Expansion of MRCTs Drug Discovery Group (DDG)
Lead Research Organisation:
LifeArc
Department Name: UNLISTED
Abstract
Abstracts are not currently available in GtR for all funded research. This is normally because the abstract was not required at the time of proposal submission, but may be because it included sensitive information such as personal details.
Technical Summary
To expand and enhance MRCTs successful early stage drug discovery resource, in order to provide capacity to engage effectively with the MRC extramural programme in drug (and biological) development funded through the MRCs Developmental Pathway Funding Scheme (DPFS).
Organisations
- LifeArc (Lead Research Organisation)
- University of Regensburg (Collaboration)
- University of Warwick (Collaboration)
- University of Laval (Collaboration)
- QUEEN MARY UNIVERSITY OF LONDON (Collaboration)
- AstraZeneca (Collaboration)
- UNIVERSITY OF EDINBURGH (Collaboration)
- Netherlands Cancer Institute (NKI) (Collaboration)
- UNIVERSITY OF ABERDEEN (Collaboration)
- University of Sheffield (Collaboration)
- Cardiff University (Collaboration)
- University of Hong Kong (Collaboration)
- Intellect Neurosciences, Inc. (Collaboration)
- Medical Research Council (MRC) (Collaboration)
- GlaxoSmithKline (GSK) (Collaboration)
- Mount Sinai Hospital (USA) (Collaboration)
- Beatson Institute for Cancer Research (Collaboration)
- BioArctic Neuroscience (Collaboration)
- University of Bristol (Collaboration)
- University of Lausanne (Collaboration)
- University College London (Collaboration)
- DiscoveRx (Collaboration)
- IMPERIAL COLLEGE LONDON (Collaboration)
- UNIVERSITY OF OXFORD (Collaboration)
- Georgetown University (Collaboration)
- University of Sussex (Collaboration)
- London School of Hygiene and Tropical Medicine (LSHTM) (Collaboration)
- UNIVERSITY OF DUNDEE (Collaboration)
People |
ORCID iD |
Justin Bryans (Principal Investigator) |
Publications
Antonios G
(2015)
Alzheimer therapy with an antibody against N-terminal Abeta 4-X and pyroglutamate Abeta 3-X.
in Scientific reports
Chapman TM
(2015)
N-Hydroxyimides and hydroxypyrimidinones as inhibitors of the DNA repair complex ERCC1-XPF.
in Bioorganic & medicinal chemistry letters
Chapman TM
(2015)
Catechols and 3-hydroxypyridones as inhibitors of the DNA repair complex ERCC1-XPF.
in Bioorganic & medicinal chemistry letters
Chapman TM
(2014)
Optimization of an imidazopyridazine series of inhibitors of Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1).
in Journal of medicinal chemistry
Chapman TM
(2012)
Substituted aminopyrimidine protein kinase B (PknB) inhibitors show activity against Mycobacterium tuberculosis.
in Bioorganic & medicinal chemistry letters
Chapman TM
(2013)
Substituted imidazopyridazines are potent and selective inhibitors of Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1).
in Bioorganic & medicinal chemistry letters
Clark A
(2016)
ACTH Antagonists
in Frontiers in Endocrinology
Clark K
(2011)
Novel cross-talk within the IKK family controls innate immunity.
in The Biochemical journal
De La Roche M
(2012)
An intrinsically labile a-helix abutting the BCL9-binding site of ß-catenin is required for its inhibition by carnosic acid
in Nature Communications
Goncalves V
(2012)
Discovery of Plasmodium vivax N-myristoyltransferase inhibitors: screening, synthesis, and structural characterization of their binding mode.
in Journal of medicinal chemistry
Hall G
(2016)
Structure of a Potential Therapeutic Antibody Bound to Interleukin-16 (IL-16): MECHANISTIC INSIGHTS AND NEW THERAPEUTIC OPPORTUNITIES.
