公开(公告)号：US10519137B2

公开(公告)日：2019-12-31

申请号：US15810521

申请日：2017-11-13

Applicant: ASTEX THERAPEUTICS LTD

Inventor： Gordon Saxty ,  Christopher William Murray ,  Valerio Berdini ,  Gilbert Ebai Besong ,  Steven John Woodhead ,  Michael Reader ,  Laurence Anne Mevellec ,  Patrick René Angibaud ,  Eddy Jean Edgard Freyne ,  Timothy Pietro Suren Perera ,  Berthold Wroblowski ,  Alexandra Papanikos ,  Olivier Alexis Georges Querolle ,  Isabelle Noëlle Constance Pilatte ,  Pascal Ghislain André Bonnet ,  Werner Constant Johan Embrechts ,  Rhalid Akkari ,  Lieven Meerpoel

IPC: C07D231/10 ,  C07D231/12 ,  A61K31/415 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D487/08 ,  A61K31/498 ,  A61K31/5377 ,  A61K45/06 ,  C07D491/113 ,  C07D401/14 ,  C07F9/6524

Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

公开(公告)号：US10144731B2

公开(公告)日：2018-12-04

申请号：US15105306

申请日：2014-12-17

Applicant: GlaxoSmithKline Intellectual Property Development Limited ,  Astex Therapeutics, Ltd

Inventor： Thomas Glanmor Davies ,  Alison Jo-anne Woolford ,  Hendrika Maria Gerarda Willems ,  David Norton ,  Thomas Daniel Heightman ,  Jeffrey K. Kerns

IPC: C07D249/18 ,  C07D417/10 ,  C07D281/02 ,  C07D291/08 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D417/14 ,  C07D419/10 ,  C07D419/14 ,  C07D471/04 ,  C07D513/04 ,  C07D515/04

Abstract: The present invention relates to bis aryl analogs, pharmaceutical compositions containing them and their use as Nrf2 regulators.

公开(公告)号：US09902714B2

公开(公告)日：2018-02-27

申请号：US15128345

申请日：2015-03-26

Applicant: ASTEX THERAPEUTICS LTD

Inventor： Wim Vermeulen ,  Steven Anna Hostyn ,  Filip Albert Celine Cuyckens ,  Russell Mark Jones ,  Diego Fernando Domenico Broggini

IPC: C07D403/04 ,  A61K31/4985 ,  A61K31/5513 ,  C07D403/14 ,  A61P35/00

CPC classification number: C07D403/14 ,  A61K31/4985 ,  A61K31/5513

Abstract: The invention relates to new quinoxaline derivative compounds of formula (I), to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

公开(公告)号：US09783538B2

公开(公告)日：2017-10-10

申请号：US15105360

申请日：2014-12-19

Applicant: ASTEX THERAPEUTICS LIMITED

Inventor： Gianni Chessari ,  Christopher Norbert Johnson ,  Steven Howard ,  James Edward Harvey Day ,  Ildiko Maria Buck ,  Charlotte Mary Griffiths-Jones ,  Gordon Saxty ,  Emiliano Tamanini ,  Nicola Elisabeth Wilsher

IPC: C07D471/04 ,  A61K31/5377

CPC classification number: C07D471/04 ,  A61K31/5377

Abstract: The invention relates to new bicyclic heterocycle compounds, to pharmaceutical compositions comprising the compounds and to the use of the compounds in the treatment of diseases, e.g. cancer.

公开(公告)号：US09676768B2

公开(公告)日：2017-06-13

申请号：US14663534

申请日：2015-03-20

Applicant: ASTEX THERAPEUTICS LIMITED

Inventor： Alison Jo-Anne Woolford ,  Steven Howard ,  Ildiko Maria Buck ,  Gianni Chessari ,  Christopher Norbert Johnson ,  Emiliano Tamanini ,  James Edward Harvey Day ,  Elisabetta Chiarparin ,  Thomas Daniel Heightman ,  Martyn Frederickson ,  Charlotte Mary Griffiths-Jones

IPC: A61K31/497 ,  A61K31/501 ,  C07D403/04 ,  C07D419/00 ,  C07D471/04 ,  C07D401/06 ,  C07D471/10 ,  C07D403/06 ,  C07D487/10 ,  C07D403/14 ,  A61K31/496 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/5377 ,  C07D413/14 ,  C07D487/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/5377 ,  C07D401/06 ,  C07D403/06 ,  C07D403/14 ,  C07D413/14 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07D519/00

Abstract: The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R1, R2a, R2b, R3a, R3b, R5, R6, R7, R8, R9, p and E are as defined herein; to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

公开(公告)号：US20170000796A1

公开(公告)日：2017-01-05

申请号：US15203424

申请日：2016-07-06

Applicant: ASTEX THERAPEUTICS LIMITED

Inventor： Gordon SAXTY ,  Christopher Charles Frederick HAMLETT ,  Valerio BERDINI ,  Christopher William MURRAY ,  Patrick René ANGIBAUD ,  Olivier Alexis Georges QUEROLLE ,  Virginie Sophie PONCELET

IPC: A61K31/519

CPC classification number: A61K31/519 ,  A61K45/06 ,  C07D475/00

Abstract: The invention relates to new pteridine derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

Abstract translation: 本发明涉及新的蝶啶衍生物化合物，包含所述化合物的药物组合物，用于制备所述化合物的方法以及所述化合物在治疗疾病中的用途。 癌症。

