公开(公告)号：US11225476B2

公开(公告)日：2022-01-18

申请号：US16795117

申请日：2020-02-19

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 Elizabeth Wilsher

IPC: 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：US20210253578A1

公开(公告)日：2021-08-19

申请号：US17023041

申请日：2020-09-16

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 ,  C07D487/08 ,  A61K31/519 ,  A61P35/00

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：US20210238162A1

公开(公告)日：2021-08-05

申请号：US16062223

申请日：2016-12-15

Applicant: GlaxoSmithKline Intellectual Property Development Limited ,  Astex Therapeutics Limited

Inventor： Rodolfo CADILLA ,  David Norman DEATON ,  Ashley Paul HANCOCK ,  Heather HOBBS ,  Simon Teanby HODGSON ,  Andrew L. LARKIN ,  Joelle LE ,  Paul N. MORTENSON ,  Daniel J. PRICE ,  Gordon SAXTY ,  Lee T. SCHALLER ,  Christie SCHULTE ,  Ian Edward David SMITH ,  Stephen Andrew THOMSON ,  Joseph Wendell WILSON

IPC: C07D401/14 ,  C07D401/12 ,  C07D215/54 ,  C07D417/12 ,  C07D405/12 ,  C07D413/12 ,  C07D413/14 ,  C07D491/056 ,  C07D491/048 ,  A61P21/00 ,  A61P11/06

Abstract: The present invention relates to compounds of Formula (XI): wherein R1a, R2a, R3a, R4a, R5a, R6a, and Aa are as defined herein, and pharmaceutically acceptable salts thereof. The compounds of the present invention are inhibitors of hematopoietic prostaglandin D synthase (H-PGDS) inhibitors and can be useful in the treatment of Duchenne Muscular Dystrophy. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting H-PGDS activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

公开(公告)号：US20210101887A1

公开(公告)日：2021-04-08

申请号：US16498207

申请日：2018-03-28

Applicant: ASTEX THERAPEUTICS LIMITED ,  CANCER RESEARCH TECHNOLOGY LIMITED

Inventor： Steven HOWARD ,  Benjamin David CONS ,  Jeffrey David ST. DENIS ,  Charlotte Mary GRIFFITHS-JONES ,  Steven Douglas HISCOCK ,  Rhian Sara HOLVEY ,  Alan Richard BURNS ,  David COUSIN ,  Hannah Louise DEXTER ,  Guillaume François PARRA ,  John Paul WATTS ,  Robert JEWELL ,  Jennifer Ann STOCKWELL ,  Kim Louise HIRST ,  Isabelle Anne LEMASSON ,  David John NASH ,  James Daniel OSBORNE ,  Jonas Calleja PRIEDE ,  Nicholas Paul RICHARDS ,  Aaron Michael DUMAS ,  Brian Christopher BISHOP ,  David PARRY-JONES ,  Jeremy Peter SCOTT ,  Meenakshi Sundaram SHANMUGHAM ,  Peter Richard MULLENS ,  David Charles LATHBURY ,  Darren James DIXON ,  Matthew James GAUNT

IPC: C07D405/06

Abstract: The invention relates to processes for preparing isoindolin-1-one derivatives, and in particular processes for preparing (2S,3S)-3-(4-chlorophenyl)-3-[(1R)-1-(4-chlorophenyl)-7-fluoro-5-[(1S)-1-hydroxy-1-(oxan-4-yl)propyl]-1-methoxy-3-oxo-2,3-dihydro-1H-isoindol-2-yl]-2-methylpropanoic acid. The invention also relates to crystalline forms of the compound (2S,3S)-3-(4-chlorophenyl)-3-[(1R)-1-(4-chlorophenyl)-7-fluoro-5-[(1S)-1-hydroxy-1-(oxan-4-yl)propyl]-1-methoxy-3-oxo-2,3-dihydro-1H-isoindol-2-yl]-2-methylpropanoic acid and its salts.

公开(公告)号：US10898482B2

公开(公告)日：2021-01-26

申请号：US15549881

申请日：2016-02-09

Applicant: ASTEX THERAPEUTICS LIMITED

Inventor： Diego Fernando Domenico Broggini

IPC: A61K31/498 ,  A61K47/18 ,  A61K47/26 ,  C09K15/20 ,  A61K9/20 ,  A61K9/48

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：US10736900B2

公开(公告)日：2020-08-11

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：US10526311B2

公开(公告)日：2020-01-07

申请号：US15763724

申请日：2016-09-29

Applicant: ASTEX THERAPEUTICS LIMITED ,  CANCER RESEARCH TECHNOLOGY LIMITED

Inventor： Gianni Chessari ,  Steven Howard ,  Ildiko Maria Buck ,  Benjamin David Cons ,  Christopher Norbert Johnson ,  Rhian Sara Holvey ,  David Charles Rees ,  Jeffrey David St. Denis ,  Emiliano Tamanini ,  Bernard Thomas Golding ,  Ian Robert Hardcastle ,  Celine Florence Cano ,  Duncan Charles Miller ,  Martin Edward Mäntylä Noble ,  Roger John Griffin ,  James Daniel Osborne ,  Joanne Peach ,  Arwel Lewis ,  Kim Louise Hirst ,  Benjamin Paul Whittaker ,  David Wyn Watson ,  Dale Robert Mitchell

IPC: C07D401/06 ,  A61K31/4439 ,  C07D401/14 ,  C07D403/06 ,  C07D407/14 ,  C07D409/14 ,  C07D417/14 ,  A61P35/00 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06

Abstract: The invention provides a compound of formula (I): or tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the various substituents are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds.

公开(公告)号：US10039759B2

公开(公告)日：2018-08-07

申请号：US15205676

申请日：2016-07-08

Applicant: ASTEX THERAPEUTICS LIMITED

Inventor： Valerio Berdini ,  Patrick René Angibaud ,  Steven John Woodhead ,  Gordon Saxty

IPC: A61K31/4709 ,  C07D401/14 ,  C07D413/14 ,  C07D215/38 ,  C07D401/04 ,  C07D407/14 ,  A61K31/47 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D405/14

CPC classification number: A61K31/4709 ,  A61K31/47 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D215/38 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D407/14 ,  C07D413/14

Abstract: The invention relates to new quinoline 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：US10004733B2

公开(公告)日：2018-06-26

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

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：US20180169110A1

公开(公告)日：2018-06-21

申请号：US15735977

申请日：2016-06-15

Applicant: GlaxoSmithKline Intellectual Property Development Limited ,  Astex Therapeutics Limited

Inventor： Jeffrey K. KERNS ,  Jamas Francis CALLAHAN ,  Hongxing YAN ,  Thomas Daniel HEIGHTMAN ,  Jeffrey Charles BOEHM ,  Alison Jo-Anne WOOLFORD

IPC: A61K31/5513 ,  A61K31/421 ,  A61K31/403 ,  A61P11/00

CPC classification number: A61K31/5513 ,  A61K31/403 ,  A61K31/421 ,  A61P11/00 ,  C07D267/14 ,  C07D403/06 ,  C07D413/06 ,  C07D413/10 ,  C07D498/04 ,  C07D519/00

Abstract: The present invention relates to aryl analogs, pharmaceutical compositions containing them and their use as NRF2 regulators.