公开(公告)号：US20190119271A1

公开(公告)日：2019-04-25

申请号：US16094564

申请日：2017-04-18

Applicant: GlaxoSmithKline Intellectual Property Development Limited

Inventor： Linda N. CASILLAS ,  John David HARLING ,  Afjal Hussain MIAH ,  Mark David RACKHAM ,  Ian Edward David Smith

IPC: C07D471/04 ,  C07D417/14 ,  C07D471/10 ,  C07D519/00

Abstract: The present invention relates to compounds, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of RIP2 kinase, including degrading RIP2 kinase, the treatment of diseases and conditions mediated by the RIP2 kinase, in particular for the treatment of inflammatory diseases or conditions.

公开(公告)号：US20160136230A1

公开(公告)日：2016-05-19

申请号：US14898832

申请日：2014-07-01

Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

Inventor： Sebastien Andre CAMPOS ,  John David HARLING

IPC: A61K38/06 ,  A61K45/06 ,  C07K5/087

CPC classification number: A61K38/06 ,  A61K45/06 ,  C07K5/06017 ,  C07K5/06043 ,  C07K5/06078 ,  C07K5/0812

Abstract: A compound of formula (I): or a pharmaceutically acceptable salt thereof, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of the estrogen receptor, including degrading the estrogen receptor, the treatment of diseases and conditions mediated by the estrogen receptor.

Abstract translation: 式（I）化合物或其药学上可接受的盐，含有所述化合物的组合物，组合和药物及其制备方法。 本发明还涉及所述化合物，组合，组合物和药物的用途，例如作为雌激素受体活性的抑制剂，包括降解雌激素受体，治疗由雌激素受体介导的疾病和病症。

公开(公告)号：US20190210996A1

公开(公告)日：2019-07-11

申请号：US16326234

申请日：2017-08-16

Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

Inventor： John David HARLING ,  Christopher TINWORTH

IPC: C07D401/14 ,  A61K47/64 ,  A61K47/66 ,  A61K45/06

CPC classification number: C07D401/14 ,  A61K45/06 ,  A61K47/64 ,  A61K47/66 ,  A61P35/00

Abstract: A method of treating disorders associated with aberrant kinase activity, wherein the kinase is. Adaptor-associated protein kinase 1 (AAK1), Aurora Kinase A (AURKA), Aurora Kinase B (AURKB), Bruton's Tyrosine Kinase (BTK), Interleukin-1 receptor-associated kinase 3 (IRAK3), Protein tyrosine kinase 2 beta (PTK2B), Tyrosine-protein kinase Tec (TEC), Serine/threonine-protein kinase Wee1 (WEE1), Cyclin G-associated kinase (GAK), Large Tumour suppressor 1 Kinase (LATS1), Focal Adhesion Kinase (PTK2), Ribosomal protein S6 kinase alpha-1 (RPS6KA1) said method comprising degrading said kinase.

公开(公告)号：US20190263798A1

公开(公告)日：2019-08-29

申请号：US16407300

申请日：2019-05-09

Applicant: GlaxoSmithKline Intellectual Property Development Limited

Inventor： John David HARLING ,  Ian Edward David SMITH

IPC: C07D417/14 ,  A61K47/66 ,  A61K47/54 ,  A61K31/4725 ,  C07D417/12 ,  A61K31/519 ,  C07D487/04

Abstract: A selective IAP binder together with a linker moiety.

公开(公告)号：US20180134688A1

公开(公告)日：2018-05-17

申请号：US15568025

申请日：2016-04-20

Applicant: GlaxoSmithKline Intellectual Property Development Limited

Inventor： Linda N. CASILLAS ,  John David HARLING ,  Afjal Hussain MIAH ,  Mark David RACKHAM ,  Ian Edward David SMITH

IPC: C07D403/14 ,  C07D401/14 ,  C07D487/04 ,  C07D417/14 ,  A61P29/00

CPC classification number: C07D403/14 ,  A61P29/00 ,  C07D401/14 ,  C07D417/14 ,  C07D487/04

Abstract: The present invention relates to compounds, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of RIP2 kinase, including degrading RIP2 kinase, the treatment of diseases and conditions mediated by the RIP2 kinase, in particular for the treatment of inflammatory diseases or conditions.