in The Journal of biological chemistry
Huart AS
(2013)
A Casein kinase 1/Checkpoint kinase 1 pyrazolo-pyridine protein kinase inhibitor as novel activator of the p53 pathway.
in Bioorganic & medicinal chemistry letters
Jenkins L
(2012)
Antagonists of GPR35 display high species ortholog selectivity and varying modes of action.
in The Journal of pharmacology and experimental therapeutics
Large JM
(2013)
Imidazopyridazines as potent inhibitors of Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1): Preparation and evaluation of pyrazole linked analogues.
in Bioorganic & medicinal chemistry letters
Lessl M
(2011)
Crowd sourcing in drug discovery.
in Nature reviews. Drug discovery
Lougheed KE
(2011)
Effective inhibitors of the essential kinase PknB and their potential as anti-mycobacterial agents.
in Tuberculosis (Edinburgh, Scotland)
McMahon RM
(2011)
Structure of HLA-A*0301 in complex with a peptide of proteolipid protein: insights into the role of HLA-A alleles in susceptibility to multiple sclerosis.
in Acta crystallographica. Section D, Biological crystallography
McNeil EM
(2015)
Inhibition of the ERCC1-XPF structure-specific endonuclease to overcome cancer chemoresistance.
in DNA repair
Meadows NA
(2011)
A high-throughput assay for modulators of NNT activity in permeabilized yeast cells.
in Journal of biomolecular screening
Neetoo-Isseljee Z
(2013)
High-throughput identification and characterization of novel, species-selective GPR35 agonists.
in The Journal of pharmacology and experimental therapeutics
Pierrat OA
(2011)
Monocyclic ß-lactams are selective, mechanism-based inhibitors of rhomboid intramembrane proteases.
in ACS chemical biology
Smith H
(2011)
The role of TBK1 and IKKe in the expression and activation of Pellino 1.
in The Biochemical journal
Southern C
(2013)
Screening ß-arrestin recruitment for the identification of natural ligands for orphan G-protein-coupled receptors.
in Journal of biomolecular screening
Vinothkumar KR
(2013)
Structure of rhomboid protease in complex with ß-lactam inhibitors defines the S2' cavity.
in Structure (London, England : 1993)
White R
(2013)
Identification of small-molecule inhibitors of the ribonuclease H2 enzyme.
in Journal of biomolecular screening
Wright PD
(2015)
A High-Throughput Electrophysiology Assay Identifies Inhibitors of the Inwardly Rectifying Potassium Channel Kir7.1.
in Journal of biomolecular screening
Description | Biomedical Catalyst |
Amount | £587,000 (GBP) |
Organisation | Innovate UK |
Sector | Public |
Country | United Kingdom |
Start | 01/2013 |
End | 12/2016 |
Description | DPFS |
Amount | £525,000 (GBP) |
Organisation | Medical Research Council (MRC) |
Sector | Public |
Country | United Kingdom |
Start | 08/2010 |
Description | DPFS |
Amount | £170,000 (GBP) |
Organisation | Medical Research Council (MRC) |
Sector | Public |
Country | United Kingdom |
Start |
Description | Michael J Fox Foundation |
Amount | £70,000 (GBP) |
Organisation | Michael J Fox Foundation |
Sector | Charity/Non Profit |
Country | United States |
Start | 07/2011 |
End | 12/2011 |
Title | Alphavbeta6 |
Description | Alphavbeta6 humanised antibody |
Type Of Material | Antibody |
Year Produced | 2011 |
Provided To Others? | Yes |
Impact | Potential partnering event |
Title | Biotinylated guanabenz |
Description | Biotinylated guanabenz |
Type Of Material | Technology assay or reagent |
Year Produced | 2010 |
Provided To Others? | Yes |
Impact | Used for target identification and association. Results pending |
Title | CCR2 |
Description | Humanised antibody |
Type Of Material | Antibody |
Provided To Others? | No |
Impact | Potential partnering event |
Title | CDPK1 |
Description | Small molecule ligands |
Type Of Material | Technology assay or reagent |
Provided To Others? | No |
Impact | Publications and further disection of pathway |
Title | FPR2 agonist |
Description | Two literature FPR2 agonists |
Type Of Material | Technology assay or reagent |
Year Produced | 2010 |
