公开(公告)号：US09763922B2

公开(公告)日：2017-09-19

申请号：US14952821

申请日：2015-11-25

申请人： Genentech, Inc. ,  Constellation Pharmaceuticals, Inc.

发明人： Marc Adler ,  Brian K. Albrecht ,  Sarah Bronner ,  Kevin X. Chen ,  Alexandre Côté ,  Terry Crawford ,  Patrick Cyr ,  Jackson Egen ,  Steven Kauder ,  Kwong Wah Lai ,  Jiangpeng Liao ,  Steven Magnuson ,  Jeremy Murray ,  Richard Pastor ,  F. Anthony Romero ,  Alexander M. Taylor ,  Vickie Hsiao-Wei Tsui ,  Fei Wang ,  Bing-Yan Zhu

IPC分类号： A61K31/437 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/498 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5415 ,  A61K31/55 ,  C07D471/04 ,  C07D519/00 ,  A61K45/06

CPC分类号： A61K31/437 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/498 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5415 ,  A61K31/55 ,  A61K45/06 ,  C07D471/04 ,  C07D519/00

摘要： The present invention relates to compounds of formula (I) or formula (II): and to salts thereof, wherein R1-R4 of formula (I) and R1-R3 of formula (II) have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) of formula (II) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.

公开(公告)号：US20170333406A1

公开(公告)日：2017-11-23

申请号：US15667227

申请日：2017-08-02

申请人： GENENTECH, INC. ,  CONSTELLATION PHARMACEUTICALS, INC.

发明人： Marc Adler ,  Brian K. Albrecht ,  Sarah Bronner ,  Kevin X. Chen ,  Alexandre Côté ,  Terry Crawford ,  Patrick Cyr ,  Jackson Egen ,  Steven Kauder ,  Kwong Wah Lai ,  Jiangpeng Liao ,  Steven Magnuson ,  Jeremy Murray ,  Richard Pastor ,  F. Anthony Romero ,  Alexander M. Taylor ,  Vickie Hsiao-Wei Tsui ,  Fei Wang ,  Bing-Yan Zhu

IPC分类号： A61K31/437 ,  C07D471/04 ,  A61K45/06 ,  A61K31/55 ,  A61K31/5415 ,  A61K31/5377 ,  A61K31/4375 ,  A61K31/506 ,  A61K31/498 ,  A61K31/496 ,  A61K31/4725 ,  A61K31/4709 ,  C07D519/00 ,  A61K31/538

CPC分类号： A61K31/437 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/498 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5415 ,  A61K31/55 ,  A61K45/06 ,  C07D471/04 ,  C07D519/00

摘要： The present invention relates to compounds of formula (I) or formula (II): and to salts thereof, wherein R1-R4 of formula (I) and R1-R3 of formula (II) have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) of formula (II) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.

公开(公告)号：US20160158207A1

公开(公告)日：2016-06-09

申请号：US14952821

申请日：2015-11-25

申请人： Constellation Pharmaceuticals, Inc. ,  Genentech, Inc.

发明人： Marc Adler ,  Brian K. Albrecht ,  Sarah Bronner ,  Kevin X. Chen ,  Alexandre Côté ,  Terry Crawford ,  Patrick Cyr ,  Jackson Egen ,  Steven Kauder ,  Kwong Wah Lai ,  Jiangpeng Liao ,  Steven Magnuson ,  Jeremy Murray ,  Richard Pastor ,  F. Anthony Romero ,  Alexander M. Taylor ,  Vickie Hsiao-Wei Tsui ,  Fei Wang ,  Bing-Yan Zhu

IPC分类号： A61K31/437 ,  A61K31/538 ,  A61K31/5415 ,  A61K31/4709 ,  A61K31/498 ,  A61K45/06 ,  A61K31/55 ,  C07D519/00 ,  A61K31/4375 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/5377 ,  C07D471/04 ,  A61K31/506

CPC分类号： A61K31/437 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/498 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5415 ,  A61K31/55 ,  A61K45/06 ,  C07D471/04 ,  C07D519/00

摘要： The present invention relates to compounds of formula (I) or formula (II): and to salts thereof, wherein R1-R4 of formula (I) and R1-R3 of formula (II) have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) of formula (II) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.

摘要翻译： 本发明涉及式（I）或式（II）化合物及其盐，其中式（I）的R 1 -R 4和式（II）的R 1 -R 3具有本文定义的任何值，组合物 及其用途。 该化合物可用作CBP和/或EP300的抑制剂。 还包括包含式（II）的式（I）化合物或其药学上可接受的盐的药物组合物，以及在治疗各种CBP和/或EP300介导的病症中使用这些化合物和盐的方法。

公开(公告)号：US20200002345A1

公开(公告)日：2020-01-02

申请号：US16561432

申请日：2019-09-05

申请人： Genentech, Inc.

发明人： Paul Gibbons ,  Emily Hanan ,  Wendy Liu ,  Joseph P. Lyssikatos ,  Steven R. Magnuson ,  Rohan Mendonca ,  Richard Pastor ,  Thomas E. Rawson ,  Michael Siu ,  Mark E. Zak ,  Aihe Zhou ,  Bing-Yan Zhu ,  Christopher Hurley

IPC分类号： C07D487/04 ,  A61P17/06 ,  A61P35/02 ,  A61K31/519 ,  A61P29/00

摘要： A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein, are useful as inhibitors of one or more Janus kinases. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient are disclosed.