公开(公告)号：US09464071B2

公开(公告)日：2016-10-11

申请号：US14505020

申请日：2014-10-02

Applicant: ASTEX THERAPEUTICS LTD

Inventor： Gordon Saxty ,  Christopher William Murray ,  Valerio Berdini ,  Gilbert Ebai Besong ,  Christopher Charles Frederick Hamlett ,  Christopher Norbert Johnson ,  Steven John Woodhead ,  Michael Reader ,  David Charles Rees ,  Laurence Anne Mevellec ,  Patrick René Angibaud ,  Eddy Jean Edgard Freyne ,  Tom Cornelis Hortense Govaerts ,  Johan Erwin Edmond Weerts ,  Timothy Pietro Suren Perera ,  Ronaldus Arnodus Hendrika Joseph Gilissen ,  Berthold Wroblowski ,  Jean Fernand Armand Lacrampe ,  Alexandra Papanikos ,  Olivier Alexis Georges Querolle ,  Elisabeth Thérèse Jeanne Pasquier ,  Isabelle Noëlle Constance Pilatte ,  Pascal Ghislain André Bonnet ,  Werner Constant Johan Embrechts ,  Rhalid Akkari ,  Lieven Meerpoel

IPC: A61K31/415 ,  C07D231/10 ,  C07D231/12 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D487/08 ,  A61K31/498 ,  A61K31/5377 ,  A61K45/06 ,  C07D491/113

CPC classification number: C07D403/04 ,  A61K31/498 ,  A61K31/5377 ,  A61K45/06 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D487/08 ,  C07D491/113 ,  C07F9/6524

Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

Abstract translation: 本发明涉及新的喹喔啉衍生物化合物，包含所述化合物的药物组合物，用于制备所述化合物的方法和所述化合物在治疗疾病中的用途。 癌症。

公开(公告)号：US20160250187A1

公开(公告)日：2016-09-01

申请号：US15010831

申请日：2016-01-29

Applicant: Astex Therapeutics Ltd ,  The Institute of Cancer Research: Royal Cancer Hospital ,  Cancer Research Technology Limited

Inventor： Valerio BERDINI ,  Gordon SAXTY ,  Marinus Leendert VERDONK ,  Steven John WOODHEAD ,  Paul Graham WYATT ,  Robert George BOYLE ,  Hannah Fiona SORE ,  David Winter WALKER ,  Ian COLLINS ,  Robert DOWNHAM ,  Robin Arthur Ellis CARR

IPC: A61K31/415 ,  A61K31/454 ,  A61K31/4439 ,  A61K31/5377 ,  A61K31/4155 ,  A61K9/20 ,  A61K31/4178 ,  A61K31/497 ,  A61K31/551 ,  A61K31/4545 ,  A61K9/00 ,  A61K9/48 ,  A61K45/06 ,  A61K31/496

CPC classification number: A61K31/415 ,  A61K9/0019 ,  A61K9/20 ,  A61K9/48 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/551 ,  A61K45/06 ,  C07D231/12 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D405/04 ,  C07D413/10

Abstract: The invention provides compounds of the formula (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom α with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom α with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R1 is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents.

Abstract translation: 本发明提供了具有蛋白激酶B抑制活性的式（I）化合物：其中A是含有1至7个碳原子的饱和烃连接基团，该连接基团具有在R1和NR2R3之间延伸的最大链长度为5个原子，以及 在E和NR2R3之间延伸的4个原子的最大链长度，其中连接基团中的一个碳原子可以任选地被氧或氮原子取代; 并且其中连接基团A的碳原子可以任选地具有一个或多个选自氧代，氟和羟基的取代基，条件是存在的羟基相对于NR 2 R 3基团不位于碳原子α，条件是 存在时的氧代基相对于NR2R3基团位于碳原子α; E是单环或双环碳环或杂环基; R1是芳基或杂芳基; 并且R 2，R 3，R 4和R 5如权利要求中所定义。 还提供含有化合物的药物组合物，制备化合物的方法及其作为抗癌剂的用途。

公开(公告)号：US20160108034A1

公开(公告)日：2016-04-21

申请号：US14855986

申请日：2015-09-16

Applicant: ASTEX THERAPEUTICS LIMITED

Inventor： Patrick Rene ANGIBAUD ,  Michel OBRINGER ,  Julien Jeremie Joseph MARIN ,  Matthieu JEANTY

IPC: C07D471/04 ,  A61K45/06 ,  A61K31/4545 ,  A61K31/444 ,  A61K31/4375 ,  A61K31/506

CPC classification number: A61K31/4375 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/506 ,  A61K45/06 ,  C07D471/04

Abstract: The invention relates to new naphthyridine derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

Abstract translation: 本发明涉及新的萘啶衍生物化合物，包含所述化合物的药物组合物，用于制备所述化合物的方法以及所述化合物在治疗疾病中的用途。 癌症。

公开(公告)号：US09309242B2

公开(公告)日：2016-04-12

申请号：US14354832

申请日：2012-10-26

Applicant: ASTEX THERAPEUTICS LIMITED

Inventor： Valerio Berdini ,  Gordon Saxty ,  Patrick Rene Angibaud ,  Olivier Alexis Georges Querolle ,  Virginie Sophie Poncelet ,  Bruno Roux ,  Lieven Meerpoel

IPC: A61K31/4985 ,  C07D241/36 ,  C07D471/04 ,  A61K31/506 ,  A61K31/5377

CPC classification number: A61K31/4985 ,  A61K31/506 ,  A61K31/5377 ,  C07D471/04

Abstract: The invention relates to new pyridopyrazine derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

Abstract translation: 本发明涉及新的吡啶并吡嗪衍生物化合物，包含所述化合物的药物组合物，用于制备所述化合物的方法以及所述化合物在治疗疾病中的用途。 癌症。