公开(公告)号：US20190194731A1

公开(公告)日：2019-06-27

申请号：US16327847

申请日：2017-08-23

Applicant: Cancer Research Technology Limited

Inventor： John Burn ,  Mohammed Ghanim Mehdi Alhilal ,  Franscisco Mauro Santibanez-Koref ,  Lisa Redford ,  Michael Stewart Jackson

IPC: C12Q1/6827 ,  C12Q1/6869

CPC classification number: C12Q1/6827 ,  C12Q1/6869 ,  C12Q2535/119

Abstract: The present invention relates to methods and kits for identifying microsatellite instability (MSI) in a sample. In particular it relates to identifying microsatellite instability in a tumor sample, which may be from a subject suspected of having colorectal cancer or Lynch syndrome. The methods and kits can be used to identify mismatch repair defects. More particularly the invention relates to a panel of markers for a sequencing based MSI test, that can differentiate between MSI-H and MSS CRCs. The invention also allows for determination of biological significance, differentiating between PCR and sequencing errors and MSI induced indels/mutations.

公开(公告)号：US20190169172A1

公开(公告)日：2019-06-06

申请号：US16266361

申请日：2019-02-04

Applicant: AstraZeneca AB ,  Cancer Research Technology Limited

Inventor： Maurice Raymond Verschoyle Finlay

IPC: C07D403/14

Abstract: A compound of Formula (I): or a pharmaceutically where R1 can be hydro, methoxy, difluoromethoxy or trifluoromethoxy; R2 can be hydro, methoxy, trifluoromethoxy or trifluoromethyl; and R3 can be hydro or methoxy. The compound of formula (I) can inhibit glutaminase, e.g., GLS1.

公开(公告)号：US20180305349A1

公开(公告)日：2018-10-25

申请号：US16025455

申请日：2018-07-02

Applicant: AstraZeneca AB ,  Cancer Research Technology Limited

Inventor： Maurice Raymond Verschoyle Finlay ,  Chukuemeka Tennyson Ekwuru ,  Mark David Charles ,  Piotr Antoni Raubo ,  Jonathan James Gordon Winter ,  Johannes Wilhelmus Maria Nissink

IPC: C07D417/14 ,  C07B59/00

CPC classification number: C07D417/14 ,  C07B59/002 ,  C07B2200/05 ,  C07B2200/13

Abstract: The specification relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, where Q, R, R1 and R2 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent GLS1 mediated disease, including cancer. The specification further relates to crystalline forms of compounds of Formula (I) and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating GLS1 kinase mediated disease, including cancer, using such compounds and salts.

公开(公告)号：US10017576B2

公开(公告)日：2018-07-10

申请号：US15040375

申请日：2016-02-10

Applicant: Københavns Universitet ,  Cancer Research Technology Limited

Inventor： Henrik Clausen ,  Joy Burchell ,  Ulla Mandel ,  Anne Louise Sørensen ,  Mads Agervig Tarp ,  Joyce Taylor-Papadimitriou

IPC: C40B50/06 ,  C07K16/28 ,  A61K39/00 ,  C07K14/47 ,  C07K16/30 ,  G01N33/574 ,  G01N33/68 ,  A61K47/64 ,  C40B30/04

CPC classification number: C07K16/2896 ,  A61K39/0011 ,  A61K47/646 ,  A61K2039/5154 ,  A61K2039/5158 ,  A61K2039/6031 ,  A61K2039/6037 ,  A61K2039/6075 ,  A61K2039/6081 ,  C07K14/4727 ,  C07K16/28 ,  C07K16/30 ,  C07K16/3092 ,  C07K2317/14 ,  C07K2317/34 ,  C07K2317/76 ,  C40B30/04 ,  C40B50/06 ,  G01N33/574 ,  G01N33/6854 ,  Y02A50/412

Abstract: The present invention provides a method for inducing a cancer specific immune response against MUC1 using an immunogenic glycopeptide. Other aspects of the invention are a pharmaceutical composition comprising the immunogenic glycopeptide and a cancer vaccine comprising the immunogenic glycopeptide. Another aspect is an antibody generated using the immunogenic glycopeptide and the use of said antibody in therapy and diagnosis.