Provided To Others? | Yes |
Impact | Target validation and disease association - ongoing |
Title | Gpr35 antagonists |
Description | Three literature Gpr35 antagonists |
Type Of Material | Technology assay or reagent |
Year Produced | 2010 |
Provided To Others? | Yes |
Impact | Used for disease association, results pending. |
Title | Migrastatin analogues |
Description | Migrastatin analogues |
Type Of Material | Technology assay or reagent |
Year Produced | 2010 |
Provided To Others? | Yes |
Impact | Target validation and disease association. Results pending |
Title | MurC compounds |
Description | Two literature MurC compounds |
Type Of Material | Technology assay or reagent |
Year Produced | 2011 |
Provided To Others? | Yes |
Impact | Target validation and co-crystallisation studies - ongoing |
Title | NK1 agonist |
Description | Literature NK1 antagonist |
Type Of Material | Technology assay or reagent |
Year Produced | 2010 |
Provided To Others? | Yes |
Impact | Material used for pathway validation. Results pending |
Title | PKG compounds |
Description | Two PfPKG inhibitors provided |
Type Of Material | Technology assay or reagent |
Year Produced | 2010 |
Provided To Others? | Yes |
Impact | Target validation - ongoing |
Title | PNKP Weinfeld compound |
Description | PNKP inhibitor published by Weinfeld et al. |
Type Of Material | Technology assay or reagent |
Year Produced | 2010 |
Provided To Others? | Yes |
Impact | Used to see if it was a good inhibitor of PNKP and for mechanistic studies. Our research identified it is not a very good inhibitor and is non-selective, hitting a wide range of kinases from the PPU panel. |
Title | PROKR1 antagonists |
Description | Six different PROKR1 antagonists were made from literature exaples |
Type Of Material | Technology assay or reagent |
Year Produced | 2010 |
Provided To Others? | Yes |
Impact | Used for target validationa dn diseae association. Work is ongoing but initial results look to be linking PROKR1 to a specific disease of interest. |
Description | ALK |
Organisation | Georgetown University |
Country | United States |
Sector | Academic/University |
PI Contribution | Antibody humanisation |
Collaborator Contribution | Antibody generation |
Impact | Ongoing |
Start Year | 2012 |
Description | APP/beta secretase |
Organisation | Cardiff University |
Country | United Kingdom |
Sector | Academic/University |
PI Contribution | Antibody generation and humanisation |
Collaborator Contribution | Assays and reagents |
Impact | Ongoing |
Start Year | 2010 |
Description | Anti-amyoid (AD) antibody humanisation |
Organisation | Intellect Neurosciences, Inc. |
Country | United States |
Sector | Private |
PI Contribution | Humanisation and optimisation of antibodies |
Impact | Antibodies humanised succesfully |
Start Year | 2009 |
Description | C5L2/Asp1 |
Organisation | University of Laval |
Country | Canada |
Sector | Academic/University |
PI Contribution | Antibody generation and humanisation |
Collaborator Contribution | Expertise and reagents |
Impact | Antibody humanisation |
Start Year | 2010 |
Description | CCR2 |
Organisation | University of Regensburg |
Country | Germany |
Sector | Academic/University |
PI Contribution | Humanisation of antibodies |
Collaborator Contribution | Provision of mouse antibodies and assays |
Impact | Ongoing |
Start Year | 2010 |
Description | CTLA4 |
Organisation | University of Aberdeen |
Country | United Kingdom |
Sector | Academic/University |
PI Contribution | Assay development |
Collaborator Contribution | Provision of reagents |
Impact | Robust assay |
Start Year | 2010 |
Description | ERCC1 |
Organisation | University of Edinburgh |
Country | United Kingdom |
Sector | Academic/University |
PI Contribution | Screening and medicinal chemistry |
Collaborator Contribution | secondary assays and target validation |
Impact | Identification of hit molecules |
Start Year | 2012 |
Description | EV71 |
Organisation | University of Hong Kong |
