公开(公告)号：US10045982B2

公开(公告)日：2018-08-14

申请号：US15019563

申请日：2016-02-09

Applicant: ASTEX THERAPEUTICS LIMITED

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

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

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

Abstract: The invention relates to new pyridopyrazine derivative compounds of formula (I-A) or formula (I-B): 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：US20180186775A1

公开(公告)日：2018-07-05

申请号：US15856998

申请日：2017-12-28

Applicant: ASTEX THERAPEUTICS LTD

Inventor： Wim VERMEULEN ,  Steven Anna HOSTYN ,  Filip Albert Celine CUYCKENS ,  Russell Mark JONES ,  Diego Fernando Domenico BROGGINI

IPC: C07D403/14 ,  A61K31/4985 ,  A61K31/5513

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：US20180179187A1

公开(公告)日：2018-06-28

申请号：US15736075

申请日：2016-06-15

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

Inventor： Jeffrey K. KERNS ,  James CALLAHAN ,  Hongxing YAN ,  Thomas Daniel HEIGHTMAN ,  Charlotte Mary GRIFFITHS-JONES ,  Alison Jo-Anne WOOLFORD ,  Tindy LI ,  Ami Lakdawala SHAH ,  Roderick S. DAVIS ,  David NORTON ,  Jeffrey Charles BOEHM ,  Paris L. HAMILTON

IPC: C07D403/10 ,  C07D413/10 ,  C07D471/04 ,  C07D413/14 ,  C07D255/04 ,  C07D498/04 ,  C07D405/10 ,  C07D487/04 ,  C07D273/01 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D233/64 ,  C07D401/10

CPC classification number: C07D403/10 ,  A61P9/00 ,  A61P11/00 ,  A61P25/00 ,  A61P27/00 ,  A61P35/00 ,  A61P37/00 ,  C07D233/60 ,  C07D233/64 ,  C07D249/18 ,  C07D255/04 ,  C07D267/14 ,  C07D273/01 ,  C07D401/10 ,  C07D401/14 ,  C07D403/14 ,  C07D405/10 ,  C07D405/14 ,  C07D413/10 ,  C07D413/14 ,  C07D451/02 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08 ,  C07D498/04

Abstract: Provided are aryl analogs, pharmaceutical compositions containing them and their use as NRF2 regulators.

公开(公告)号：US20180155351A1

公开(公告)日：2018-06-07

申请号：US15886014

申请日：2018-02-01

Applicant: Novartis AG ,  Astex Therapeutics Ltd.

Inventor： Gilbert Besong ,  Christopher Thomas Brain ,  Clinton A. Brooks ,  Miles Stuart Congreve ,  Claudio Dagostin ,  Guo He ,  Ying Hou ,  Steven Howard ,  Yue Li ,  Yipin Lu ,  Paul Mortenson ,  Troy Smith ,  Moo Je Sung ,  Steven Woodhead ,  Wojciech Wrona ,  Bharat Lagu

IPC: C07D487/04 ,  A61K31/519

CPC classification number: C07D487/04 ,  A61K31/519 ,  C07D487/08

Abstract: The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein.

公开(公告)号：US20180021332A1

公开(公告)日：2018-01-25

申请号：US15549881

申请日：2016-02-09

Applicant: ASTEX THERAPEUTICS LIMITED

Inventor： Diego Fernando Domenico BROGGINI

IPC: A61K31/498 ,  A61K47/18

CPC classification number: A61K31/498 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/4858 ,  A61K47/18 ,  A61K47/26

Abstract: The invention relates to pharmaceutical compositions comprising N-(3,5-dimethoxyphenyl)-N′-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine, or a pharmaceutically acceptable salt thereof or a solvate thereof; to processes for the preparation of said compositions and to the use of said compositions for the manufacture of a medicament for the prophylaxis of or the treatment, in particular the treatment, of diseases, e.g. cancer

公开(公告)号：US09856236B2

公开(公告)日：2018-01-02

申请号：US14816565

申请日：2015-08-03

Applicant: ASTEX THERAPEUTICS LTD

Inventor： Gordon Saxty ,  Christopher William Murray ,  Valerio Berdini ,  Gilbert Ebai Besong ,  Christopher Charles Frederick Hamlett ,  Steven John Woodhead ,  Yannick Aime Eddy Ligny ,  Patrick René Angibaud

IPC: C07D241/40 ,  C07D403/04 ,  C07D401/14 ,  C07D403/14

CPC classification number: C07D403/04 ,  C07D401/14 ,  C07D403/14

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：US20170334907A1

公开(公告)日：2017-11-23

申请号：US15585908

申请日：2017-05-03

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: C07D471/04 ,  C07D487/10 ,  C07D487/04 ,  C07D471/10 ,  C07D413/14 ,  C07D403/14 ,  A61K31/496 ,  C07D401/06 ,  A61K31/5377 ,  A61K31/506 ,  A61K31/5025 ,  A61K31/501 ,  A61K31/497 ,  C07D403/06 ,  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：US20170100406A1

公开(公告)日：2017-04-13

申请号：US15128347

申请日：2015-03-26

Applicant: Astex Therapeutics Ltd

Inventor： Eleonora JOVCHEVA ,  Timothy Pietro Suren PERERA

IPC: A61K31/53 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/519

Abstract: The invention relates to a combination of a FGFR inhibitor and an IGF1R inhibitor. The combination is for use in the treatment of a proliferative disorder, in particular for the treatment of cancer. The FGFR inhibitor and the IGFR inhibitor can be administered simultaneously, separately or sequentially. The invention further relates to a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a combination according to the invention.

公开(公告)号：US20150239883A1

公开(公告)日：2015-08-27

申请号：US14404188

申请日：2013-05-30

Applicant: ASTEX THERAPEUTICS LIMITED

Inventor： Patrick René Angibaud ,  Isabelle Noëlle Constance Pilatte ,  Olivier Alexis Georges Querolle

IPC: C07D471/04 ,  A61K45/06 ,  A61K31/5377 ,  A61K31/5025 ,  A61K31/4375

CPC classification number: A61K31/5377 ,  A61K31/4375 ,  A61K31/4985 ,  A61K31/5025 ,  A61K45/06 ,  C07D403/04 ,  C07D471/04

Abstract: The invention relates to new pyridopyrazine and 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。

公开(公告)号：US20150105368A1

公开(公告)日：2015-04-16

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 ,  Oliver Alexis Georges QUEROLLE ,  Elisabeth Thérèse Jeanne PASQUIER ,  Isabelle Noëlle Constance PILATTE ,  Pascal Ghislain André BONNET ,  Werner Constant Johan EMBRECHTS ,  Rhalid AKKARI ,  Lieven MEERPOEL

IPC: C07D403/04 ,  A61K45/06 ,  C07D413/14 ,  A61K31/5377 ,  A61K31/498 ,  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。