,  A61K31/4375 ,  A61K31/4196 ,  C07D401/14 ,  C07D403/14 ,  C07D471/08 ,  C07D405/14

CPC分类号： A61K31/4439 ,  A61K31/4196 ,  A61K31/4375 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D471/08 ,  C07D471/18 ,  C07D491/14

摘要： Polycyclic aryl and polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl catalytic activity are also disclosed.

摘要翻译： 公开了多环芳基和多环杂芳基取代的三唑和含有这些化合物的药物组合物可用于抑制受体蛋白酪氨酸激酶Ax1的活性。 还公开了使用该化合物治疗与Axl催化活性相关的疾病或病症的方法。

公开(公告)号：US08741898B2

公开(公告)日：2014-06-03

申请号：US13423924

申请日：2012-03-19

申请人： Dane Goff ,  Jing Zhang ,  Rajinder Singh ,  Sacha Holland ,  Jiaxin Yu ,  Thilo J. Heckrodt ,  Pingyu Ding ,  Joane Litvak

发明人： Dane Goff ,  Jing Zhang ,  Rajinder Singh ,  Sacha Holland ,  Jiaxin Yu ,  Thilo J. Heckrodt ,  Pingyu Ding ,  Joane Litvak

IPC分类号： A61K31/502

CPC分类号： C07D401/14 ,  A61K31/502 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D417/04 ,  C07D417/14 ,  C07D451/04 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D491/04 ,  C07D491/20 ,  C07D495/04 ,  C07D519/00

摘要： Polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.

摘要翻译： 公开了多环杂芳基取代的三唑和含有这些化合物的药物组合物可用于抑制受体蛋白酪氨酸激酶Ax1的活性。 还公开了使用该化合物治疗与Axl活性相关的疾病或病症的方法。

公开(公告)号：US20090111816A1

公开(公告)日：2009-04-30

申请号：US11967163

申请日：2007-12-29

申请人： Rajinder Singh ,  Dane Goff ,  Jiaxin Yu ,  Sacha Holland ,  Thilo J. Heckrodt ,  Pingyu Ding ,  Joane Litvak ,  Jing Zhang

发明人： Rajinder Singh ,  Dane Goff ,  Jiaxin Yu ,  Sacha Holland ,  Thilo J. Heckrodt ,  Pingyu Ding ,  Joane Litvak ,  Jing Zhang

IPC分类号： A61K31/502 ,  C07D225/06 ,  A61P35/02 ,  A61P35/00 ,  C07D237/26

CPC分类号： A61K31/4439 ,  A61K31/4196 ,  A61K31/4375 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D471/08 ,  C07D471/18 ,  C07D491/14

摘要： Polycyclic aryl and polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl catalytic activity are also disclosed.

摘要翻译： 公开了多环芳基和多环杂芳基取代的三唑和含有这些化合物的药物组合物可用于抑制受体蛋白酪氨酸激酶Ax1的活性。 还公开了使用该化合物治疗与Axl催化活性相关的疾病或病症的方法。

公开(公告)号：US20080176847A1

公开(公告)日：2008-07-24

申请号：US11966942

申请日：2007-12-28

申请人： Dane Goff ,  Jing Zhang ,  Rajinder Singh ,  Sacha Holland ,  Jiaxin Yu ,  Pingyu Ding ,  Joane Litvak

发明人： Dane Goff ,  Jing Zhang ,  Rajinder Singh ,  Sacha Holland ,  Jiaxin Yu ,  Pingyu Ding ,  Joane Litvak

IPC分类号： A61K31/5377 ,  A61P9/00 ,  A61P17/06 ,  A61P35/00 ,  A61P27/02 ,  A61P19/00 ,  C07D413/14 ,  C07D403/14 ,  C07D495/04 ,  C07D471/18 ,  A61K31/496 ,  A61K31/4375 ,  A61K31/435 ,  A61K31/519 ,  A61K31/517

CPC分类号： C07D495/04 ,  C07D249/14 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07D453/06 ,  C07D471/18

摘要： Bridged bicyclic aryl or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.

摘要翻译： 公开了桥连双环芳基或杂芳基取代的三唑和含有这些化合物的药物组合物可用于抑制受体蛋白酪氨酸激酶Ax1的活性。 还公开了使用该化合物治疗与Axl活性相关的疾病或病症的方法。

公开(公告)号：US20170369476A1

公开(公告)日：2017-12-28

申请号：US15633258

申请日：2017-06-26

申请人： Yan Chen ,  Rose Yen ,  Jiaxin Yu ,  Vanessa Taylor ,  Rajinder Singh

发明人： Yan Chen ,  Rose Yen ,  Jiaxin Yu ,  Vanessa Taylor ,  Rajinder Singh

IPC分类号： C07D403/12 ,  C07D405/14 ,  C07D401/14

摘要： Compounds within the scope of the present invention have a Formula 1 or a salt or prodrug thereof, where ring A is selected from cycloaliphatic; ring B is aryl; R1 is selected from (C1-C10)alkyl, (C3-C10)cycloalkyl, halo, aryl, and heteroaryl; and R2 and R3 are independently selected from hydrogen and (C1-C6)alkyl. Disclosed compounds may have an IRAK4 IC50 of from 0.003 μM to 3.7 μM; a TAK1 IC50 of from 0.008 μM to 132 μM; and/or an IRAK4/TAK1 selectivity of from 1 to 450. Particular compounds may have an IRAK4/TAK1 selectivity of from 100 to 500. Disclosed compositions may be formulated as pharmaceutical compositions. A method for using the compounds and/or compositions also are disclosed. The method may comprise administering to a subject an effective amount of a compound within the scope of the present invention, particularly to selectively inhibit IRAK 1 and/or IRAK4 over TAK1.