Country | Hong Kong |
Sector | Academic/University |
PI Contribution | Humanisation and optimisation of antibody |
Collaborator Contribution | In vitro and in vivo testing |
Impact | Antibody for partnering |
Start Year | 2015 |
Description | FPR2 |
Organisation | Queen Mary University of London |
Country | United Kingdom |
Sector | Academic/University |
PI Contribution | Assay development and screening. |
Collaborator Contribution | Expertise and reagents |
Impact | Assays developed. Full drug discovery collaboration - biology, chemistry, pharmacology |
Start Year | 2010 |
Description | Fascin |
Organisation | Beatson Institute for Cancer Research |
Country | United Kingdom |
Sector | Academic/University |
PI Contribution | HTS screening versus target, hit validation and medicinal chemistry |
Collaborator Contribution | Fragment screening and supporting biology |
Impact | Ongoing |
Start Year | 2010 |
Description | GPCR Deorphanisation |
Organisation | DiscoveRx |
Country | United States |
Sector | Private |
PI Contribution | Screening and validation of hits versus 90 orphan GPCRS |
Collaborator Contribution | Provision of ligand library and screening capabilityProvision of cell lines for screening |
Impact | Deorphanised GPCR 88 and 35. GPRR88 subject of succesful MJFF grant. |
Start Year | 2009 |
Description | GPCR Deorphanisation |
Organisation | GlaxoSmithKline (GSK) |
Country | Global |
Sector | Private |
PI Contribution | Screening and validation of hits versus 90 orphan GPCRS |
Collaborator Contribution | Provision of ligand library and screening capabilityProvision of cell lines for screening |
Impact | Deorphanised GPCR 88 and 35. GPRR88 subject of succesful MJFF grant. |
Start Year | 2009 |
Description | GalR2-ADC |
Organisation | University of Bristol |
Country | United Kingdom |
Sector | Academic/University |
PI Contribution | Generation of GalR2 antibody drug conjugate |
Collaborator Contribution | Biology expertise |
Impact | Generation of novel GalR2 based ADC |
Start Year | 2013 |
Description | IL-16 |
Organisation | Mount Sinai Hospital (USA) |
Country | United States |
Sector | Hospitals |
PI Contribution | Antibody humnisation |
Collaborator Contribution | antibody generation |
Impact | Publication and poster |
Start Year | 2012 |
Description | IL17BR |
Organisation | Medical Research Council (MRC) |
Department | MRC Laboratory of Molecular Biology (LMB) |
Country | United Kingdom |
Sector | Academic/University |
PI Contribution | Humanisation and affinity maturation of a potent antibody |
Collaborator Contribution | Animal models and biology expertise |
Impact | Generation of a potent antibody plus supporting in vivo data for partnering |
Start Year | 2012 |
Description | Integrin alpha v beta 6 |
Organisation | University College London |
Country | United Kingdom |
Sector | Academic/University |
PI Contribution | Antibody generation and humanisation |
Collaborator Contribution | Expertise and reagents |
Impact | Humanised antibody for partnering |
Start Year | 2010 |
Description | MALT1 |
Organisation | University of Lausanne |
Country | Switzerland |
Sector | Academic/University |
PI Contribution | Assay development and screening |
Collaborator Contribution | Biology expertise |
Impact | Development of HTS assay |
Start Year | 2014 |
Description | MC2 |
Organisation | Queen Mary University of London |
Country | United Kingdom |
Sector | Academic/University |
PI Contribution | Drug discovery expertise, assay development and screening |
Collaborator Contribution | Expertise and reagents |
Impact | Ongoing |
Start Year | 2010 |
Description | MC3 |
Organisation | Queen Mary University of London |
Country | United Kingdom |
Sector | Academic/University |
PI Contribution | Assay development, screening and small molecule ligand ID |
Collaborator Contribution | Expertise and reagents |
Impact | ID of novel chemical series which were partnered with a major Pharma company |