公开(公告)号：US20180170911A1

公开(公告)日：2018-06-21

申请号：US15512661

申请日：2015-09-18

Applicant: CANCER RESEARCH TECHNOLOGY LIMITED

Inventor： Tristan REUILLON ,  Duncan MILLER ,  Stephanie MYERS ,  Lauren MOLYNEUX ,  Celine CANO ,  Ian HARDCASTLE ,  Roger GRIFFIN ,  Laurent RIGOREAU ,  Bernard GOLDING ,  Martin NOBLE

IPC: C07D403/12 ,  C07D401/14 ,  C07D413/14 ,  C07D413/12 ,  C07D405/14 ,  C07D401/12 ,  C07D403/14 ,  A61P35/00

CPC classification number: C07D403/12 ,  A61P35/00 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14

Abstract: The invention provides compounds of formula (I) or a tautomer, stereoisomer, N-oxide, pharmaceutically acceptable salt or solvate thereof. The compounds are useful for the prophylaxis or treatment of a disease state or condition mediated by ERK5, in particular cancers.

公开(公告)号：US20180118684A1

公开(公告)日：2018-05-03

申请号：US15715900

申请日：2017-09-26

Applicant: CANCER RESEARCH TECHNOLOGY LIMITED

Inventor： Bernard Thomas GOLDING ,  Christiane RIEDINGER ,  Roger John GRIFFIN ,  Ian Robert HARDCASTLE ,  Eric VALEUR ,  Anna Frances WATSON ,  Martin NOBLE

IPC: C07D209/49 ,  A61K45/06 ,  A61K31/4402 ,  C07D209/48 ,  C07D403/06 ,  C07D401/06 ,  A61K31/4035

CPC classification number: C07D209/49 ,  A61K31/4035 ,  A61K31/4402 ,  A61K45/06 ,  C07D209/48 ,  C07D401/06 ,  C07D403/06

Abstract: A compound of formula (I) or a compound of formula (II) or pharmaceutically acceptable salts thereof, wherein R1-R7 and X are as defined in the description, and the use of these compounds in therapy, in particular in treating cancer or as an inhibitor of the interaction of the MDM2 protein with p53.

公开(公告)号：US09938265B2

公开(公告)日：2018-04-10

申请号：US15363018

申请日：2016-11-29

Applicant: AstraZeneca AB ,  Cancer Research Technology Limited

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

IPC: C07D417/14

CPC classification number: C07D417/14 ,  A61K31/501 ,  A61K31/53

Abstract: A compound of Formula (I): or a pharmaceutically acceptable salt thereof, where: Q can be 5-methylpyridazin-3-yl,5-chloropyridazin-3-yl, 6-methylpyridazin-3-yl, or 6-fluoropyridazin-3-yl; R can be hydrogen, fluoro, or methoxy; R1 can be hydrogen, methoxy, difluoromethoxy, or trifluoromethoxy; and R2 can be methyl or ethyl. The compound of formula (I) can inhibit glutaminase, e.g., GLS1.

公开(公告)号：US20180093955A1

公开(公告)日：2018-04-05

申请号：US15563501

申请日：2016-04-01

Applicant: Cancer Research Technology Limited

Inventor： Keith Jones ,  Matthew Cheeseman ,  Nicola Chessum ,  Elise Pasqua ,  Lindsay Evans ,  Michael Tucker ,  Birgit Wilding ,  Ngal Yi Mok

IPC: C07D215/48 ,  C07D405/12

CPC classification number: C07D215/48 ,  C07D405/12

Abstract: The present invention relates to compounds of formula I wherein R, R4 and Q are each as defined herein. The compounds of the present invention are inhibitors of heat shock factor 1 pathway (HSF1 pathway). 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：US09834552B2

公开(公告)日：2017-12-05

申请号：US15091980

申请日：2016-04-06

Applicant: Cancer Research Technology Limited

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

IPC: A01N43/90 ,  A61K31/519 ,  C07D471/04 ,  C07D401/14 ,  C07D413/14 ,  C07D401/04 ,  C07D405/04 ,  C07D519/00

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：US09834541B2

公开(公告)日：2017-12-05

申请号：US14437561

申请日：2013-10-02

Applicant: Merck Patent GmbH ,  CANCER RESEARCH TECHNOLOGY LIMITED

Inventor： Kai Schiemann ,  Frank Stieber ,  Julian Blagg ,  Aurelie Mallinger ,  Dennis Waalboer ,  Christian Rink ,  Simon Ross Crumpler

IPC: C07D471/10 ,  A61K31/444 ,  A61K31/4545 ,  C07D401/04 ,  C07D401/14 ,  A61K31/5377 ,  A61K31/499 ,  A61K31/4709 ,  C07D417/14 ,  C07D491/10 ,  C07D498/10

CPC classification number: C07D401/14 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/499 ,  A61K31/5377 ,  C07D401/04 ,  C07D417/14 ,  C07D471/10 ,  C07D491/10 ,  C07D498/10

Abstract: The invention provides novel substituted 2-aminopyridine compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases such as cancer, inflammatory or degenerative diseases.