公开(公告)号：US20190382381A1

公开(公告)日：2019-12-19

申请号：US16547734

申请日：2019-08-22

Applicant: GlaxoSmithKline Intellectual Property Development Limited

Inventor： Linda N. CASILLAS ,  John David HARLING ,  Afjal Hussain MIAH ,  Mark David RACKHAM ,  Ian Edward David SMITH

IPC: C07D403/14 ,  A61P29/00 ,  C07D487/04 ,  C07D417/14 ,  C07D401/14

Abstract: The present invention relates to compounds, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of RIP2 kinase, including degrading RIP2 kinase, the treatment of diseases and conditions mediated by the RIP2 kinase, in particular for the treatment of inflammatory diseases or conditions.

公开(公告)号：US20190152946A1

公开(公告)日：2019-05-23

申请号：US16308542

申请日：2017-06-08

Applicant: GlaxoSmithKline Intellectual Property Development Limited

Inventor： John David HARLING ,  Christopher TINWORTH

IPC: C07D401/12 ,  A61P35/00 ,  C07K5/12 ,  A61K47/64 ,  A61K47/65

Abstract: A method of treating disorders associated with aberrant kinase activity, wherein the kinase is. IRAK3, GAK, TEC, PTK2B(PYK2), AURKA, RPS6KA1(RSK3), MAPK9(JNK2), BTK, PTK2 or AKT2, said method comprising degrading said kinase.

公开(公告)号：US20180118733A1

公开(公告)日：2018-05-03

申请号：US15568006

申请日：2016-04-20

Applicant: GlaxoSmithKline Intellectual Property Development Limited

Inventor： John David HARLING ,  Ian Edward David SMITH

IPC: C07D417/14 ,  C07D417/12 ,  C07D487/04 ,  A61K31/4725 ,  A61K31/519

CPC classification number: C07D417/14 ,  A61K31/4725 ,  A61K31/519 ,  A61K47/545 ,  A61K47/66 ,  C07D417/12 ,  C07D487/04

Abstract: The present invention relates to compounds, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of RIP2 kinase, including degrading RIP2 kinase, the treatment of diseases and conditions mediated by the RIP2 kinase, in particular for the treatment of inflammatory diseases or conditions.

公开(公告)号：US20160368911A1

公开(公告)日：2016-12-22

申请号：US14898782

申请日：2014-07-01

Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

Inventor： Sebastien Andre CAMPOS ,  John David HARLING ,  Afjal Hussain MIAH ,  Ian Edward, David SMITH

IPC: C07D417/14 ,  C07D413/14 ,  A61K31/422 ,  A61K45/06 ,  C07D471/10 ,  A61K31/435 ,  C07K5/062 ,  A61K38/05 ,  A61K31/427 ,  A61K31/496

CPC classification number: C07D417/14 ,  A61K31/422 ,  A61K31/427 ,  A61K31/435 ,  A61K31/496 ,  A61K38/05 ,  A61K45/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D471/10 ,  C07K5/06052

Abstract: A compound of formula (I): or a pharmaceutically acceptable salt thereof, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of the estrogen receptor, including degrading the estrogen receptor, the treatment of diseases and conditions mediated by the estrogen receptor,

Abstract translation: 或其药学上可接受的盐，含有所述化合物的组合物，组合和药物及其制备方法。 本发明还涉及所述化合物，组合，组合物和药物的用途，例如作为雌激素受体活性的抑制剂，包括降解雌激素受体，治疗由雌激素受体介导的疾病和病症，