Start Year | 2010 |
Description | MCR2 |
Organisation | Queen Mary University of London |
Country | United Kingdom |
Sector | Academic/University |
PI Contribution | Assay development, screening and medicinal chemistry |
Collaborator Contribution | Biology expertise |
Impact | Identification of novel small molecule ligands |
Start Year | 2013 |
Description | MNK1 |
Organisation | AstraZeneca |
Country | United Kingdom |
Sector | Private |
PI Contribution | Medicinal chemistry and primary screening |
Collaborator Contribution | Secondary assays and phrmacology |
Impact | Research collaboration |
Start Year | 2011 |
Description | Mouse hybridomas |
Organisation | BioArctic Neuroscience |
Country | Sweden |
Sector | Private |
PI Contribution | Raising and humanisation of mouse antibodies |
Impact | Antibodies raised and humanised |
Start Year | 2009 |
Description | Nicastrin |
Organisation | Imperial College London |
Country | United Kingdom |
Sector | Academic/University |
PI Contribution | Antibody humanisation |
Collaborator Contribution | Antibody generation |
Impact | Ongoing |
Start Year | 2012 |
Description | Novel Anti-malarial agents |
Organisation | London School of Hygiene and Tropical Medicine (LSHTM) |
Country | United Kingdom |
Sector | Academic/University |
PI Contribution | Assay development, screening and medicinal chemistry to support a drug discovery programme |
Collaborator Contribution | The collaborator is an expert in his field and has in depth knowledge of the target as well as secondary assays to support a drug discovery programme. Note that the £525,000 finacial contribution is from a succesful DPFS application. This will be offset against the £5m grant. |
Impact | Successful DPFS grant application. Multidisciplinary invoilving, biology, chemistry, pharmacology, ADME. |
Start Year | 2009 |
Description | Novel anti-bacterial compounds |
Organisation | University of Warwick |
Country | United Kingdom |
Sector | Academic/University |
PI Contribution | Assay development, screening and medicinal chemistry for a full drug discovery programme. |
Collaborator Contribution | Provision of protein production and crystallography. Expert knowledge of target - experts in the field. Secondary assays. |
Impact | DPFS application - invited to Full Application which has yet to be reviewed by the Panel. Multidisciplinary involving biology, chemistry, pharmacology and ADME |
Start Year | 2009 |
Description | Novel anti-cancer agents |
Organisation | University of Sussex |
Country | United Kingdom |
Sector | Academic/University |
PI Contribution | Provision of assay development, screening and chemistry resources to support a drug discovery programme |
Collaborator Contribution | Our collaborator has brought a wealth of expertise and relevant knowledge to the porogramme as well as direct experience of the target in question and he is an opinion leader in his field. |
Impact | This programme has directly produced a collaboration with AZ (see Screening Compounds collaboration). Screening is ongoing to identify plausible hits for drug discovery. Multidisciplinary invoilving, biology, chemistry, pharmacology, ADME. |
Start Year | 2010 |
Description | PAICS |
Organisation | Netherlands Cancer Institute (NKI) |
Country | Netherlands |
Sector | Academic/University |
PI Contribution | Screening and development of potent selective inhibitors |
Collaborator Contribution | In vitro and in vivo testing |
Impact | Small molecule inhibitors |
Start Year | 2014 |
Description | PAICS |
Organisation | Netherlands Cancer Institute (NKI) |
Country | Netherlands |
Sector | Academic/University |
PI Contribution | Screening and medicinal chemistry |
Collaborator Contribution | Secondary assays and target validation |
Impact | Hit structures for optimisation |
Start Year | 2012 |
Description | PfCDPK1 |
Organisation | Medical Research Council (MRC) |
Department | MRC National Institute for Medical Research (NIMR) |
Country | United Kingdom |