公开(公告)号：US20160333011A1

公开(公告)日：2016-11-17

申请号：US15220087

申请日：2016-07-26

申请人： Genentech, Inc.

发明人： Bing-Yan Zhu ,  Michael Siu ,  Steven R. Magnuson ,  Richard Pastor ,  He Haiying ,  Xiao Yisong ,  Zheng Jifu ,  Xu Xing ,  Zhao Junping ,  Christopher Hurley ,  Jun Liang ,  Wendy Liu ,  Joseph P. Lyssikatos

IPC分类号： C07D471/04

CPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/496 ,  A61K31/5377 ,  C07D487/04

摘要： A compound of Formula I, enantiomers, diastereomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of JAK kinase activity in a patient are disclosed.

公开(公告)号：US20150152117A1

公开(公告)日：2015-06-04

申请号：US14615873

申请日：2015-02-06

申请人： Genentech, Inc.

发明人： Paul Gibbons ,  Emily Hanan ,  Wendy Liu ,  Joseph P. Lyssikatos ,  Steven R. Magnuson ,  Rohan Mendonca ,  Richard Pastor ,  Thomas E. Rawson ,  Michael Siu ,  Mark E. Zak ,  Aihe Zhou ,  Bing-Yan Zhu

IPC分类号： C07D487/04

CPC分类号： C07D487/04 ,  A61K31/519 ,  A61P17/06 ,  A61P29/00 ,  A61P35/02

摘要： A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein, are useful as inhibitors of one or more Janus kinases. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient are disclosed.

摘要翻译： 其中R 1，R 2和R 3在本文中定义的式I化合物，对映异构体，非对映异构体，互变异构体或其药学上可接受的盐可用作一种或多种Janus激酶的抑制剂。 公开了包含式I化合物和药学上可接受的载体，佐剂或媒介物的药物组合物，以及对患者中Janus激酶活性的抑制作出反应的疾病或病症的严重程度的治疗或减轻的方法。

公开(公告)号：US20140378449A1

公开(公告)日：2014-12-25

申请号：US14483485

申请日：2014-09-11

申请人： Genentech, Inc.

发明人： Bing-Yan Zhu ,  Michael Siu ,  Steven R. Magnuson ,  Richard Pastor ,  He Haiying ,  Xiao Yisong ,  Zheng Jifu ,  Xu Xing ,  Zhao Junping ,  Wendy Liu

IPC分类号： C07D471/04 ,  A61K45/06 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545

CPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06

摘要： A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of JAK kinase activity in a patient are disclosed.

摘要翻译： 其中R 1，R 2，R 3，R 4和R 5在本文中定义的式I化合物，对映异构体，非对映异构体，互变异构体或其药学上可接受的盐可用作JAK激酶抑制剂。 公开了包含式I化合物和药学上可接受的载体，佐剂或载体的药物组合物，以及治疗或减轻对患者中JAK激酶活性的抑制作用的疾病或病症的严重程度的方法。

公开(公告)号：US20170283424A1

公开(公告)日：2017-10-05

申请号：US15627847

申请日：2017-06-20

申请人： Genentech, Inc.

发明人： Paul Gibbons ,  Emily Hanan ,  Wendy Liu ,  Joseph P. Lyssikatos ,  Steven R. Magnuson ,  Rohan Mendonca ,  Richard Pastor ,  Thomas E. Rawson ,  Michael Siu ,  Mark E. Zak ,  Aihe Zhou ,  Bing-Yan Zhu ,  Christopher Hurley

IPC分类号： C07D487/04

CPC分类号： C07D487/04 ,  A61K31/519 ,  A61P17/06 ,  A61P29/00 ,  A61P35/02

摘要： A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein, are useful as inhibitors of one or more Janus kinases. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient are disclosed.

公开(公告)号：US20140107099A1

公开(公告)日：2014-04-17

申请号：US14134150

申请日：2013-12-19

申请人： Genentech, Inc.

发明人： Jeffrey Blaney ,  Paul A. Gibbons ,  Emily Hanan ,  Joseph P. Lyssikatos ,  Steven R. Magnuson ,  Richard Pastor ,  Thomas E. Rawson ,  Aihe Zhou ,  Bing-Yan Zhu

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： The invention provides JAK kinase inhibitors of Formula Ia, enantiomers, diasteriomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R7 and Z are defined herein, a pharmaceutical composition that includes a compound of Formula Ia and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a JAK kinase activity in a patient.

摘要翻译： 本发明提供了式Ia的JAK激酶抑制剂，其对映体，非对映异构体或其药学上可接受的盐，其中R1，R2，R7和Z在本文中定义，药物组合物包括式Ia化合物和药学上可接受的载体，佐剂或载体 以及对患者中JAK激酶活性的抑制作出反应的疾病或病症的严重程度的治疗或减轻的方法。

公开(公告)号：US20140038939A1

公开(公告)日：2014-02-06

申请号：US14049458

申请日：2013-10-09

申请人： Genentech, Inc.

发明人： Bing-Yan Zhu ,  Michael Siu ,  Steven R. Magnuson ,  Richard Pastor ,  He Haiying ,  Xiao Yisong ,  Zheng Jifu ,  Xu Xing ,  Zhao Junping ,  Christopher Hurley ,  Jun Liang ,  Wendy Liu ,  Joseph P. Lyssikatos

IPC分类号： C07D487/04 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/437

CPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/496 ,  A61K31/5377 ,  C07D487/04

摘要： A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of JAK kinase activity in a patient are disclosed.