公开(公告)号：US20250152729A1

公开(公告)日：2025-05-15

申请号：US18718334

申请日：2022-12-12

Applicant: Cancer Research Technology Limited ,  Medimmune Limited

Inventor： Alexandra Addyman ,  Georgina Anderson ,  Mark Austin ,  Michelle Barnard ,  Denice Tsz Yau Chan ,  Michael Chapman ,  Agata Diamandakis ,  Maria Groves ,  William Hawthorne ,  Stuart Haynes ,  Lesley Jenkinson ,  Jean-Martin Lapointe ,  Kirsty-Jane Martin ,  Louise Slater ,  Tristan Vaughan

IPC: A61K47/68 ,  C07K14/725 ,  C07K16/28

Abstract: An antibody-drug conjugate (ADC) comprising an anti-human SEMA4A humanised or human antibody, a linker and a cytotoxin.

公开(公告)号：US20250074900A1

公开(公告)日：2025-03-06

申请号：US18785847

申请日：2024-07-26

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：US12071429B2

公开(公告)日：2024-08-27

申请号：US17164045

申请日：2021-02-01

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: C07D405/14 ,  A61K31/4035 ,  A61P35/00 ,  C07D209/48 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D413/06 ,  C07D413/12 ,  C07F9/572

CPC classification number: C07D405/14 ,  A61K31/4035 ,  A61P35/00 ,  C07D209/48 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D413/06 ,  C07D413/12 ,  C07F9/5728 ,  C07B2200/05

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：US20240254110A1

公开(公告)日：2024-08-01

申请号：US18461253

申请日：2023-09-05

Applicant: CANCER RESEARCH TECHNOLOGY LIMITED

Inventor： Keith Jones ,  Carl Rye ,  Nicola Chessum ,  Matthew D. Cheeseman ,  Adele E. Pasqua ,  Kurt G. Pike ,  Paul F. Faulder

IPC: C07D405/12 ,  C07D319/18 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/08 ,  C07D491/056

CPC classification number: C07D405/12 ,  C07D319/18 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/08 ,  C07D491/056

Abstract: The present invention relates to compounds of formula I wherein A1, A2 R4 and Q are as defined herein. The compounds of the present invention are inhibitors of heat shock factor 1 (HSF1). In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.

公开(公告)号：US20240132504A1

公开(公告)日：2024-04-25

申请号：US18312069

申请日：2023-05-04

Applicant: Cancer Research Technology Limited

Inventor： Allan Jordan ,  Rebecca Newton ,  George Hynd ,  Jonathan Mark Sutton ,  Bohdan Waszkowycz

IPC: C07D487/04

CPC classification number: C07D487/04

Abstract: The present invention relates to compounds of formula I that function as inhibitors of RET (rearranged during transfection) kinase enzyme activity:






wherein HET, bonds a, b, c and d, X1, X2, X3, X4, R2, and R3 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which RET kinase activity is implicated.

公开(公告)号：US11897877B2

公开(公告)日：2024-02-13

申请号：US17319231

申请日：2021-05-13

Applicant: Cancer Research Technology Limited

Inventor： Swen Hoelder ,  Julian Blagg ,  Savade Solanki ,  Hannah Woodward ,  Sebastien Gaston Andre Naud ,  Vassilios Bavetsias ,  Peter Sheldrake ,  Paolo Innocenti ,  Kwai-Ming J. Cheung ,  Butrus Atrash

IPC: C07D471/04 ,  C07D401/14 ,  C07D413/14 ,  C07D401/04 ,  C07D405/04 ,  C07D519/00 ,  A61K31/519

CPC classification number: C07D471/04 ,  A61K31/519 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D413/14 ,  C07D519/00

Abstract: The present invention relates to compounds of formula I




wherein R1, R4, Ar, W, X and Z are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.

公开(公告)号：US11873341B2

公开(公告)日：2024-01-16

申请号：US16979932

申请日：2019-03-13

Applicant: Tusk Therapeutics Ltd. ,  Cancer Research Technology Limited

Inventor： Anne Goubier ,  Beatriz Goyenechea Corzo ,  Josephine Salimu ,  Kevin Moulder ,  Pascal Merchiers ,  Sergio Quezada

IPC: C07K16/28 ,  A61P35/02 ,  C12N15/85 ,  A61P35/00 ,  A61K39/395 ,  C07K14/55 ,  A61K45/06 ,  A61K39/00 ,  C07K14/05

CPC classification number: C07K16/2866 ,  A61K39/39533 ,  A61K39/39541 ,  A61K39/39558 ,  A61K39/39566 ,  A61K45/06 ,  A61P35/00 ,  A61P35/02 ,  C07K14/05 ,  C07K16/2818 ,  C07K16/2827 ,  C12N15/85 ,  A61K2039/505 ,  A61K2039/507 ,  C07K2317/20 ,  C07K2317/21 ,  C07K2317/24 ,  C07K2317/31 ,  C07K2317/32 ,  C07K2317/33 ,  C07K2317/34 ,  C07K2317/40 ,  C07K2317/41 ,  C07K2317/52 ,  C07K2317/54 ,  C07K2317/55 ,  C07K2317/56 ,  C07K2317/565 ,  C07K2317/567 ,  C07K2317/569 ,  C07K2317/60 ,  C07K2317/622 ,  C07K2317/73 ,  C07K2317/732 ,  C07K2317/74 ,  C07K2317/76 ,  C07K2317/92 ,  C12N2015/8518