Sector | Academic/University |
PI Contribution | Discovery of new PfCDPK1 |
Collaborator Contribution | Identification of novel CDPK1 inhibnitors |
Impact | Publications |
Start Year | 2011 |
Description | PfPKG |
Organisation | London School of Hygiene and Tropical Medicine (LSHTM) |
Country | United Kingdom |
Sector | Academic/University |
PI Contribution | DIscovery of novel small molecule inhibitors of PfPKG |
Collaborator Contribution | Provision of in vitro and in vivo testing |
Impact | Publications and patent |
Start Year | 2011 |
Description | Screening Libraries |
Organisation | AstraZeneca |
Country | United Kingdom |
Sector | Private |
PI Contribution | Provision of screens and reagents plus personnel to run screens and validate hits |
Collaborator Contribution | Provision of 100,000 compounds in screening ready plates for screening versus up to 10 biochemical targets, 5 selected by AZ and 5 by MRCT. |
Impact | To date three targets has been selected for screening by AZ. Multidisciplinary invoilving, biology, chemistry, pharmacology, ADME. |
Start Year | 2010 |
Description | TPL2 |
Organisation | Medical Research Council (MRC) |
Department | MRC National Institute for Medical Research (NIMR) |
Country | United Kingdom |
Sector | Academic/University |
PI Contribution | Assay development and screening |
Collaborator Contribution | Biology and reagents |
Impact | Development of a novel screen protocol |
Start Year | 2013 |
Description | Transglutaminase 2 |
Organisation | University of Sheffield |
Country | United Kingdom |
Sector | Academic/University |
PI Contribution | Drug discovery, assay development, screening |
Collaborator Contribution | EXpertise and reagents |
Impact | We have partnered the project and a potential drug to a major Pharma company. The asset has just completed Ph I studies. |
Start Year | 2010 |
Description | ULK |
Organisation | University of Dundee |
Country | United Kingdom |
Sector | Academic/University |
PI Contribution | Screening and medicinal chemistry |
Collaborator Contribution | Secndary assays and target validation |
Impact | None yet |
Start Year | 2013 |
Description | VCAM-1 |
Organisation | University of Oxford |
Country | United Kingdom |
Sector | Academic/University |
PI Contribution | Antibody generation |
Collaborator Contribution | Provision of expertise and assays |
Impact | Successful DPFS application |
Start Year | 2009 |
Description | iC3b |
Organisation | University College London |
Country | United Kingdom |
Sector | Academic/University |
PI Contribution | Drug discovery capapability and expertise. |
Collaborator Contribution | Expertise and reagents |
Impact | Ongoing |
Start Year | 2010 |
Title | COMPOUNDS |
Description | A compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, wherein R1 is selected from: aryl; heteroaryl; -NHR3; fused aryl-C4-7-heterocycloalkyI; -CONR4R5; -NHCOR6; -C3-7-cycloalkyl; -O-C3-7-cycloalkyl; -NR3R6; and optionally substituted -C1-6 alkyl; wherein said aryl, heteroaryl, fused aryl-C4-7-heterocycloalkyl and C4-7-heterocycloalkyl are each optionally substituted; R2 is selected from hydrogen, aryl, C1-6-alkyl, C2-6-alkenyl, C3-7-cycloalkyl, heteroaryl, C4-7 heterocycloalkyl and halogen, wherein said C1-6-alkyl, C2-6-alkenyl, aryl, heteroaryl and C4-7-heterocycloalkyl are each optionally substituted. Further aspects relate to pharmaceutical compositions, therapeutic uses and process for preparing compounds of formula (I). |
IP Reference | WO2010106333 |
Protection | Patent application published |
Year Protection Granted | 2010 |
Licensed | Commercial In Confidence |
Impact | First known selective inhibitor of this kinase |
Title | HEPATITIS C VIRUS COMBINATION THERAPY |
Description | The present invention relates to methods and compositions for the treatment or prevention of hepatitis C virus comprising the administration of a combination of anti-hepatitis C virus antibodies and a -interferon. |
IP Reference | WO2010080528 |
Protection | Patent application published |
Year Protection Granted | 2010 |
Licensed | Commercial In Confidence |
Impact | New antibodies for treating disease |
Title | MC3 |
Description | Identification of novel small molecule ligands |
IP Reference | |
Protection | Protection not required |
Year Protection Granted | 2014 |
Licensed | Commercial In Confidence |
Impact | Identification of novel small molecule ligands to support candidate seeking programme |
Title | PYRIMIDINE DERIVATIVES CAPABLE OF INHIBITING ONE OR MORE KINASES |
Description | A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, formula (I): wherein: R1 is C3-8-cycloalkyl; X is O, NR7 or C3-6-heterocycloalkyl; R2 is aryl, heteroaryl, fused or unfused aryl-C3-6-heterocycloalkyl or fused or unfused heteroaryl-C3-6-heterocycIoalkyl, each of which is optionally substituted by one or more substitutents selected from aryl, heteroaryl, C1-6-alkyl, C3-7-cycloalkyl and a group A, wherein said C1-6-alkyl group is optionally substituted by one or more substituents selected from aryl, heteroaryl, R10 and a group A, said heteroaryl group is optionally substituted by one or more R10 groups; and wherein said C3-6-heterocycloalkyl group optionally contains one or more groups selected from oxygen, sulfur, nitrogen and CO; R3 is C1-6-alkyl optionally substituted by one or more substituents selected from aryl, heteroaryl, -NR4R5, -OR6, -NR7(CO)R6, -NR7(CO)NR4R5, -NR7SO2R6, -NR7COOR7, -CONR4R5, C3-6-heterocycloalkyl and formula (a, b, c): wherein R4-7 and A are as defined in the claims. Further aspects relate to the use of said compounds in the treatment of various therapeutic disorders, and more particularly as inhibitors of one or more kinases. |
IP Reference | WO2009122180 |
Protection | Patent application published |
Year Protection Granted | 2009 |
Licensed | No |
Impact | Selective tool compounds for disease association studies |
Title | PYRROLOPYRIMIDINES USED AS KINASE INHIBITORS |
Description | The invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, wherein: R1 is -NR7(CO)R11; R2 is aryl, heteroaryl, fused aryl-C3-6-heterocycloalkyl or fused heteroaryl-C3-6- heterocycloalkyl, each of which is optionally substituted; each R7 is selected from hydrogen, C1-6-alkyl and C3-7-cycloalkyl, wherein said C1-6-alkyl is optionally substituted by one or more halogens; each R11 is independently selected from C1-6-alkyl, C3-7-cycloalkyl, C1-6alkyl-C3-7-cycloalkyl, C^-heterocycloalkyl, aryl and heteroaryl, each of which may be optionally substituted. Further aspects of the invention relate to pharmaceutical compositions comprising the same, and methods for treating or preventing a disorder selected from cancer, septic shock, Primary open Angle Glaucoma (POAG), hyperplasia, rheumatoid arthritis, psoriasis, artherosclerosis, retinopathy, osteoarthritis, endometriosis, chronic inflammation and Alzheimer's disease. Another aspect of the invention relates to the use of a compound as described above in the preparation of a medicament for the prevention or treatment of a disorder caused by, associated with or accompanied by any abnormal kinase activity, wherein the kinase is selected from TBK1, ERK8, CDK2, MARK3, YES1, VEG-FR, IKKepsilon and combinations thereof. |
IP Reference | WO2010100431 |
Protection | Patent application published |
Year Protection Granted | 2010 |
Licensed | No |
Impact | Highly selective inhibitors as tool compounds for disease association |
Title | TG2 |
Description | Identification of novel TG2 humanised antibody |
IP Reference | |
Protection | Protection not required |
Year Protection Granted | 2014 |
Licensed | Commercial In Confidence |
Impact | Expansion of scientific knowledge and preclinical candidate licensed |
Title | MCR3 |
Description | Small molecule ligands |
Type | Therapeutic Intervention - Drug |
Current Stage Of Development | Initial development |
Year Development Stage Completed | 2015 |
Development Status | Under active development/distribution |