Abstract: The present disclosure provides antibody sequences found in antibodies that bind to human CD25, in particular an anti CD25-a-674 antibody which do not block the binding of CD25 to IL-2 or IL-2 signalling. The claimed antibody binds to the epitopes: YQCVQGYRALHRGP (150 to 163) or SVCKMTHGKTRWTQP (166 to 180) on CD25 Antibodies and antigen-binding portions thereof including such sequences can be used in pharmaceutical compositions and methods of treatment, in particular for treating cancer.

公开(公告)号：US20240011037A1

公开(公告)日：2024-01-11

申请号：US18254324

申请日：2021-11-24

Applicant: CANCER RESEARCH TECHNOLOGY LIMITED

Inventor： Monika Gullerova

IPC: C12N15/113 ,  C12N9/22 ,  A61P35/00

CPC classification number: C12N15/1135 ,  C12N9/22 ,  C12Y301/26003 ,  A61P35/00 ,  C12N2310/531 ,  C12N2310/14 ,  C12N2320/31

Abstract: The present invention relates to a method of inhibiting expression of a gene in a biological system. The method of the present invention comprises introducing a tRNA-derived polynucleotide into the biological system. The tRNA-derived polynucleotide of 5 the present invention comprises a sequence that is complementary to an intronic region or exonic region of the gene whose expression is to be inhibited.

公开(公告)号：US11753405B2

公开(公告)日：2023-09-12

申请号：US17231164

申请日：2021-04-15

Applicant: Cancer Research Technology Limited

Inventor： Johannes Wilhelmus Maria Nissink ,  Maurice Raymond Verschoyle Finlay ,  Mark David Charles

IPC: C07D417/14

CPC classification number: C07D417/14

Abstract: A compound of Formula (I):




or a pharmaceutically acceptable salt thereof, where: Q can be 1,2,4-triazin-3-yl, pyridazin-3-yl, 6-methylpyridazin-3-yl, or 6-fluoropyridazin-3-yl; R1 can be hydrogen, methoxy, trifluoromethoxy, oxetan-3-yl, 3-fluoroazetidin-1-yl, 3-methoxyazetidin-1-yl, or 3,3-difluoroazetidin-1-yl; R2 can be hydrogen or fluoro; R3 can be hydrogen or methoxy; and R4 can be methoxy, ethoxy, or methoxymethyl; provided that when R1 is hydrogen, methoxy or trifluoromethoxy, then R3 is not hydrogen, and/or R4 is methoxymethyl. The compound of formula (I) can inhibit glutaminase, e.g., GLS1.

公开(公告)号：US11697688B2

公开(公告)日：2023-07-11

申请号：US16979935

申请日：2019-03-13

Applicant: Tusk Therapeutics Ltd. ,  Cancer Research Technology Limited

Inventor： Anne Goubier ,  Beatriz Goyenechea Corzo ,  Josephine Salimu ,  Kevin Moulder ,  Pascal Merchiers ,  Mark Brown ,  James Geoghegan ,  Bianka Prinz ,  Sergio Quezada

IPC: C07K16/28 ,  A61P35/02 ,  C12N15/85 ,  A61P35/00 ,  A61K39/395 ,  C07K14/55 ,  A61K45/06 ,  A61K39/00

CPC classification number: C07K16/2866 ,  A61K39/39533 ,  A61K39/39541 ,  A61K39/39558 ,  A61K39/39566 ,  A61K45/06 ,  A61P35/00 ,  A61P35/02 ,  C07K14/55 ,  C07K16/2818 ,  C07K16/2827 ,  C12N15/85 ,  A61K2039/505 ,  A61K2039/507 ,  C07K2317/20 ,  C07K2317/21 ,  C07K2317/24 ,  C07K2317/31 ,  C07K2317/32 ,  C07K2317/33 ,  C07K2317/34 ,  C07K2317/40 ,  C07K2317/41 ,  C07K2317/52 ,  C07K2317/54 ,  C07K2317/55 ,  C07K2317/56 ,  C07K2317/565 ,  C07K2317/567 ,  C07K2317/569 ,  C07K2317/60 ,  C07K2317/622 ,  C07K2317/73 ,  C07K2317/732 ,  C07K2317/74 ,  C07K2317/76 ,  C07K2317/92 ,  C12N2015/8518

Abstract: The present disclosure provides antibody sequences found in antibodies that bind to human CD25, in particular an anti CD25-a-674 antibody which do not block the binding of CD25 to IL-2 or IL-2 signalling. The claimed antibody binds to the epitopes: QCVQGYRA and RWTQPQLICTG on CD25 Antibodies and antigen-binding portions thereof including such sequences can be used in pharmaceutical compositions and methods of treatment, in particular for treating cancer.