Impact | New tools made available |
Title | TG2 |
Description | TG2 antibody for fibrosis |
Type | Therapeutic Intervention - Drug |
Current Stage Of Development | Initial development |
Year Development Stage Completed | 2013 |
Development Status | Under active development/distribution |
Impact | Novel approach to treating pulmonary fibrosis |
Title | alphavbeta6 |
Description | alphavbeta6 humanised antibody |
Type | Therapeutic Intervention - Drug |
Current Stage Of Development | Refinement. Non-clinical |
Year Development Stage Completed | 2011 |
Development Status | Actively seeking support |
Impact | Potential new drug |
Description | AstraZeneca |
Form Of Engagement Activity | A talk or presentation |
Part Of Official Scheme? | No |
Geographic Reach | International |
Primary Audience | Participants in your research and patient groups |
Results and Impact | Talk to senior executives. Signing of compound screening agreement |
Year(s) Of Engagement Activity | 2009,2010 |
Description | Crowd Sourcing Conference |
Form Of Engagement Activity | A talk or presentation |
Part Of Official Scheme? | No |
Geographic Reach | International |
Primary Audience | Public/other audiences |
Results and Impact | Invited audience of 150 delegates Requests for more information |
Year(s) Of Engagement Activity | 2011 |
Description | Dementia consortium |
Form Of Engagement Activity | A press release, press conference or response to a media enquiry/interview |
Part Of Official Scheme? | No |
Geographic Reach | National |
Primary Audience | Media (as a channel to the public) |
Results and Impact | Interviews resulted in articles in the Guardian and Times newspapers Sparked other press agencies contacting us for quotes and input. |
Year(s) Of Engagement Activity | 2014 |
Description | ELRIG conference |
Form Of Engagement Activity | A talk or presentation |
Part Of Official Scheme? | No |
Geographic Reach | National |
Primary Audience | Professional Practitioners |
Results and Impact | Conference talk |
Year(s) Of Engagement Activity | 2015 |
Description | Eisai Pharma |
Form Of Engagement Activity | A talk or presentation |
Part Of Official Scheme? | No |
Geographic Reach | International |
Primary Audience | Public/other audiences |
Results and Impact | Talk to six senior executives fro Eisai Desire by Eisai to work with MRCT on new targets |
Year(s) Of Engagement Activity | 2010 |
Description | GSK |
Form Of Engagement Activity | A talk or presentation |
Part Of Official Scheme? | No |
Geographic Reach | National |
Primary Audience | Participants in your research and patient groups |
Results and Impact | Presentation on output from GPCR de-orphainsation programme Interest from GSK in further collaborations and in-licencing |
Year(s) Of Engagement Activity | 2009,2010 |
Description | Global Alliance on Drug Discovery |
Form Of Engagement Activity | A formal working group, expert panel or dialogue |
Part Of Official Scheme? | No |
Geographic Reach | International |
Primary Audience | Other academic audiences (collaborators, peers etc.) |
Results and Impact | Awareness of drug discovery respource for academics worldwide Approaches by academics to access resource and work with Alliance |
Year(s) Of Engagement Activity | 2013 |
Description | Miptech Conference |
Form Of Engagement Activity | A talk or presentation |
Part Of Official Scheme? | No |
Geographic Reach | International |
Primary Audience | Public/other audiences |
Results and Impact | Over 200 people attended Requests for more information |
Year(s) Of Engagement Activity | 2011 |
Description | SBS conference |
Form Of Engagement Activity | A talk or presentation |
Part Of Official Scheme? | No |
Geographic Reach | National |
Primary Audience | Public/other audiences |
Results and Impact | talk in front of several hundred pharma, biotech and academic scientists More approaches to MRCT about collaborations |
Year(s) Of Engagement Activity | 2009,2010 |